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This study aimed to evaluate nefopam's analgesic properties, explore caffeine's potential adjuvant effects, and examine its impact on renal and hepatic function. The study involved 56 female albino mice, divided into seven groups: Group A, as the control group, received distilled water; Group B received 0.75 mg per body weight of nefopam orally; Group C received 0.71 mg/B.W. of nefopam and 0.125 mg/B.W. of caffeine; Group D received 0.67 mg/B.W. of nefopam and 0.25 mg/B.W. of caffeine; and Group E received 0.63 mg/B.W. of nefopam and 0.37 mg/B.W. of caffeine. Group F received 0.6 mg/B.W. nefopam and 0.5 mg/B.W. caffeine orally; Group G received 0.56 mg/B.W. of nefopam and 0.62 mg/B.W. of caffeine. Several experimental models have been utilised to investigate the analgesic advantages. The hot plate test is a method used to assess the response time to thermal stimuli. Group D produced the most prolonged response duration to thermal stimuli, namely thermal pain, while the writhing test involves the injection of acetic acid, resulting in a significant decrease in the frequency of writhing observed in Group D. Inconclusion, Nefopam demonstrated analgesic properties in all experimental groups, even when augmented with caffeine, without any observed changes in renal or liver function. [ABSTRACT FROM AUTHOR]

Getachew Ashagrie,1,2 Fentaw Girmaw,1 Abebe Tarekegn,1 Tenaw Baye,1 Abebe Dagne3 1Department of Pharmacy, College of Health Science, Woldia University, Woldia, Ethiopia; 2Department of Pharmacology and Clinical Pharmacy, School of Pharmacy, College of Health Sciences, Addis Ababa University, Addis Ababa, Ethiopia; 3Department of Pharmacy, College of Health science, Debre Markos University, Debre Markos, EthiopiaCorrespondence: Getachew Ashagrie, Email getachewashagrie16@gmail.comBackground: The roots of Impatiens rothii has been used as a traditional remedy for painful conditions, rheumatism, isthmus and crural aches. However, the analgesic and anti-inflammatory properties of this plant have yet to be scientifically confirmed. The purpose of this study was to explore possible analgesic and anti-inflammatory activities 80% methanolic root extract of Impatiens rothii.Methods: To obtain the crude extract, the roots of Impatiens rothii that had been dried and ground up were macerated in 80% methanol. The analgesic activity was determined using acetic acid-induced writhing and hot plate tests in mice, whereas the anti-inflammatory activity was analyzed using carrageenan-induced paw edema model in rats. The extract was orally administered at a dose of 100, 200 and 400 mg/kg.Results: All tested doses of Impatiens rothii extract showed significant analgesic activity (p< 0.05) at observations of 30 to 120 minutes compared to the negative control in the hot plate test. In acetic acid-induced writhing test all tested doses of the 80% methanol extract of Impatiens rothii significantly (p < 0.001) reduced the number of writhing. In comparison to the control group, all tested doses displayed a significant decrease in paw edema, which appeared 2– 5 hours after induction (p< 0.05).Conclusion: From the results of this study, it can be stated that 80% methanolic extract of Impatiens rothii possessed substantial analgesic and anti-inflammatory activities, hence providing scientific basis for the use of this plant in the treatment of pain and inflammatory diseases.Keywords: Impatiens rothii, analgesic, hot plate, anti-inflammatory, carrageenan- induced paw edema

