异丙铂及其二价代谢产物顺-二氯-双异丙胺铂（II）与DNA的结合
DNA binding of iproplatin and its divalent metabolite cis-dichloro-bis-isopropylamine platinum (II).
作者信息
Pendyala L, Arakali A V, Sansone P, Cowens J W, Creaven P J
机构信息
Department of Medicine, Roswell Park Memorial Institute, Buffalo, NY 14263.
出版信息
Cancer Chemother Pharmacol. 1990;27(3):248-50. doi: 10.1007/BF00685722.
The quadrivalent second-generation platinum complex iproplatin and an in vivo divalent metabolite of iproplatin, cis-dichloro-bis-isopropylamine platinum (CIP) were tested for binding to DNA in vitro. DNA binding was determined according to radioactivity measured using [14C]-iproplatin and [14C]-CIP and also by platinum content. Results indicate that (a) iproplatin shows negligible binding to DNA, (b) CIP binds to DNA in a time-dependent fashion, and (c) the isopropylamine ligand is intact when CIP is bound to DNA. Glutathione (GSH) inhibits the binding of CIP to DNA, possibly by inhibiting binding to DNA of the aquated form of CIP.
对四价第二代铂配合物异丙铂及其体内二价代谢物顺式二氯双异丙胺铂（CIP）进行了体外与DNA结合的测试。根据使用[14C] - 异丙铂和[14C] - CIP测量的放射性以及铂含量来确定DNA结合情况。结果表明：（a）异丙铂与DNA的结合可忽略不计；（b）CIP以时间依赖性方式与DNA结合；（c）当CIP与DNA结合时，异丙胺配体保持完整。谷胱甘肽（GSH）可能通过抑制水合形式的CIP与DNA的结合来抑制CIP与DNA的结合。
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