[关键词]
[摘要]
目的:从57个中药化合物筛选具有抑制3T3-L1脂肪细胞脂质堆积的活性成分。方法:3T3-L1细胞培养至融合后用化合物进行干预,并诱导使其分化,采用高内涵影像方法检测细胞中脂滴含量。对发现的活性成分用ToxInsight体外毒性检测方法评价其肝毒性。结果:发现并验证活性成分齐墩果酸(OA)具有显著的脂质形成抑制作用,其半数抑制浓度(IC50)为14.5 μmol·L-1,且在60 μmol·L-1测试浓度范围内对HepG2 细胞无显著损伤作用。结论:OA 具有显著的降低脂质形成作用,是潜在的降脂候选化合物。
[Key word]
[Abstract]
A collection of 57 natural compounds derived from Chinese herbal medicines were evaluated for their anti-adipogenic effects. The lipid droplets in differentiated 3T3-L1 adipocytes treated with tested substrate were detected by an image-based assay. The results demonstrated that oleanolic acid (OA) inhibited lipid droplets accumulation in 3T3-L1 adipocytes in a dose-dependent manner with the IC50 value of 14.5 μmol·L-1. In addition, ToxInsight assay showed that OA was free of liver injury for HepG2 cells within 60 μmol·L-1. It was concluded that OA, which had an obvious anti-adipogenic effect, can be a candidate for hyperlipidemia therapy.
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[基金项目]
科学技术部国家科技支撑计划项目(2008BAI51B01):中药有效成分群辨识技术研究,负责人:张宏桂;北京中医药大学开放课题(2013-SYSK-FKT-04):中药基础与新药研究重点实验室,负责人:乔延江。