Getachew Ashagrie,1 Abiy Abebe,2 Shemsu Umer3 1Department of Pharmacy, College of Health Sciences, Woldia University, Woldia, Ethiopia; 2Biomedical Research Team, Traditional and Modern Medicine Research Directorate, Ethiopian Public Health Institute, Addis Ababa, Ethiopia; 3Department of Pharmacology and Clinical Pharmacy, School of Pharmacy, College of Health Sciences, Addis Ababa University, Addis Ababa, EthiopiaCorrespondence: Getachew Ashagrie, Tel +251927368467, Email Getachewashagrie16@gmail.comBackground: Ethnobotanical studies in various districts of Ethiopia reported that Ehretia cymosa (E. cymosa) is used for the management of headache, abdominal pain, arthritis and rheumatism. However, there is no scientific investigation done so far to confirm these traditional claims. Thus, the aim of this study was to assess the analgesic and anti-inflammatory effects of the 80% methanol extract and fractions of E. cymosa leaves.Methods: The dried and pulverized leaves of E. cymosa were soaked with 80% methanol to obtain a crude extract. Fractionation was done using chloroform, ethyl acetate and water by a soxhlet apparatus. The analgesic effects of the crude extract and solvent fractions were assessed using acetic acid-induced writhing and hot plate tests whereas anti-inflammatory activities were investigated using carrageenan-induced paw edema and cotton-pellet-induced granuloma models.Results: In all the tested doses, the 80% methanol extract and solvent fractions revealed substantial (p < 0.001) analgesic activities in acetic acid induced writhing test. In the hot plate method, all the tested doses of E. cymosa crude extract and the solvent fractions produced significant analgesic activities (p < 0.05). In the carrageenan-induced acute inflammation model, all tested doses of the crude extract and solvent fractions resulted in a significant decline in paw edema. The 80% methanol extract and solvent fractions of E. cymosa at all the tested doses significantly reduced inflammatory exudates and granuloma mass formations (p < 0.001).Conclusion: From the results of this investigation, it can be stated that 80% methanol extract, aqueous, ethyl acetate and chloroform fractions of E. cymosa exhibited considerable analgesic and anti-inflammatory activities, supporting the plant’s traditional use as a remedy for a variety of painful and inflammatory conditions.Keywords: analgesic, hot plate, anti-inflammatory, Ehretia cymosa, carrageenan-induced paw edema, cotton pellet granuloma

Introduction: Nonsteroidal anti-inflammatory drugs (NSAIDs) are one of the most widely used drugs in the treatment of pain and inflammation. Although, their side effects i.e.; gastrointestinal and renal adverse effects, limit the use of these drugs. Therefore, investigating new compounds with higher efficacy and fewer side effects is considerable issue. In this study, the analgesic activity of rosmarinic acid at different doses was compared with piroxicam (known standard NSAID).Methods: To evaluate the analgesic effects of rosmarinic acid, two well-known methods, Hot plate, and Tail-flick, were used. The experiments were performed in 10 groups (6 male mice per group) including the experimental groups (rosmarinic acid), the positive control group (piroxicam), and the negative control group (normal saline). All administrations were through intraperitoneal injection. The obtained data were analyzed separately by SPSS software and an independent student t test.Results: Rosmarinic acid at doses of 10 mg/kg and higher had significant analgesic effects compared with the control group, 30 minutes after injection in both hot plate and tail flick tests (P < 0.05). Concomitant injection of 50 mg/kg of rosmarinic acid with 15 mg/kg of piroxicam produced significant painkiller effects when compared with the dose of 15 mg/kg piroxicam injection alone.Conclusion: Rosmarinic acid was able to exert analgesic effects in pharmacological tests in a dose-dependent manner. Concomitant use of rosmarinic acid and piroxicam may lead to synergic pain relief, especially in acute and severe pain in patients, reducing the therapeutic dose of piroxicam and subsequently, its side effects.

Genus Astragalus belongs to the family Fabaceae and is one among the largest genera consisting of around 3000 species. The plants have been used traditionally in treatment of various ailments in folklore. The study was planned to assess the analgesic and inflammatory activity of Astragulus spinosus (Forssk.) Muschl extract of the stem. Course powder of stems of Astragulus spinosus was extracted using chloroform and methanol as solvents. Folin ciocalteu method was employed for determination of the phenolic acid content. Aluminum chloride colorimetric procedure was followed for estimating the flavonoid content. Both chloroform and methanolic extracts at 250 and 500 mg/kg, were tested for the analgesic activity, however, only methanolic extract was selected for anti-inflammatory property based on the results of analgesic activity. The analgesic effect was executed on male rats by the hot plate model. The anti-inflammatory effect was studied in the carrageenan rat paw edema model. The experimental information was interpreted statistically using one-way ANOVA and p < 0.05 was used to express importance of the results. The total phenolics of the methanol extract was 420 µg and that of chloroform extract was 265 µgwhile total flavonoid content in terms of quercetin was found to be 68 µg and 17.5 µg for methanol and chloroform extract respectively. Only methanolic extract exhibited significant (p < 0.001) analgesic activity by elevating the pain threshold starting from 15 min. The methanolic extract inhibited (p < 0.001) the edema in carrageenan induced model. The performance of higher dose (500 mg/kg) was better with reference to lower dose (250 mg/kg). Outcome of the results show that the methanolic stem extracts exhibited significant analgesic and anti-inflammatory-like activity with reference to chloroform extract. Credit of which is given to flavonoids and phenolic content present in the methanolic extract. However, more research is suggested to establish the safety and effectiveness of the herbal drug to manage diseased states including pain and inflammation. [ABSTRACT FROM AUTHOR]

