水翁花提取物的PPARγ配体活性鉴定  

Identify and Characterize the PPARγ Ligand-binding Activity of Extracts of Cleistocalyx Operculatus

作　　者：金晓辉[1] 魏孝义[1] 黄志伟[2] 吴东海[2] 

机构地区：[1]中国科学院华南植物园,广东广州510650 [2]中国科学院广州生物医药与健康研究院,广东广州510663

出　　处：《安徽农业科学》2008年第21期9106-9109,共4页Journal of Anhui Agricultural Sciences

基　　金：国家自然科学基金资助项目(30670457);国家973计划资助项目(2004CB720102)

摘　　要：[目的]鉴定水翁花提取物2,4-二羟基-6-甲氧基-3,5-二甲基查耳酮(DMC)的PPARγ配体结合活性及其特点。[方法]用GAL4嵌合体报告基因试验检测DMC的PPARγ配体结合活性;用油红O染色法检测DMC对3T3-L1前脂肪细胞分化的影响;用[3H]-2-脱氧葡萄糖摄取试验检测DMC对3T3-L1脂肪细胞葡萄糖摄取的影响;用荧光实时定量PCR检测经DMC处理的3T3-L1脂肪细胞中PPARγ靶基因的表达情况。[结果]DMC能以剂量依赖型的方式对PPARγ产生激活作用,促进脂肪细胞的分化,显著提高脂肪细胞的葡萄糖摄取率,并且提高脂肪细胞中一些PPARγ靶基因的表达量。[结论]DMC能通过激活PPARγ促进脂肪细胞的葡萄糖摄取。[Objective] To identify and characterize the peroxisome proliferator-activated receptor-γ（PPARγ） ligand-binding activity of 2,4-dihydroxy-6-methoxy-3,5-dimethylchalcone, a chalcone derivative extracted from the dried flower of Cleistocalyx operculatus.[Method] The PPARγ-transactivation activity of DMC was examined by using a GAL4 hybrid reporter gene assay. The effect of DMC on adipogenesis was measured by oil red O staining. The glucose uptake rate was measured by using [^3H]-2-deoxy glucose in 3T3-L1 adipocytes after treatment with DMC. The effect of DMC on expression of PPARγ target genes in differentiated 3T3-L1 adipocytes was examined by real-time PCR. [Results] DMC can selectively activate PPARγ with a dose-dependent manner. Result of oil red O staining showed that DMC can promote adipocyte differentiation. DMC can also strongly enhance glucose uptake in 3T3-L1 adipocytes. Furthermore, the result of real-time PCR showed the DMC can modulate some PPARγ-responsive genes in differentiated 3T3-L1 adipocytes. [Conclusion] Our data establish DMC as a natural PPARγ ligand with capability of promoting glucose uptake in 3T3-L1 adipocytes.

关 键 词：水翁花 PPARΓ 葡萄糖摄取 

分 类 号：S571.9[农业科学—作物学]