Novel Oxovanadium Complex VO(hntdtsc)(NPIP): Anticancer Activity and Mechanism of Action on HeLa Cells

• Published in: Frontiers in pharmacology Vol. 11; p. 608218
• Main Authors: Bai, Yinliang, Zhang, Honghua, Wang, Yali, Zhu, Longqing, Shi, Tao, Wei, Hangzhi, Xiao, Jiyuan, Zhang, Youcheng, Wang, Zhen
• Format: Journal Article
• Language: English
• Published: Switzerland Frontiers Media S.A 08.02.2021
• Subjects: antiproliferative activity; HeLa xenograft; mitochondrial-dependent apoptosis; oxovanadium (IV) complexes; Pharmacology; VO(hntdtsc)(NPIP); HeLa xenograft; VO(hntdtsc)(NPIP); oxovanadium (IV) complexes; mitochondrial-dependent apoptosis; antiproliferative activity
• ISSN: 1663-9812; 1663-9812
• DOI: 10.3389/fphar.2020.608218

Oxovanadium complexes, particularly vanadyl (IV) derivatives with hybrid ligands of Schiff base and polypyridyl, have been demonstrated to possess great anticancerous therapeutic efficacy. However, most of the studies on the activity of these oxovanadium complexes have mainly focused on studies, and animal studies are extremely scarce. Based on the antitumor test results of four novel oxovanadium complexes in our previous work, this work further conducted a comprehensive antitumor activity study and on VO(hntdtsc)(NPIP), which owned the strongest inhibitory activity on multiple tumor cell proliferation. The cellular mechanism study suggested that VO(hntdtsc)(NPIP) inhibited the cell proliferation arresting the cell cycle at G0/G1 phase through the p16-cyclin D1-CDK4-p-Rb pathway and inducing cell apoptosis through mitochondrial-dependent apoptosis pathway on HeLa cells. Inconsistent with the effects , VO(hntdtsc)(NPIP) significantly inhibited the growth of tumor and induced the apoptosis of cancer cells in mice xenograft models according to the results of nude mice image detection, H&E pathological examination, and immunohistochemical detection of p16/Ki-67 protein expression. Collectively, all the results, particularly studies demonstrated that VO(hntdtsc)(NPIP) hold a potential to be the lead compound and further to be an anticervical cancer drug.