Oku Yukio, Takahashi Naomichi, Yokoyama Koji
Central Research Laboratory, Zenyaku Kogyo Co. Ltd., 2-33-7 Ohizumi-machi, Nerima-ku, Tokyo, Japan.
Nihon Ishinkin Gakkai Zasshi. 2009;50(1):9-13. doi: 10.3314/jjmm.50.9.
The fungicidal activities of the thiocarbamate antifungal agent liranaftate were compared to those of luliconazole, amorolfine hydrochloride and ketoconazole against twelve stock strains of three species of dermatophytes. The MICs of 0.001-0.009 microg/ml of luliconazole against Trichophyton rubrum (n=6)were the lowest among the agents tested, but its MCCs were considerably higher. Consequently, the antifungal potency of luliconazole was considered fungistatic. In contrast to this, the MCCs of 0.009-0.039 microg/ml of liranaftate against T. rubrum were the lowest and similar to its MICs. These results showed that liranaftate was fungicidal. All antifungals except ketoconazole tended to be fungicidal against both T. mentagrophytes (n=3)and Microsporum gypseum (n=3). In time-kill studies, liranaftate showed the greatest decrease to a below detection limit in viable counts of T. rubrum. The degree of killing of the strain by amorolfine was not greater than that seen by liranaftate, and little reduction of the viable counts by luliconazole and ketoconazole was observed irrespective of concentrations of the agents. Conversely, there were no differences among four agents in fungicidal activities against T.mentagrophytes. The killing activities of liranaftate against M. gypseum were also higher than those of comparable agents, as true of T. rubrum described above. In this study we found that it was harder to kill T. rubrum than other dermatophytes. Therefore, liranaftate with its potent fungicidal activities was suggested an efficacious agent for the treatment of dermatophytes.
将硫代氨基甲酸盐类抗真菌药利拉萘酯的杀菌活性与卢立康唑、盐酸阿莫罗芬和酮康唑针对三种皮肤癣菌的12个标准菌株的杀菌活性进行了比较。卢立康唑对红色毛癣菌(n = 6)的最低抑菌浓度(MIC)为0.001 - 0.009μg/ml,在所测试的药物中是最低的,但其最低杀菌浓度(MCC)则高得多。因此,卢立康唑的抗真菌效力被认为是抑菌性的。与此相反,利拉萘酯对红色毛癣菌的最低杀菌浓度为0.009 - 0.039μg/ml,是最低的且与其最低抑菌浓度相近。这些结果表明利拉萘酯具有杀菌作用。除酮康唑外,所有抗真菌药对须癣毛癣菌(n = 3)和石膏样小孢子菌(n = 3)都倾向于具有杀菌作用。在时间 - 杀菌研究中,利拉萘酯使红色毛癣菌活菌数降至检测限以下的降幅最大。盐酸阿莫罗芬对该菌株的杀灭程度不比利拉萘酯高,并且无论药物浓度如何,卢立康唑和酮康唑对活菌数的降低作用都很小。相反,四种药物对须癣毛癣菌的杀菌活性没有差异。利拉萘酯对石膏样小孢子菌的杀灭活性也高于同类药物,与上述红色毛癣菌的情况相同。在本研究中,我们发现杀灭红色毛癣菌比其他皮肤癣菌更难。因此,利拉萘酯因其强大的杀菌活性被认为是治疗皮肤癣菌的有效药物。