96 results on '"Antispasmodic"'
Search Results
2. Antispasmodic, cardioprotective and blood-pressure lowering properties of Gomphrena perennis L. and its mechanisms of action
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Adriana Milena Bonilla Bonilla, Tatiana C. Gavilánez Buñay, Matías Bayley, Germán A. Colareda, Soledad I. Matera, María Luján Flores, Osvaldo León Córdoba, Julián J. Prieto, María Esperanza Ruiz, Alicia E. Consolini, and María Inés Ragone
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Gomphrena perennis ,Antispasmodic ,Blood pressure ,Cardioprotection ,Nitric oxide ,Medicine - Abstract
Background: Gomphrena perennis L. is a native plant of South America whose pharmacological properties have not been studied yet. Aim: To evaluate the cardiovascular and intestinal pharmacological effects of Gomphrena perennis L. leaves tincture (GphT) and the mechanisms involved. Experimental procedure: The chromatographic profile of GphT was done. Its ex vivo effects were evaluated by contractile concentration-response curves (CRCs) obtained from the agonist carbachol or calcium found in isolated rat small intestine, as well as in the relaxant CRCs. Cardiac effects were evaluated on isolated rat hearts exposed to ischemia/reperfusion (I/R). Experiments in vivo were performed to evaluate the diuretic activity in conscious rats and the hypotensive effect in anaesthetised rats. Results: Fifteen flavonoids were identified in GphT by HPLC-UV, including diosmin. GphT induced a non-competitive inhibition in both carbachol and calcium CRCs on rat small intestine. The first was not affected by indomethacin. Moreover, GphT, unlike diosmin, relaxed the contracture produced by a high-potassium solution in a dose-dependently way. Neither propranolol nor l-NAME changed it. GphT did not show diuretic activity but induced hypotension insensitive to l-NAME. While GphT perfusion of isolated hearts increased injury consequent to I/R, oral administration was cardioprotective and reversed by l-NAME. However, diosmin did not improve the post-ischemic recovery. Conclusions: This study supports the use of Gomphrena perennis L. tincture as an antispasmodic and hypotensive agent. Moreover, it has been demonstrated to be preventive of post-ischemic cardiac dysfunction. However, diosmin would not be responsible for these effects.
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- 2024
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3. A Study on the Antibacterial, Antispasmodic, Antipyretic, and Anti-Inflammatory Activity of ZnO Nanoparticles Using Leaf Extract from Jasminum sambac (L. Aiton).
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Sugitha, S. K. Johnsy, Venkatesan, Raja, Latha, R. Gladis, Vetcher, Alexandre A., Al-Asbahi, Bandar Ali, and Kim, Seong-Cheol
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PRECIPITATION (Chemistry) , *ANTI-inflammatory agents , *JASMINE , *ZINC oxide synthesis , *ESCHERICHIA coli , *HISTAMINE , *ZINC oxide - Abstract
The green synthesis of zinc oxide nanoparticles (ZnO NPs) using plants has grown in significance in recent years. ZnO NPs were synthesized in this work via a chemical precipitation method with Jasminum sambac (JS) leaf extract serving as a capping agent. These NPs were characterized using UV-vis spectroscopy, FT-IR, XRD, SEM, TEM, TGA, and DTA. The results from UV-vis and FT-IR confirmed the band gap energies (3.37 eV and 3.50 eV) and the presence of the following functional groups: CN, OH, C=O, and NH. A spherical structure and an average grain size of 26 nm were confirmed via XRD. The size and surface morphology of the ZnO NPs were confirmed through the use of SEM analysis. According to the TEM images, the ZnO NPs had an average mean size of 26 nm and were spherical in shape. The TGA curve indicated that the weight loss starts at 100 °C, rising to 900 °C, as a result of the evaporation of water molecules. An exothermic peak was seen during the DTA analysis at 480 °C. Effective antibacterial activity was found at 7.32 ± 0.44 mm in Gram-positive bacteria (S. aureus) and at 15.54 ± 0.031 mm in Gram-negative (E. coli) bacteria against the ZnO NPs. Antispasmodic activity: the 0.3 mL/mL sample solution demonstrated significant reductions in stimulant effects induced by histamine (at a concentration of 1 µg/mL) by (78.19%), acetylcholine (at a concentration of 1 µM) by (67.57%), and nicotine (at a concentration of 2 µg/mL) by (84.35%). The antipyretic activity was identified using the specific Shodhan vidhi method, and their anti-inflammatory properties were effectively evaluated with a denaturation test. A 0.3 mL/mL sample solution demonstrated significant reductions in stimulant effects induced by histamine (at a concentration of 1 µg/mL) by 78.19%, acetylcholine (at a concentration of 1 µM) by 67.57%, and nicotine (at a concentration of 2 µg/mL) by 84.35%. These results underscore the sample solution's potential as an effective therapeutic agent, showcasing its notable antispasmodic activity. Among the administered doses, the 150 mg/kg sample dose exhibited the most potent antipyretic effects. The anti-inflammatory activity of the synthesized NPs showed a remarkable inhibition percentage of (97.14 ± 0.005) at higher concentrations (250 µg/mL). Furthermore, a cytotoxic effect was noted when the biologically synthesized ZnO NPs were introduced to treated cells. [ABSTRACT FROM AUTHOR]
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- 2024
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4. Efficacy and safety of pinaverium bromide as an add‐on therapy in refractory dyspepsia: A randomized controlled trial.
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Kamolsripat, Thansita, Thinrungroj, Nithi, Pinyopornpanish, Kanokwan, Kijdamrongthum, Phuripong, Leerapun, Apinya, Chitapanarux, Taned, Thongsawat, Satawat, Praisontarangkul, Ong‐Ard, and Pojchamarnwiputh, Suwalee
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RANDOMIZED controlled trials ,INDIGESTION ,BROMIDES ,REFRACTORY materials ,OMEPRAZOLE - Abstract
Background and Aim: Functional dyspepsia (FD) remains a therapeutic challenge, and the efficacy of antispasmodic agents as adjunctive therapy is not well established. This study aimed to evaluate the efficacy and safety of pinaverium bromide added to omeprazole in treating refractory FD. Methods: We conducted a randomized, placebo‐controlled trial in patients with refractory dyspepsia. Participants were randomly assigned to receive pinaverium (50 mg, 3 times/day, n = 36) or placebo (n = 36) in addition to omeprazole for 8 weeks. The primary endpoint was the responder rate for adequate relief. Secondary outcomes included the Global Overall Symptom Scale (GOSS), quality of life, and safety profile. Results: No statistically significant differences were observed in the adequate relief response rate between the pinaverium bromide and control group at week 2 (58.3% vs. 62.9%, P = 0.697), week 4 (62.9% vs. 78.1%, P = 0.173), week 6 (64.7% vs. 75.0%, P = 0.363), and week 8 (64.7% vs. 75.0%, P = 0.363). Additionally, there were no significant differences observed in the decline of symptom score between the two groups at week 4 (8.4 ± 7.6 vs. 7.7 ± 7.1, P = 0.702) and week 8 (10.9 ± 8.2 vs. 8.4 ± 7.2, P = 0.196). Similarly, there were no significant differences in terms of quality of life between the two groups. Adverse event rates were also comparable between the two groups. Conclusion: Pinaverium bromide was found to be safe in the treatment of refractory dyspepsia, but it did not demonstrate a significant benefit in improving symptoms. [ABSTRACT FROM AUTHOR]
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- 2024
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5. Aromatherapy - An overview
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Kancharla, Sravya, Sundar, S., Padmalatha, K., Lakshmidevi, S, Ooha, D, and Mounika, P
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- 2023
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6. Pharmacotherapy for gastric and intestinal cramping pain: current and emerging therapies.
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Mousavi, Taraneh, Sharifnia, Mohammadhossein, Nikfar, Shekoufeh, and Abdollahi, Mohammad
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Acute gastrointestinal cramping pain (GICP) is a debilitating condition that affects many people worldwide, significantly reducing their quality of life. As such, prompt treatment is crucial. This article will explore relevant literature from databases such as PubMed, Scopus, Google Scholar, Cochrane Library, and Web of Science. Additionally, we searched ClinicalTrials.gov and the WHO ICTRP database for the latest clinical trials. Consensus dictates that antispasmodics such as hyoscine-N-butyl bromide and mebeverine should be the primary treatment for GICP. If these prove ineffective, patients can switch to an antispasmodic with a different mode of action or add acetaminophen/NSAIDs for more severe cases. Currently, several antispasmodics are undergoing clinical trials, including drotaverine, alverine, pinaverium, otilonium bromide, fenoverine, tiropramide, otilonium bromide, trimebutine, and peppermint oil. Well-designed head-to-head studies are necessary to evaluate current antispasmodics' safety, efficacy, pharmacokinetic, and pharmacoeconomics profiles. Recent studies have shown that fixed-dose combinations of antispasmodics + NSAIDs or two different antispasmodics can improve patient compliance and synergistically reduce GICP. Therefore, it is recommended that the global availability and accessibility of these products be enhanced. [ABSTRACT FROM AUTHOR]
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- 2023
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7. Efficacy and safety of pinaverium bromide as an add‐on therapy in refractory dyspepsia: A randomized controlled trial
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Thansita Kamolsripat, Nithi Thinrungroj, Kanokwan Pinyopornpanish, Phuripong Kijdamrongthum, Apinya Leerapun, Taned Chitapanarux, Satawat Thongsawat, Ong‐Ard Praisontarangkul, and Suwalee Pojchamarnwiputh
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antispasmodic ,functional dyspepsia ,omeprazole ,pinaverium ,randomized Controlled Trail ,Diseases of the digestive system. Gastroenterology ,RC799-869 - Abstract
Abstract Background and Aim Functional dyspepsia (FD) remains a therapeutic challenge, and the efficacy of antispasmodic agents as adjunctive therapy is not well established. This study aimed to evaluate the efficacy and safety of pinaverium bromide added to omeprazole in treating refractory FD. Methods We conducted a randomized, placebo‐controlled trial in patients with refractory dyspepsia. Participants were randomly assigned to receive pinaverium (50 mg, 3 times/day, n = 36) or placebo (n = 36) in addition to omeprazole for 8 weeks. The primary endpoint was the responder rate for adequate relief. Secondary outcomes included the Global Overall Symptom Scale (GOSS), quality of life, and safety profile. Results No statistically significant differences were observed in the adequate relief response rate between the pinaverium bromide and control group at week 2 (58.3% vs. 62.9%, P = 0.697), week 4 (62.9% vs. 78.1%, P = 0.173), week 6 (64.7% vs. 75.0%, P = 0.363), and week 8 (64.7% vs. 75.0%, P = 0.363). Additionally, there were no significant differences observed in the decline of symptom score between the two groups at week 4 (8.4 ± 7.6 vs. 7.7 ± 7.1, P = 0.702) and week 8 (10.9 ± 8.2 vs. 8.4 ± 7.2, P = 0.196). Similarly, there were no significant differences in terms of quality of life between the two groups. Adverse event rates were also comparable between the two groups. Conclusion Pinaverium bromide was found to be safe in the treatment of refractory dyspepsia, but it did not demonstrate a significant benefit in improving symptoms.
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- 2024
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8. Chemical composition, in vitro and in silico approaches of the relaxant effect of the jejunum using Thymus algeriensis Boiss. and Reut essential oil
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Leila Beyi, Mohamed Marghich, Ouafa Amrani, Ahmed Karim, Tarik Harit, and Mohammed Aziz
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Thymus algeriensis ,Essential oil ,Antispasmodic ,Cholinergic receptor ,Voltage-dependent calcium channel ,Thujone ,Other systems of medicine ,RZ201-999 - Abstract
Background: Gastrointestinal problems are among the most common diseases in Morocco people, who frequently use aromatic and medicinal plants to eliminate these problems. Thymus algeriensis is one of these plants widely used to treat gastrointestinal problems. This research aimed to identify the phytochemical compounds present in Thymus algeriensis essential oil (TaEO), assess its acute toxicity, and investigate its potential myorelaxant and antispasmodic effects. Methods: In vitro experiments were conducted on rat and rabbit jejunum using an isotonic transducer and in silico docking calculations were conducted on l-type voltage-gated Ca2+and muscarinic receptor active sites. Results: The GC–MS analysis of TaEO revealed the presence of 11 compounds, with 89.77 % of the compounds identified being oxygenated monoterpenes, among which Thujone dominates the composition with 32.89 %. The administration of TaEO did not produce any observable signs of toxicity or mortality at 1 g/Kg.bw. TaEO exhibit a dose-dependent decrease in the basal contractions of the rabbit jejunum with an IC50 value of 5.66 ± 1.88 µg/mL. In addition, TaEO induced an antispasmodic effect on KCl and CCh-induced contractions in the rat jejunum. The inhibitory effect demonstrated are similar to those produced by a non-competitive antagonist of voltage-dependent calcium channel and cholinergic receptors. These results are boosted by the docking study when we showed that Thujone could bind to the active site of muscarinic receptor and, l-type voltage-gated Ca2+ with a binding energy equal to -59.401 and, -47.441 Kcal/mol respectively. Conclusions: These results provide strong confirmation for the traditional use of Thymus algeriensis in Moroccan as an effective antispasmodic remedy and give a new lead to find a phytomedicament against gastrointestinal problems.
