【摘要】 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。更多还原

【Abstract】 Objective To reviewthe progress of scavenger receptor class B type I( SR-BI) up-regulators.Methods The relevant 29 papers on SR-BI up-regulators were summarized and analyzed. Results SR-BI,a high density lipoprotein( HDL) receptor,plays a key role in mediating selective HDL cholesterol( HDL-C)uptake in the liver. SR-BI over-expression in the liver have markedly accelerated cholesterol and reduced plasma cholesterol levels. Therefore,SR-BI up-regulator may be an attractive newdrug aimed at atherosclerosis. Many reported natural or synthetic compounds showed SR-BI up-regulate activity and were deserved further study. Conclusions The compounds’ activity were not very well and difficult to develop as SR-BI up-regulator candidates,bnt they can be used as lead compounds for the development of novel SR-BI up-regulators.更多还原