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目的:探讨中药厚朴的重要成份厚朴酚对肝X受体α(liver X receptorα,LXRα)介导的脂代谢的影响。方法:在人肝癌细胞系HepG2及人单核细胞株THP-1中,通过哺乳动物细胞单杂交,哺乳动物细胞转录激活以及Western blot检测不同浓度的厚朴酚与LXRα的结合,转录活性及其对下游基因(ABCA1和ABCG1)表达的影响。结果:厚朴酚与LXRα呈浓度依赖性,并调节LXRα的转录活性,并且能够调节THP1巨噬细胞中LXRα下游ABCA1和ABCG1蛋白呈剂量依赖性的增加。结论:厚朴酚能够作用于LXRα,这可能为厚朴酚降脂功能提供了一种新的分子机制。
Objective: To investigate the effect of magnolol, an important component of Magnolia officinalis, on lipid metabolism mediated by liver X receptor α (LXRα). METHODS: The binding and transactivating activities of different concentrations of honokiol and LXRα in human hepatocellular carcinoma cell line HepG2 and human monocytic cell line THP-1 were examined by mammalian cell single-hybridization, mammalian cell transcriptional activation and Western blotting On downstream genes (ABCA1 and ABCG1) expression. Results: Magnolol reacted with LXRα in a concentration-dependent manner and regulates the transcriptional activity of LXRα, and can regulate the dose-dependent increase of ABCA1 and ABCG1 protein downstream of LXRα in THP1 macrophages. CONCLUSION: Magnolol can act on LXRα, which may provide a new molecular mechanism for honokiol lipid-lowering function.