Medicinal plants continue to attract attention as an alternative form of therapy. Phytochemical screening, analgesic properties and probable mechanism/s of action of the methanol leaf extract of Manniophyton fulvum were carried out following claimed folkloric usefulness in this regard. Standard methods were used to screen for classes of phytochemicals. Acetic acid-induced writhing and hot plate tests in albino mice were used to evaluate the peripheral and central analgesic effects using acetylsalicylic acid and morphine respectively as positive controls, while 50% DMSO served as negative control. Elucidation of the possible mechanism/s of action of the extract was carried using phenoxybenzamine, naloxen, ondansetron, atropine and haloperidol. Alkaloids, saponins, carbohydrates, terpenoids, steroids tannins, and flavonoids were detected in the extract. At 100 mg/kg dose, significant (P<0.01) reduction in pain stimuli, compared to the negative control group in both models was observed. Higher doses of extract (200 and 400 mg/kg) did not produce any significant effect. Observed results suggest that the leaf extract of M. fulvum may have an analgesic effect that is centrally and peripherally mediated at a lower dose compared to the high dose. The findings provide possible scientific basis for the ethnomedicinal use of the plant in several pain conditions. [ABSTRACT FROM AUTHOR]

Trees and shrubs of the genus Cordia are widely distributed in the warmer regions, including Indonesia. The aim of this study was to evaluate the analgesic and anti-inflammatory properties of the ethanolic extract of plant leaves in Wistar albino rats. The analgesic activity was evaluated using the hot plate method and acetic acid-induced writhing, and the anti-inflammatory activity was determined using carrageenan-induced paw oedema. The results showed that the Cordia sebestena ethanol extract (100, 200 and 400 mg/kg) exhibited significant analgesic effects in a dose-dependent manner in the two pain models tested. The extract also exhibited significant anti-inflammatory effects in the carrageenan-induced inflammation test. The data obtained support the traditional folklore therapeutic claim about its analgesic and anti-inflammatory properties. Nonetheless, further scientific investigation is required to establish its analgesic and anti-inflammatory properties in other experimental models and clinical settings.

The plant world represents an important source of potential therapeutic agents, but concomitant administration of herbal and conventional medications may result in interactions with subsequent beneficial or adverse effects. This study was designed to examine the analgesic effect of thyme tincture and thyme syrup, two commonly used thyme formulations, and their interactions with codeine, paracetamol, pentobarbital and diazepam in mice. The identification and quantification of thymol and carvacrol were carried out by GC/MS and GC/FID. The analgesic activity was studied using a hot plate method. Effects of thyme syrup on diazepam-induced motor coordination impairment in rotarod test and on pentobarbital-induced sleeping time were also determined. Thymol (175.3 µg/mL and 9.73 µg/mL) and carvacrol (10.54 µg/mL and 0.55 µg/mL) concentrations were measured in tincture and syrup, respectively. Thyme syrup and tincture exhibited effective analgesic activity in the hot plate pain model. Pretreatment with thyme formulations reduced analgesic activity of codeine, and potentiated the analgesic activity of paracetamol. Co-administration of thyme formulations has led to potentiation of diazepam and pentobarbital depressive central nervous system effects. Thyme formulations interacted with tested conventional drugs, probably through interference with their metabolic pathways and succeeding altered concentrations and pharmacological effects.

