14种钯抗癌络合物初步筛选的荧光法研究

本文提出抗癌络合物初步筛选的荧光新方法,对所合成的14种钯(Ⅱ)/邻菲咯啉/氨基酸/氯离子(Pd(Ⅱ)/phen/aa/Cl)络合物作为非顺铂抗癌药物进行了体外筛选及结合作用研究,发现荧光筛选法结果与其它如甲烯蓝试管法、苔盼蓝染料排斥法基本一致,其中络合物[Pd(phen)(lys)]Cl,[Pd(phen)(arg)]Cl,[Pd(phen)(pro)]Cl对小鼠S-180瘤株抑瘤率分别为56％,50％,48％,这同它们与DNA结合常数7.96×10~6,4.52×10~6,1.0×10~6顺序相一致,表明荧光筛选法具有一定可靠性,并且荧光法具有操作简便、耗费低廉、周期较短等优点,适于抗癌络合物的初步筛选。     

Preliminary Fluorimetric Screening of Fourteen Palladium Complexes as Potential Antitumor Agents

Making use of the fact that the combination of a drug substance with DNA may inhibit the duplication, synthesis and proliferation of DNA and the consistency of the in vivo and in vitro interactions, the authors worked out a preliminary screening method for testing complex agents as potential antitumor drugs using ethidium bromide as a fluorescence probe. In this report, the method was applied for in vitro testing fourteen synthesized palladium(Ⅱ)/phenanthroline/amino acid/chloride complexes as potential non-platinum antitumor agents. The fluorimetric screening method was compared with methylene blue tube test and trypan blue dye exclusion assay. All three methods gave agreeable results. Among the complexes tested, [Pd(phen)(lys)]Cl, [Pd(phen)(arg)]Cl and [Pd(phen)(pro)]Cl showed antineoplastic ratios for animal tumor S-180 56%, 50% and 48%, respectively, in accordance with the order of their binding constants with DNA, 7.96×10~6, 4.52×10~6 and 1.0×10~6, respectively. The test results show that fluor