用两性霉素B-细胞模型法筛选胆固醇内源性合成抑制剂

The Use of Amphotericin B-Cells to Detect Inhibitors of Cellular Cholesterol Biosynthesis

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。

A new method for detecting inhibitors of cellular cholesterol biosynthesis is reported.It was established according to the,principle that amphotericin B binds sterols in the membranes of animal cells to form a complex which kills the cells.The method was simple,reliable and easy to handle. Morever,the-cost was low.Using this method,the authors had screened twenty Chinese herbs and found that Salvia miltiorrhiza and its extracts inhibit cellular cholesterol biosynthesis efficiently.