Purpose: To investigate the analgesic effects of oxytocin (OT) and elucidate the role of dopaminergic system in its mechanisms. Methods: In this study, 72 male (n=6 for each group) 230-250 gr Wistar Albino rats were used. Firstly, dose studies were performed with 100 μg/kg, 200 μg/kg and 400 μg/kg to determine the optimal analgesic effect of oxytocin. Optimal dose was found at 200 μg/kg, and then animals were divided into nine groups: Saline, D1 agonist (SKF 38393; 0.1 mg/kg), D1 antagonist (SCH-23390; 0.1 mg/kg), D1 agonist + oxytocin, D1 antagonist + oxytocin, D2 agonist (Cabergoline; 0,5 mg/kg), D2 antagonist (Sulpride; 10 mg/kg), D2 agonist + oxytocin and D2 antagonist + oxytocin. Serum physiologic saline was given to the saline group and other drugs were administered intraperitoneally at the indicated doses. Tail-flick and hot-plate tests were used to measure analgesic effects. Analgesic tests were measured in 30 min-intervals (at 30th, 60th, 90th, and 120th min) and recorded in seconds. To evaluate maximum antinociceptive effect (% MPE), the tail-flick and hot-plate latencies were converted to the antinociceptive effectiveness Results: The results show that D1 antagonist SCH-23390 (0.1 mg/kg) and D2 agonist cabergoline (0.5 mg/kg) created strong analgesia while the D1 agonist SKF 38393 (0.1 mg/kg) and D2 antagonist sulpiride (10 mg/kg) did not have any analgesic effect. However, only D2 antagonist sulpiride blocked the analgesic effect produced by OT Conclusion: OT may be one of the primary agents participating in spinal analgesia, and the dopaminergic system is one of the central mechanisms of action for this important molecule. The dopaminergic system may also be one of the targets for 'descending' analgesic system. [ABSTRACT FROM AUTHOR]

A number of novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole derivatives 2 were obtained by alkylation mainly in the 1H-tautomeric form of 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole or its 8,9-dimethyl-substituted analog 4-chlorobenzyl bromide, 4-chloroacetic acid fluoroanilide, and 4-tert-butylphenacyl bromide in neutral medium. Compounds 3 were cyclized and synthesized earlier with 11-phenacyl-substituted diazepino[1,2-a]benzimidazoles upon heating in conc. HBr. The chemical structures of the compounds were clarified by using the 1H Nuclear Magnetic Resonance Spectroscopy (1H-NMR) technique. Anxiolytic properties were evaluated using the elevated plus maze (EPM) and open field (OF) tests. The analgesic effect of compounds was estimated with the tail flick (TF) and hot plate (HP) methods. Besides, possible the influence of the test compounds on motor activities of the animals was examined by the Grid, Wire, and Rotarod tests. Compounds 2d and 3b were the most active due to their prominent analgesic and anxiolytic potentials, respectively. The results of the performed in silico analysis showed that the high anxiolytic activity of compound 3b is explained by the combination of a pronounced interaction mainly with the benzodiazepine site of the GABAA receptor with a prominent interaction with both the specific and allosteric sites of the 5-HT2A receptor.

Solanum incanum Linnaeus is traditionally used for treatment of pain and other ailments. But there is no scientific evidence on its analgesic activity to-date. Thus the aim of this study was to evaluate the analgesic activities of 80% methanol leaf extract of S.incanum in mice. After extraction of the crude using 80% methanol, S.incanum extract was evaluated for analgesic activity in hot plate test and acetic-acid induced writhing test. Mice were randomly assigned to different groups and treated with 100, 200 and 400 mg/kg doses of the extract and reference control groups (morphine 5mg/kg and Aspirin 150 mg/kg) and negative control were treated with 2% tween 80. In the hot-plate method, all doses of the extract and the standard drug of morphine prolonged the reaction time significantly (p<0.05, or p<0.01 or p<0.001) as compared to negative control throughout the observation period. Prolongation of reaction time produced by 100mg/kg of the extract was lower (p<0.01) compared to morphine, 200mg/kg, and 400mg/kg at 90 and 120 min. However, middle and higher dose exerts comparable result at 30, 60 and 90and 120 min in relation to the standard drug. In addition 80% methanol extract of S.incanum showed a significant protection (p<0.05) against acetic acid induced writhing compared to negative control. The extract produced a significant analgesic activity with 55.6, 38.2 and 44.8% inhibition of number of writhing at 100, 200 and 400 mg/kg dose levels, respectively. In conclusion, this study clearly suggests that 80% methanol leaf extract of S. incanum is endowed with central and peripheral analgesic activity. Hence, the findings collectively uphold the traditional use of the plant for pain treatment. [ABSTRACT FROM AUTHOR]

