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The present study aimed to conduct phytochemical and pharmacological profiling of methanolic crude extract of leaves of Bombax ceiba Linn. via experimental and computational approaches. Six secondary metabolites were isolated chromatographically, and the structures were elucidated by extensive analyses of high-resolution 1H and 13C NMR data. The separated compounds were characterized as β-sitosterol (1), β-amyrin (2), β-amyrin acetate (3), β-amyrin palmitate (4), β-amyrone (5), and isoscopoletin (6). DPPH free radical scavenging assay, tail-tipping method, writhing assay, and castor oil-induced diarrheal mice methods, respectively, were used to assess the antioxidant, hypoglycemic, analgesic, and anti-diarrheal activities of the leaf extract of B. ceiba plant species. The study observed significant reductions (p

Background: Liver disease is any disease that negatively affects the normal function of the liver, and it is a major health problem that challenges not only healthcare professionals, but also the pharmaceutical industry and drug regulatory agencies. Similarly, diarrhea is the second leading cause of death among children under five globally next to pneumonia. The available synthetic drugs for the treatment of liver disorders and diarrhoea have limited safety and efficacy. Objective: To evaluate the in vivo hepatoprotective and antidiarrheal activities of hydroalcoholic leaf and fruit extracts of Schinus molle L. (Anacardiaceae) in mice. Methods: Hepatoprotective activity of the extracts was evaluated by using CCl4 induced hepatotoxicity in mice model. In this model, mice were divided into groups and treated as follows. The normal control and toxicant control groups were treated with the vehicle used for reconstitution, the positive control was treated with the standard drug (silymarin), and the test groups were treated with different doses of plant extracts daily in the morning for seven days. Additionally, all groups except the normal control were treated with CCl4 (2 mg/kg, IP) on the 4th day of treatment, 30 min post-dose. On the 7th day, blood was collected from each mouse via a cardiac puncture. The collected blood was centrifuged, and serum levels of ALT, AST, and ALP were determined using an automated chemistry analyser. Data were analysed using one-way analysis of variance (ANOVA) followed by Tukey's post-hoc test.The antidiarrheal activity of the extract was investigated using castor oil-induced diarrhoea, enteropooling, and small intestine transit. The test groups received various doses (100, 200, and 400 mg/kg) of the extract, whereas the positive control received loperamide (3 mg/kg), and the negative control received the vehicle (distilled water, 10 ml/kg). Result: Hepatoprotective activity: The leaf and fruit crude extracts showed significant improvement in the body weight and liver weight of mice compared to the untreated toxicant control. Additionally, treatment with hydromethanol leaf and fruit extracts caused a significant (P 0.05) the level of albumin compared with the toxicant control.Antidiarrheal activity: In the castor oil-induced diarrheal model, the 80 % methanol extract delayed the onset of defaecation and significantly reduced the number and weight of faeces at all tested doses compared to the negative control. In the enteropooling test, 80 ME significantly (P

Background and aim: Secretory diarrhea is the most common type of diarrhea. This study aimed at exploring the possible mechanism of antisecretory action of Annona senegalensis stem bark and to identify the bioactive compounds. Experimental procedure: The ability of three crude extract; aqueous, dichloromethane and hexane stem bark extracts to inhibit castor oil-induced stooling in albino rats were assessed. Bioactivity guided fractionation of the most active extract was done using solvent-solvent partitioning (with hexane, dichloromethane, ethylacetate) and column chromatography. In vitro antioxidant activity of the most active sub-fraction was done using standard methods. The most active sub-fraction (25 mg/kg b. wt.) was administered to castor oil-induced diarrheal rats. Diarrheal rats small intestinal malondialdehyde concentration, antioxidant enzyme, cyclooxygenase II and Na+- K+ ATPase activities were determined using standard procedures. GC-MS analysis was done to identify the chemical compounds in the sub-fraction. Result and conclusion: Aqueous extract significantly decreased the number of wet stools. Sub-fraction 1 of ethylacetate fraction of aqueous stem bark extract (EFAS1) showed the highest stool inhibition. The H2O2 scavenging activity of EFAS1 was significantly greater than ascorbic acid. The sub-fraction significantly increased (p

