Josephy P D, Palcic B, Skarsgard L D
Br J Cancer. 1981 Apr;43(4):443-50. doi: 10.1038/bjc.1981.65.
Misonidazole (MISO) is a nitroimidazole drug currently undergoing clinical trials as a radiosensitizer of hypoxic tumour cells. The drug is also toxic to such cells, probably because of metabolic activation of the nitro group under hypoxia. The metabolic fate of 14C-labelled MISO is examined, using hypoxic mammalian (CHO) cells in vitro. Organic-soluble and acid-soluble metabolites are formed, and radioactivity is bound to macromolecules. The organic-soluble products are separated by TLC and HPLC. Evidence is presented to show that one of the metabolites is hydroxylamino-misonidazole. The significance of metabolic nitroreduction is discussed.
米索硝唑（MISO）是一种硝基咪唑类药物，目前正作为缺氧肿瘤细胞的放射增敏剂进行临床试验。该药物对这类细胞也有毒性，可能是由于缺氧条件下硝基的代谢活化所致。使用体外缺氧的哺乳动物（CHO）细胞研究了14C标记的米索硝唑的代谢命运。形成了有机可溶和酸可溶的代谢产物，并且放射性与大分子结合。通过薄层色谱法（TLC）和高效液相色谱法（HPLC）分离有机可溶产物。有证据表明其中一种代谢产物是羟氨基米索硝唑。讨论了代谢性硝基还原的意义。
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