Van den Bossche H, Willemsens G, Cools W, Cornelissen F, Lauwers W F, van Cutsem J M
Antimicrob Agents Chemother. 1980 Jun;17(6):922-8. doi: 10.1128/AAC.17.6.922.
Ketoconazole, an orally active antimycotic drug, is a potent inhibitor of ergosterol biosynthesis in Candida albicans when added to culture media which support yeast or mycelial growth or to cultures containing outgrown mycelium. This inhibition coincides with accumulation of sterols with a methyl group at C-14 and can thus be attributed to an interference with one of the reactions involved in the removal of the 14 alpha-methyl group of lanosterol. When administered to rats infected with C. albicans, ketocanazole also inhibits fungal synthesis of ergosterol. A six-times-higher dose is required to effect cholesterol synthesis by rat liver.
酮康唑是一种口服活性抗真菌药物,当添加到支持酵母或菌丝体生长的培养基中,或添加到含有已生长出的菌丝体的培养物中时,它是白色念珠菌中麦角甾醇生物合成的有效抑制剂。这种抑制作用与C-14位带有甲基的甾醇积累相吻合,因此可归因于对羊毛甾醇14α-甲基去除过程中所涉及的一种反应的干扰。当给感染白色念珠菌的大鼠给药时,酮康唑也会抑制真菌麦角甾醇的合成。而抑制大鼠肝脏胆固醇合成则需要高六倍的剂量。