奥沙利铂二水合物配合物的合成及细胞毒性

Synthesis and cytotoxicity of the dihydrated complex of oxaliplatin.

作者信息

Videhult Pernilla, Yachnin Jeffrey, Jerremalm Elin, Lewensohn Rolf, Ehrsson Hans

机构信息

Karolinska Pharmacy, Karolinska Hospital, SE-171 76 Stockholm, Sweden.

出版信息

Cancer Lett. 2002 Jun 28;180(2):191-4. doi: 10.1016/s0304-3835(02)00002-2.

DOI:10.1016/s0304-3835(02)00002-2

PMID:12175551

Abstract

A new way of synthesizing the dihydrated oxaliplatin complex (DOC) is presented and its cytotoxicity is compared to that of oxaliplatin and cisplatin. By hydrolyzing oxaliplatin in aqueous sodium hydroxide at 70 degrees C, DOC was formed in less than 1 h. Cytotoxicity was studied in the non-small cell lung cancer cell line A549 using the fluorescent microculture cytotoxic assay. Oxaliplatin and cisplatin had similar cytotoxicity profiles, whereas DOC was found to be considerably more toxic. The cytotoxicity of oxaliplatin might, at least in part, be mediated through the formation of DOC.

摘要

本文介绍了一种合成二水合奥沙利铂络合物（DOC）的新方法，并将其细胞毒性与奥沙利铂和顺铂进行了比较。通过在70℃的氢氧化钠水溶液中水解奥沙利铂，不到1小时即可形成DOC。使用荧光微量培养细胞毒性试验在非小细胞肺癌细胞系A549中研究细胞毒性。奥沙利铂和顺铂具有相似的细胞毒性谱，而DOC的毒性则明显更高。奥沙利铂的细胞毒性可能至少部分是通过DOC的形成介导的。