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- 2023
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9. Pharmacological management of irritable bowel syndrome.
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Kasmani, Ilkin
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Irritable bowel syndrome (IBS) is a common longstanding condition with a variety of symptoms including constipation, diarrhoea and abdominal cramps or bloating. There are no specific causes of IBS; therefore, symptoms and management are individualised to each patient. Management strategies involve lifestyle advice on diet and exercise, medications and psychological therapies. IBS can be extremely debilitating to patients' quality of life and is usually diagnosed as a process of elimination of other gastrointestinal conditions that can have similar symptoms, such as inflammatory bowel disease. Medications to manage IBS include laxatives, antispasmodics, antimotility agents and neuromodulators, as IBS is believed to be a disorder of the gut--brain axis. [ABSTRACT FROM AUTHOR]
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- 2023
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10. Antispasmodic and Relaxant Effects of Thymus algeriensis Dichloromethane fraction on Intestinal Smooth Muscle Motility of Wistar rats.
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Beyi, Leila, Marghich, Mohamed, Karim, Ahmed, Amrani, Ouafa, and Aziz, Mohammed
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DIGESTIVE organs ,SMOOTH muscle ,CALCIUM channels ,INTESTINAL diseases ,RESPONSE inhibition - Abstract
Digestive disorders are common reasons for medical consultations, making natural remedies based on medicinal plants increasingly popular. This study explored the potential benefits of Thymus algeriensis on the motility of the smooth intestinal muscle to address digestive tract disorders. The study focused on an in vitro test using the rat jejunum to evaluate the antispasmodic and relaxant effects of its dichloromethane fraction. The results showed that the dichloromethane fraction caused a significant relaxing effect on spontaneous contraction and an antispasmodic effect on rat jejunum precontracted with carbachol or KCl in a dose-response manner (p ˂ 0.001). The inhibitory activity demonstrated was comparable to those produced by a non-competitive antagonist of voltage-dependent Calcium channel and cholinergic receptors. These findings highlight the potential of Thymus algeriensis dichloromethane fraction to address digestive disorders. [ABSTRACT FROM AUTHOR]
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- 2023
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11. A Study on the Antibacterial, Antispasmodic, Antipyretic, and Anti-Inflammatory Activity of ZnO Nanoparticles Using Leaf Extract from Jasminum sambac (L. Aiton)
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S. K. Johnsy Sugitha, Raja Venkatesan, R. Gladis Latha, Alexandre A. Vetcher, Bandar Ali Al-Asbahi, and Seong-Cheol Kim
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green synthesis ,Jasminum sambac ,ZnO NPs ,antibacterial ,antispasmodic ,antipyretic ,Organic chemistry ,QD241-441 - Abstract
The green synthesis of zinc oxide nanoparticles (ZnO NPs) using plants has grown in significance in recent years. ZnO NPs were synthesized in this work via a chemical precipitation method with Jasminum sambac (JS) leaf extract serving as a capping agent. These NPs were characterized using UV-vis spectroscopy, FT-IR, XRD, SEM, TEM, TGA, and DTA. The results from UV-vis and FT-IR confirmed the band gap energies (3.37 eV and 3.50 eV) and the presence of the following functional groups: CN, OH, C=O, and NH. A spherical structure and an average grain size of 26 nm were confirmed via XRD. The size and surface morphology of the ZnO NPs were confirmed through the use of SEM analysis. According to the TEM images, the ZnO NPs had an average mean size of 26 nm and were spherical in shape. The TGA curve indicated that the weight loss starts at 100 °C, rising to 900 °C, as a result of the evaporation of water molecules. An exothermic peak was seen during the DTA analysis at 480 °C. Effective antibacterial activity was found at 7.32 ± 0.44 mm in Gram-positive bacteria (S. aureus) and at 15.54 ± 0.031 mm in Gram-negative (E. coli) bacteria against the ZnO NPs. Antispasmodic activity: the 0.3 mL/mL sample solution demonstrated significant reductions in stimulant effects induced by histamine (at a concentration of 1 µg/mL) by (78.19%), acetylcholine (at a concentration of 1 µM) by (67.57%), and nicotine (at a concentration of 2 µg/mL) by (84.35%). The antipyretic activity was identified using the specific Shodhan vidhi method, and their anti-inflammatory properties were effectively evaluated with a denaturation test. A 0.3 mL/mL sample solution demonstrated significant reductions in stimulant effects induced by histamine (at a concentration of 1 µg/mL) by 78.19%, acetylcholine (at a concentration of 1 µM) by 67.57%, and nicotine (at a concentration of 2 µg/mL) by 84.35%. These results underscore the sample solution’s potential as an effective therapeutic agent, showcasing its notable antispasmodic activity. Among the administered doses, the 150 mg/kg sample dose exhibited the most potent antipyretic effects. The anti-inflammatory activity of the synthesized NPs showed a remarkable inhibition percentage of (97.14 ± 0.005) at higher concentrations (250 µg/mL). Furthermore, a cytotoxic effect was noted when the biologically synthesized ZnO NPs were introduced to treated cells.
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- 2024
- Full Text
- View/download PDF
12. Calcium Channel Inhibitory Effect of Marjoram (Origanum majorana L.): Its Medicinal Use in Diarrhea and Gut Hyperactivity
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Najeeb Ur Rehman, Mohd Nazam Ansari, Wasim Ahmad, and Abuzer Ali
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o. majorana ,antispasmodic ,ca++ channel blocker ,gc-ms ,verapamil ,crcs ,Biochemistry ,QD415-436 ,Biology (General) ,QH301-705.5 - Abstract
Background: The leaves of Origanum majorana (O. majorana) are traditionally renowned for treating diarrhea and gut spasms. This study was therefore planned to evaluate its methanolic extract. Methods: Gas chromatography–mass spectrometry (GC-MS) was used to identify the phytochemicals, and Swiss albino mice were used for an in vivo antidiarrheal assay. Isolated rat ileum was used as an ex vivo assay model to study the possible antispasmodic effect and its mechanism(s). Results: The GC-MS analysis of O. majorana detected the presence of 21 compounds, of which alpha-terpineol was a major constituent. In the antidiarrheal experiment, O. majorana showed a substantial inhibitory effect on diarrheal episodes in mice at an oral dosage of 200 mg/kg, resulting in 40% protection. Furthermore, an oral dosage of 400 mg/kg provided even greater protection, with 80% effectiveness. Similarly, loperamide showed 100% protection at oral doses of 10 mg/kg. O. majorana caused complete inhibition of carbachol (CCh, 1 µM) and high K+ (80 mM)-evoked spasms in isolated ileal tissues by expressing significantly higher potency (p < 0.05) against high K+ compared to CCh, similar to verapamil, a Ca++ antagonist. The verapamil-like predominant Ca++ ion inhibitory action of O. majorana was further confirmed in the ileal tissues that were made Ca++-free by incubating the tissues in a physiological salt solution having ethylenediaminetetraacetic acid (EDTA) as a chelating agent. The preincubation of O. majorana at increasing concentrations (0.3 and 1 mg/mL) shifted towards the right of the CaCl2-mediated concentration-response curves (CRCs) with suppression of the maximum contraction. Similarly, verapamil also caused non-specific suppression of Ca++ CRCs towards the right, as expected. Conclusions: Thus, this study conducted an analysis to determine the chemical constituents of the leaf extract of O. majorana and provided a detailed mechanistic basis for the medicinal use of O. majorana in hyperactive gut motility disorders.
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- 2024
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13. Essential Oil of Satureja montana L. from Herzegovina: Assessment of Composition, Antispasmodic, and Antidiarrheal Effects.
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Kulić, Milan, Drakul, Dragana, Sokolović, Dragana, Kordić-Bojinović, Jelena, Milovanović, Slobodan, and Blagojević, Duško
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ESSENTIAL oils , *SAVORY (Herb) , *MONOTERPENES , *LABORATORY rats , *PHENOLS , *TANNINS , *ELECTRIC stimulation - Abstract
Satureja montana L. (SM) has a long traditional use as a spice and a medicine for various gastrointestinal disorders, including painful spasms and diarrhea. Contrary to conventional drugs, administration of SM and its extracts are considered safe. Previous studies have shown that the essential oils (EOs) of SM from different areas are rich in monoterpenes, sesquiterpenes, diterpens, and phenolic compounds, including flavonoids, tannins, and acids with great composition variability. Determination of composition of EO from Herzegovinian SM done by gas chromatographyflame ionization detection and gas chromatography mass spectrometry (GC-FID and GC/MS, respectively) revealed carvacrol as a primary substance followed by γ-terpinene, p-cymene, and ß-caryophyllene. Ex vivo spasmolitic activity caused by EO was evident in different types of isolated rat ileum function with the most potent effect on spontaneous activity followed by electrical field stimulation and KCl- and CaCl2-induced activity. SMEO produced in vivo antidiarreal activity on castor oil-induced diarrhea in young rats and showed the potential to cause a decrese water content in the feces of adult Wistar rats. This study indicates that effects of SM on the intestinum could be mediated through combination of Kv channel activation and Ca channel blockade, but additional mechanisms might be involved. The results of this study corroborate the traditional use of SM as antispasmodic, antidiarrheal, and antisecretory agents. [ABSTRACT FROM AUTHOR]
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- 2023
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14. Acorus calamus: A Review on Its Phytochemical and Pharmacological Profile
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Afzal, Suhaib, Ayoub, Mehrose, Raja, Weekar Younis, Masoodi, Mubashir Hussain, editor, and Rehman, Muneeb U, editor
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- 2022
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15. Biological Characterization of Polystichum lonchitis L. for Phytochemical and Pharmacological Activities in Swiss Albino Mice Model.
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Sher, Jan, Jan, Gul, Israr, Muhammad, Irfan, Muhammad, Yousuf, Nighat, Ullah, Fazal, Rauf, Abdur, Alshammari, Abdulrahman, and Alharbi, Metab
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LABORATORY mice ,ANIMAL disease models ,PHYTOCHEMICALS ,SCIENTIFIC method - Abstract
Polystichum lonchitis L. is a fern belonging to the family Dryopteridaceae. The present study was conducted to evaluate its pharmacological, antioxidant, and phytochemical properties, and to conduct GC–MS screening of P. lonchitis. The acetic acid-induced writhing test, yeast-induced hyperpyrexia method, carrageenan-induced rat paw edema model, and charcoal meal test model were carried out to assess analgesic, antipyretic, anti-inflammatory, and antispasmodic activity, respectively. DPPH was used as an antioxidant, while the phytochemical screening was conducted using standard scientific methods. Among the pharmacological activities, the most significant effects were observed in the analgesic and anti-inflammatory activities, followed by the antipyretic and antispasmodic activities, at a dose of 450 mg/kg after the 4th hour, compared with 150 mg/kg and 300 mg/kg. For the evaluation of antioxidant activities, the most significant results were detected in the methanolic and aqueous extracts. The detection of flavonoids and phenol occurred most significantly in the methanolic extract, and then in the ethanolic and aqueous extracts. The main compounds detected using GC–MS analysis with a high metabolic rate was -D-Galactopyranoside, which had a metabolic rate of 0.851, and methyl and n-hexadecanoic, which had a metabolic rate of 0.972. Overall, the results suggested that P. lonchitis had a strong potential for pharmacological activities. The suggested assessment provided a way to isolate the bioactive constituents and will help to provide new medicines with fewer side effects. Due to the fern's effectiveness against various diseases, the results provide clear evidence that they also have the potential to cure various diseases. [ABSTRACT FROM AUTHOR]
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- 2023
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16. Antispasmodic and nephroprotective potentials of native Algerian propolis and bee pollen: An experimental study in mice.
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Ali Haimoud, S., Allem, R., Medjekane, M., Benyahla Djeffaland, K., Lembarki, N. E., Boutara, K., and Belhache, F.
