硫代氨基甲酸盐类抗真菌剂托萘酯和托西拉酯对麦角固醇生物合成的抑制作用。
Ergosterol biosynthesis inhibition by the thiocarbamate antifungal agents tolnaftate and tolciclate.
作者信息
Ryder N S, Frank I, Dupont M C
出版信息
Antimicrob Agents Chemother. 1986 May;29(5):858-60. doi: 10.1128/AAC.29.5.858.
Abstract
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.
摘要
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。
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Properties of a particulate squalene epoxidase from Candida albicans.白色念珠菌中一种颗粒状角鲨烯环氧化酶的特性
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Effect of the antimycotic drug naftifine on growth of and sterol biosynthesis in Candida albicans.抗真菌药物萘替芬对白色念珠菌生长及甾醇生物合成的影响。
Antimicrob Agents Chemother. 1984 Apr;25(4):483-7. doi: 10.1128/AAC.25.4.483.
7
Specific inhibition of fungal sterol biosynthesis by SF 86-327, a new allylamine antimycotic agent.新型烯丙胺类抗真菌剂SF 86-327对真菌甾醇生物合成的特异性抑制作用。
Antimicrob Agents Chemother. 1985 Feb;27(2):252-6. doi: 10.1128/AAC.27.2.252.
8
Effects of antifungal agents on ergosterol biosynthesis in Candida albicans and Trichophyton mentagrophytes: differential inhibitory sites of naphthiomate and miconazole.抗真菌剂对白色念珠菌和须癣毛癣菌麦角固醇生物合成的影响：萘硫酯和咪康唑的不同抑制位点
J Invest Dermatol. 1985 Nov;85(5):434-7. doi: 10.1111/1523-1747.ep12277141.
9
Effect of allylamine antimycotic agents on fungal sterol biosynthesis measured by sterol side-chain methylation.通过甾醇侧链甲基化测定烯丙胺抗真菌剂对真菌甾醇生物合成的影响。
J Gen Microbiol. 1985 Jul;131(7):1595-602. doi: 10.1099/00221287-131-7-1595.
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Inhibition of squalene epoxidase by allylamine antimycotic compounds. A comparative study of the fungal and mammalian enzymes.烯丙胺抗真菌化合物对角鲨烯环氧酶的抑制作用。真菌和哺乳动物酶的比较研究。
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