Background: Jyotishmati, scientifically known as Celastrus paniculatus Wild (Celastraceae) is one of the most important medicinal plants in Ayurveda. The plant has shown significant pharmacological activities like anti-arthritic, wound healing, hypolipidemic, and antioxidant. Objective: To study possible effects of alcoholic extract of Celastrus paniculatus seeds (AlcE) in experimentally induced pain and inflammation in mice. Materials and Methods: The antinociceptive activity was evaluated in Swiss albino mice by tail immersion, hot plate, and acetic-acid-induced writhing tests at doses of 250, 500, and 1,000 mg/kg. Anti-inflammatory activity was evaluated in model of carrageenan-induced acute plantar inflammation in Wistar rats. Results: In tail immersion test, AlcE showed significant (P < 0.05) increase in tail withdrawal response at dose of 250 mg/kg with maximum possible effect of 15.71%. The maximum possible effect of 23.32% and 30.16% (P < 0.001) was seen at dose of 500 and 1000 mg/kg at 3 hours after administration of extract, respectively. In hot plate test, increase in paw licking time was reported at dose of 500 and 1000 mg/kg. AlcE (1,000 mg/kg) showed maximum response (6.23 ± 0.46) when compared with control (3.20 ± 0.18) at 90 min. In acetic acid induced writhings, AlcE at dose of 250, 500, and 1,000 mg/kg body weight showed 32.35%, 49.01%, and 58.82% inhibition in writhings, respectively. AlcE treated animals (500 and 1,000 mg/kg) showed significant decrease in paw edema at 3 hours and 4 hours, when compared with control animals. Conclusion: Jyotishmati seed extract possesses significant antinociceptive and anti-inflammatory activity.

In this present study, the analgesic activity of the aqueous extract of the leaves of Dichrostachy cinerea was investigated in mice using acetic acid-induced writhing and hot plate test, while the anti-inflammatory activity was investigated in rats using the carrageenan and dextran- induced paw edema. The extract (400, 800mg/kg) exhibited a dose dependent inhibition of abdominal writhing in mice compared to control. The effects of the extract were not significantly different from that of aspirin. The extract (800mg/kg) caused a significant (p

Background Vanda tessellata (Orchidaceae) has been used in different sorts of ailments such as inflammations, rheumatism, dysentery, bronchitis, dyspepsia and fever in folk medicine. In this study we evaluated the antinociceptive and cytotoxic effect of methanol and aqueous extracts of V. tessellata leaf. Methods Oral administration of V. tessellata aqueous (VTA) and methanol (VTM) leaf extracts at 200 and 400 mg/kg body weight (bw) doses were assessed for antinociceptive activity in acetic acid-induced writhing test, hot plate test, and tail immersion test in mice. In this study we also screened for cytotoxicity of the extracts by the brine shrimp (Artemia salina) lethality assay. Results The extracts, at both doses, exhibited a significant (p < 0.05 - < 0.01) dose-dependent antinociceptive activity in hot plate and tail immersion test. The reaction time was increased to the thermal stimuli at 200 and 400 mg/kg doses up to 90 min. In acetic acid-induced writhing test, oral administration of VTA and VTM (200 and 400 mg/kg) also decreased the writhing significantly while compared to control. The dose 400 mg/kg showed maximum percentage of pain inhibition 42.37% and 45.08% for VTA and VTM respectively. Diclofenac sodium (10 mg/kg) and nalbuphine (10 mg/kg) were used as reference antinociceptive drugs. Very low cytotoxicity was observed on brine shrimps lethality assay. Conclusions The leaf extract has potential antinociceptive activity with minimum cytotoxicity. The present study supports the use of V. tessellata in different inflammatory disorders. [ABSTRACT FROM AUTHOR]

The anti-nociceptive effect of Rhizophora mucronata was evaluated on chemically and thermally induced nociception in mice. Albino mice received a dose of 10, 15, 20, or 25 mg/kg of alkaline chloroform fraction (Alk-CF) of R . mucronata by oral administration. Compared with controls, Alk-CF decreased the writhing numbers ( P < 0.01) in a dose-dependent manner. Further, we determined that Alk-CF contained, a potent compared to control, also potent anti-nociceptive agent that acted via opioid receptors and using HPLC, identified this compound as luteolin. Docking simulation demonstrated that luteolin interacted strongly with cyclooxygenase, forming a number of specific hydrogen bonds. This study identified peripheral and central anti-nociceptive activities of R. mucronata that involve opioid receptor, and in which the active compound is luteolin as a source of new anti-nociceptive agent. [ABSTRACT FROM AUTHOR]