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PROPOLIS ,BEE pollen ,MICE ,DRUG discovery ,HONEYBEES ,INTRAPERITONEAL injections ,VISCERAL pain ,ACETIC acid ,BIOACTIVE compounds - Abstract
The present work examined the in vivo antispasmodic and nephroprotective potentials of methanolic extracts obtained from Algerian native propolis and bee pollen. The in vivo antispasmodic activity was assessed by the intraperitoneal injection of acetic acid (1%) which induced long-lasting visceral pain in mice. The renal damage was modelled by intraperitoneal injection of a cisplatin (CP; 10 mg/kg) followed by histopathological changes in kidneys. In addition, the beehive by-products were screened for their bioactive content and in vitro antioxidant activities. The propolis and bee pollen are rich sources of bioactive compounds. The propolis showed the highest antioxidant potencies as evaluated by β-carotene bleaching system (87.16 ± 3.69%), DPPH (176.05 ± 0.20 μg/mL), and FRAP (0.61 ± 0.002 μmol Fe(II)/g) assays. The antispasmodic test revealed that propolis extract (250 mg/kg) significantly inhibited the number of spasms (61.04 ± 3.92%) induced by acetic acid. Based on histopathology examinations, bee pollen extract at 250 mg/kg significantly reduced nephrotoxic effects induced by CP injection. These results provided a good scientific basis for future research on antispasmodic and nephroprotective effects and/or mechanisms of propolis and bee pollen, which confer them a real application in drug discovery. [ABSTRACT FROM AUTHOR]
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- 2023
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17. Pharmacological Basis for the Antidiarrheal and Antispasmodic Effects of Cuminaldehyde in Experimental Animals: In Silico, Ex Vivo and In Vivo Studies
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Mohd Nazam Ansari, Najeeb Ur Rehman, Abdul Samad, and Wasim Ahmad
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cuminaldehyde ,antispasmodic ,k+ channel opener ,ca++ channel blocker ,glibenclamide ,Biochemistry ,QD415-436 ,Biology (General) ,QH301-705.5 - Abstract
Background: Medicinal herbs are frequently used for the management of gastrointestinal disorders because they contain various compounds that can potentially amplify the intended therapeutic effects. Cuminaldehyde is a plant-based constituent found in oils derived from botanicals such as cumin, eucalyptus, myrrh, and cassia and is responsible for its health benefits. Despite the utilization of cuminaldehyde for several medicinal properties, there is currently insufficient scientific evidence to support its effectiveness in treating diarrhea. Hence, the present investigation was carried out to evaluate the antidiarrheal and antispasmodic efficacy of cuminaldehyde, with detailed pharmacodynamics explored. Methods: An in vivo antidiarrheal test was conducted in mice following the castor oil-induced diarrhea model, while an isolated small intestine obtained from rats was used to evaluate the detailed mechanism(s) of antispasmodic effects. Results: Cuminaldehyde, at 10 and 20 mg/kg, exhibited 60 and 80% protection in mice from episodic diarrhea compared to the saline control group, whereas this inhibitory effect was significantly reversed in the pretreated mice with glibenclamide, similar to cromakalim, an ATP-dependent K+ channel opener. In the ex vivo experiments conducted in isolated rat tissues, cuminaldehyde reversed the glibenclamide-sensitive low K+ (25 mM)-mediated contractions at significantly higher potency compared to its inhibitory effect against high K+ (80 mM), thus showing predominant involvement of ATP-dependent K+ activation followed by Ca++ channel inhibition. Cromakalim, a standard drug, selectively suppressed the glibenclamide-sensitive low K+-induced contractions, whereas no relaxation was observed against high K+, as expected. Verapamil, a Ca++ channel inhibitor, effectively suppressed both low and high K+-induced contractions with similar potency, as anticipated. At higher concentrations, the inhibitory effect of cuminaldehyde against Ca++ channels was further confirmed when the preincubated ileum tissues with cuminaldehyde (3 and 10 mM) in Ca++ free medium shifted CaCl2-mediated concentration-response curves (CRCs) towards the right with suppression of the maximum peaks, similar to verapamil, a standard Ca++ ion inhibitor. Conclusions: Present findings support the antidiarrheal and antispasmodic potential of cuminaldehyde, possibly by the predominant activation of ATP-dependent K+ channels followed by voltage-gated Ca++ inhibition. However, further in-depth assays are recommended to know the precise mechanism and to elucidate additional unexplored mechanism(s) if involved.
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- 2024
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18. Antidiarrheal, antisecretory and intestinal smooth muscle relaxant effects of Platanus orientalis in mice.
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Bashir, Deeba, Khan, Taous, Ahmad, Taseer, and Shah, Abdul Jabbar
- Abstract
Platanus orientalis is traditionally used to treat diarrhea and spasm. However, studies are lacking on its mechanism of action in diarrhea and spasm. Pharmacological in-vivo activities were performed. In-vitro activities were carried out to explore the underlying mechanism(s) of action in isolated tissue preparations of mice jejunum and ileum. Crude extract of Platanus orientalis, loperamide and verapamil were used. The crude extract provided dose-dependent protection in castor oil diarrhea like verapamil and reduced the intestinal fluid accumulation and charcoal meal transit distance. In-vitro studies produced spasmolytic effect on the spontaneous (EC
50 value=0.21mg/mL), high K+ (EC50 value=0.37mg/mL) and carbachol (CCh)-induced contractions 5.35mg/mL (3.88-6.85) respectively. The quiescent ileum responded well to the high K+ and carbachol (CCh)-induced contractions when tested against crude extract. It caused inhibition of the induced contraction with EC50 values of 0.20mg/mL (0.10-0.30) and 3.25mg/mL (2-4.5) respectively and showed potent effect against CCh-induced contractions. Calcium response curves produced a similar effect to verapamil. The crude extract of Platanus orientalis remained safe up to 5g/kg dose. [ABSTRACT FROM AUTHOR]- Published
- 2023
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19. Detection rates of colorectal neoplasia during colonoscopies and their associated factors in the SCREESCO study.
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Sekiguchi, Masau, Westerberg, Marcus, Ekbom, Anders, Hultcrantz, Rolf, and Forsberg, Anna
- Subjects
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VIRTUAL colonoscopy , *FECAL occult blood tests , *ADENOMA , *TUMORS , *EARLY detection of cancer , *RANDOMIZED controlled trials , *COLORECTAL cancer - Abstract
Background and Aim: Colonoscopy quality, including lesion detectability, is variable, and factors influencing lesion detection are not fully understood. This study investigated lesion detection rates during colonoscopies and the associated factors in the SCREEning of Swedish COlons (SCREESCO) study. Methods: In this cross‐sectional analysis of data from SCREESCO, a large‐scale randomized controlled trial of colorectal cancer screening in the Swedish population aged 60 years, we assessed data of first‐time colonoscopies performed in both colonoscopy and fecal immunochemical test (FIT) arms. Results: This study included 16 552 individuals. The adenoma detection rate was 23.9% and 37.8% in colonoscopy and FIT arms, respectively. Regarding colonoscopy procedures, a withdrawal time ≥ 6 min was associated with higher detection rates of advanced adenomas (adjusted odds ratio [AOR] 2.474, 95% confidence interval [CI] 1.295–4.723), adenomas (2.181, 1.515–3.140), and proximal serrated lesions (pSLs) (1.713, 1.007–2.915). Antispasmodic use was associated with higher detection rates of these lesions and sessile serrated lesions (SSLs) (AOR, 95% CI: 1.523, 1.295–1.791; 1.361, 1.217–1.522; 1.450, 1.247–1.687; and 1.810, 1.512–2.167, respectively). Insertion time > 20 min was related to lower detection rates of adenomas, pSLs, and SSLs (AOR, 95% CI: 0.753, 0.639–0.887; 0.640, 0.495–0.828; and 0.704, 0.518–0.955, respectively). The relationship between a recent period and higher detection rates of pSLs and SSLs was also demonstrated. Conclusion: Lesion detectability in SCREESCO was mostly acceptable with room for improvement. In addition to sufficient withdrawal time, antispasmodic use and acquiring skills enabling short insertion time may improve lesion detection. Trial registration: ClinicalTrials.gov, ID: NCT02078804. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
20. The effect of thymol on acetylcholine-induced contractions of the rat ileum and uterus under ex vivo conditions.
- Author
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Bajuk, Blanka Premrov, Prem, Luka, Vake, Tilen, Žnidaršič, Neža, and Snoj, Tomaž
- Subjects
THYMOL ,SMOOTH muscle contraction ,ILEUM ,MYOMETRIUM ,UTERINE contraction ,UTERUS - Abstract
Thyme (Thymus vulgaris L.) is a well-known medicinal plant, the aerial parts of which have long been used internally or externally as a traditional remedy for various diseases. Thyme essential oils have important pharmaceutical applications and are regularly used in the pharmaceutical, food and cosmetic industries. In folk medicine, thyme preparations are used to treat respiratory, digestive, cardiovascular and nervous disorders, as well as to relieve dysmenorrhea. Thymol, a major constituent of Thymus vulgaris essential oil, has been shown to affect skeletal and smooth muscle excitation and contraction. Therefore, the main objective of this study was to evaluate its effect on acetylcholine (ACh)-induced rat intestinal and uterine preparations. Isolated ileum and uterine horn preparations were placed in a 20-ml organ bath containing Tyrode or De Jalon solution and exposed to graded concentrations of ACh (0.036, 0.109, 0.36, 1.09, 3,6, 10.9, and 36 µM) and either 0.02 or 0.2 mM thymol. Additionally, the dose-response relationship of thymol impact on intestinal and uterine contraction was evaluated. Contraction changes were monitored using an isometric transducer. Thymol at the higher dose (0.2 mM) significantly reduced ACh-induced intestinal and uterine contractions. Thus, this study provides new important data on competitive actions between thymol and ACh. In the dose-response study, the IC50 values were calculated as 5.26 mM for the ileum and 5.35mM for the uterus. Our results demonstrated the efficacy of thymol in reducing ileal and uterine smooth muscle contractions, thus supporting the use of thyme in traditional medicine in the treatment of digestive disorders and painful menstrual cramps. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
21. Effects of Extracts and Flavonoids from Drosera rotundifolia L. on Ciliary Beat Frequency and Murine Airway Smooth Muscle.
- Author
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Hake, Alexander, Begrow, Frank, Spiegler, Verena, Symma, Nico, Hensel, Andreas, and Düfer, Martina
- Subjects
- *
SMOOTH muscle , *COMMON cold , *AIRWAY (Anatomy) , *ETHANOL , *FLAVONOIDS , *QUERCETIN - Abstract
Extracts from Drosera rotundifolia are traditionally used to treat cough symptoms during a common cold. The present study aimed to investigate the impact of extracts from D. rotundifolia and active compounds on the respiratory tract. Tracheal slices of C57BL/6N mice were used ex vivo to examine effects on airway smooth muscle (ASM) and ciliary beat frequency (CBF). Phosphodiesterase (PDE) inhibition assays were carried out to test whether PDE1 or PDE4 are targeted by the active compounds. An ethanol–water extract, as well as an aqueous fraction of this extract, exerted antispasmodic properties against acetylcholine-induced contractions. In addition, contractions induced by 60 mM K+ were abrogated by the aqueous fraction. Effects on ASM could be attributed to the flavonoids quercetin, 2″-O-galloylhyperoside and hyperoside. Moreover, the Drosera extract and the aqueous fraction increased the CBF of murine tracheal slices. Quercetin and 2″-O-galloylhyperoside were identified as active compounds involved in the elevation of CBF. Both compounds inhibited PDE1A and PDE4D. The elevation of CBF was mimicked by the subtype-selective PDE inhibitor rolipram (PDE4) and by 8-methoxymethyl-IBMX. In summary, our study shows, for the first time, that a Drosera extract and its flavonoid compounds increase the CBF of murine airways while antispasmodic effects were transferred to ASM. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
22. Pharmacological activities and gas chromatography-mass spectrometry analysis for the identification of bioactive compounds from Justicia adhatoda L.
- Author
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Musa, Muhammad, Jan, Gul, Jan, Farzana Gul, Hamayun, Muhammad, Irfan, Muhammad, Rauf, Abdur, Alsahammari, Abdulrahman, Alharbi, Metab, Suleria, Hafiz A. R., and Ali, Niaz
- Subjects
GAS chromatography/Mass spectrometry (GC-MS) ,ETHYL acetate ,BIOACTIVE compounds - Abstract
The current study aimed to assess the pharmacological potential of Justicia adhatoda by evaluating the presence of biologically active compounds using the gas chromatography-mass spectrometry approach and to undertake biological activities for the effectiveness of the present compounds using standard tests. A total of 21 compounds were identified in the gas chromatography-mass spectrometry analysis of the ethyl acetate fraction in which 14 of the identified compounds are recognized for their pharmacological potential in the literature. In total, four fractions (ethyl acetate, chloroform, n-hexane, and aqueous) were evaluated for pharmacological activities. In carrageenan-induced inflammation, the chloroform fraction exhibited high anti-inflammatory activity (46.51%). Similarly, the analgesic potential of ethyl acetate fraction was the most effective (300 mg/kg) in the acetic acid-induced test. Similarly, in the formalin test, ethyl acetate fraction exhibited maximum inhibition in both early (74.35%) and late phases (88.38). Maximum inhibition of pyrexia (77.98%) was recorded for the ethyl acetate fraction (300 mg/kg). In DPPH assay, the ethyl acetate fraction revealed the highest scavenging potential among other fractions (50 µg/ml resulted in 50.40% and 100 µg/ml resulted in 66.74% scavenging). [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
23. The effect of thymol on acetylcholine-induced contractions of the rat ileum and uterus under ex vivo conditions
- Author
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Blanka Premrov Bajuk, Luka Prem, Tilen Vake, Neža Žnidaršič, and Tomaž Snoj
- Subjects
Thymus vulgaris L ,thymol ,isolated organs ,antispasmodic ,dose-response ,cholinergic system ,Therapeutics. Pharmacology ,RM1-950 - Abstract
Thyme (Thymus vulgaris L.) is a well-known medicinal plant, the aerial parts of which have long been used internally or externally as a traditional remedy for various diseases. Thyme essential oils have important pharmaceutical applications and are regularly used in the pharmaceutical, food and cosmetic industries. In folk medicine, thyme preparations are used to treat respiratory, digestive, cardiovascular and nervous disorders, as well as to relieve dysmenorrhea. Thymol, a major constituent of Thymus vulgaris essential oil, has been shown to affect skeletal and smooth muscle excitation and contraction. Therefore, the main objective of this study was to evaluate its effect on acetylcholine (ACh)-induced rat intestinal and uterine preparations. Isolated ileum and uterine horn preparations were placed in a 20-ml organ bath containing Tyrode or De Jalon solution and exposed to graded concentrations of ACh (0.036, 0.109, 0.36, 1.09, 3,6, 10.9, and 36 μM) and either 0.02 or 0.2 mM thymol. Additionally, the dose–response relationship of thymol impact on intestinal and uterine contraction was evaluated. Contraction changes were monitored using an isometric transducer. Thymol at the higher dose (0.2 mM) significantly reduced ACh-induced intestinal and uterine contractions. Thus, this study provides new important data on competitive actions between thymol and ACh. In the dose–response study, the IC50 values were calculated as 5.26 mM for the ileum and 5.35 mM for the uterus. Our results demonstrated the efficacy of thymol in reducing ileal and uterine smooth muscle contractions, thus supporting the use of thyme in traditional medicine in the treatment of digestive disorders and painful menstrual cramps.
