Berg D, Draber W, von Hugo H, Hummel W, Mayer D
Z Naturforsch C Biosci. 1981 Sep-Oct;36(9-10):798-803.
Clotrimazole and triadimefon are known as potent inhibitors of ergosterol synthesis in pathogenic yeast and fungi, respectively. As their mode of action generally the inhibition of sterol desmethylation reactions is accepted. We report about a second effect, a "feed-back" inhibition of 3-hydroxy-3-methyl-glutaryl (HMG)-CoA-reductase by accumulation of ergosterol precursors. Addition of lanosterol to intact cells leads to an inhibition of HMG-CoA-reductase as well, but not to fungistatic effects. From the reported data the influences of clotrimazole and triadimefon have to be considered as an inhibition of desmethylation reactions involved in ergosterol synthesis of yeast and fungi with a concomitant decreased production of mevalonate.
克霉唑和三唑酮分别是致病性酵母和真菌中麦角固醇合成的有效抑制剂。一般认为它们的作用方式是抑制甾醇去甲基化反应。我们报道了第二种效应，即麦角固醇前体的积累对3-羟基-3-甲基戊二酰辅酶A（HMG）还原酶的“反馈”抑制。向完整细胞中添加羊毛甾醇也会导致HMG还原酶受到抑制，但不会产生抑菌作用。根据所报道的数据，必须将克霉唑和三唑酮的影响视为对酵母和真菌麦角固醇合成中去甲基化反应的抑制，同时甲羟戊酸的产生减少。
