Radiosensitizer Sanazole (AK-2123) Enhances γ-Radiation-induced Apoptosis in Murine Fibrosarcoma

概要

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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 40mg/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.
日本放射線影響学会の論文
2003-12-15