- Published
- 2022
- Full Text
- View/download PDF
24. Pharmacological activities and gas chromatography–mass spectrometry analysis for the identification of bioactive compounds from Justicia adhatoda L.
- Author
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Muhammad Musa, Gul Jan, Farzana Gul Jan, Muhammad Hamayun, Muhammad Irfan, Abdur Rauf, Abdulrahman Alsahammari, Metab Alharbi, Hafiz A. R. Suleria, and Niaz Ali
- Subjects
antioxidant ,analgesic ,antispasmodic ,anti-inflammatory ,antibacterial ,medicinal plants ,Therapeutics. Pharmacology ,RM1-950 - Abstract
The current study aimed to assess the pharmacological potential of Justicia adhatoda by evaluating the presence of biologically active compounds using the gas chromatography–mass spectrometry approach and to undertake biological activities for the effectiveness of the present compounds using standard tests. A total of 21 compounds were identified in the gas chromatography–mass spectrometry analysis of the ethyl acetate fraction in which 14 of the identified compounds are recognized for their pharmacological potential in the literature. In total, four fractions (ethyl acetate, chloroform, n-hexane, and aqueous) were evaluated for pharmacological activities. In carrageenan-induced inflammation, the chloroform fraction exhibited high anti-inflammatory activity (46.51%). Similarly, the analgesic potential of ethyl acetate fraction was the most effective (300 mg/kg) in the acetic acid-induced test. Similarly, in the formalin test, ethyl acetate fraction exhibited maximum inhibition in both early (74.35%) and late phases (88.38). Maximum inhibition of pyrexia (77.98%) was recorded for the ethyl acetate fraction (300 mg/kg). In DPPH assay, the ethyl acetate fraction revealed the highest scavenging potential among other fractions (50 μg/ml resulted in 50.40% and 100 μg/ml resulted in 66.74% scavenging).
- Published
- 2022
- Full Text
- View/download PDF
25. AGA Clinical Practice Guideline on the Pharmacological Management of Irritable Bowel Syndrome With Constipation.
- Author
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Chang, Lin, Sultan, Shahnaz, Lembo, Anthony, Verne, G. Nicholas, Smalley, Walter, and Heidelbaugh, Joel J.
- Abstract
Irritable bowel syndrome (IBS) is a common disorder of gut–brain interaction associated with significant disease burden. This American Gastroenterological Association guideline is intended to support practitioners in decisions about the use of medications for the pharmacological management of IBS-C and is an update of a prior technical review and guideline. The Grading of Recommendations Assessment, Development and Evaluation framework was used to assess evidence and make recommendations. The technical review panel prioritized clinical questions and outcomes according to their importance for clinicians and patients and conducted an evidence review of the following agents: tenapanor, plecanatide, linaclotide, tegaserod, lubiprostone, polyethylene glycol laxatives, tricyclic antidepressants, selective serotonin reuptake inhibitors, and antispasmodics. The Guideline Panel reviewed the evidence and used the Evidence-to-Decision Framework to develop recommendations. The panel agreed on 9 recommendations for the management of patients with IBS-C. The panel made a strong recommendation for linaclotide (high certainty) and conditional recommendations for tenapanor, plecanatide, tegaserod, and lubiprostone (moderate certainty), polyethylene glycol laxatives, tricyclic antidepressants, and antispasmodics (low certainty). The panel made a conditional recommendation against the use of selective serotonin reuptake inhibitors (low certainty). [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
26. Differential Nutrition-Health Properties of Ocimum basilicum Leaf and Stem Extracts.
- Author
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Bensaid, Aicha, Boudard, Frederic, Servent, Adrien, Morel, Sylvie, Portet, Karine, Guzman, Caroline, Vitou, Manon, Bichon, Florence, and Poucheret, Patrick
- Subjects
TUMOR necrosis factors ,BASIL ,AROMATIC plants ,SMOOTH muscle ,MEDICINAL plants ,EXTRACTS ,LAMIACEAE - Abstract
(1) Background: Ocimum basilicum L. is an aromatic medicinal plant of the Lamiaceae family known as sweet basil. It is used in traditional medicine for its beneficial effects on gastrointestinal disorders, inflammation, immune system, pyrexia or cancer among others. Ocimum basilicum (OB) leaf extracts contain many phytochemicals bearing the plant health effects but no reports is available on the potential bioactivity of stem extracts. Our investigation aimed at assessing the differential biological activity between basil leaf and stem to promote this co-product valorization. (2) Method: For this purpose we explored phytochemical composition of both parts of the plant. Antioxidant activity was evaluated through total polyphenol content measure, DPPH and ORAC tests. Anti-inflammatory markers on stimulated macrophages, including NO (nitric oxide), TNFa (tumor necrosis factor alpha), IL-6 (interleukin 6), MCP1 (monocyte attractant protein 1) and PGE-2 (prostaglandin E2), were evaluated. In addition, we investigated OB effects on jejunum smooth muscle contractility. (3) Results: OB extracts from leaves and stems demonstrated a different biological activity profile at the level of both antioxidant, anti-inflammatory and smooth muscle relaxation effects. (4) Conclusion: Taken together our results suggest that Ocimum basilicum extracts from co-product stems, in addition to leaves, may be of interest at the nutrition-health level with specific therapeutic potential. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
27. Dual Inhibition of Phosphodiesterase and Ca ++ Channels Explains the Medicinal Use of Balanites aegyptiaca (L.) in Hyperactive Gut Disorders.
- Author
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Rehman, Najeeb Ur, Ansari, Mohd Nazam, Ahmad, Wasim, and Ahamad, Syed Rizwan
- Subjects
ILEUM ,SPASMS ,PHOSPHODIESTERASE inhibitors ,CARBACHOL ,VERAPAMIL ,CASTOR oil ,SMALL intestine - Abstract
The present study attempted to evaluate and rationalize the medicinal use of the methanolic extract of the fruits of Balanites aegyptiaca (B. aegyptiaca) in the treatment of hyperactive gut disorders. The in vivo, castor oil-induced diarrhea model in mice was followed to test its antidiarrheal effect. To test the antispasmodic effect and to explore its pharmacodynamic details, isolated small intestines (ileum) obtained from rats were selected to provide physiological conditions for the ex vivo assays. In the in vivo assays, the orally administered extract of B. aegyptiaca protected mice from diarrheal drops with resultant percent inhibitions of 40% and 80% at the respective doses of 200 mg/kg and 400 mg/kg, while the highest protection (100%) was observed with a positive control drug, loperamide, at 10 mg/kg. In the ileum, B. aegyptiaca produced an antispasmodic effect in a concentration-dependent manner by inhibiting the carbachol (CCh; 1 µM) and high K
+ (80 mM)-evoked spasms with resultant EC50 values of 1.44 mg/mL (1.08–1.78) and 1.27 mg/mL (0.98–1.66), respectively. Papaverine, a known phosphodiesterase enzyme (PDE) inhibitor and blocker of Ca++ channels (CCB), also inhibited both CCh and high K+ induced contractions at comparable EC50 values of 8.72 µM (7.92–9.24) and 8.14 µM (7.62–8.84), respectively. Contrary to the extract and papaverine, verapamil showed distinctly higher potency in regard to inhibiting high K+ , compared to CCh-evoked spasms that had EC50 values of 0.16 µM (0.13–0.261) and 2.54 µM (2.28–2.92), respectively. The inhibitory effects of B. aegyptiaca on PDE were further confirmed when the pre-incubated extract shifted the isoprenaline-mediated relaxation curves (CRCs) towards the left, similar to papaverine, whereas the CCB-like effect was confirmed when the pre-incubated tissues with B. aegyptiaca caused deflection in the Ca++ CRCs towards the right, constructed in Ca++ free medium with suppression of the maximum response. Thus, this study provides detailed, mechanistic support for the medicinal use of B. aegyptiaca in the treatment of hyperactive gut disorders. [ABSTRACT FROM AUTHOR]- Published
- 2022
- Full Text
- View/download PDF
28. Possible Mechanisms Underlying the Antispasmodic, Bronchodilator, and Antidiarrheal Activities of Polarity–Based Extracts of Cucumis sativus L. Seeds in In Silico, In Vitro, and In Vivo Studies.
- Author
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Wahid, Muqeet, Saqib, Fatima, Akhtar, Saeed, Ali, Anam, Wilairatana, Polrat, and Mubarak, Mohammad S.
- Subjects
- *
CUCUMBERS , *ANTIDIARRHEALS , *ANTISPASMODICS , *SMOOTH muscle contraction , *SEEDS , *CONTRACTILE proteins , *MOLECULAR pharmacology , *NUTRITIONAL value - Abstract
Apart from the nutritional value, Cucumis sativus L. has also been used in the traditional medicine of Iran, Pakistan, and India. Its seeds are used by herbalists to treat gastrointestinal, respiratory, and urinary problems. However, more investigations are required to explain its mechanisms for treating GI, respiratory, and urinary diseases. Accordingly, the aim of the present work was to investigate the antispasmodic, bronchodilator, and antidiarrheal activities of C. sativus seeds extracts and the underlying mechanisms of action. For this purpose, sequential extracts of C. sativus seeds were prepared in n-hexane, dichloromethane, ethanol, and water. Bioactive compounds in C. sativus seed extracts were identified and quantified by utilizing LC ESI–MS/MS and HPLC. Moreover, network pharmacology and molecular docking were employed to examine the antispasmodic and bronchodilator effects of the bioactive substances in the extracts. In vitro and in vivo experiments were also conducted to validate the mechanistic insights gained from the in silico analysis. Results indicated the presence of kaempferol with a concentration of 813.74 µg/g (highest concentration) in the seed extract of C. sativus, followed by quercetin (713.83 µg/g), narcissin (681.87 µg/g), and orientin (676.19 µg/g). In silico investigations demonstrated that the bioactive chemicals in C. sativus seeds inhibited the expression of the target genes involved in smooth muscle contraction and calcium-mediated signaling. Sequential seed extracts of C. sativus caused a dose-dependent relaxant response for spasmolytic reaction and resulted in a relaxation of K+ (80 mM) spastic contraction. In animal models, C. sativus seed extracts exhibited partial or complete antiperistalsis, antidiarrheal, and antisecretory actions. By modulating the contractile response through calcium-mediated signaling target proteins, C. sativus seeds generated bronchodilator, antispasmodic, and antidiarrheal therapeutic effects. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
29. Comparison of 5 Rectal Preparation Strategies for Prostate MRI and Impact on Image Quality.
- Author
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Sathiadoss, Paul, Haroon, Mohammad, Osman, Heba, Ahmad, Faraz, Papadatos, Philip, and Schieda, Nicola
- Subjects
- *
KRUSKAL-Wallis Test , *STATISTICS , *THREE-dimensional imaging , *ANALYSIS of variance , *BOWEL preparation (Procedure) , *PROSTATE , *MAGNETIC resonance imaging , *COMPARATIVE studies , *T-test (Statistics) , *PARASYMPATHOLYTIC agents , *DATA analysis , *ENEMA , *MEDICAL artifacts - Abstract
Purpose: To compare 5 different rectal preparation strategies for prostate MRI. Methods: This 5-arm quality-assurance study evaluated 56 patients per arm (280 patients) including: no preparation, clear-fluids diet (CFD) beginning at 00:00 hours on the day of MRI, Fleet®-enema, enema + CFD, enema + CFD + IV-antispasmodic agent. The study was powered to 0.80 with alpha-error of 0.05. Three blinded radiologists independently evaluated T2-Weighted (T2W) and Diffusion Weighed Imaging (DWI) for: rectal diameter (maximal AP diameter), rectal content (stool, fluid, gas), rectal motion, T2W/DWI image quality, T2W image sharpness and DWI susceptibility artifact using 5-point Likert scales. Overall comparisons were performed using analysis of variance (ANOVA) and Kruskal-Wallis, with pair-wise comparisons using paired t-tests and Wilcoxon sign-rank tests. Results: Rectal diameter and amount of gas were lower in enema compared to non-enema groups (p < 0.001), with smallest diameter and least gas in the enema + CFD + IV-antispasmodic group (p = 0.022-<0.001). T2W image quality and sharpness were highest in the enema + CFD groups (p < 0.001) with no difference comparing enema + CFD with/without IV-antispasmodic (p = 0.064, 0.084). Motion artifact was least in enema + CFD + IV-antispasmodic group compared to all other groups (p < 0.001), followed by the enema + CFD group (p = 0.008-<0.001). DWI image quality was highest (p < 0.001) and DWI susceptibility artifact lowest (p < 0.001) in the enema + CFD groups (p < 0.001) and did not differ comparing enema + CFD with/without anti-spasmodic (p = 0.058-0.202). Conclusions: Use of enema + clear-fluids diet before prostate MRI yields the highest T2W and DWI image quality with the least DWI artifact. IV-antispasmodic use reduces motion on T2W but does not improve image quality on T2W or DWI, or lessen DWI artifact compared to enema + clear-fluids diet. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
30. New insights into the characterization of the mechanism of action of hyoscine butylbromide in the human colon ex vivo.
