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KMID : 1204320100260040353
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Laboratory Animal Research
2010 Volume.26 No. 4 p.353 ~ p.359
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Antifungal Effects of New Synthetic Materials, KAF-200522 and KAF-200522-HCl, on in vitro and in vivo Models
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Jung Ju-Young
Kong Kwang-Han
Koo Kyo-Hwan
Song Si-Whan
Kim Kap-Ho
Han Zhong-Ze
Lee Yeo-Jin
Han Jin-Soo
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Abstract
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KAF-200522 and its chloride form, KAF-200522-HCl, were invented in Chemon inc. as new triazole antifungal agents with excellent activities in vivo and in vitro against wide range of fungi. As a result of in vitro susceptibility measurements, 80% minimum inhibitory concentrations (MIC??) of both test articles against Candida albican sp. and Aspergillus fumigatus sp. were below 0.0156 ㎍/mL, which were over 4,100 times lower than those of fluconazole against fluconazole resistant C. albican sp. and A. fumigatus sp., and were over 16 times lower than those of amphotericin B against above same fungi. Additionally, against representative dermatophytes, Trichophyton sp., the MIC??s of both test articles were below 0.0156 ㎍/mL which were over 64 times lower than those of fluconazole and amphotericin B. As in vivo antifungal activities in A. fumigatus sp. infected mouse models, KAF-200522 treatment group at 600 ㎎/㎏ showed 80% survival rate which was 2 times higher than that of amphotericin B and showed 13.7 days in the mean survival time (MST) which was about 2.1 times higher than that of amphotericin B. But in KAF-200522-HCl treatment groups, all animals were found dead in contrast to 40% survival rate in amphotericin B treatment group, however dose dependent increases in MST was revealed. In conclusion, antifungal activities of KAF-200522 and its mimics, KAF-200522-HCl in vitro and in vivo were confirmed in this study, therefore the potentiality of the present compounds to be developed into new antifungal drug was expected.
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KEYWORD
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Antifungal effects, KAF-200522, KAF-200522-HCl, MIC80
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