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Your search keyword '"Qin, Jiao"' showing total 9 results
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9 results on '"Qin, Jiao"'

8. Oxoaporphine Metal Complexes (CoII, NiII, ZnII) with High Antitumor Activity by Inducing Mitochondria-Mediated Apoptosis and S-phase Arrest in HepG2.

Author

Qin, Jiao-Lan, Shen, Wen-Ying, Chen, Zhen-Feng, Zhao, Li-Fang, Qin, Qi-Pin, Yu, Yan-Cheng, and Liang, Hong

Abstract

Three new oxoaporphine Co(II), Ni(II) and Zn(II) complexes 1-3 have been synthesized and fully characterized. 1-3 have similar mononuclear structures with the metal and ligand ratio of 1:2. 1-3 exhibited higher cytotoxicity than the OD ligand and cisplatin against HepG2, T-24, BEL-7404, MGC80-3 and SK-OV-3/DDP cells, with IC50 value of 0.23−4.31 μM. Interestingly, 0.5 μM 1-3 significantly caused HepG2 arrest at S-phase, which was associated with the up-regulation of p53, p21, p27, Chk1 and Chk2 proteins, and decrease in cyclin A, CDK2, Cdc25A, PCNA proteins. In addition, 1-3 induced HepG2 apoptosis via a caspase-dependent mitochondrion pathway as evidenced by p53 activation, ROS production, Bax up-regulation and Bcl-2 down-regulation, mitochondrial dysfunction, cytochrome c release, caspase activation and PARP cleavage. Furthermore, 3 inhibited tumor growth in HepG2 xenograft model, and displayed more safety profile in vivo than cisplatin. [ABSTRACT FROM AUTHOR]

Published
2017
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9. Oxoaporphine Metal Complexes (Co II , Ni II , Zn II ) with High Antitumor Activity by Inducing Mitochondria-Mediated Apoptosis and S-phase Arrest in HepG2.

Author

Qin JL, Shen WY, Chen ZF, Zhao LF, Qin QP, Yu YC, and Liang H

Subjects
Animals, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Aporphines chemical synthesis, Aporphines chemistry, Calcium metabolism, Caspases metabolism, Cell Shape drug effects, Coordination Complexes chemical synthesis, Coordination Complexes chemistry, Cytochromes c metabolism, DNA Damage, DNA Topoisomerases, Type II metabolism, Down-Regulation drug effects, Hep G2 Cells, Humans, Ligands, Membrane Potential, Mitochondrial drug effects, Mice, Mitochondria drug effects, Models, Biological, Reactive Oxygen Species metabolism, Signal Transduction drug effects, Tumor Burden drug effects, Tumor Suppressor Protein p53 metabolism, Up-Regulation drug effects, Xenograft Model Antitumor Assays, Antineoplastic Agents pharmacology, Apoptosis drug effects, Aporphines pharmacology, Cell Cycle Checkpoints drug effects, Coordination Complexes pharmacology, Metals pharmacology, Mitochondria metabolism, S Phase drug effects
Abstract

Three new oxoaporphine Co(II), Ni(II) and Zn(II) complexes 1-3 have been synthesized and fully characterized. 1-3 have similar mononuclear structures with the metal and ligand ratio of 1:2. 1-3 exhibited higher cytotoxicity than the OD ligand and cisplatin against HepG2, T-24, BEL-7404, MGC80-3 and SK-OV-3/DDP cells, with IC 50 value of 0.23-4.31 μM. Interestingly, 0.5 μM 1-3 significantly caused HepG2 arrest at S-phase, which was associated with the up-regulation of p53, p21, p27, Chk1 and Chk2 proteins, and decrease in cyclin A, CDK2, Cdc25A, PCNA proteins. In addition, 1-3 induced HepG2 apoptosis via a caspase-dependent mitochondrion pathway as evidenced by p53 activation, ROS production, Bax up-regulation and Bcl-2 down-regulation, mitochondrial dysfunction, cytochrome c release, caspase activation and PARP cleavage. Furthermore, 3 inhibited tumor growth in HepG2 xenograft model, and displayed more safety profile in vivo than cisplatin.

Published
2017
Full Text
View/download PDF

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