Ryder N S, Frank I, Dupont M C
Antimicrob Agents Chemother. 1986 May;29(5):858-60. doi: 10.1128/AAC.29.5.858.
The thiocarbamate antimycotics tolnaftate and tolciclate blocked sterol biosynthesis in fungal cells and cell extracts, with accumulation of squalene. This point of action was confirmed by the direct inhibition of microsomal squalene epoxidase from Candida albicans. There was no inhibition of other steps in ergosterol biosynthesis. In whole Candida cells, ergosterol biosynthesis inhibition was not complete at drug concentrations up to 100 mg/liter, whereas full inhibition occurred in a cell-free test system. Rat liver cell-free cholesterol biosynthesis was much less sensitive to the drugs. The biochemical action of tolnaftate and tolciclate is thus similar to that of the allylamine antimycotics naftifine and terbinafine.
硫代氨基甲酸盐类抗真菌药托萘酯和托西拉酯可阻断真菌细胞和细胞提取物中的甾醇生物合成，并导致角鲨烯积累。通过直接抑制白色念珠菌的微粒体角鲨烯环氧化酶，证实了这一作用点。麦角固醇生物合成的其他步骤未受抑制。在完整的白色念珠菌细胞中，药物浓度高达100毫克/升时，麦角固醇生物合成抑制并不完全，而在无细胞测试系统中则出现完全抑制。大鼠肝细胞无细胞胆固醇生物合成对这些药物的敏感性要低得多。因此，托萘酯和托西拉酯的生化作用与烯丙胺类抗真菌药萘替芬和特比萘芬相似。
