苦瓜降血糖活性部位的高通量筛选研究.pdfVIP

天然产物研究与开发 NatProdResDev，2007，19：26-30 文章编号：1001-6880(2007)Suppl-O026-05 苦瓜降血糖活性部位的高通量筛选研究 何新益，刘仲华 ，黄建安 湖南农业大学天然产物研究中心，长沙410128 摘 要：PPAR与2型糖尿病存在密切关系，该受体已成为抗2型糖尿病的主要靶点。苦瓜是一种民间的中草 药，药理实验文献报道具有显著的降血糖作用。本文以PPAR三种亚型PPARa、PPAR3,和PPARD／8为靶点的 高通量筛选模型，对苦瓜多糖进行活性筛选。筛选结果表明MC-3对PPAR8和PPA脚具有较强的激活效果，其 激活倍数分别达1．995、1．689。MC．3是一种潜在的降糖、降脂的活性部位。 关键词：PPAR；HTS；苦瓜；2型糖尿病 中图分类号：R96 文献标识码：A Studies on Screening Anti-diabetic Agonist from Momordica charanti a L．by HTS ． HE Xin—yi，LIU Zhong—hua ，HUANG Jian—an Research Center ofNaturalProducts，HunanAgricultural University，Changsha410128，China Abstract：It iS found that type 2 diabetes millitus is closely related to PPAR in recent years．Therefore．PPAR is now em． ployed as main target in developing anti—diabetes for treatment of type 2 diabetes miUitus．Momordica charantia L．is a traditional Chinese medical herb．References research showed that there were some hypoglycemlc active components in Momordica charantin L．Screening PPARa，B／8， agonist from Momordica charantia extracts by HTS was studied in this paper．Results showed that MC·3 was an agonist of PPAR~and PPARD／8 and the activity times were 1．689 and 1．995． respectively．MC一3 can be a potential anti·diabetic agent． Key words：PPAR；HTS；Momordica charantia L．；type 2 diabetes meatus 随着多种研究手段的介人，对糖尿病药物的研 模型。近年来发展起来的高通量筛选 (High 究以酶或受体为靶点的药物筛选成为寻找新药的关 throughput screening，HTS)是一种快速高效的体外 键途径…。2型糖尿病与过氧化物酶增殖体化受体 药物活性筛选方法，首先用体外方法寻找对特定靶 (peroxisome proliferator·activated receptor，PPAR)存 点有生物活性的化合物，然后根据已获得信息进一 在密切的关系 剖。PPAR属于由配体激活的