Ferula assa-foetida L. is distributed throughout central Asia and Mediterranean area and grows wildly in Iran and Afghanistan. Asafoetida is an oleo-gum-resin that is the exudates of the roots of Ferula assa-foetida and some other Ferula species. In Iranian traditional medicine, asafoetida is considered to be sedative, analgesic, carminative, antispasmodic, diuretic, antihelmintic, emmenagogue and expectorant. The aim of this study was to evaluate the antinociceptive effect of asafoetida in mice. The analgesic activity of asafoetida (25, 50 and 100 mg/kg) was compared with that of sodium diclofenac (30 mg/kg) or morphine sulfate (8 mg/kg) by using hot plate and acetic acid induced writhing tests. In hot plate test, the percentage of maximum possible effect (%MPE) against the thermal stimulus at 15 min post treatment time point for all doses of asafoetida was significantly greater than the control group. The number of writhes in all three doses of asafoetida was significantly less than the control group. GraphPad Prism 5 software was used to analyze the behavioral responses. Data were analyzed using repeated measure one-way ANOVA and P<0.05 was considered as the significant level. According to our findings, asafoetida exhibited a significant antinociceptive effect on chronic and acute pain in mice. These effects probably involve central opioid pathways and peripheral anti-inflammatory action. [ABSTRACT FROM AUTHOR]

Context: Tarragon [ Artemisia dracunculus L. (Asteraceae)] is used as a commercial flavoring and in perfumery. In traditional folk medicine, tarragon has been used for treatment of pain and gastrointestinal disturbances. Objective: This study investigated the antinociceptive effect of the essential oil of A. dracunculus (EOAD) in various experimental models. Materials and methods: The median lethal dose (LD50) of EOAD was estimated using the method of Lorke. The antinociceptive effect was assessed using chemical (formalin and acetic acid) and thermal (hot-plate) nociceptive tests in rats and mice. In all experiments, EOAD was administered intraperitoneally at the doses of 10, 30, 100 and 300 mg/kg. Results: In the acute toxicity test, the value of estimated LD50 for EOAD was 1250 mg/kg. EOAD (100 and 300 mg/kg) significantly reduced ( p < 0.001) the pain response in the first (59.5 and 91.4%) and second (52.5 and 86.3%) phases of the formalin test, respectively. Central involvement in analgesic profile was confirmed by the hot-plate test, in which the EOAD showed a significant analgesic activity by increasing latency time. EOAD (10, 30, 100 and 300 mg/kg) significantly ( p < 0.001) inhibited (89, 95, 97 and 97%) the nociception produced by acetic acid. Naloxone failed to antagonize the antinociceptive effect of the essential oil in the acetic acid-induced writhing test. It seems that mechanism(s) other than opioid receptors is (are) involved in the analgesic effect of EOAD. Conclusions: This study reported the peripheral and central antinociceptive activity of the EOAD and rationalized the traditional use of the plant in the treatment of different painful conditions. [ABSTRACT FROM AUTHOR]

Abstract: Ziziyphus nummularia (family: Rhamnaceae) is a thorny small bush, grows in abundance in the grazing lands of the arid areas of Rajasthan, India. It is an important ethnomedicinal plant of the Thar Desert; local inhabitants use every part of the plant as medicine. Kernels are prescribed in pregnancy as soporific, antiemetic and for relieving abdominal pain. The insect gall is powered and given orally with water to cure bone fracture. Crushed root is applied on the paining shoulder of the bullock. The decoction of leaves is used for the treatment of cough and cold; leaves are also regarded as diaphoretic and prescribed in typhoid. Paste of leaves is used for healing of cuts, boils and cutaneous disease. It is widely used in pain and inflammatory conditions. Z. nummularia contains a unique group of alkaloids known as cyclopeptide alkaloids, in continuation of our work carried out on the leaves of Z. nummularia , present study was initiated to explore antiinflammatory and analgesic potential of cyclopeptide alkaloids isolated from the leaves of Z. nummularia (IFZN). Anti-inflammatory activity was tested against rat paw oedema, mouse peritonitis and cotton pellet granuloma. For screening of analgesic activity, acetic acid induced writhing, tail flick and hot plate test were performed. IFZN 30mg/kg shows the anti-oedematogenic effect against paw oedema induced by carrageenan, dextran, serotonin and histamine; IFZN 20 and 30mg/kg were found to have highly significant anti-nociceptive effects. Result of pharmacological studies indicated that IFZN is a potent and efficacious analgesic agent. The analgesic activity of IFZN is mediated by the peripheral as well as central pathways. [Copyright &y& Elsevier]

