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目的综述B类I型清道夫受体(scavenger receptor class B type I,SR-BI)基因表达上调剂的研究进展。方法查阅近年来国内外相关文献29篇,对其进行归纳总结和分析。结果 SR-BI是高密度脂蛋白(high density lipoprotein,HDL)受体,能选择性介导胆固醇和HDL颗粒中胆固醇酯的吸收,在HDL的代谢中起重要作用。提高SR-BI基因表达,可促进胆固醇外流,降低血浆胆固醇水平,因此SR-BI基因表达上调剂有望成为新型抗动脉粥样硬化药物。许多报道的天然或合成小分子化合物具有SR-BI基因表达上调活性,有进一步研究价值。结论已报道的化合物虽然活性值不高,直接作为SR-BI基因表达上调剂候选药物应用较为困难,但以其为先导化合物,进行结构优化,对发现新的结构新颖、活性显著的SR-BI基因表达上调剂有重要意义。
OBJECTIVE: To summarize the research progress of the gene expression regulation of type I scavenger receptor class B type I (SR-BI). Methods To review 29 related literatures at home and abroad in recent years, summarize and analyze them. Results SR-BI, a high density lipoprotein (HDL) receptor, selectively mediates the uptake of cholesterol esters in cholesterol and HDL granules and plays an important role in the metabolism of HDL. Improve SR-BI gene expression, can promote cholesterol efflux and lower plasma cholesterol levels, so upregulation of SR-BI gene expression is expected to become a new anti-atherosclerotic drug. Many reported natural or synthetic small molecule compounds have SR-BI gene expression upregulation activity, with further research value. CONCLUSION: The reported compounds are difficult to be directly used as drug candidates for the up-regulation of SR-BI gene expression. However, SR-BI, a new structurally novel and active SR-BI Up-regulation of gene expression is of great importance.