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  • 标题:Radiosensitizer Sanazole (AK-2123) enhances γ-radiation-induced Apoptosis in murine fibrosarcoma
  • 其他标题:Radiosensitizer Sanazole (AK-2123) enhances γ-radiation-induced Apoptosis in murine fibrosarcoma
  • 本地全文:下载
  • 作者:REMA RAJAGOPALAN ; TSUTOMU V. KAGIYA ; CHERUPALLY KRISHNAN KRISHNAN NAIR
  • 期刊名称:Journal of Radiation Research
  • 印刷版ISSN:0449-3060
  • 电子版ISSN:1349-9157
  • 出版年度:2003
  • 卷号:44
  • 期号:4
  • 页码:359-365
  • DOI:10.1269/jrr.44.359
  • 摘要:Sanazole (AK-2123) (N-2′-methoxy ethyl)-2-(3″-nitro-1″-triazolyl)acetamide, which has completed phase III clinical trials as a radiosensitizer, enhanced γ-radiation induced apoptosis in murine fibrosarcoma upon i.p. administration at 40 mg/kg body weight one hour prior to irradiation. A microscopic examination of Giemsa-May-Grunwald stained cells has shown a higher frequency of condensed nuclei and fragmented nuclei in the tumor cells. The administration of sanazole to tumor-bearing animals enhanced the radiation-induced internucleosomal fragmentation in the nuclear genome of tumor cells. Higher levels of caspase-3 activity were also observed in the cell extracts of tumours from AK-2123 administered mice. Exposure to γ-radiation of AK-2123-treated mouse further enhanced the caspase-3 activity, indicating the induction of apoptosis. The radiation sensitization property of sanazole was discernible by comparing the relative tumor diameter following irradiation after i.p. administration of AK-2123 and irradiation alone; it was higher during the first few days followed by the treatment.
  • 关键词:Sanazole;AK-2123;γ-radiation;DNA damage;Apoptosis;Radiosensitizer
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