以控制LDLR基因表达的调控元件SRE为靶位点 ,使用含有荧光素酶报告基因的转染人肝细胞系HepG2筛选模型高通量筛选微生物来源的能够增加低密度脂蛋白受体 (LDLR)基因表达的具有潜在的降胆固醇作用的生物活性物质。在筛选过程中 ,通过对一株真菌产生的化合物ascofuranone的研究发现该化合物对测活用细胞株的LDLR荧光素酶报告基因的表达有中等强度的激活作用 ,其SC150 为 40 .4μmol/L。Ascofuranone激活LDLR基因表达这一新的生物活性的发现为深入研究该化合物的降血脂作用提供了新的重要启示 The SRE, a regulatory element that controls LDLR gene expression, was used as a target site for high-throughput screening of microbial-derived low density lipoprotein receptor (LDLR) genes using a HepG2 screening model of a transfected human hepatocyte line with a luciferase reporter Expressed biologically active substances that have a potential hypocholesterolemic effect. In the screening process, the compound ascofuranone produced by a strain of fungi was found to have a moderate activation of the LDLR luciferase reporter gene expression in the assay cell line with a SC150 of 40.4 μmol / L. The discovery that Ascofuranone activates the new biological activity of LDLR gene expression provides new important insights into the hypolipidemic effects of this compound