Diarrhea is a prevalent gastrointestinal problem associated with fatal implications. It is a huge public health concern that requires better alternatives to current drugs. This study investigated the mechanisms involved in the antidiarrheal activity of Anacardium occidentale (Ao) stem bark extract, a plant commonly used in the management of diarrhea in Nigeria. Methanolic stem bark extract of the plant was partitioned into three fractions: hexane fraction, ethyl acetate fraction (AoEF) and methanol fraction. In vitro studies on the effect of these fractions on guinea pig ileum (GPI) strips, as well as the modulatory effect of AoEF on standard agonists- and antagonists-induced GPI contraction and relaxation, revealed AoEF as the most active fraction. In vivo studies to assess the effect of AoEF on the dopaminergic, muscarinic, and serotonergic pathways were carried out using gastric emptying (GE) and gastrointestinal transit (GT) as experimental end points. AoEF was subjected to GC-MS analysis, while the identified compounds were docked with the muscarinic acetylcholine receptor M3 (CHRM3) using AutodockVina. Results indicated that AoEF inhibited GE and GT via inhibition of CHRM3. In addition, GC-MS analysis revealed the presence of 24 compounds in AoEF, while docking indicated that octadecanoic acid 2-(2-hydroxylethoxy) ethyl ester exhibited the highest binding affinity to CHRM3. This study indicated that the antidiarrheal activity of Ao is through its antimotility effect via the inhibition of the muscarinic pathway. And since none of the identified compounds exhibited higher binding affinity to CHRM3 relative to loperamide, the antimotility activity of these phytoconstituents may be via synergism.

Background: Traditional usage (typhoid, diarrhea, sore throat) and previously performed studies (antioxidative and anticancer activity) have asserted that Eurya acuminata has a widespread therapeutic potential. However, most of the pharmacological aspects of this plant are yet to be explored.Methods: Broth dilution method was selected to determine the minimum inhibitory concentration (MIC) of the plant extract. Antidiarrheal activity was figured out following the castor oil-induced diarrheal inhibition method. The oral glucose tolerance test (OGTT) was performed to assess antihyperglycemic activity. Alpha-glucosidase inhibitory assay was conducted according to the supplier's method. Acetic acid-induced writhing inhibition method was used to evaluate the peripheral analgesic activity.Results: HPLC analysis detected the presence of (-)-epicatechin, p-coumaric acid, trans-ferulic acid, rosmarinic acid, myricetin, and trans-cinnamic acid. In the broth dilution method, the extract exhibited MIC of 16 μg/ml against E. coli and S. aureus and 8 μg/ml against P. aeruginosa. In castor oil-induced antidiarrheal assay, E. acuminata extract significantly reduced 44.82% and 67.24% defecation, respectively at the doses of 250 and 500 mg/kg. Furthermore, in in vivo antihyperglycemic activity, E. acuminata extract reduced blood glucose levels to 6.8 mM and 4.68 mM, at the doses of 250 and 500 mg/kg, respectively at 60 min although the extract demonstrated no α-glucosidase enzyme inhibitory activity. Apart from that, in in vivo analgesic activity, the extract inhibited writhing reflexes dose-dependently, 15.16% and 37.13% at the doses of 250 and 500 mg/kg.Conclusion: This study shows that E. acuminata might be a good source to explore antidiarrheal, antihyperglycemic, and antimicrobial compounds for new drug development.

