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本文介绍一种新的筛选胆固醇(Ch)内源性合成抑制剂的细胞模型。该模型利用两性霉素 B 可与动物细胞膜上的 Ch 形成复合物,从而使细胞膜上出现微孔并进而导致细胞死亡的原理,在缺乏外源性 Ch 供给的条件下,筛选 Ch 内源性合成抑制剂,能抑制 Ch合成的制剂可阻止上述复合物的形成,因而细胞存活。用本法筛选多种中草药后发现丹参及其提取物丹参素能显著抑制细胞内源性 Ch 合成,与对照组比 P<0.001。本法主要适于大量初筛及定性 Ch 合成抑制剂,对开发降 Ch 药物具有实际意义。
This article describes a new cell model for screening cholesterol (Ch) endogenous synthetic inhibitors. This model utilizes the principle that amphotericin B forms complexes with Ch on animal cell membranes, thereby allowing the appearance of micropores on the cell membrane and thereby leading to cell death. Screening Ch for endogenous synthesis in the absence of exogenous Ch supply Inhibitors, agents that inhibit Ch synthesis can prevent the formation of complexes described above, and thus cells survive. After screening a variety of Chinese herbal medicines by this method, it was found that Salvia miltiorrhiza and its extract, Danshensu, can significantly inhibit the endogenous Ch synthesis of cells, with P<0.001 compared with the control group. This method is mainly suitable for a large number of primary screening and qualitative Ch synthesis inhibitors, and has practical significance for the development of Ch-lowering drugs.