Bismuth(III) and diorganotin(IV) complexes of bis(2-acetylpyridine) thiocarbonohydrazone: Synthesis, characterization, and apoptosis mechanism of action in vitro

• Published in: Polyhedron Vol. 155; pp. 254 - 260
• Main Authors: Fang, Yan, Wang, Yu-Ting, Zhao, Meng, Lu, Yan-Li, Li, Ming-Xue, Zhang, Ya-Hong
• Format: Journal Article
• Language: English
• Published: OXFORD Elsevier Ltd 15.11.2018; Elsevier
• Subjects: Apoptosis mechanism; Chemistry; Chemistry, Inorganic & Nuclear; Complex; Crystal structure; Crystallography; Cytotoxicity; Physical Sciences; Science & Technology; Thiosemicarbazone; Cytotoxicity; Thiosemicarbazone; Apoptosis mechanism; Complex; Crystal structure; CRYSTAL-STRUCTURE; SPECTRAL CHARACTERIZATION; ANTICANCER ACTIVITY; 2-ACETYLPYRIDINE; ORGANOTIN(IV) COMPLEXES; BIOLOGICAL EVALUATION; SPECTROSCOPIC CHARACTERIZATION; CHEMISTRY; SCHIFF-BASE; N-PHENYLTHIOSEMICARBAZONE
• ISSN: 0277-5387
• DOI: 10.1016/j.poly.2018.08.049

Molecular mechanism of 1 inducing apoptosis against human hepatocellular carcinoma HepG2 cells has been discussed in detail. Biological research illustrated that 1 exhibited higher activity against HepG2 cells. Cytotoxicity experiments involving with mitochondria indicated that 1 restrained cells growth in a dose-dependent manner. Protein analysis revealed that 1 restrained Bcl-2 expression and accelerated Bax expression, inducing caspase-3 activation. [Display omitted] In this paper, three bismuth(III) and diorganotin(IV) complexes based on bis(2-acetylpyridine) thiocarbonohydrazone (H2L) have been fully designed. The tests of the complexes on inhibiting human hepatocellular carcinoma HepG2 cells growth in vitro revealed that the complexes have higher activity against HepG2 cells but much less toxicity toward normal hepatocyte QSG7701 cells. Particularly, 1 exhibited higher activity with a lower IC50 value (compound concentration that produces 50% of cell death, 3.42 ± 0.25 µM). Moreover, cytotoxicity experiments involving with mitochondria confirmed that 1 restrained cells growth in a dose-dependent manner. Protein analysis indicated that 1 restrained Bcl-2 expression and accelerated Bax expression, inducing caspase-3 activation.