类姜黄素-芳基钌配合物的合成、结构和光照激活抗癌活性

Synthesis,Structure and Photoactivated Anticancer Activity of Ruthenium-Arene Complexes with Curcuminoids

合成了3种含姜黄素衍生物(L^(1)~L^(3))和1,3,5-三氮杂-7-磷金刚烷(PTA)配体的芳基钌配合物[(η^(6)-p-cymene)Ru(L)(PTA)]PF6(1~3,L=L^(1)~L^(3)),通过X射线单晶衍射、核磁共振波谱、高分辨质谱、元素分析等方法表征了这些配合物的结构,并用MTT法研究了它们在λ>400 nm的光照辅助下对Hep G2人肝癌细胞的增殖抑制活性。结果表明,这3个配合物均为半三明治型结构;光辅助下,配合物抗癌活性明显提高,其中配合物3对HepG2细胞的IC50值从(60.3±1.1)μmol·L^(-1)降低至(45.0±6.1)μmol·L^(-1)。说明光照可以有效提高此类配合物的抗肿瘤活性。

Three ruthenium-arene complexes with curcuminoids(1~3)were synthesized through the reaction of[(η^(6)-p-cymene)Ru Cl2]2and the corresponding curcuminoids derivative(L^(1)~L^(3))followed by the reaction with 1,3,5-tiaza-7-phosphaadamantane(PTA).The complexes were structurally characterized by single crystal XRD,1H NMR,MS and elemental analysis.The inhibitory activities of the complexes towards HepG2 human liver cancer cell lines were investigated by MTT with light(λ>400 nm).The results show that three complexes present half-sandwich structure.Anticancer activity of the complexes was significantly improved by light,among which the IC50of complex3decreased from(60.3±1.1)μmol·L^(-1)to(45.0±6.1)μmol·L^(-1)against HepG2,indicating that light can effectively improve the anticancer activity of this kind of complexes.CCDC:1514601,1;1514600,2;1514603,3.