Affiliation:
1. State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources, Collaborative Innovation Center for Guangxi Ethnic Medicine, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University , Guilin 541004 , P. R. China
Abstract
Abstract
The development of metal complexes of Schiff base has attracted much attention due to their DNA binding properties and extensive biological activities. We reported here five copper(II) complexes [Cu(L1)] (1), [Cu(L2)] (2), [Cu(L3)] (3), [Cu2(L4)(OAc)] (4), and [Cu2(L5)(HCOO)] (5) bearing the bis-Schiff base ligands of bis(5-chlorosalicylidene)-1,3-propanediamine (H2L1), bis(5-chlorosalicylidene)-2-methyl-1,3-propanediamine (H2L2), bis(5-bromosalicylidene)-2-methyl-1,3-propanediamine (H2L3), bis(5-chlorosalicylidene)-2-hydroxyl-1,3-propanediamine (H3L4), and bis(5-bromosalicylidene)-2-hydroxyl-1,3-propanediamine (H3L5), respectively. The single crystal X-ray diffraction analysis results revealed that complexes 1–3 present mononuclear structures and complexes 4 and 5 show dinuclear structures. It was also shown that all of these complexes are stable under physiological conditions. The in vitro antitumor activities of the five complexes were evaluated. Anticancer selectivity was also found for complex 2 on different cell lines with the lowest IC50 value on Hela cells. Further mechanistic studies showed that the three mononuclear Cu(II) complexes can induce apoptosis through the mitochondrial pathway by decreasing mitochondrial membrane potential and increasing the reactive oxygen species (ROS) and Ca2+ levels. They can activate caspase-3 and caspase-9, and can also regulate the expression of pro-apoptotic protein and anti-apoptotic protein in cells. All of these results showed that complex 2 is a potential anticancer drug.
Funder
National Natural Science Foundation of China
Guangxi Natural Science Foundation
Guangxi Normal University
Publisher
Oxford University Press (OUP)
Subject
Metals and Alloys,Biochemistry,Biomaterials,Biophysics,Chemistry (miscellaneous)
Cited by
1 articles.
订阅此论文施引文献
订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献