target for anticancer agents. In this work, three Ru(II) complexes with salicylate as ligand, [Ru(phen)2(SA)] (phen = 1,10-phenanthroline, SA = salicylate, 1), [Ru(dmb)2(SA)] (dmb = 4,4'-dimethyl-2,2'-bipyridine, 2) and [Ru(bpy)2(SA)] (bpy = 2,2'-bipyridine, 3), were synthesized and characterized. The anticancer effect exerted by them was evaluated. Complex 1 was found to exhibit obvious anticancer activity
硫氧还蛋白还原酶(TrxR)是
硫氧还蛋白系统的主要组成部分,在调节细胞氧化还原信号中起着至关重要的作用,并且在许多人类癌细胞中被过度表达。TrxR已成为抗癌药的诱人靶标。在这项工作中,三个Ru(II)配合物以
水杨酸酯为
配体,[Ru(phen)2(
SA)](phen = 1,10-
菲咯啉,
SA =
水杨酸酯,1),[Ru(dmb)2(
SA)合成并表征了](dmb = 4,4′-二甲基-2,2′-联
吡啶,2)和[Ru(bpy)2(
SA)](bpy = 2,2′-联
吡啶,3)。评价了它们发挥的抗癌作用。与
顺铂相比,发现复合物1对癌
细胞系具有明显的抗癌活性,同时对正常
细胞系BEAS-2B的毒性较低。在A549细胞中研究了复合物1癌细胞生长抑制的机制。复合物1通过诱导凋亡和触发细胞周期停滞在G0 / G1期发挥其抗癌作用。复合物1可以选择性抑制TrxR活性,从而促进活性氧(ROS)的生成和积累,随后触