Abstract: Aim: Dasyatis jenkinsii is used traditionally to treat inflammatory complaints and arthritis by the fisherman community and local population. The present study was designed to scientifically investigate the traditional practice through the analgesic, anti-inflammatory, and organ toxicity studies and characterization of bioactive compounds of crude extracts of D. jenkinsii. Method: Solvent extract of homogenized fresh fish was prepared using petroleum ether and diethyl ether. The chemical and spectral analyses of extracts were carried out using FT-IR and GC-MS. Analgesic and anti-inflammatory activities were assessed by hot plate, tail clip, and carrageenan induced rat paw edema methods. The organ toxicity of each extract was assessed on brain, liver, and kidney of mice. Results: The IR spectrum indicated the presence of aromatic and aliphatic compounds. GC-MS analysis revealed the presence of 1-(4-carboxy)phenylnona-2, 5-diene and 3-hydroxymono-glyceryl hydrogen phthalate in the petroleum ether extract and carboxyl serine, dihydrotryptophan, and indolyl carboxylic acid in the diethyl ether extract. Both extracts showed significant analgesic and anti-inflammatory effects in all the methods tested. The vital organs of the test animals were not affected by the crude extracts significantly. Conclusions: The presence of biologically active compounds in the crude extracts with analgesic and anti-inflammatory properties justifies the traditional knowledge and paves the way for isolation of these compounds for further experimentation. [Copyright &y& Elsevier]

Background: The methanolic extract of Sargassum ilicifolium (Pheophyceae) was used to evaluate its analgesic and anti-inflammatory activity in the present study. Materials and Methods: Analgesic activity was tested using Acetic acid writhing method and Eddy hot plate method in Male albino mice and Wister rats respectively at a dose level of 1, 10, 50, 100mg/kg p.o. At the same dose, its anti-inflammatory activity was also tested using Carrageenan induced rat paw edema method Result Acetic acid writhing test and Eddy's hot plate episodes were significantly and dose dependently reduced. Carrageenan (a standard inflammatory agent) induced paw edema in rats was significantly reduced after intraperitonal administration of methanolic extract. Results: showed dose dependant significant activity in comparison with standard and control. Conclusion: Methanolic extracts of the brown seaweeds Sargassum ilicifolium have potent analgesic and anti-inflammatory activity at moderate doses. [ABSTRACT FROM AUTHOR]

A number of novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole derivatives 2 were obtained by alkylation mainly in the 1H-tautomeric form of 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole or its 8,9-dimethyl-substituted analog 4-chlorobenzyl bromide, 4-chloroacetic acid fluoroanilide, and 4-tert-butylphenacyl bromide in neutral medium. Compounds 3 were cyclized and synthesized earlier with 11-phenacyl-substituted diazepino[1,2-a]benzimidazoles upon heating in conc. HBr. The chemical structures of the compounds were clarified by using the 1H Nuclear Magnetic Resonance Spectroscopy (1H-NMR) technique. Anxiolytic properties were evaluated using the elevated plus maze (EPM) and open field (OF) tests. The analgesic effect of compounds was estimated with the tail flick (TF) and hot plate (HP) methods. Besides, possible the influence of the test compounds on motor activities of the animals was examined by the Grid, Wire, and Rotarod tests. Compounds 2d and 3b were the most active due to their prominent analgesic and anxiolytic potentials, respectively. The results of the performed in silico analysis showed that the high anxiolytic activity of compound 3b is explained by the combination of a pronounced interaction mainly with the benzodiazepine site of the GABAA receptor with a prominent interaction with both the specific and allosteric sites of the 5-HT2A receptor. [ABSTRACT FROM AUTHOR]