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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。
In this paper, a new fluorescence method for the preliminary screening of anticancer complexes was proposed. The 14 complexes of Pd (Ⅱ) / phenanthroline / amino acid / chloride (Pd (Ⅱ) / phen / aa / Cl) Non-cisplatin anticancer drugs in vitro screening and binding studies found that the results of fluorescence screening methods and other such as the methyl blue test tube method, trypan blue dye rejection method is basically the same, wherein the complex [Pd (phen) (lys) The antitumor rates of mice with S-180 tumor cells were 56%, 50%, 48%, respectively, compared with those of DNA binding constants of 7.96 × 10 ~ 6, 4.52 × 10 ~ 6, 1.0 × 10 ~ 6 sequence consistent, indicating that the fluorescence screening method has a certain reliability, and the fluorescence method has the advantages of easy operation, low cost, short cycle, etc., suitable Preliminary screening of anti-cancer complexes.