钯铂抗癌配合物初步筛选的荧光法研究

用溴化乙锭/DNA体系荧光筛选法,对以二齿胺或氨为第一配体、硝酸根或生物大分子(小牛血清白蛋白或葡聚糖)为第二配体合成的14种钯、铂配合物进行了研究。确定了配合物的抗癌活性及其DNA的结合常数K_M;发现低浓度下硝酸根配体配合物以插入方式与DNA结合,而大分子配体配合物与DNA作用并非单一的插入方式。本法操作简便、受环境影响小,且对抗癌配合物筛选结果与其它体外法基本接近。

Preliminary Screening of Some Platinum and Palladium Complexes as Antitumour Agents Using Fluorimetry

A fluorimetric method based on ethidium bromide/DNA system was used for preliminary screening of some platinum and palladium complexes with potential antitumour activities. 14 complexes of palladium and platinum with ammonia or bidentate amine as the first ligand, and nitrate, bovine serum albumin(BSA) or dextran sulphate(DS) as the second ligand were studied. The antitumour activities of complexes and the associated constants of these complexes with DNA were estimated. At the low concentration level the association reaction between complexes and DNA was of intercalation mode for small ligands such as nitrate; while for macromolecular lig-ands such as BSA or DS the intercalation mode was not the unique reaction mode. The results of the proposed fluorimetric screening method are in reasonable agreement with those obtained by other in vitro screening procedures.