- Author
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Traserra, Sara, Alcalá-González, Luis Gerardo, Barber, Claudia, Landolfi, Stefania, Malagelada, Carolina, Lange, Robert, Forestier, Sylvie, Corsetti, Maura, and Jimenez, Marcel
- Subjects
- *
MUSCARINIC receptors , *NERVE block , *NEURAL pathways , *COLON (Anatomy) , *MOTOR neurons , *ATROPINE , *ELECTRIC stimulation , *CHOLINERGIC receptors - Abstract
Hyoscine butylbromide (HBB) is one of the most used antispasmodics in clinical practice. Recent translational consensus has demonstrated a similarity between human colonic motor patterns studied ex vivo and in vivo, suggesting ex vi vo can predict in vivo results. It is unclear whether the mechanism of action of antispasmodics can predict different use in clinical practice. The aim of the present study is to bridge this gap dissecting HBB's role in excitatory and inhibitory neural pathways. Methods: 309 colon samples from 48 patients were studied in muscle bath experiments. HBB was tested on: 1-spontaneous phasic contractions (SPCs); 2-carbachol-induced contractility; electrical field stimulation (EFS)-induced selective stimulation of 3-excitatory and 4-inhibitory pathways and 5- SPCs and EFS-induced contractions enhanced by neostigmine. Atropine, AF-DX116 (M2 blocker) and DAU-5884 (M3 blocker) were used as comparators. In the presence of tetrodotoxin (TTX), HBB and atropine 1 μM reduced SPCs. HBB and atropine concentration-dependently reduced carbachol- and EFS-induced contractions. Inhibitory effects of DAU-5884 on EFS-induced contractions were more potent than of AF-DX116. HBB did not affect the off-response associated to neural inhibitory responses. Neostigmine enhanced both SPCs and EFS-induced contractions. In the presence of TTX and ω-conotoxin (GVIA), neostigmine still enhanced SPCs. Addition of HBB and atropine reduced these responses. This study demonstrates that HBB inhibits neural cholinergic contractions associated to muscarinic (mainly M3) receptors. HBB has a potential role in reducing colonic spasm induced by the release of acetylcholine from enteric motor neurons and from an atypical source including a potential non-neuronal origin. • Hyoscine Butylbromide (HBB) reduced colonic contractions. • The receptor involved in the response is mainly the M3 muscarinic receptor. • Neural-mediated relaxation and its off-contraction were unaffected by HBB. • After neural blockade, HBB reduced contractions enhanced with neostigmine. • HBB reduces spasms of neural and potentially non-neural origin. [ABSTRACT FROM AUTHOR]
- Published
- 2024
- Full Text
- View/download PDF
31. Biological Characterization of Polystichum lonchitis L. for Phytochemical and Pharmacological Activities in Swiss Albino Mice Model
- Author
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Jan Sher, Gul Jan, Muhammad Israr, Muhammad Irfan, Nighat Yousuf, Fazal Ullah, Abdur Rauf, Abdulrahman Alshammari, and Metab Alharbi
- Subjects
analgesic ,anti-inflammatory ,antipyretic ,antispasmodic ,antioxidant ,phytochemistry ,Botany ,QK1-989 - Abstract
Polystichum lonchitis L. is a fern belonging to the family Dryopteridaceae. The present study was conducted to evaluate its pharmacological, antioxidant, and phytochemical properties, and to conduct GC–MS screening of P. lonchitis. The acetic acid-induced writhing test, yeast-induced hyperpyrexia method, carrageenan-induced rat paw edema model, and charcoal meal test model were carried out to assess analgesic, antipyretic, anti-inflammatory, and antispasmodic activity, respectively. DPPH was used as an antioxidant, while the phytochemical screening was conducted using standard scientific methods. Among the pharmacological activities, the most significant effects were observed in the analgesic and anti-inflammatory activities, followed by the antipyretic and antispasmodic activities, at a dose of 450 mg/kg after the 4th hour, compared with 150 mg/kg and 300 mg/kg. For the evaluation of antioxidant activities, the most significant results were detected in the methanolic and aqueous extracts. The detection of flavonoids and phenol occurred most significantly in the methanolic extract, and then in the ethanolic and aqueous extracts. The main compounds detected using GC–MS analysis with a high metabolic rate was 𝛼-D-Galactopyranoside, which had a metabolic rate of 0.851, and methyl and n-hexadecanoic, which had a metabolic rate of 0.972. Overall, the results suggested that P. lonchitis had a strong potential for pharmacological activities. The suggested assessment provided a way to isolate the bioactive constituents and will help to provide new medicines with fewer side effects. Due to the fern’s effectiveness against various diseases, the results provide clear evidence that they also have the potential to cure various diseases.
- Published
- 2023
- Full Text
- View/download PDF
32. GC–MS Analysis and In Vivo and Ex Vivo Antidiarrheal and Antispasmodic Effects of the Methanolic Extract of Acacia nilotica.
- Author
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Rehman, Najeeb Ur, Ansari, Mohd Nazam, Ahmad, Wasim, and Amir, Mohd
- Subjects
- *
ANTIDIARRHEALS , *ACACIA nilotica , *CALCIUM antagonists , *GAS chromatography/Mass spectrometry (GC-MS) , *FATTY acid esters , *PHOSPHODIESTERASE inhibitors , *LABORATORY mice , *MUSCARINIC acetylcholine receptors - Abstract
This present study evaluated and rationalized the medicinal use of the fruit part of Acacia nilotica methanolic extract. The phytochemicals were detected using gas chromatography–mass spectrometry (GC–MS) while the in vivo antidiarrheal test was done using Swiss albino mice. To determine the details of the mechanism(s) involved in the antispasmodic effect, isolated rat ileum was chosen using different ex vivo assays by maintaining a physiological environment. GC–MS results showed that A. nilotica contained pyrogallol as the major polyphenol present (64.04%) in addition to polysaccharides, polyphenol, amino acid, steroids, fatty acid esters, and triterpenoids. In the antidiarrheal experiment, A. nilotica inhibited diarrheal episodes in mice significantly (p < 0.05) by 40% protection of mice at 200 mg/kg, while 80% protection was observed at 400 mg/kg by the orally administered extract. The highest antidiarrheal effect was observed with loperamide (p < 0.01), used as a control drug. In the ex vivo experiments, A. nilotica inhibited completely in increasing concentrations (0.3 to 10 mg/mL) the carbachol (CCh; 1 µM) and high K+ (80 mM)-evoked spasms in ileum tissues at equal potencies (p > 0.05), similar to papaverine, a dual inhibitor of the phosphodiesterase enzyme (PDE) and Ca++ channels. The dual inhibitory-like effects of A. nilotica on PDE and Ca++ were further validated when A. nilotica extract (1 and 3 mg/mL)-pre-incubated ileum tissues potentiated and shifted isoprenaline relaxation curves towards lower doses (leftward), similar to papaverine, thus confirming the PDE inhibitory-like mechanism whereas its CCB-like effect of the extract was confirmed at 3 and 5 mg/mL by non-specific inhibition of CaCl2-mediated concentration response curves towards the right with suppression of the maximum peaks, similar to verapamil, used as standard CCB. Thus, this study characterized the chemical composition and provides mechanistic support for medicinal use of A. nilotica in diarrheal and hyperactive gut motility disorders. [ABSTRACT FROM AUTHOR]
- Published
- 2022
- Full Text
- View/download PDF
33. Antidiarrheal and Antioxidant Activities of the Aerial Parts of Caralluma dalzielii N. E. Brown.
- Author
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Ugwah-Oguejiofor, Chinenye J., Mshelia, Halilu E., Bello, Junaidu, Inuwa, Isah, and Sulaiman, Abdullahi
- Subjects
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ANTIDIARRHEALS , *GASTROINTESTINAL motility , *FERRIC chloride , *ANIMAL droppings , *VITAMIN C , *SMOOTH muscle contraction , *LABORATORY rats - Abstract
Background: Caralluma dalzielii N.E. Brown is commonly referred to as "Karan massalanci" in the Northwest Nigeria where it is used in treating several ailments including pain, diarrhea and stomach issues. Objectives: This study was aimed to investigate the antidiarrheal and antioxidant activities of aqueous aerial parts extract of Caralluma dalzielii. Materials and Methods: The aqueous aerial parts extract of Caralluma dalzielii (CDE) (100, 200 and 400 mg/kg) was evaluated for antidiarrheal properties against gastrointestinal motility, castor oil-induced and prostaglandin-E2 (PGE2) enteropooling models in Wistar rats. Its antioxidant properties were studied by determining the total phenolic content (TPC) using Folin-Ciocalteu reagent, its free radical scavenging activity using 1, 1-Diphenyl-2-Picrylhydrazyl (DPPH) and its ferric reducing antioxidant power (FRAP) assays using potassium ferrocyanide ferric chloride methods. Ascorbic acid was used as the reference. Spasmolytic effect was studied in isolated rabbit jejunum preparations in an organ bath experiment using acetylcholine (ACh). Results: CDE significantly (p<0.05) reduced gastrointestinal transit of charcoal meal and the total number of diarrheal feces in the animals. The total phenolic content was determined to be 36.67±3.33 mg GAE/g. IC50 value of 63.44 mg/mL was calculated in DPPH assay. The FRAP value was found to increase as the concentration of the extract increased. CDE inhibited acetylcholine-induced contraction of the rabbit jejunum in a concentration dependent manner with complete inhibition at 20.48 mg/mL of the extract. Conclusion: The extract of Caralluma dalzielii possesses antidiarrheal activities which may be related to its antimotility, antioxidant and antispasmodic properties. [ABSTRACT FROM AUTHOR]
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- 2022
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34. Intestinal/uterine antispasmodics, sedative effects of Fuchsia magellanica Lam. leaves’ and flowers’ extracts and their flavonolic components
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Ana María Bernal Ochoa, MSc, Germán A. Colareda, PhD, Soledad Matera, MSc, María Inés Ragone, PhD, Santiago Isolabella, Rosana Filip, PhD, and Alicia E. Consolini, PhD
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Fuchsia magellanica ,Antispasmodic ,Intestine ,uterus ,Open-field test ,Flavonoids ,Other systems of medicine ,RZ201-999 - Abstract
Background: Fuchsia magellanica Lam. (Onagraceae) is a native plant of the Andean-Patagonian region, and it is also naturalized in Argentina and other parts of the world. Leaves are used for treating indigestion, stomachache, as sedative, for difficult delivery and as antiemmenagogue. However, up to now the pharmacological basis of such uses were not studied. Purpose: This work evaluates the gastrointestinal, uterine and sedative effects of leaves (L) and flowers (F) tinctures of F. magellanica from wild patagonian (T-Fm-P) and naturalized (T-Fm-BA) plants, as well as the mechanism of action and the flavonoids profile of both plants. Methods: Phytochemical studies were evaluated by using TLC and HPLC methodologies. The ex-vivo effects of T-Fm-BA and T-Fm-P were evaluated on contractile concentration-response curves (CRC) of carbachol (CCh) and calcium (Ca2+) in rat isolated intestinal and uterine tissues. In vivo tests for intestinal transit, elevated cross plus-maze and open-field tests were performed in mice. Results: Wild and cultivated leaves and flowers ethanolic extracts induced antispasmodic effect, as a non-competitive inhibitor of the CCh-CRC in intestine, with IC50 of 272.8 ± 64.3 µg/ml for T-L-Fm-P and 257.4 ± 36 µg/ml for T-L-Fm-BA. A similar effect was obtained in Ca2+-CRC with IC50 of 152.9 ± 29.1 µg/ml and 138.4 ± 48.6 µg/ml respectively. Mice intestinal transit was reduced at oral doses of 73.5 mg/kg of T-L-Fm-P. In uterine tissues, both T-L-Fm reduced the contractions of CCh CRC´s as non-competitive antagonists, with IC50 near those in intestine. The T-L-Fm-BA also inhibited the serotonin CRC´s and contribution of other relaxing mechanisms was investigated. Although extracts didn't show anxiolytic effect in the elevated cross plus-maze test, they reduced the spontaneous activity of mice in the open-field at 32.7 mg/kg T-L-Fm-P and 41.7 mg/kg T-L-Fm-BA. Conclusions: Leaves and flowers ethanolic extracts from wild and cultivated plant F. magellanica showed intestinal and uterine antispasmodic effects, mainly by interfering with Ca2+ influx. In mice, the ethanolic extracts reduced the intestinal transit and showed sedative effect. The effects agree with the presence of flavonoids, such as quercetin and kaempferol. This is the first study which gives experimental support for some of the traditional uses of F. magellanica.
