咪唑类抗真菌剂的抗真菌活性与疏水性之间的相关性。

Correlation between antifungal activity and hydrophobicity of imidazole antifungal agents.

作者信息

Hashiguchi T, Itoyama T, Kodama A, Uchida K, Yamaguchi H

机构信息

Tsukuba Research Laboratories, Hisamitsu Pharmaceutical Co., Inc., Japan.

出版信息

Arzneimittelforschung. 1997 Nov;47(11):1263-5.

PMID:9428985

Abstract

To examine the effects of the affinity of antifungal imidazole agents to cell membranes on the in vitro antifungal activity, the correlation between antifungal activity and hydrophobicity of these drugs was investigated. The capacity factor (k') in HPLC was used as a parameter of hydrophobicity, and the minimum inhibitory concentration (MIC) as a parameter of antifungal activity. Consequently, a significant portion correlation was noted in the case of Candida albicans. However, no obvious correlation was noted for Trichophyton mentagrophytes and Trichophyton rubrum. Therefore, the mechanism of action of imidazole derivatives for Candida albicans was considered to mainly consist in the membrane action.

摘要

为研究抗真菌咪唑类药物与细胞膜的亲和力对其体外抗真菌活性的影响，考察了这些药物的抗真菌活性与疏水性之间的相关性。采用高效液相色谱法中的容量因子（k'）作为疏水性参数，最小抑菌浓度（MIC）作为抗真菌活性参数。结果发现，对于白色念珠菌，二者存在显著的部分相关性。然而，对于须癣毛癣菌和红色毛癣菌，未观察到明显的相关性。因此，认为咪唑衍生物对白色念珠菌的作用机制主要在于膜作用。