银杏叶聚戊烯醇金属配合物的合成及其光控活性

Synthesis and Light-controlled Activity of Ginkgo biloba Leaves Polyprenols Metal Complex

以银杏叶聚戊烯醇(GBP)为原料,通过化学改性手段将其末端羟基替换成氰基,之后将氰基聚戊烯醇与钌多吡啶配合物络合,合成了聚戊烯醇-钌多吡啶配合物,并对其进行表征,考察了配合物的脂水分配系数、光致配体解离能力和光控抗肿瘤活性。核磁共振表征结果表明,氰基聚戊烯醇和聚戊烯醇-钌多吡啶配合物成功合成。合成的配合物具有较好的脂水分配系数(1.35),有利于其穿透细胞膜。此外,合成的配合物在光照下逐渐发生配体解离,在光照条件下,其对A549肿瘤细胞的半数抑制浓度(IC_(50))为29.3μmol/L,展示出比聚戊烯醇(IC_(50)=45.8μmol/L)更好的抗肿瘤活性,且配合物的光控抗肿瘤活性极可能与其DNA结合能力有关。

Ginkgo biloba leaves polyprenols(GBP)was used as raw material,and its terminal hydroxyl group was replaced with cyano group by chemical modification method.On this basis,cyano-GBP and ruthenium polypyridine complex were utilized as raw materials,the GBP-ruthenium polypyridine metal complex was synthesized and characterized by complex reaction.The lipid-water partition coefficient,photo-induced ligand dissociation ability and light-controlled antitumor activity of the complex were investigated.NMR results showed that the cyano-GBP and GBP-ruthenium polypyridine metal complex were successfully synthesized.The synthesized complex has good lipid-water partition coefficient(1.35),which was conducive to its penetration of cell membranes.In addition,cyano-GBP ligand of the synthesized complex gradually dissociated under light and exhibited better antitumor activity with the half inhibitory concentration(IC_(50))against A549 tumor cell of 29.3μmol/L than GBP(IC_(50)=45.8μmol/L).Moreover,The light-controlled antitumor activity of the complex may be related to its DNA binding ability.