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- 2021
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35. Effects of Extracts and Flavonoids from Drosera rotundifolia L. on Ciliary Beat Frequency and Murine Airway Smooth Muscle
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Alexander Hake, Frank Begrow, Verena Spiegler, Nico Symma, Andreas Hensel, and Martina Düfer
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Drosera rotundifolia ,antispasmodic ,trachea ,ciliary beat frequency ,phosphodiesterase ,Organic chemistry ,QD241-441 - Abstract
Extracts from Drosera rotundifolia are traditionally used to treat cough symptoms during a common cold. The present study aimed to investigate the impact of extracts from D. rotundifolia and active compounds on the respiratory tract. Tracheal slices of C57BL/6N mice were used ex vivo to examine effects on airway smooth muscle (ASM) and ciliary beat frequency (CBF). Phosphodiesterase (PDE) inhibition assays were carried out to test whether PDE1 or PDE4 are targeted by the active compounds. An ethanol–water extract, as well as an aqueous fraction of this extract, exerted antispasmodic properties against acetylcholine-induced contractions. In addition, contractions induced by 60 mM K+ were abrogated by the aqueous fraction. Effects on ASM could be attributed to the flavonoids quercetin, 2″-O-galloylhyperoside and hyperoside. Moreover, the Drosera extract and the aqueous fraction increased the CBF of murine tracheal slices. Quercetin and 2″-O-galloylhyperoside were identified as active compounds involved in the elevation of CBF. Both compounds inhibited PDE1A and PDE4D. The elevation of CBF was mimicked by the subtype-selective PDE inhibitor rolipram (PDE4) and by 8-methoxymethyl-IBMX. In summary, our study shows, for the first time, that a Drosera extract and its flavonoid compounds increase the CBF of murine airways while antispasmodic effects were transferred to ASM.
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- 2022
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36. Possible Mechanisms Underlying the Antispasmodic, Bronchodilator, and Antidiarrheal Activities of Polarity–Based Extracts of Cucumis sativus L. Seeds in In Silico, In Vitro, and In Vivo Studies
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Muqeet Wahid, Fatima Saqib, Saeed Akhtar, Anam Ali, Polrat Wilairatana, and Mohammad S. Mubarak
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Cucumis sativus ,cucumber ,LC ESI–MS/MS ,bronchodilator ,antispasmodic ,antidiarrheal effects ,Medicine ,Pharmacy and materia medica ,RS1-441 - Abstract
Apart from the nutritional value, Cucumis sativus L. has also been used in the traditional medicine of Iran, Pakistan, and India. Its seeds are used by herbalists to treat gastrointestinal, respiratory, and urinary problems. However, more investigations are required to explain its mechanisms for treating GI, respiratory, and urinary diseases. Accordingly, the aim of the present work was to investigate the antispasmodic, bronchodilator, and antidiarrheal activities of C. sativus seeds extracts and the underlying mechanisms of action. For this purpose, sequential extracts of C. sativus seeds were prepared in n-hexane, dichloromethane, ethanol, and water. Bioactive compounds in C. sativus seed extracts were identified and quantified by utilizing LC ESI–MS/MS and HPLC. Moreover, network pharmacology and molecular docking were employed to examine the antispasmodic and bronchodilator effects of the bioactive substances in the extracts. In vitro and in vivo experiments were also conducted to validate the mechanistic insights gained from the in silico analysis. Results indicated the presence of kaempferol with a concentration of 813.74 µg/g (highest concentration) in the seed extract of C. sativus, followed by quercetin (713.83 µg/g), narcissin (681.87 µg/g), and orientin (676.19 µg/g). In silico investigations demonstrated that the bioactive chemicals in C. sativus seeds inhibited the expression of the target genes involved in smooth muscle contraction and calcium-mediated signaling. Sequential seed extracts of C. sativus caused a dose-dependent relaxant response for spasmolytic reaction and resulted in a relaxation of K+ (80 mM) spastic contraction. In animal models, C. sativus seed extracts exhibited partial or complete antiperistalsis, antidiarrheal, and antisecretory actions. By modulating the contractile response through calcium-mediated signaling target proteins, C. sativus seeds generated bronchodilator, antispasmodic, and antidiarrheal therapeutic effects.
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- 2022
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37. Dual Inhibition of Phosphodiesterase and Ca++ Channels Explains the Medicinal Use of Balanites aegyptiaca (L.) in Hyperactive Gut Disorders
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Najeeb Ur Rehman, Mohd Nazam Ansari, Wasim Ahmad, and Syed Rizwan Ahamad
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B. aegyptiaca ,antispasmodic ,Ca++ channel blocker ,phosphodiesterase inhibitor ,Botany ,QK1-989 - Abstract
The present study attempted to evaluate and rationalize the medicinal use of the methanolic extract of the fruits of Balanites aegyptiaca (B. aegyptiaca) in the treatment of hyperactive gut disorders. The in vivo, castor oil-induced diarrhea model in mice was followed to test its antidiarrheal effect. To test the antispasmodic effect and to explore its pharmacodynamic details, isolated small intestines (ileum) obtained from rats were selected to provide physiological conditions for the ex vivo assays. In the in vivo assays, the orally administered extract of B. aegyptiaca protected mice from diarrheal drops with resultant percent inhibitions of 40% and 80% at the respective doses of 200 mg/kg and 400 mg/kg, while the highest protection (100%) was observed with a positive control drug, loperamide, at 10 mg/kg. In the ileum, B. aegyptiaca produced an antispasmodic effect in a concentration-dependent manner by inhibiting the carbachol (CCh; 1 µM) and high K+ (80 mM)-evoked spasms with resultant EC50 values of 1.44 mg/mL (1.08–1.78) and 1.27 mg/mL (0.98–1.66), respectively. Papaverine, a known phosphodiesterase enzyme (PDE) inhibitor and blocker of Ca++ channels (CCB), also inhibited both CCh and high K+ induced contractions at comparable EC50 values of 8.72 µM (7.92–9.24) and 8.14 µM (7.62–8.84), respectively. Contrary to the extract and papaverine, verapamil showed distinctly higher potency in regard to inhibiting high K+, compared to CCh-evoked spasms that had EC50 values of 0.16 µM (0.13–0.261) and 2.54 µM (2.28–2.92), respectively. The inhibitory effects of B. aegyptiaca on PDE were further confirmed when the pre-incubated extract shifted the isoprenaline-mediated relaxation curves (CRCs) towards the left, similar to papaverine, whereas the CCB-like effect was confirmed when the pre-incubated tissues with B. aegyptiaca caused deflection in the Ca++ CRCs towards the right, constructed in Ca++ free medium with suppression of the maximum response. Thus, this study provides detailed, mechanistic support for the medicinal use of B. aegyptiaca in the treatment of hyperactive gut disorders.
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- 2022
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38. GC–MS Analysis and In Vivo and Ex Vivo Antidiarrheal and Antispasmodic Effects of the Methanolic Extract of Acacia nilotica
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Najeeb Ur Rehman, Mohd Nazam Ansari, Wasim Ahmad, and Mohd Amir
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A. nilotica ,antispasmodic ,Ca++ channel blocker ,GC-MC ,phosphodiesterase inhibitor ,Organic chemistry ,QD241-441 - Abstract
This present study evaluated and rationalized the medicinal use of the fruit part of Acacia nilotica methanolic extract. The phytochemicals were detected using gas chromatography–mass spectrometry (GC–MS) while the in vivo antidiarrheal test was done using Swiss albino mice. To determine the details of the mechanism(s) involved in the antispasmodic effect, isolated rat ileum was chosen using different ex vivo assays by maintaining a physiological environment. GC–MS results showed that A. nilotica contained pyrogallol as the major polyphenol present (64.04%) in addition to polysaccharides, polyphenol, amino acid, steroids, fatty acid esters, and triterpenoids. In the antidiarrheal experiment, A. nilotica inhibited diarrheal episodes in mice significantly (p < 0.05) by 40% protection of mice at 200 mg/kg, while 80% protection was observed at 400 mg/kg by the orally administered extract. The highest antidiarrheal effect was observed with loperamide (p < 0.01), used as a control drug. In the ex vivo experiments, A. nilotica inhibited completely in increasing concentrations (0.3 to 10 mg/mL) the carbachol (CCh; 1 µM) and high K+ (80 mM)-evoked spasms in ileum tissues at equal potencies (p > 0.05), similar to papaverine, a dual inhibitor of the phosphodiesterase enzyme (PDE) and Ca++ channels. The dual inhibitory-like effects of A. nilotica on PDE and Ca++ were further validated when A. nilotica extract (1 and 3 mg/mL)-pre-incubated ileum tissues potentiated and shifted isoprenaline relaxation curves towards lower doses (leftward), similar to papaverine, thus confirming the PDE inhibitory-like mechanism whereas its CCB-like effect of the extract was confirmed at 3 and 5 mg/mL by non-specific inhibition of CaCl2-mediated concentration response curves towards the right with suppression of the maximum peaks, similar to verapamil, used as standard CCB. Thus, this study characterized the chemical composition and provides mechanistic support for medicinal use of A. nilotica in diarrheal and hyperactive gut motility disorders.
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- 2022
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39. Calcium Channel Inhibitory Effect of Marjoram ( Origanum majorana L.): Its Medicinal Use in Diarrhea and Gut Hyperactivity.
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Rehman NU, Ansari MN, Ahmad W, and Ali A
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- Rats, Mice, Animals, Jejunum, Plant Extracts pharmacology, Plant Extracts therapeutic use, Plant Extracts chemistry, Castor Oil pharmacology, Castor Oil therapeutic use, Diarrhea drug therapy, Verapamil pharmacology, Verapamil therapeutic use, Calcium Channels, Spasm drug therapy, Antidiarrheals pharmacology, Antidiarrheals therapeutic use, Antidiarrheals chemistry, Origanum
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Background: The leaves of Origanum majorana ( O. majorana ) are traditionally renowned for treating diarrhea and gut spasms. This study was therefore planned to evaluate its methanolic extract., Methods: Gas chromatography-mass spectrometry (GC-MS) was used to identify the phytochemicals, and Swiss albino mice were used for an in vivo antidiarrheal assay. Isolated rat ileum was used as an ex vivo assay model to study the possible antispasmodic effect and its mechanism(s)., Results: The GC-MS analysis of O. majorana detected the presence of 21 compounds, of which alpha-terpineol was a major constituent. In the antidiarrheal experiment, O. majorana showed a substantial inhibitory effect on diarrheal episodes in mice at an oral dosage of 200 mg/kg, resulting in 40% protection. Furthermore, an oral dosage of 400 mg/kg provided even greater protection, with 80% effectiveness. Similarly, loperamide showed 100% protection at oral doses of 10 mg/kg. O. majorana caused complete inhibition of carbachol (CCh, 1 µM) and high K+ (80 mM)-evoked spasms in isolated ileal tissues by expressing significantly higher potency ( p < 0.05) against high K+ compared to CCh, similar to verapamil, a Ca++ antagonist. The verapamil-like predominant Ca++ ion inhibitory action of O. majorana was further confirmed in the ileal tissues that were made Ca++-free by incubating the tissues in a physiological salt solution having ethylenediaminetetraacetic acid (EDTA) as a chelating agent. The preincubation of O. majorana at increasing concentrations (0.3 and 1 mg/mL) shifted towards the right of the CaCl2-mediated concentration-response curves (CRCs) with suppression of the maximum contraction. Similarly, verapamil also caused non-specific suppression of Ca++ CRCs towards the right, as expected., Conclusions: Thus, this study conducted an analysis to determine the chemical constituents of the leaf extract of O. majorana and provided a detailed mechanistic basis for the medicinal use of O. majorana in hyperactive gut motility disorders., Competing Interests: The authors declare no conflict of interest., (© 2024 The Author(s). Published by IMR Press.)
