丙亚胺（ICRF 159）对柔红霉素（NSC 82151）代谢及DNA络合的影响。

Effect of razoxane (ICRF 159) on daunomycin (NSC 82151) metabolism and DNA complexation.

作者信息

Wang G M, Finch M

出版信息

Drug Chem Toxicol. 1980;3(2):213-25. doi: 10.3109/01480548009108284.

Abstract

Daunomycinol and deoxyaglycone were the two major metabolites obtained from daunomycin in vitro metabolism by rat and mouse liver preparations. Pretreatment with razoxane (ICRF 159) in these animals did not appear to alter these major metabolic enzymes. In an in vitro system, it was found that daunomycin reacted with DNA instantly and reached steady states within two minutes as evidenced by the diminishing, shifting or disappearance of certain and visible regions. Preincubation of razoxane with DNA did not alter the latter's capacity to interact with daunomycin. We suggest that the mode of razoxane-protected daunomycin-induced toxicities in mice is not mediated through an alteration in daunomycin metabolism or its complexation with DNA.

摘要

柔红霉素醇和脱氧糖苷配基是大鼠和小鼠肝脏制剂对柔红霉素进行体外代谢所产生的两种主要代谢产物。在这些动物中用丙亚胺（ICRF 159）进行预处理似乎并未改变这些主要的代谢酶。在体外系统中，发现柔红霉素能立即与DNA发生反应，并在两分钟内达到稳态，这可通过某些可见区域的减少、移位或消失得到证明。丙亚胺与DNA预孵育不会改变后者与柔红霉素相互作用的能力。我们认为，丙亚胺对柔红霉素诱导的小鼠毒性的保护作用方式并非通过改变柔红霉素的代谢或其与DNA的络合作用来介导。