Anisomeles indica (L.) Kuntze is an ethnomedicinally important plant that has long been used in traditional medicine to treat a variety of ailments, including dyspepsia, abdominal pain, colic, allergies, inflammation, and rheumatic arthritis. However, the scientific framework underlying these medicinal properties is not well known. This study aimed to investigate the antidepressive, antidiarrheal, thrombolytic, and anti-inflammatory potential of a methanol extract of A. indica (MeOH-AI). The potential bioactive compounds in the MeOH-AI were identified using gas chromatography-mass spectrometry (GC-MS), and antidepressant activities were evaluated using the tail suspension test (TST) and forced swim test (FST). Antidiarrheal effects were also assayed in castor oil-induced diarrhea and gastrointestinal motility studies. The anti-inflammatory activities were explored by examining the effects on protein inhibition and denaturation in heat- and hypotonic solution-induced hemolysis assays. The thrombolytic activity was evaluated using the clot lysis test in human blood. BIOVIA and Schrödinger Maestro (v11.1) were applied for docking analysis to determine binding interactions, and the absorption, distribution, metabolisms, excretion/toxicity (ADME/T) properties of bioactive compounds were explored using a web-based method. The GC-MS analysis of MeOH-AI revealed the presence of several bioactive compounds. MeOH-AI administration resulted in significant (p

Background: Cuscuta reflexa (dodder) belonging to the family Convolvulaceae has many ethno-medicinal uses such as antidiarrheal and antiemetic. This plant has been employed to treat diarrhea, where the antidiarrheal use of this plant is well established in different communities around the world without scientific bases. In addition, the antibacterial, anthelmintic, anticholinergic, and antihistaminic effects of this parasitic vine are partly responsible for the folkloric antidiarrheal use of this plant. In the present study, the antidiarrheal activity of C. reflexa was evaluated in pigeons (Columba livia) using the juice (JCR), aqueous (CRAE), and methanol (CRME) extracts. Methods: The antidiarrheal effect of C. reflexa was evaluated using different reported research models, with few modifications. In pigeons, diarrhea was induced by administration of castor oil (6 mL/kg, PO), ampicillin (250 mg/kg, IP), magnesium sulfate (2 gm/kg, PO), and cisplatin (6 mg/kg, IV). In these experiments, loperamide (2 mg/kg, IM) was used as a positive control, whereas JCR (1 mL/kg (1%) and 1 mL/kg (2%), CRAE (50, 100 and 200 mg/kg) and CRME (50, 100 and 200 mg/kg) were administered intramuscularly at different doses into each pigeon in the test groups. Results: In addition to cisplatin-induced diarrhea, all paradigms tested gave significant results (P < 0.01). The JCR, at different doses, exhibited a significant (p < 0.01) a dose-dependent antidiarrheal effect on both the frequency and the onset of diarrhea. Similarly, CRAE and CRME, at doses of 100 and 200 mg/kg, showed considerable (p < 0.001) inhibition against the onset and frequency of diarrhea. On the other hand, JCR, CRAE, and CRME exerted significant effects (p < 0.001) on the percentage inhibition (PI) of diarrhea and gastrointestinal charcoal transit in a dose-dependent manner. In this respect, the maximum PI (p < 0.01) of JCR, CRAE, and CRME in different experimental paradigms was 43.13, 49.14, and 55.99 %, respectively. Conclusions: Taken all together, results from this study reveal that the juice, aqueous, and methanol extract of C. reflexa exhibit significant anti-motility and anti-secretory potential. These findings may explain the medicinal use of C. reflexa in folk medicine as an antidiarrheal medicinal plant.

Millettia peguensis, popular for its ethnopharmacological uses, was employed to evaluate its different pharmacological properties in this study. The analgesic studies of the plant have been performed by acetic acid-induced writhing and formalin-induced licking tests respectively, whereas the antidiarrheal experiment was done by castor oil-induced diarrheal test. Besides, antioxidant, cytotoxic, antimicrobial, thrombolytic evaluations were performed by DPPH scavenging with phenol content determination, brine shrimp lethality, disc diffusion and clot lysis methods respectively. Moreover, in silico study of the phytoconstituents was carried out by molecular docking and ADME/T analysis.The methanol extract of Millettia peguensis (MEMP) revealed significant biological activity in the analgesic and antidiarrheal test (p

