Preliminary Fluorimetric Screening of Fourteen Palladium Complexes as Potential Antitumor Agents  

作　　者：林辉祥 李志良 戴桂林 毕琼斯 俞汝勤 

机构地区：[1]Department of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, PRC

出　　处：《Science China Chemistry》1993年第10期1216-1223,共8页中国科学（化学英文版）

基　　金：Project supported by the National Education Commission Foundation and the National Natural Science Foundation of China.

摘　　要：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 fluorimetric method is simple, cheap and rapid. suitable for preliminary screening of antitumor complexes.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

关 键 词：fluorimetric SCREENING palladium(Ⅱ) COMPLEXES PRELIMINARY SCREENING of ANTITUMOR DRUGS fluorescence probe. 

分 类 号：O6[理学—化学]