Comparison of D0870, a new triazole antifungal agent, to fluconazole for inhibition of Candida albicans cytochrome P-450 by using in vitro assays

被引：24

作者：

Venkateswarlu, K

Denning, DW

Manning, NJ

Kelly, SL

机构：

[1] UNIV SHEFFIELD,KREBS INST BIOMOLEC RES,DEPT MOLEC BIOL & BIOTECHNOL,SHEFFIELD S10 2UH,S YORKSHIRE,ENGLAND

[2] SHEFFIELD CHILDRENS HOSP,NEONATAL SCREENING LAB,SHEFFIELD S10 2UH,S YORKSHIRE,ENGLAND

[3] UNIV MANCHESTER,N MANCHESTER GEN HOSP,DEPT TROP MED & INFECT DIS,SALFORD M6 8HD,LANCS,ENGLAND

[4] UNIV MANCHESTER,N MANCHESTER GEN HOSP,DEPT MED,SALFORD M6 8HD,LANCS,ENGLAND

[5] HOPE HOSP,SALFORD M6 8HD,LANCS,ENGLAND

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 1996年 / 40卷 / 06期

关键词：

D O I：

10.1128/AAC.40.6.1382

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

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.

引用

页码：1382 / 1386

页数：5

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