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- 2024
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40. Phytochemical Analysis, Antispasmodic, Myorelaxant, and Antioxidant Effect of Dysphania ambrosioides (L.) Mosyakin and Clemants Flower Hydroethanolic Extracts and Its Chloroform and Ethyl Acetate Fractions
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Fahd Kandsi, Raffaele Conte, Mohamed Marghich, Fatima Zahra Lafdil, Mohamed F. Alajmi, Mohamed Bouhrim, Hamza Mechchate, Christophe Hano, Mohammed Aziz, and Nadia Gseyra
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antispasmodic ,rat jejunum ,rabbit jejunum ,carbachol ,verapamil ,extraction ,Organic chemistry ,QD241-441 - Abstract
Dysphania ambrosioides (L.) Mosyakin and Clemants is an annual or ephemeral perennial herb used traditionally in the Mediterranean region in folk medicine to treat various illnesses, including those related to the digestive system. This study aims to assess the antispasmodic, myorelaxant, and antioxidant effects of D. ambrosioides flower hydroethanolic extract and its chloroform and ethyl acetate fractions in a comparative study to evaluate the result of the extraction type on the potential activity of the extract. Both rat and rabbit jejunum were used to evaluate the antispasmodic and myorelaxant effect, while the antioxidant effect was evaluated using DPPH, a ferric reducing power assay, and a beta-carotene bleaching test. LC/MS-MS analysis was carried out to reveal the composition of the different types of extract. Following the results, the hydroethanolic extract showed a significant myorelaxant effect (IC50 = 0.39 ± 0.01 mg/mL). Moreover, it was shown that the hydroethanolic extract demonstrated the best antispasmodic activity (IC50 = 0.51 ± 0.05 mg/mL), followed by the ethyl acetate (IC50 = 4.05 ± 0.32 mg/mL) and chloroform (IC50 = 4.34 ± 0.45 mg/mL) fractions. The antioxidant tests showed that the hydroethanolic extract demonstrated high antioxidant activity, followed by the ethyl acetate and chloroform fractions. The LC/MS-MS analysis indicates that the plant extract was rich in flavonoids, to which the extract activity has been attributed. This study supports the traditional use of this plant to treat digestive problems, especially those with spasms.
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- 2021
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41. Pharmacological Basis for the Antidiarrheal and Antispasmodic Effects of Cuminaldehyde in Experimental Animals: In Silico , Ex Vivo and In Vivo Studies.
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Ansari MN, Rehman NU, Samad A, and Ahmad W
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- Rats, Mice, Animals, Cromakalim adverse effects, Glyburide adverse effects, Plant Extracts pharmacology, Jejunum, Diarrhea chemically induced, Diarrhea drug therapy, Verapamil adverse effects, Adenosine Triphosphate, Antidiarrheals adverse effects, Parasympatholytics adverse effects, Cymenes, Benzaldehydes
- Abstract
Background: Medicinal herbs are frequently used for the management of gastrointestinal disorders because they contain various compounds that can potentially amplify the intended therapeutic effects. Cuminaldehyde is a plant-based constituent found in oils derived from botanicals such as cumin, eucalyptus, myrrh, and cassia and is responsible for its health benefits. Despite the utilization of cuminaldehyde for several medicinal properties, there is currently insufficient scientific evidence to support its effectiveness in treating diarrhea. Hence, the present investigation was carried out to evaluate the antidiarrheal and antispasmodic efficacy of cuminaldehyde, with detailed pharmacodynamics explored., Methods: An in vivo antidiarrheal test was conducted in mice following the castor oil-induced diarrhea model, while an isolated small intestine obtained from rats was used to evaluate the detailed mechanism(s) of antispasmodic effects., Results: Cuminaldehyde, at 10 and 20 mg/kg, exhibited 60 and 80% protection in mice from episodic diarrhea compared to the saline control group, whereas this inhibitory effect was significantly reversed in the pretreated mice with glibenclamide, similar to cromakalim, an ATP-dependent K+ channel opener. In the ex vivo experiments conducted in isolated rat tissues, cuminaldehyde reversed the glibenclamide-sensitive low K+ (25 mM)-mediated contractions at significantly higher potency compared to its inhibitory effect against high K+ (80 mM), thus showing predominant involvement of ATP-dependent K+ activation followed by Ca++ channel inhibition. Cromakalim, a standard drug, selectively suppressed the glibenclamide-sensitive low K+-induced contractions, whereas no relaxation was observed against high K+, as expected. Verapamil, a Ca++ channel inhibitor, effectively suppressed both low and high K+-induced contractions with similar potency, as anticipated. At higher concentrations, the inhibitory effect of cuminaldehyde against Ca++ channels was further confirmed when the preincubated ileum tissues with cuminaldehyde (3 and 10 mM) in Ca++ free medium shifted CaCl2-mediated concentration-response curves (CRCs) towards the right with suppression of the maximum peaks, similar to verapamil, a standard Ca++ ion inhibitor., Conclusions: Present findings support the antidiarrheal and antispasmodic potential of cuminaldehyde, possibly by the predominant activation of ATP-dependent K+ channels followed by voltage-gated Ca++ inhibition. However, further in-depth assays are recommended to know the precise mechanism and to elucidate additional unexplored mechanism(s) if involved., Competing Interests: The authors declare no conflict of interest., (© 2024 The Author(s). Published by IMR Press.)
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- 2024
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42. Antispasmodic and antidiarrheal effects of Juniperus oxycedrus L. on the jejunum in rodents.
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Amrani O, Karim A, Marghich M, Beyi L, Bouknana S, and Aziz M
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- Animals, Mice, Rats, Male, Gastrointestinal Transit drug effects, Rats, Wistar, Gastrointestinal Motility drug effects, Muscle, Smooth drug effects, Muscle Contraction drug effects, Jejunum drug effects, Jejunum metabolism, Antidiarrheals pharmacology, Parasympatholytics pharmacology, Plant Extracts pharmacology, Juniperus chemistry, Diarrhea drug therapy, Diarrhea chemically induced, Castor Oil
- Abstract
Functional bowel disorders (FBD) have a major potential to degrade the standards of public life. Juniperus oxycedrus L. (J. oxycedrus) (Cupressaceae) has been described as a plant used in traditional medicine as an antidiarrheal medication. The present study is the first to obtain information on the antispasmodic and antidiarrheic effects of J. oxycedrus aqueous extract through in vitro and in vivo studies. An aqueous extract of J. oxycedrus (AEJO) was extracted by decoctioning air-dried aerial sections of the plant. Antispasmodic activity was tested in an isolated jejunum segment of rats exposed to cumulative doses of drogue extract. The antidiarrheic activity was tested using diarrhea caused by castor oil, a transit study of the small intestine, and castor oil-induced enteropooling assays in mice. In the jejunum of rats, the AEJO (0.1, 0.3 and 1 mg/ml) diminished the maximum tone induced by low K
+ (25 mM), while it exhibited a weak inhibitory effect on high K+ (75 mM) with an IC50 =0.49 ± 0.01 mg/ml and IC50 =2.65 ± 0.16 mg/ml, respectively. In the contractions induced by CCh (10-6 M), AEJO diminished the maximum tone, similar to that induced by low K+ (25 mM). with an IC50 =0.45 ± 0.02 mg/ml. The inhibitory effect of AEJO on low K+ induced contractions was significantly diminished in the presence of glibenclamide (GB) (0.3 µM) and 4-aminopyrimidine (4-AP) (100 µM), with IC50 values of 1.84 ± 0.09 mg/ml. and 1.63 ± 0.16 mg/ml, respectively). The demonstrated inhibitory effect was similar to that produced by a non-competitive antagonist acting on cholinergic receptors and calcium channels. In castor oil-induced diarrhea in mice, AEJO (100, 200, and 400 mg/kg) caused an extension of the latency time, a reduced defecation frequency, and a decrease in the amount of wet feces compared to the untreated group (distilled water). Moreover, it showed a significant anti-motility effect and reduced the amount of fluid accumulated in the intestinal lumen at all tested doses. These findings support the conventional use of Juniperus oxycedrus L. as a remedy for gastrointestinal diseases.- Published
- 2024
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43. Antispasmodic, antidepressant and anxiolytic effects of extracts from Schinus lentiscifolius Marchand leaves
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Germán A. Colareda, Daiana Retta, Julián J. Prieto, Matías Bayley, María Inés Ragone, Alicia E. Consolini, María Esperanza Ruiz, Soledad Inés Matera, Catalina Vanegas Andrade, and Catalina van Baren
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SCHINUS LENTISCIFOLIUS ,Schinus ,biology ,Traditional medicine ,medicine.drug_class ,ANTIDEPRESSANT ,ANXIOLYTIC ,purl.org/becyt/ford/3.1 [https] ,biology.organism_classification ,Anxiolytic ,law.invention ,ESSENTIAL OIL ,Complementary and alternative medicine ,Smooth muscle ,law ,SMOOTH MUSCLE ,medicine ,Antidepressant ,purl.org/becyt/ford/3 [https] ,Antispasmodic ,Essential oil ,medicine.drug - Abstract
Schinus lentiscifolius (Anacardiaceae) is widely used in folk medicine for treating gastrointestinal and emotional complaints but there are no scientific studies that support these uses. This work aims at evaluating the antispasmodic and central effects of S. lentiscifolius as well as the flavonoids presence in the tincture (SchT) and the composition of the essential oil (SchO). SchT inhibited the concentration-response curves (CRC) of carbachol and calcium in a non-competitive way in isolated rat intestine, bladder and uterus. SchT also non-competitively inhibited the CRC of histamine in guinea-pig intestine and the CRCs of serotonin and oxytocin in rat uterus. Isoquercetin and rutin were identified in SchT. The behavioral effects of SchT, SchO and infusion of S. lentiscifolius leaves (SchW) were tested in mice. These extracts showed an anxiolytic-like effect in the novelty-suppressed feeding test, which was reversed by flumazenil except in SchO-treated mice. Only SchO reduced the spontaneous locomotor function in the open field test. Also, SchT and SchW decreased immobility time in both, the tail suspension (TST) and forced swimming tests, while SchO produced the same effect in the TST. D-limonene and α-santalol were the main components found in SchO. The results demonstrated that extracts obtained from S. lentiscifolius leaves were effective as intestinal, urinary and uterine antispasmodics. SchT and SchW exhibited anxiolytic and antidepressant properties without sedation, whereas SchO showed also sedative properties. Therefore, the present study gives preclinical support to the traditional use of this plant for gastrointestinal and depressive or emotional symptoms. Fil: Vanegas, Carolina. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina Fil: Matera, Soledad Inés. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina Fil: Bayley, Matias. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina Fil: Colareda, German Andres. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina Fil: Ruiz, María Esperanza. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Control de Calidad de Medicamentos; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina Fil: Prieto, Julián José. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Control de Calidad de Medicamentos; Argentina Fil: Retta, Daiana Sabrina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Metabolismo del Fármaco; Argentina Fil: Van Baren, Catalina Maria. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Metabolismo del Fármaco. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Química y Metabolismo del Fármaco; Argentina Fil: Consolini, Alicia Elvira. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina Fil: Ragone, María Inés. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Departamento de Ciencias Biológicas. Cátedra de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina
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- 2022
44. Supplementary materials for 'Biological Activities of Fungus Aspergillus ficuum: In vivo, In vitro, and In silico Analyses'
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Zafar Ali Shah, Khalid Khan, Tanzeel Shah, Nasir Ahmad, Akhtar Muhammad, and Haroon ur Rashid
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Antifungal ,Anticancer ,Antispasmodic ,Urease Inhibition ,Molecular Docking ,A. ficuum - Abstract
Various fatal diseases such as cancer, candidiasis, hepatic coma, gastritis, etc. have critically affected human health all over the world. Exploring nature for the treatment of such devastating diseases remains an area of immense interest to the scientific community. In this context, the genus Aspergillus was selected to explore its hidden therapeutic potential as a continuation of our research. As reported, the genus Aspergillus produces several new biologically-active compounds. Therefore, the current study was conducted to assess the biological and pharmacological potency of the less-studied Aspergillus ficuum (FCBP-DNA-1266) (A. ficuum). An in vitro assay was used to investigate the antifungal, anticancer, and urease inhibitory potential of n-hexane and ethyl acetate extracts of A. ficuum. Similarly, antispasmodic activity was assessed in an in vivo model. In silico model was applied to support the results obtained from the antifungal, anticancer, and urease inhibition. The antifungal studies indicated that both n-hexane and ethyl acetate extracts were significantly effective against Candida albicans with their zone of inhibitions (ZOI) of 19 ±1.06 mm and 25 ±0.55 mm, respectively at a dose of 30 µgmL-1. The in vivo pharmacological study of A. ficuum demonstrated significant antispasmodic activity at 150 mgkg-1. In vitro cytotoxicity versus different cancer cell lines for example HeLa, fibroblast 3T3, prostrate PC3, and breast MCF-7 was performed. The ethyl acetate extract of A. ficuum was found to be significantly active versus MCF-7 with its IC50 value of 40.29 µgmL-1. No substantial effect on the percent cell death of HeLa cancer cell lines was observed. In addition, the A. ficuum extracts also inhibited the urease enzyme compared to standard thiourea. Molecular docking results also supported the antifungal, anticancer, and antiurease potency of A. ficuum. The results display the promising aspects of A. ficuum as a future pharmacological source.
