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In vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis.抗真菌药物酮康唑对甾醇合成的体外和体内作用。
Antimicrob Agents Chemother. 1980 Jun;17(6):922-8. doi: 10.1128/AAC.17.6.922.
2
Inhibition of ergosterol synthesis in Candida albicans by ketoconazole [proceedings].
Arch Int Physiol Biochim. 1979 Oct;87(4):849-51.
3
The mechanism of action of the new antimycotic ketoconazole.新型抗真菌药酮康唑的作用机制。
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4
Correlation of inhibition of sterol synthesis with growth-inhibitory action of imidazole antimycotics in Candida albicans.
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A new era in antimycotic agents.
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6
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本文引用的文献

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Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
The effect of sterol structure on the permeability of lipomes to glucose, glycerol and Rb + .甾醇结构对脂质体对葡萄糖、甘油和铷离子通透性的影响。
Biochim Biophys Acta. 1972 Jan 17;255(1):321-30. doi: 10.1016/0005-2736(72)90031-4.
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State of molecular motion of cholesterol in lecithin bilayers.卵磷脂双分子层中胆固醇的分子运动状态
Nature. 1975 Aug 14;256(5518):582-4. doi: 10.1038/256582a0.
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The action of miconazole of the growth of Candida albicans.咪康唑对白色念珠菌生长的作用。
Sabouraudia. 1975 Mar;13 Pt 1:63-73.
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Oral therapy for experimental coccidioidomycosis with R41 400 (ketoconazole), a new imidazole.
Am Rev Respir Dis. 1978 Oct;118(4):715-21. doi: 10.1164/arrd.1978.118.4.715.
6
Speculations on the evolution of sterol structure and function.关于固醇结构与功能演变的推测
CRC Crit Rev Biochem. 1979 Nov;7(1):1-5. doi: 10.3109/10409237909102566.
7
Antimycotic imidazoles. part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent.抗真菌咪唑类。第4部分。酮康唑的合成及抗真菌活性,一种新型强效口服活性广谱抗真菌剂。
J Med Chem. 1979 Aug;22(8):1003-5. doi: 10.1021/jm00194a023.
8
Effects of miconazole and dodecylimidazole on sterol biosynthesis in Ustilago maydis.咪康唑和十二烷基咪唑对玉米黑粉菌中甾醇生物合成的影响。
Antimicrob Agents Chemother. 1979 Apr;15(4):603-7. doi: 10.1128/AAC.15.4.603.
9
Ketoconazole -- a new broad spectrum orally active antimycotic.酮康唑——一种新型口服活性广谱抗真菌药。
Experientia. 1979 May 15;35(5):606-7. doi: 10.1007/BF01960348.
10
Promotion of pseudomycelium formation of Candida albicans in culture: a morphological study of the effects of miconazole and ketoconazole.培养中白色念珠菌假菌丝形成的促进作用:咪康唑和酮康唑作用效果的形态学研究
Postgrad Med J. 1979 Sep;55(647):687-91. doi: 10.1136/pgmj.55.647.687.

抗真菌药物酮康唑对甾醇合成的体外和体内作用。

In vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis.

作者信息

Van den Bossche H, Willemsens G, Cools W, Cornelissen F, Lauwers W F, van Cutsem J M

出版信息

Antimicrob Agents Chemother. 1980 Jun;17(6):922-8. doi: 10.1128/AAC.17.6.922.

DOI:10.1128/AAC.17.6.922
PMID:6250469
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC283904/
Abstract

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.

摘要

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。