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希夫碱和菲咯啉混合配体氧钒(IV)配合物的合成及体外抗肿瘤活性。

Synthesis and In Vitro Antitumor Activity of Two Mixed-Ligand Oxovanadium(IV) Complexes of Schiff Base and Phenanthroline.

机构信息

Department of Biology, School of Basic Courses, Guangdong Pharmaceutical University, Guangzhou, Guangdong 510006, China.

出版信息

Bioinorg Chem Appl. 2013;2013:437134. doi: 10.1155/2013/437134. Epub 2013 Jan 29.

Abstract

Two oxovanadium(IV) complexes of [VO(msatsc)(phen)], (1) (msatsc = methoxylsalicylaldehyde thiosemicarbazone, phen = phenanthroline) and its novel derivative [VO (4-chlorosatsc)(phen)], (2) (4-chlorosatsc = 4-chlorosalicylaldehyde thiosemicarbazone), have been synthesized and characterized by elemental analysis, IR, ES-MS, (1)H NMR, and magnetic susceptibility measurements. Their antitumor effects on BEL-7402, HUH-7, and HepG2 cells were studied by MTT assay. The antitumor biological mechanism of these two complexes was studied in BEL-7402 cells by cell cycle analysis, Hoechst 33342 staining, Annexin V-FITC/PI assay, and detection of mitochondrial membrane potential (ΔΨm). The results showed that the growth of cancer cells was inhibited significantly, and complexes 1 and 2 mainly caused in BEL-7402 cells G0/G1 cell cycle arrest and induced apoptosis. Both 1 and 2 decreased significantly the ΔΨm, causing the depolarization of the mitochondrial membrane. Complex 2 showed greater antitumor efficiency than that of complex 1.

摘要

两种[VO(msatsc)(phen)](1)(msatsc = 甲氧基水杨醛缩硫代氨基脲,phen = 邻菲罗啉)和其新型衍生物[VO(4-chlorosatsc)(phen)](2)(4-chlorosatsc = 4-氯水杨醛缩硫代氨基脲)的氧钒(IV)配合物已通过元素分析、IR、ES-MS、(1)H NMR 和磁化率测量进行了合成和表征。通过 MTT 测定法研究了它们对 BEL-7402、HUH-7 和 HepG2 细胞的抗肿瘤作用。通过细胞周期分析、Hoechst 33342 染色、Annexin V-FITC/PI 测定和线粒体膜电位(ΔΨm)检测研究了这两种配合物在 BEL-7402 细胞中的抗肿瘤生物机制。结果表明,癌细胞的生长受到显著抑制,配合物 1 和 2 主要导致 BEL-7402 细胞 G0/G1 细胞周期停滞并诱导细胞凋亡。1 和 2 均显著降低ΔΨm,导致线粒体膜去极化。配合物 2 显示出比配合物 1 更高的抗肿瘤效率。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9407/3569890/0e0ea85af190/BCA2013-437134.sch.001.jpg

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