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- 2023
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45. Moringa oleifera: A Tree of Life as a Promising Medicinal Plant for Neurodegenerative Diseases
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Saurav Ghimire, Lalita Subedi, Namrata Acharya, and Bhakta Prasad Gaire
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Antifungal ,Traditional medicine ,medicine.drug_class ,business.industry ,General Chemistry ,Neuroprotection ,Cardiac stimulant ,Moringa ,Functional food ,medicine ,Antispasmodic ,General Agricultural and Biological Sciences ,business ,medicine.drug - Abstract
Moringa oleifera, popularly known as a miracle tree or tree of life, has been extensively used as a functional food and nutritional asset worldwide. Ethnomedicinal and traditional uses of M. oleifera indicate that this plant might have a pleiotropic therapeutic efficacy against most human ailments. In fact, M. oleifera is reported to have several pharmacological activities, including antioxidant, antibacterial, antifungal, antidiabetic, antipyretic, antiulcer, antispasmodic, antihypertensive, antitumor, hepatoprotective, and cardiac stimulant properties. Recently, a few experimental studies reported the neuroprotective effects of M. oleifera against Alzheimer's disease, dementia, Parkinson's disease, stroke, and neurotoxicity-related symptoms. In addition, several neuroprotective phytochemicals have been isolated from M. oleifera, which signifies that it can have promising neuroprotective effects. Therefore, this review aimed to explore the current updates and future prospective of neuroprotective efficacies of M. oleifera.
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- 2021
46. Antidiarrheal and antispasmodic activities of Trillium govanianum rhizomes extract: involvement of calcium channel blockade
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Niaz Ali, Shafiq Ur Rahman, Omer Shehzad, Marcello Iriti, Hilal Uddin, Muhammad Ismail, Ikram ul Haq, Sara Vitalini, Muhammad Shahid, Haya Hussain, Shujaat Ahmad, Abid Ullah, Aslam Khan, and Naveed Muhammad
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Sodium picosulfate ,Lactitol ,biology ,medicine.drug_class ,Calcium channel ,Organic Chemistry ,Plant Science ,Calcium channel blocker ,Pharmacology ,biology.organism_classification ,Biochemistry ,Analytical Chemistry ,Jejunum ,chemistry.chemical_compound ,medicine.anatomical_structure ,chemistry ,medicine ,Trilliaceae ,Verapamil ,Antispasmodic ,medicine.drug - Abstract
The antidiarrheal effect of methanolic extract of Trillium govanianum Wall. ex D. Don (Melanthiaceae alt. Trilliaceae) was studied at doses of 12.5, 25, and 50 mg/kg in different animal models of diarrhea including castor oil (6 mL/kg), magnesium sulfate (2 gm/kg), sodium picosulfate (2 mL/kg) and lactitol (0.25 mL/kg). The antispasmodic effect of T. govanianum was studied on isolated rabbit's jejunum, using acetylcholine as tissue stabiliser and verapamil as calcium channel blocker. T. govanianum attenuated the diarrhea by producing a significant decrease in the number and weight of stool, and an increase in stool latency time. T. govanianum completely inhibited both spontaneous as well as high potassium induced contractions of isolated rabbit's jejunum, which was analogous to verapamil. Moreover, T. govanianum produced a right shift in calcium concentration response curve, confirming its calcium channel blocking activity. These findings provide scientific ground to its medicinal use in diarrhea and gut spasms.
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- 2021
47. Pharmacological interventions for pediatric irritable bowel syndrome
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Eugenia Bruzzese, Giovanni Sarnelli, Anna Rybak, Osvaldo Borrelli, Marcella Pesce, Maria Giovanna Puoti, Marta Andreozzi, Pesce, M., Puoti, M. G., Rybak, A., Andreozzi, M., Bruzzese, E., Sarnelli, G., and Borrelli, O.
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medicine.medical_specialty ,antispasmodic ,Functional disorder ,Irritable Bowel Syndrome ,pharmacotherapy ,Pharmacotherapy ,Functional gastrointestinal disorder ,Retrospective Studie ,Intervention (counseling) ,medicine ,Humans ,Pharmacology (medical) ,Child ,Intensive care medicine ,Irritable bowel syndrome ,Retrospective Studies ,Pharmacology ,antidepressant ,business.industry ,Retrospective cohort study ,General Medicine ,Placebo Effect ,medicine.disease ,Abdominal Pain ,pediatric ,functional abdominal pain disorder ,multidisciplinary approach ,Etiology ,business ,Psychosocial ,Human - Abstract
Introduction Irritable bowel syndrome is a common functional gastrointestinal disorder in children, characterized by recurrent abdominal pain associated with altered bowel habits in terms of both frequency and consistency. According to change in stool consistency it is categorized into 4 subtypes. From the etiological perspective, it is a multifactorial functional disorder with both central (psychosocial) and peripheral factors (altered bowel sensitivity, motility and microbiota) implied in the genesis of the symptoms. Several treatment options, addressing each underlying pathophysiological mechanism have been proposed. However, since in most cases a combination of factors takes part in symptoms' generation, the overall treatment response rate is often unsatisfactory if a multidisciplinary is not pursued. Areas covered The aim of this manuscript is to summarize the current pharmacotherapy in paediatric irritable bowel syndrome in order to aid clinicians in treating this challenging disorder. Expert opinion Most evidence involving paediatric populations rely on open label or retrospective studies and/or are not specifically designed for irritable bowel syndrome but tend to generalise their results to mixed populations of children with functional gastrointestinal disorders. A high placebo response rate combined with poor patients' selection could account for the overall weak evidence supporting the use of pharmacological agents in paediatric irritable bowel syndrome. Given the multifaceted nature of the disorder, multidisciplinary approaches combining pharmacotherapy with alternative treatments is highly recommendable.
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- 2021
48. Antispasmodic, cardioprotective and blood-pressure lowering properties of Gomphrena perennis L. and its mechanisms of action.
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Bonilla Bonilla AM, Gavilánez Buñay TC, Bayley M, Colareda GA, Matera SI, Flores ML, Córdoba OL, Prieto JJ, Ruiz ME, Consolini AE, and Ragone MI
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Background: Gomphrena perennis L. is a native plant of South America whose pharmacological properties have not been studied yet., Aim: To evaluate the cardiovascular and intestinal pharmacological effects of Gomphrena perennis L. leaves tincture (GphT) and the mechanisms involved., Experimental Procedure: The chromatographic profile of GphT was done. Its ex vivo effects were evaluated by contractile concentration-response curves (CRCs) obtained from the agonist carbachol or calcium found in isolated rat small intestine, as well as in the relaxant CRCs. Cardiac effects were evaluated on isolated rat hearts exposed to ischemia/reperfusion (I/R). Experiments in vivo were performed to evaluate the diuretic activity in conscious rats and the hypotensive effect in anaesthetised rats., Results: Fifteen flavonoids were identified in GphT by HPLC-UV, including diosmin. GphT induced a non-competitive inhibition in both carbachol and calcium CRCs on rat small intestine. The first was not affected by indomethacin. Moreover, GphT, unlike diosmin, relaxed the contracture produced by a high-potassium solution in a dose-dependently way. Neither propranolol nor l-NAME changed it. GphT did not show diuretic activity but induced hypotension insensitive to l-NAME. While GphT perfusion of isolated hearts increased injury consequent to I/R, oral administration was cardioprotective and reversed by l-NAME. However, diosmin did not improve the post-ischemic recovery., Conclusions: This study supports the use of Gomphrena perennis L. tincture as an antispasmodic and hypotensive agent. Moreover, it has been demonstrated to be preventive of post-ischemic cardiac dysfunction. However, diosmin would not be responsible for these effects., Competing Interests: We have no known conflicts of interest in the publication of this article: Antispasmodic, cardioprotective and blood-pressure lowering properties of Gomphrena perennis L. and mechanisms of action., (© 2023 Center for Food and Biomolecules, National Taiwan University. Production and hosting by Elsevier Taiwan LLC.)
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- 2023
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49. Myorelaxant and antispasmodic effects of the essential oil of Artemisia campestris L., and the molecular docking of its major constituents with the muscarinic receptor and the L-type voltage-gated Ca2+channel.
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Marghich, Mohamed, Amrani, Ouafa, Karim, Ahmed, Harit, Tarik, Beyi, Leila, Mekhfi, Hassane, Bnouham, Mohamed, and Aziz, Mohammed
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MUSCLE relaxants , *ESSENTIAL oils , *JEJUNUM , *ANIMAL experimentation , *MUSCARINIC agonists , *RABBITS , *PARASYMPATHOLYTIC agents , *GAS chromatography , *RATS , *MASS spectrometry , *DESCRIPTIVE statistics , *PLANT extracts , *COMPUTER-assisted molecular modeling - Abstract
Gastrointestinal disorders are among the most common diseases that cause discomfort to people who are affected. In Morocco, aromatic and medicinal plants are widely used to calm these pains and eliminate their symptoms. Among these plants, Artemisia campestris L. which is used in eastern Morocco to treat digestive system problems. Our study aimed to experimentally verify the traditional use of this plant by evaluating the myorelaxant and antispasmodic effects of the essential oil of Artemisia campestris L. (EOAc). Gas Chromatography-Mass Spectrometry analysis (GC-MS) was performed to identify the compounds present in the EOAc. Then, these molecules were subjected to the in silico study for molecular docking. The myorelaxant and antispasmodic evaluation of the EOAc were tested in vitro on an isolated rabbit and rat jejunum mounted on an organ bath. Then, an isotonic transducer connected to an amplifier recorded the graph related to intestinal contractility. GC-MS analysis of the essential oil of Artemisia campestris L. showed the presence of m-Cymene (17.308%), Spathulenol (16.785%), β Pinene (15.623%), α Pinene (11.352%), α.-Campholenal (8.848%) as main constituents. The EOAc gave a dose-dependent and reversible myorelaxant effect on the spontaneous contractions of jejunum isolated from rabbits, with an IC 50 equal to 72.16 ± 15.93 μg/mL. This effect did not occur through adrenergic receptors. The EOAc has an antispasmodic effect on the contractions of rat jejunal induced by a medium with low (25 mM) or high concentration (75 mM) of KCl, and carbachol 10−6 M. The obtained inhibitory effects are comparable to those of a non-competitive antagonist of cholinergic receptors. The major compounds of EOAc allowed the establishment of a relationship between these phytoconstituents and the antispasmodic effect found by the EOAc. The obtained results are also supported by a docking study. The obtained results confirm favorably the use of Artemisia campestris L. in traditional Moroccan medicine for the treatment of digestive tract illness, which gives us a new route to valorize the effects obtained by a phytomedicine specific for the digestive tract. [Display omitted] • Essential oil of Artemisia campestris L. (EOAc) showed the presence of m-Cymene , Spathulenol , β Pinene , and α Pinene. • The EOAc gave a dose-dependent and reversible myorelaxant effect on the spontaneous contractions of rabbit jejunum. • The EOAc had an antispasmodic effect on the contractions of rat jejunum induced byKCl, and Carbachol. • The inhibitory effects obtained by EOAc are comparable to those of a non-competitive antagonist of cholinergic receptors. • Spathulenol was the best component among those of EOAc that could bind to voltage-gated Ca2+ and Muscarinic receptor. [ABSTRACT FROM AUTHOR]
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- 2023
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50. Patient preparation for prostate MRI: A scoping review.
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Prabhakar, Suman and Schieda, Nicola
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PROSTATE cancer , *CANCER diagnosis , *LITERATURE reviews , *PROSTATE , *MAGNETIC resonance imaging - Abstract
To perform a scoping review of the literature evaluating patient preparation for prostate MRI. We conducted a search of English language literature, between 1989 and 2022 using MEDLINE and EMBASE for key terms: diet, enema, gel, catheter and anti-spasmodic agents linked to prostate MRI. Studies were reviewed for: level of evidence (LOE), study design and key results. Knowledge gaps were identified. Three studies evaluated dietary modification in 655 patients. LOE was 3. All studies showed improved DWI and T2W image quality (IQ) and reduced DWI artifact. Nine studies evaluated enema use in 1551 patients. Mean LOE was 2.8 (range 2–3). Six studies reported IQ; DWI and T2W IQ were significantly improved with enema in 5/6 and 4/6 studies respectively. Only one study evaluated DWI/T2W lesion visibility which was improved with enema. One study evaluated impact of enema on eventual prostate cancer diagnosis, showing no benefit in false negative reduction. One study (LOE = 2, 150 patients) evaluated rectal gel; however, in combination with enema showing improved DWI and T2W IQ, lesion visibility and PI-QUAL compared to no preparation. Two studies evaluated use of rectal catheter in 396 patients. LOE was 3. One study showed improved DWI and T2W IQ and artifact compared to no preparation; however, the other showed inferior results comparing rectal catheter to enema. Six studies evaluated anti-spasmodic agent use in 888 patients. Mean LOE was 2.8 (range 2–3). Benefit of anti-spasmodic agent use on image quality and artifact on DWI and T2W are conflicting with no clear benefit. Data evaluating patient preparation for prostate MRI is limited by level of evidence, study design and conflicting results. The majority of published studies do not evaluate impact of patient preparation on eventual prostate cancer diagnosis. [ABSTRACT FROM AUTHOR]
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- 2023
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