title: The Cu/ligand stoichiometry effect on the coordination behavior of aroyl hydrazone with copper(II): Structure, anticancer activity and anticancer mechanism.
abstract: In an effort to better understand the biological efficacy of the tridentate aroyl hydrazone Cu(II) complexes, three Cu(II) complexes of acetylpyridine benzoyl hydrazone (HL), [Cu(L)(NO3) (H2O)]·H2O (C1), [Cu(L)2] (C2) and [Cu(L)(HL)]·(NO3)(Sas) (C3) (Sas=salicylic acid) were synthesized and characterized. X-ray crystal structures and infrared (IR) spectra of the complexes reveal that the L(-) ligand of C1 and C2 are predominantly in the enolate resonance form, while one L(-) ligand in C3 is represented enolate resonance form and the other HL ligand exhibits keto resonance form. All Cu(II) complexes showed significantly more anticancer activity than the ligand alone. Interestingly, the Cu complexes where the ligand/metal ratio was 1:1 (C1) rather than 2:1 (C2 and C3) had higher antitumor efficacy. Moreover, the 1:1 Cu/ligand complex, C1, promotes A549 cell apoptosis possibly through the intrinsic reactive oxygen species (ROS) mediated mitochondrial pathway, accompanied by the regulation of Bcl-2 family proteins.
authors.affiliation: Affiliated Hospital, Guilin Medical College, Guilin, Guangxi, China. Electronic address: sanchuanok@163.com.
authors.forename: JunGang
authors.initials: J
authors.lastname: Deng
authors.affiliation: Affiliated Hospital, Guilin Medical College, Guilin, Guangxi, China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Gou
authors.affiliation: Affiliated Hospital, Guilin Medical College, Guilin, Guangxi, China.
authors.forename: Wei
authors.initials: W
authors.lastname: Chen
authors.affiliation: Affiliated Hospital, Guilin Medical College, Guilin, Guangxi, China.
authors.forename: Xiang
authors.initials: X
authors.lastname: Fu
authors.affiliation: Affiliated Hospital, Guilin Medical College, Guilin, Guangxi, China.
authors.forename: Hang
authors.initials: H
authors.lastname: Deng
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000031:analogs & derivatives / Q000494:pharmacology; D003300:Copper / Q000737:chemistry* / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D006801:Humans; D006835:Hydrazones / Q000737:chemistry* / Q000494:pharmacology*; D008024:Ligands; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D017382:Reactive Oxygen Species / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D006835:Hydrazones; D008024:Ligands; D017382:Reactive Oxygen Species; D003300:Copper
keywords: Anticancer activity; Anticancer mechanism; Cell apoptosis; Copper(II) complex