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KMID : 0370219960400050608
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Yakhak Hoeji
1996 Volume.40 No. 5 p.608 ~ p.615
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The Evaluation of Antifungal Activities and Safeties of 6-[(N-3,4-Difluorophenyl)amino]-7-Chloro-5,8-Quinolinedione
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유충규/Ryu CK
김동현/윤여표/이병무/허문영/정해문/권상미/정성희/Kim DH/Yun YP/Lee BM/Heo MY/Chung HM/Kwon SM/Jung SH
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Abstract
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6-[(N-3,4-Difluorophenyl)amino]-7-chloro-5,8-quinolinedione(RCK4) was tested for antifungal activities, against systemic infections with Candida albicans in normal mice. The therapeutic potential of RCK4 had been assessed in comparison with ketoconazole and fluconazole. RCK4 had ED50, 0.30 +/- 0.14mg/kg but ketoconazole and fluconazole had ED50, 8.00 +/- 0.73, 10.00 +/- 0.43mg/kg respectively. Intraperitoneally administered RCK3 at the ED50 for 7 days and 14 days reduced Candida albicans colony count in the kidneys and liver as well as ketoconazole and fluconazole at these ED50. And administered RCK4 at the ED50 for 14 days improved survival rates as well as ketoconazole. Acute oral toxicity studies of RCK4 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK4 were low and LD50 values were over 2,850mg/kg in ICR mice. The genotoxicities of RCK4 had been evaluated. RCK4 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK4 with in vivo mouse micronucleus assay. RCK4 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK4 has no genotoxic potential under these experimental conditions.
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