Antifungal Effects of New Synthetic Materials, KAF-200522 and KAF-200522-HCl, on in vitro and in vivo Models.
10.5625/lar.2010.26.4.353
- Author:
Ju Young JUNG
1
;
Kwang Han KONG
;
Kyo Hwan KOO
;
Si Whan SONG
;
Kap Ho KIM
;
Zhong Ze HAN
;
Yeo Jin LEE
;
Jin Soo HAN
Author Information
1. Institute for the 3Rs & Department of Laboratory Animal Medicine, College of Veterinary Medicine, Konkuk University, Seoul, Korea. labvet@konkuk.ac.kr
- Publication Type:In Vitro ; Original Article
- Keywords:
Antifungal effects;
KAF-200522;
KAF-200522-HCl;
MIC80
- MeSH:
Amphotericin B;
Animals;
Antifungal Agents;
Arthrodermataceae;
Aspergillus fumigatus;
Candida albicans;
Fluconazole;
Fungi;
Mice;
Microbial Sensitivity Tests;
Survival Rate;
Trichophyton
- From:Laboratory Animal Research
2010;26(4):353-359
- CountryRepublic of Korea
- Language:Korean
-
Abstract:
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 (MIC80) of both test articles against Candida albican sp. and Aspergillus fumigatus sp. were below 0.0156 microg/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 MIC80s of both test articles were below 0.0156 microg/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 mg/kg 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.
