The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide
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摘要: 目的 研究抗真菌药物布替萘芬对真菌麦角甾醇生物合成的影响。 方法 通过真菌活细胞[1-14C]乙酸钠掺入和离细胞液[2-14C]甲羟戊酸掺入实验,考察布替萘芬对真菌麦角甾醇生物合成的影响。 结果 布替萘芬能使真菌中麦角甾醇的合成减少,而增加角鲨烯的含量,两种方法测得布替萘芬对真菌细胞麦角甾醇生物合成的IC50分别为136.19 nmol/L和203.15 nmol/L。 结论 布替萘芬为角鲨烯环氧化酶抑制剂,核素掺入法能定量考察布替萘芬对角鲨烯环氧化酶的抑制活性,且效果优于薄层色谱扫描法。Abstract: Objective To study the effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide. Methods The inhibitory effect of butenafine on ergosterol biosynthesis in whole-cell fungi was studied by measuring the incorporation of [1-14C] acetate into nonsaponifiable lipids( NSLs), while the effect in cell-free extracts was studied by measuring the incorporation of [2-14C] mevalonate into NSLs. Results The synthesis of ergosterol in fungi was significantly decreased after butenafine treatment, whereas the level of squalene was increased. The IC50 value of butenafine on ergosterol biosynthesis was 136.19 nmol/L in whole-cell study and 203.15 nmol/L in cell-free study. Conclusion The method to measure the incorporation of [1-14C]acetate and [2-14C] mevalonate into NSLs of fungi, which could indicate the level of squalene, might be widely used to study the mechanism of inhibitor of squalene epoxidase.
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Key words:
- butenafine /
- ergosterol /
- squalene epoxidase /
- fluid flash counter /
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