ABSTRACT
In recent years highly selective COX-2inhibitors were withdrawn from the market because of an increased risk of cardiovascular complications. In this study we were looking for potent compounds with moderate selectivity for COX-2. So, four analogues of 4, 5-diaryl-2-[2-alkylthio-5-imidazolyl] imidazole derivatives were synthesized and their anti-inflammatory and anti-nociceptive activities were evaluated on male BALB/c mice [25-30 g]. Molecular modeling and in vitro COX-1 and COX-2 isozyme inhibition studies were also performed. 2-[2-Alkylthio-5-imidazolyl]-4,5-diphenylimidazole compounds were obtained by the reaction of benzyl with 2-alkylthio-1-benzylimidazole-5-carbaldehyde, in the presence of ammonium acetate. Spectroscopic data and elemental analysis of compounds were obtained and their structures elucidated. Anti-nociception effects were examined using writhing test in mice. The effect of the analogues [7.5, 30, 52.5 and 75 mg/kg] against acute inflammation were studied using xylene-induced ear edema test in mice. Celecoxib [75 mg/kg] was used as positive control. All four analogues exhibited anti-nociceptive activity against acetic acid induced writhing, but did not show significant analgesic effect [P< 0.05] compared with celecoxib. It was shown that analogues injected 30 min before xylene application reduced the weight of edematic ears. All analogues were found to have less selectivity for COX-2 in comparison to celecoxib. Injected doses of synthesized analogues possesses favorite anti-nociceptive effect and also has anti-inflammatory effects, but comparing with celecoxib this effect is not significantly different. On the other hand selectivity index for analogues is less than celecoxib and so we expect less cardiovascular side effects for these compounds
ABSTRACT
Pistacia sp. has been used in folk medicine for many years and previous studies have demonstrated its hypnotic effects. In this research, the effects of P. vera gum hydroalcoholic extract on muscle relaxation, sleep and anxiety were studied in mice. The effects of the intraperitoneal injection of the extract on muscle relaxation and coordination [traction and Rotarod tests, 30 and 60 min. after injection, respectively], sleep latency and duration of the sleep induced by pentobarbital [injected 30 min. after the extract], anti-anxiety effects [Elevated plus maze, 30 min. after injection] and locomotion activity [Open field test, 60 min. after injection] were studied. The extract [doses of 0.25, 0.5 and 1 g/kg] showed hypnotic effect, increase in duration of sleep by all doses and decrease in the sleep latency only by the dose of 1 g/kg], anti-anxiety effect in elevated plus maze, muscle relaxant effect [only effective at the dose of 1 g/kg in the traction test] and locomotion depressant effect at all doses [P<0.001]. This study showed that the hydroalcoholic extract of P. vera gum has hypnotic, anti-anxiety and muscle relaxant activities. Thus, it may be effective in the alleviation of the muscles contractions disorders, insomnia and anxiety
Subject(s)
Animals, Laboratory , Plant Extracts , Medicine, Traditional , Mice , Neuromuscular Agents , Anti-Anxiety Agents , Hypnotics and SedativesABSTRACT
This study was initiated to investigate the effect of Portulaca oleraceae on morphine dependence in mice. Dependence was induced using the subcutaneous injections of morphine for 3 days. On the day 4, morphine injected 2 h prior to intraperitoneal injection of naloxone. The plant extracts ethanolic or aqueous administered 0.5 h before the final dose of morphine. The number of jumping during the 30 min period after naloxone injection was considered as a measure of withdrawal syndrome. Both extracts reduced the jumping episodes dose-dependently. The maximum effect was observed at doses of 0.28 g/kg and 1.4 g/kg for the aqueous and ethanolic extracts, respectively. Clonidine and extracts decreased the total activity in locomotion test. These findings indicated that Portulacea oleraceae extracts can decrease morphine dependence in mice