Adenia trilobata, locally known as akandaphal in Bangladesh, has some traditional uses. Leaves and stems extracted with pure methanol (MEATL, MEATS) and fractioned by n-hexane (NFATL, NFATS), which was subjected to qualitative phytochemical analysis. The qualitative phytochemical analysis of four extracts showed the presence of secondary metabolites such as alkaloid, carbohydrate, glycosides, flavonoids, phenols, flavonol, and saponins. All four extracts of A. trilobata, exhibited a strong antioxidant activity while a moderately (MEATS = 328 μg/mL) to weakly toxic (NFATL = 616.85 μg/mL) LC50 observed in brine shrimp lethality bioassay. In thrombolytic test, MEATL (18.54 ± 2.18%; P

Medicinal plants are the major sources of traditional treatment of disease in Indian subcontinent due to abundant presence of plants and vast side effects of synthetic drug. The present study was subjected to observe in vitro thrombolytic, antibacterial, and in vivo antidiarrheal activities of methanol soluble fraction of fruits of Annona muricata. In thrombolytic activity assay, various concentrations (2 ─ 10 mg/ml) of methanol soluble fraction was used and dose dependently less potent activity was found. The maximum clot lysis 18.33% (p* < 0.05) was achieved at 10 mg/ml of methanolic fruit extract, whereas standard drug streptokinase showed 55.50% (p*** < 0.001) clot lysis. In antibacterial assay, disc diffusion method was used comprising two gram positive (S. aureus and Micrococcus luteus) and two gram negative (E. coli and P. aeruginosa) bacteria. None of four (0.25, 0.5, 1, and 5 mg/disc) concentration of fruit extract showed antibacterial potentiality, whereas standard amikacin (3 mg/disc) revealed strong antibacterial activities (=~ 23 ─ 24 mm of MIC). To evaluate antidiarrheal activity, castor oil induced diarrhea was created in Swiss albino mice and different doses (100, 200, and 400 mg/kgbw) of fruit extract was introduced post orally. All of three different doses of fruit extract showed significant (p < 0.05 ─ 0.001) antidiarrheal activities. Notably, the percent inhibition of diarrhea by methanolic extract of fruits of Annona muricata was found to be 58.38% at a dose of 400 mg/kgbw. The effect of vehicle saline (10 ml/kgbw) was considered as control and loperamide (5 mg/kgbw) as standard that provided 67.01% inhibition of diarrhea. The results suggest that, the fruits of Annona muricata possess potent antidiarrheal properties, providing scientific basis of using the plant parts in the treatment of diarrheal disease.

Diarrheal diseases are the second highest cause of mortality of children under 5 years worldwide. There is a continuous search for developing a cost-effective treatment for diarrhea as the present ones are facing challenges. Medicinal plants can be explored further as an alternative treatment for diarrhea. Psidium guajava leaves have been used as an antidiarrheal globally. Citrobacter rodentium, a common mouse pathogen, is known to mimic the pathogenecity of enteropathogenic and enterohemorrhagic E. coli. It can thus present an effective model to study infectious diarrhea. In the present study, the P. guajava leaf extract was tested for its efficacy in treating infectious diarrhea using a C. rodentium mouse model. The mice in the test group (treated with P. guajava leaf extract) showed quicker clearance of infection as compared with the control group. The bacterial load in the fecal sample of the mice in the test group was high on Day 4 as compared with that in the control group, suggesting a flush out of the bacteria. In the test group, 6/7 (85.71%) mice showed clearance of infection by Day 19. The control group continued to show infection till Day 29. P. guajava leaf extract thus has the potential for use in the treatment of infectious diarrhea.

