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巨噬细胞中胆固醇流出并转运到肝脏的过程是抗动脉粥样硬化的主要机制之一。在动脉粥样硬化的发生发展中,核受体超家族成员肝X受体α(LXRα)和其上游基因过氧化物酶体增殖物活化受体γ(PPARγ)可通过调控ATP结合盒转运体(ABC)A1、B族清道夫受体1和ABCG1等介导细胞内胆固醇的流出。因此,PPARγ-LXRα-ABC通路在巨噬细胞胆固醇流出机制中具有重要作用。目前,临床使用的化学类降脂药物在改善动脉粥样硬化方面具有良好作用。研究表明,很多中药来源的天然产物可有效促胆固醇流出。本文对改善胆固醇流出的相关作用靶分子及相关药物研究进展做简要综述。
The process of cholesterol efflux and transport to the liver in macrophages is one of the major anti-atherogenic mechanisms. In the development of atherosclerosis, hepatic X receptor α (LXRα) and its upstream gene peroxisome proliferator activated receptorγ (PPARγ), a member of the nuclear receptor superfamily, can regulate the ATP binding cassette transporter (ABC) A1, B group scavenger receptor 1 and ABCG1 and other mediated intracellular cholesterol efflux. Therefore, the PPARγ-LXRα-ABC pathway plays an important role in macrophage cholesterol efflux mechanism. At present, the clinical use of chemical lipid-lowering drugs in the improvement of atherosclerosis has a good effect. Studies have shown that many natural products of traditional Chinese medicine can effectively promote cholesterol efflux. This review summarizes the progress of research on the related target molecules and related drugs to improve cholesterol efflux.