Nimura K, Niwano Y, Ishiduka S, Fukumoto R
Pharmaceutical Research Department, Sato Pharmaceutical Co., Ltd., 8-5 Higashi-ohi, 6-Chome, Shinagawa-ku, 140-0011, Tokyo, Japan.
Int J Antimicrob Agents. 2001 Aug;18(2):173-8. doi: 10.1016/s0924-8579(01)00365-x.
In vitro anti-dermatophyte, anti-Candida albicans and anti-Malassezia furfur activities of amorolfine hydrochloride (AMF), terbinafine hydrochloride (TBF), butenafine hydrochloride (BTF), neticonazole hydrochloride (NCZ) and ketoconazole (KCZ), all of which were introduced for the treatment of dermatomycoses in the 1990s in Japan, were compared. Although all of the test drugs are classified as an ergosterol biosynthesis inhibitor, the antifungal properties were found to be different. TBF and BTF exerted extremely potent antifungal activity against Trichophyton spp. but not against C. albicans and M. furfur, whilst KCZ and NCZ showed potent antifungal activity against C. albicans and M. furfur rather than Trichophyton spp. AMF exhibited potent antifungal activity against all of the fungal species tested. Fungicidal activities of these antifungal agents against T. rubrum were determined by using neutral red staining. The fungicidal potentialities correlated with those obtained in the in vitro susceptibility test as determined by MICs against dermatophytes. TBF, BTF and AMF exerted more potent fungicidal action than NCZ and KCZ.
对盐酸阿莫罗芬（AMF）、盐酸特比萘芬（TBF）、盐酸布替萘芬（BTF）、盐酸奈替康唑（NCZ）和酮康唑（KCZ）的体外抗皮肤癣菌、抗白色念珠菌和抗糠秕马拉色菌活性进行了比较，所有这些药物于20世纪90年代在日本被引入用于治疗皮肤真菌病。尽管所有受试药物均归类为麦角固醇生物合成抑制剂，但发现它们的抗真菌特性有所不同。TBF和BTF对毛癣菌属具有极强的抗真菌活性，但对白色念珠菌和糠秕马拉色菌无活性，而KCZ和NCZ对白色念珠菌和糠秕马拉色菌显示出较强的抗真菌活性，而非对毛癣菌属。AMF对所有受试真菌均表现出较强的抗真菌活性。通过中性红染色测定了这些抗真菌剂对红色毛癣菌的杀菌活性。杀菌潜力与通过对皮肤癣菌的最低抑菌浓度（MIC）测定的体外药敏试验结果相关。TBF、BTF和AMF比NCZ和KCZ具有更强的杀菌作用。