Background: In addition to the nutritional benefits of Cucumis melo L., herbalists in Pakistan and India employ seeds to treat various ailments. This study aimed to determine the regulatory role of C. melo seeds in calcium-mediated smooth muscle contraction., Methods: We identified and quantified the phytochemicals of C. melo with LC ESI-MS/MS and HPLC, then conducted in vitro and in vivo tests to confirm the involvement in smooth muscle relaxation. Then, diarrhea-predominant irritable bowel syndrome gene datasets from NCBI GEO were acquired, DEGs and WGCNA followed by functional enrichment analysis. Next, molecular docking of key genes was performed., Results: The quantification of C. melo seeds revealed concentrations of rutin, kaempferol, and quercetin were 702.38 μg/g, 686.29 μg/g, and 658.41 μg/g, respectively. In vitro experiments revealed that C. melo seeds had a dose-dependent relaxant effect for potassium chloride (80 mM)-induced spastic contraction and exhibited calcium antagonistic response in calcium dose-response curves. In in vivo studies, Cm.EtOH exhibited antidiarrheal, antiperistaltic, and antisecretory effects. The functional enrichment of WGCNA and DEGs IBS-associated pathogenic genes, including those involved in calcium-mediated signaling, MAPK cascade, and inflammatory responses. MAPK1 and PIK3CG were identified as key genes with greater binding affinity with rutin, quercitrin, and kaempferol in molecular docking., Conclusions: The bronchodilator and antidiarrheal effects of C. melo were produced by altering the regulatory genes of calcium-mediated smooth contraction., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 The Authors. Published by Elsevier Ltd.. All rights reserved.)

A phytochemical study on the root extracts of Neorautanenia mitis, a Nigerian medicinal plant used in the management of diarrhea, led to the isolation of one new and 19 known natural products. These compounds and crude extracts were evaluated for Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Cl - channel and calcium-activated Cl - channel (TMEM16A) inhibitory activities in T84 and Calu-3 cells, respectively. Four compounds namely dolineon, neodulin, pachyrrhizine, and neotenone inhibited cAMP-induced Cl- secretion across T84 cell monolayers with IC 50 values of ~0.81 μM, ~2.42 μM, ~2.87 μM, and ~4.66 μM, respectively. Dolineon having the highest inhibitory activity also inhibited a Ca + activated Cl - channel (TMEM16A) with an IC 50 value of ~4.38 μM. The in vitro antidiarrheal activity of dolineon was evaluated on cholera toxin (CT) induced chloride secretion in T84 cells, where it inhibited CT-induced chloride secretion by >70% at 100 μM. Dolineon also inhibited CT-induced fluid secretion by ~70% in an in vivo mouse closed loop model at a dose of 16.9 μg/loop. The cytotoxicity of the extracts and compounds was evaluated on KB, Vero and BHK21 cells, dolineon showed low cytotoxicity of >29.6 μM and 57.30 + 6.77 μM against Vero and BHK21 cells, respectively. Our study revealed that several compounds isolated from N. mitis showed antidiarrheal activity. The most active compound dolineon can potentially serve as a lead compound towards the development of CFTR and TMEM16A inhibitors as future therapeutics for secretory diarrhea., (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Diarrheal diseases are the second highest cause of mortality of children under 5 years worldwide. There is a continuous search for developing a cost-effective treatment for diarrhea as the present ones are facing challenges. Medicinal plants can be explored further as an alternative treatment for diarrhea. Psidium guajava leaves have been used as an antidiarrheal globally. Citrobacter rodentium, a common mouse pathogen, is known to mimic the pathogenecity of enteropathogenic and enterohemorrhagic E. coli. It can thus present an effective model to study infectious diarrhea. In the present study, the P. guajava leaf extract was tested for its efficacy in treating infectious diarrhea using a C. rodentium mouse model. The mice in the test group (treated with P. guajava leaf extract) showed quicker clearance of infection as compared with the control group. The bacterial load in the fecal sample of the mice in the test group was high on Day 4 as compared with that in the control group, suggesting a flush out of the bacteria. In the test group, 6/7 (85.71%) mice showed clearance of infection by Day 19. The control group continued to show infection till Day 29. P. guajava leaf extract thus has the potential for use in the treatment of infectious diarrhea.