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7,12-二甲基苯并[a]蒽及其弱致癌性5-氟类似物的比较代谢与DNA结合

Comparative metabolism and DNA binding of 7,12-dimethylbenz[a]anthracene and its weakly carcinogenic 5-fluoro analog.

作者信息

Daniel F B, Cazer F D, D'Ambrosio S M, Hart R W, Kim W H, Witiak D T

出版信息

Cancer Lett. 1979 Apr;6(4-5):263-72. doi: 10.1016/s0304-3835(79)80044-0.

Abstract

Cultured Syrian hamster embryo cells readily convert both the carcinogenic polycyclic aromatic hydrocarbon, 7,12-dimethylbenz[a]anthracene (DMBA), and its weakly carcinogenic analogue, 5-fluoro-7,12-dimethylbenz[a]anthracene (5F-DMBA), to water soluble metabolites. DMBA, however, binds to the hamster cell DNA at least 2.8-3.0 times more extensively than 5F-DMBA. Likewise, 5F-DMBA is converted to water soluble metabolites by liver microsomal preparations at a rate equal to DMBA, but the latter compound binds to DNA 2.6-3.2 times more effectively.

摘要

培养的叙利亚仓鼠胚胎细胞能轻易地将致癌多环芳烃7,12-二甲基苯并[a]蒽(DMBA)及其弱致癌类似物5-氟-7,12-二甲基苯并[a]蒽(5F-DMBA)转化为水溶性代谢产物。然而,DMBA与仓鼠细胞DNA的结合程度至少比5F-DMBA广泛2.8至3.0倍。同样,5F-DMBA被肝微粒体制剂转化为水溶性代谢产物的速率与DMBA相同,但后一种化合物与DNA的结合效率高2.6至3.2倍。

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