YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

The Evaluation of in Vivo Antifungal Activities and Toxicities of 6-[(N-4-Chlorophenyl)amino]-7-Chloro-5,8-Quinolinediones

6-[(N-4-클로로페닐)아미노-7-클로로-5,8-퀴놀린디온의 in vivo 항진균 작용 및 독성평가

  • Published : 1995.08.01
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Abstract

6-[(N-4-Chlorophenyl)amino]-7-chloro-5,8-quinolinedione (RCK20) was tested for antifungal activities, in vivo, against Candida albicans. RCK20 was compared vath ketoconazole and fluconazole in the treatment of systemic infection with Candida albicans in normal rats. The therapeutic potential of RCK20 had been assessed by evaluating their activities (survival rate) against systemic infections with in normal mice with Candida albicans. RCK20 improved survival rates as well as ketokonazole. RCK20 had ED$_{50}$. 0.25$\pm$0.18 mg/kg but ketoeonazole and fluconazole had ED$_{50}$, 8.00$\pm$0.73, 10$\pm$0.43 mg/kg respectively. Activities of RCK20 showed superior to that of ketoconazole and fluconazole. Intraperitoneauy administered RCK20 at the ED$_{50}$, 0.25 mg/kg for 7days and 14days reduced Candida albicans colony count in the kidneys and livers as well as ketoconazole and fluconazole at these ED$_{50}$, 8.00 and 10 mg/kg. Acute oral toxicity studies of RCK20 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK20 were low and LD$_{50}$ values were over 2.850 mg/kg in ICR mice. The Genotoxicities of RCK20 had been evaluated. RCK20 was negative in Ames test with Salmonella typhimurium (TA98 and TA100). The clastogenicity was tested on the RCK20 with in vivo mouse micronucleus assay. RCK20 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK20 has no genotoxic potential under these experimental condition.

Keywords

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