Gálvez J, Crespo M E, Jiménez J, Suárez A, Zarzuelo A
Department of Pharmacology, School of Pharmacy, University of Granada, Spain.
J Pharm Pharmacol. 1993 Feb;45(2):157-9. doi: 10.1111/j.2042-7158.1993.tb03706.x.
Quercitrin, a flavonoid isolated from Euphorbia hirta, shows antidiarrhoeic activity at doses of 50 mg kg-1, against castor oil- and PGE2-induced diarrhoea in mice, but not when magnesium sulphate is used as a cathartic agent. It also delays rat small intestinal transit if this is accelerated with castor oil. However, the flavonoid does not modify the fluid transport across the colonic mucosa when it is administered intraluminally, either in normal conditions or when this transport is altered by PGE2 or sodium picosulphate. However, quercetin, the aglycone of quercitrin, increases the colonic fluid absorption only in the presence of secretagogue compounds, such as PGE2 and sodium picosulphate. It is concluded that the antidiarrhoeic activity of quercitrin is due to its aglycone, quercetin, which is released by the glycoside in the intestine.
槲皮苷是从大戟属植物中分离出的一种黄酮类化合物,在50mg/kg剂量时对蓖麻油和PGE2诱导的小鼠腹泻有止泻活性,但以硫酸镁作为泻剂时则无此活性。如果用蓖麻油加速大鼠小肠蠕动,它也会延缓小肠蠕动。然而,无论在正常情况下还是当PGE2或匹可硫酸钠改变这种转运时,腔内给予该黄酮类化合物均不会改变其跨结肠黏膜的液体转运。但是,槲皮苷的苷元槲皮素仅在存在促分泌化合物(如PGE2和匹可硫酸钠)时才会增加结肠液体吸收。得出的结论是,槲皮苷的止泻活性归因于其苷元槲皮素,槲皮素由糖苷在肠道中释放。