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一种来自南非叶下珠属植物的食欲抑制剂。

An appetite suppressant from Hoodia species.

作者信息

van Heerden Fanie R, Marthinus Horak R, Maharaj Vinesh J, Vleggaar Robert, Senabe Jeremiah V, Gunning Philip J

机构信息

School of Chemistry, University of KwaZulu-Natal, Private Bag X01, Scottsville 3209, South Africa.

出版信息

Phytochemistry. 2007 Oct;68(20):2545-53. doi: 10.1016/j.phytochem.2007.05.022. Epub 2007 Jul 2.

Abstract

Studies conducted at the Council for Scientific and Industrial Research (CSIR, South Africa) identified extracts from Hoodia species, in particular Hoodia pilifera and Hoodia gordonii, as possessing appetite suppressing properties. Two pregnane glycosides were isolated by fractionation of the dried stems of H. gordonii. Their structures were determined as 3beta-[beta-D-thevetopyranosyl-(1-->4)-beta-D- cymaropyranosyl-(1-->4)-beta-D-cymaropyranosyloxy]-12beta-tigloyloxy-14beta-hydroxypregn-5-en-20-one (1) and 3beta-[beta-D-cymaropyranosyl-(1-->4)-beta-D-6-thevetopyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranosyloxy]-12beta-tigloyloxy-14beta-hydroxypregn-5-en-20-one (2) on the basis of spectroscopic studies and conversion to known compounds. Compounds 1 and 2 were also isolated from H. pilifera. Compound 1 was tested for its appetite suppressant properties in rats by oral gavage at 6.25-50 mg/kg and the results showed that all doses resulted in a decrease of food consumption over an eight day period and a body mass decrease when compared to the control sample receiving only the vehicle. In a comparative study against a fenfluramine control sample, compound 1 resulted in a reduction in food intake over the study period, with a concomitant overall decrease in body weight while fenfluramine resulted in a small decrease in food intake, but an increase in body weight (though less than control group) over the same period of time.

摘要

南非科学与工业研究理事会(CSIR)开展的研究表明,多种南非仙人掌属植物的提取物,尤其是皮尔费拉仙人掌(Hoodia pilifera)和戈登氏仙人掌(Hoodia gordonii)的提取物,具有抑制食欲的特性。通过对戈登氏仙人掌干燥茎进行分馏,分离出了两种孕烷糖苷。基于光谱研究以及转化为已知化合物,确定它们的结构分别为3β-[β-D-葡糖醛酸基-(1→4)-β-D- cymaropyranosyl-(1→4)-β-D-cymaropyranosyloxy]-12β-惕各酰氧基-14β-羟基孕-5-烯-20-酮(1)和3β-[β-D-cymaropyranosyl-(1→4)-β-D-6-葡糖醛酸基-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranosyloxy]-12β-惕各酰氧基-14β-羟基孕-5-烯-20-酮(2)。化合物1和2也从皮尔费拉仙人掌中分离得到。通过对大鼠进行口服灌胃,以6.25 - 50 mg/kg的剂量测试了化合物1的食欲抑制特性,结果显示,与仅接受赋形剂的对照样品相比,所有剂量在八天内均导致食物摄入量减少以及体重下降。在一项与芬氟拉明对照样品的对比研究中,化合物1在研究期间导致食物摄入量减少,同时体重总体下降,而芬氟拉明导致食物摄入量略有减少,但在同一时间段内体重增加(尽管低于对照组)。

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