通过体外试验比较新型三唑类抗真菌药D0870与氟康唑对白色念珠菌细胞色素P-450的抑制作用。
Comparison of D0870, a new triazole antifungal agent, to fluconazole for inhibition of Candida albicans cytochrome P-450 by using in vitro assays.
作者信息
Venkateswarlu K, Denning D W, Manning N J, Kelly S L
机构信息
Department of Molecular Biology and Biotechnology, Krebs Institute for Biomolecular Research, Sheffield University, United Kingdom.
出版信息
Antimicrob Agents Chemother. 1996 Jun;40(6):1382-6. doi: 10.1128/AAC.40.6.1382.
Abstract
D0870 was 12 to 15 times more active than fluconazole in experiments to determine the MIC for growth arrest for two isolates of Candida albicans. A biochemical comparison of in vitro sterol biosynthesis in cell extracts showed only a twofold superiority of D0870 over fluconazole. A large differentiation (10-fold) in 50% saturating concentrations obtained by examining the binding of the azoles to microsomal P-450 was observed in a type II binding spectrophotometric assay, possibly reflecting the differential affinity for more than one P-450 enzyme. Additional mechanisms besides affinity for the target enzyme sterol 14 alpha-demethylase, such as differential intracellular accumulation of drug, may contribute to the differences in antifungal activity.
摘要
在确定两种白色念珠菌分离株生长停滞的最低抑菌浓度（MIC）的实验中，D0870的活性比氟康唑高12至15倍。对细胞提取物中体外甾醇生物合成的生化比较显示，D0870仅比氟康唑有两倍的优势。在II型结合分光光度测定法中，通过检测唑类与微粒体P-450的结合，观察到50%饱和浓度存在很大差异（10倍），这可能反映了对一种以上P-450酶的不同亲和力。除了对目标酶甾醇14α-脱甲基酶的亲和力外，其他机制，如药物在细胞内的不同积累，可能导致抗真菌活性的差异。
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