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标题：Studies of Methyl 2-Nitroimidazole-1-acetohydroxamate (KIN-804) 1 : Effect on Free Radical Scavenging System in Mice Bearing Ehrlish Ascites Carcinoma
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作者：Medhat ABU-ZEID ; Hitoshi HORI ; Hideko NAGASAWA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2000
卷号：23
期号：2
页码：190-194
DOI：10.1248/bpb.23.190
出版社：The Pharmaceutical Society of Japan
摘要：Methyl 2-nitroimidazole-1-acetohydroxamate (KIN-804) is a 2-nitroimidazole derivative containing a hydroxamate side chain designed to enhance the radiosensitization response of hypoxic cells. The possible sensitization of tumor tissue by KIN-804 can be evaluated through investigation of the levels of the free radical scavengers; namely, glutathione (GSH) and its complex enzyme system including glutathione reductase (GR) and glutathione peroxidase (GSH-Px), as well as glucose-6-phosphate dehydrogenase (G-6-PD). Female albino mice were inoculated with Ehrlich carcinoma in the thigh. Administration of KIN-804 (i.p. 80 mg/kg body weight) was carried out 20 min before localized irradiation of 10 Gy. The data revealed that KIN-804 administration, followed or not by gamma irradiation, resulted in a significant decrease in GSH content in tumor tissues associated with inhibition in GR and G-6-PD activities. Blood GSH-Px was enhanced in tumor inoculated mice and the administration of KIN-804 returned it to the normal value. These changes were more noticeable in tumor bearing mice exposed to both KIN-804 and irradiation.
关键词：KIN-804;glutathione;glutathione reductase;glutathione peroxidase;glucose-6-phosphate dehydrogenase