Antidiabetic and antidiarrhoeal effects on ethanolic extract of Psidium guajava(L.) Bat.leaves in Wister rats

Objective:To evaluate the antidiabetic and the antidiarrhoeal effects of ethanolic extracts of Psidium guajava leave(EEPGL) in Wisier rais to support its traditional uses.Methods:Oral glucose tolerance test model and alloxan induced diabetic test model were performed to evaluate antidiabetic activity of EEPGL at doses of 1.00.0.50 and 0.75 g/kg respectively.For antidiarrhoeal effects of EEPGL.castor oil-induced diarrhoea model and gastrointestinal motility test with barium sulphate milk model were also assessed at doses of750.500 and 250 mg/kg.respectively.Results:Administration of EEPGL at doses 1.00 and 0.50 g/kg significantly(P<0.05)decreased blood glucose levels in oral glucose tolerance test model as well as 0.75 g/kg dose in alloxan induced diabetic test model in Wister rats(P<0.001).Application of EEPGL at doses of 750 and 500 mg/kg showed antidiarrhoeal effect in castor oil-induced diarrhoeal model(P<0.00 l and P<0.01,respectively),and 750 mg/kg(P<0.01),500 and 250 mg/kg(P<0.05)doses in barium sulphate milk model in aforesaid animals.Conclusions:These results exhibited the significant antidiabetic and antidiarrhoeal activities of ethanolic extracts of Psidium guajava leave in Wister rats.

Therapeutic effects of Byrsocarpus coccineus root bark extract on bacterially and chemically induced diarrhea in the Wistar albino rat(Rattus norvegicus domestica)

Background : Diarrhea can be caused by pathogenic microorganisms and chemicals. In view of this, Byrsocarpus coccineus Schum and Thonn(Connaraceae) was used to treat diarrhea induced by castor oil or bacteria in Wistar albino rats. Methods : Qualitative and quantitative analyses of an aqueous root back extract of B. coccineus were made and the acute toxicity, antidiarrhea properties, and in vitro and in vivo antimicrobial activities of the extract were investigated in rats. Results : The phytochemical analysis of the root bark extract revealed the presence of flavonoids, alkaloid, saponins, tannins, and phenols. The quantitative analysis showed that saponins formed 10.6% of the extract, tannins 7.6%, flavonoids 6.2%, phenol 5.8% and alkaloids 4.4%. A dose limit of 5000 mg/kg was safe to use in the rats. At a dose of 100 mg/kg, the extract decreased distance travelled by activated charcoal in the gastrointestinal tract, frequency of defecation, and number of unformed faeces caused by castor oil-induced diarrhea, and led to 74.96% inhibition of the diarrhea effects. Escherichia coli and Salmonella pullorum were susceptible to higher concentrations of the extract with a minimum inhibitory concentration of 0.3125 mg/m L. E. coli-infected rats showed depression, weight loss, anorexia, diarrhea, and weakness, which was ameliorated by the extract on day 2 post treatment. Observed congestion, cellular infiltration and necrosis of the liver, intestine and kidney following infection were improved by the extract. Conclusion : B. coccineus extract can be used in the treatment of anaemia, and castor oil-and E. coli-induced diarrhea in rats.

盐酸洛哌丁胺的合成及成盐工艺研究

目的:研究盐酸洛哌丁胺、一种用于治疗骨质疏松症药物的关键中间体的制备方法。方法:以2,2-二苯基-γ-丁内酯为起始原料,经开环、SN2取代、酰氯化、季铵化、缩合和成盐制得。结果:当反应温度为25℃,反应时间为24 h,开环和SN2取代的产率为81%。第二步反应,当n(SOCl2):n(2,2-苯基-4-溴丁酸)=2:1、反应温度为回流时,HPLC显示2,2-苯基-4-溴丁酰氯(4)的含量为97.25%。第三步反应,当n(4):n(Na2CO3):n(二甲胺)的投料比为1.0:1.2:1.5,反应温度为0～5℃,关键中间体二甲基-(四氢-3,3-二苯基-2-呋喃叉基)溴化铵(5)的产率由文献报导的50%提高到68%。第四步洛哌丁胺游离碱的制备,较好的投料比为n(7’):n(Na2CO3):n(羟基哌啶)=1.0:1.2:1.1,收率为85%。最后一步成盐,在无水乙醇中调节pH为3左右,收率为89.6%。整个合成步骤(包括精制)的收率为34%,HPLC检测纯度达99.86%。其结构经IR、1H-NMR、13C-NMR和MS表征确认。结论:本制备方法克服了文献所报道的制备工艺的缺点,与现有技术相比,本发明后处理更简单,更适合工业化生产。