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BOUCHARDATINE AND BOUCHARDATINE DERIVATIVES, AND PREPARATION METHOD AND APPLICATION THEREFOR

机译:布卡他汀和布卡他汀衍生物及其制备方法和应用

摘要

Disclosed is an application of natural product bouchardatine and bouchardatine derivatives in the preparation of a drug combatting obesity and/or easing fatty liver generation. The structural formula of the bouchardatine derivatives is shown in formula (I), wherein: R is -(CH2)nR1, n being 0, 1, 2 or 3; R1 is selected from: (1) a phenyl group substituted with one or a plurality of R2s; (2) a morpholino group or a piperidyl group; (3) an N,N-dimethylamino group or an N,N-diethylamino group; R2 is a fluoro group, a methoxy group or a nitro group. The natural product and the derivatives thereof significantly inhibit the differentiation of 3T3-L1 preadipocytes and thereby reduce lipid accumulation within 3T3-L1 adipocytes, reduce the accumulation of lipids in human hepatoma cells caused by sodium oleate, and have the effects of reducing animal cell triglyceride levels, combatting obesity and easing fatty liver generation.
机译:公开了天然产物布加达汀和布加达汀衍生物在制备抗肥胖和/或减轻脂肪肝产生的药物中的应用。布加达丁衍生物的结构式如式(I)所示,其中:R为-(CH 2 n R 1 ,n为0、1、2或3; R 1 选自:(1)被一个或多个R 2 取代的苯基。 (2)吗啉代基或哌啶基; (3)N,N-二甲基氨基或N,N-二乙基氨基。 R 2 是氟,甲氧基或硝基。天然产物及其衍生物显着抑制3T3-L1前脂肪细胞的分化,从而减少3T3-L1脂肪细胞内的脂质蓄积,减少由油酸钠引起的人肝癌细胞中脂质的蓄积,并具有减少动物细胞甘油三酸酯的作用。降低肥胖,减轻脂肪肝的产生。

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