多吡啶金属配合物的合成及药物活性

Synthesis and Medicine Activity of Polypyridyl Metals Complexes

设计合成了钉、钻多吡啶配合物，在体外细胞培养内，采用ＭＴＴ染色法，对其进行了抗肿瘤活性的筛选，用于实验的肿瘤细胞有人白血病细胞株（ＨＬ－６０），肝癌细胞株（ＨｅｐＧ－２），测定了配合物在细胞培养内对肿瘤细胞的抑制作用结果表明； ３种配合物［ Ｃｏ（ ｂｐｙ）２（ ＰＩＰ）］３＋、 ［Ｃｏ（ｐｈｅｎ）２（ＰＩＰ）］３＋、［Ｒｕ（ｂｐｙ）（ｐ２ｔｐ）２］２＋对ＨＬ－６０和 ＨｅｐＧ－２，均表现出强烈的抑制作用，配合物的浓度为 １００ ｕｇ／ｍＬ时，对肿瘤细胞生长的抑制率在 ７２％－ ８６％之间，配合物的毒性实验表明：浓度为 １００ ｕｇ／ｗＬ时，对 ＭＤＣＫ和 Ｖｅｒｏ细胞无毒性．

A series of metal complexes of polypyridine have been synthesized. The anticancer activities of these complexes were investigated by MTT on two human tumor cells (HepG-2) and human leucocythemia cancer cells (HL-60). It’s found that there are three complexes [Co (bpy)2 (PIP) ]3+, [ Co (phen)2 (PIP) ]3+ and [Ru (bpy) (pztp)2]2+, behave high anticancer activity to HL-60 and HepG-2 cells. When the concentration of these complexes is 100 (g/mL, the inhibitory rate for cancer cells is 72%-86% and the complexes have no toxicity for MDCK and Vero cells. It is indicated that these complexes can inhibit cancer cells selectivity. The correlation between the anticancer activity and the structure of complexes has been discussed briefly.