Rofstad E K, Brustad T
Br J Radiol. 1978 May;51(605):381-6. doi: 10.1259/0007-1285-51-605-381.
The radiosensitizing effect of two electron-affinic nitroimidazoles, metronidazole and misonidazole (Ro-07-0582), has been tested on a human malignant melanoma grown subcutaneously in the athymic mutant nude mouse. A 60Co therapy unit was used for local irradiation of the mice. Metronidazole in doses of 750 mg/kg and misonidazole in doses of 500 mg/kg were administered intraperitoneally to the animals 45 min before exposure to 1250 rad. The time necessary for the tumours to regrow to their original sizes was compared with that of tumours treated with 1250, 1875 and 2500 rad without drug. The enhancement ratios were found to be 1.2-1.3 and 1.4-1.5 for metronidazole and misonidazole respectively. It is concluded that misonidazole is a more efficient hypoxic cell radiosensitizer for this human malignant melanoma than metronidazole. The former may prove to be of value in human radiotherapy.
已在无胸腺突变裸鼠皮下生长的人恶性黑色素瘤上测试了两种亲电子硝基咪唑(甲硝唑和米索硝唑(Ro-07-0582))的放射增敏作用。使用一台60Co治疗机对小鼠进行局部照射。在暴露于1250拉德前45分钟,给动物腹腔注射750毫克/千克剂量的甲硝唑和500毫克/千克剂量的米索硝唑。将肿瘤重新生长至其原始大小所需的时间与用1250、1875和2500拉德照射且未用药的肿瘤的时间进行比较。发现甲硝唑和米索硝唑的增强比分别为1.2 - 1.3和1.4 - 1.5。得出的结论是,对于这种人恶性黑色素瘤,米索硝唑是比甲硝唑更有效的乏氧细胞放射增敏剂。前者可能在人类放射治疗中被证明具有价值。