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Coordination environment dependence of anticancer activity in cyclometalated bismuth(III) complexes with C,O-chelating ligands.
Lei, Jian; Liu, Yongping; Yin, Mingming; Li, Shan; Wang, Zixiu; Chen, Yi.
Afiliação
  • Lei J; School of Medicine, Hunan University of Chinese Medicine, Changsha 410208, PR China; Key Laboratory of Prevention and Treatment of Cardiovascular and Cerebrovascular Disease of the Ministry of Education, Key Laboratory for Tissue Engineering of Jiangxi Province, College of Pharmacy, Gannan Medical U
  • Liu Y; School of Medicine, Hunan University of Chinese Medicine, Changsha 410208, PR China.
  • Yin M; State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082, PR China.
  • Li S; Key Laboratory of Prevention and Treatment of Cardiovascular and Cerebrovascular Disease of the Ministry of Education, Key Laboratory for Tissue Engineering of Jiangxi Province, College of Pharmacy, Gannan Medical University, Ganzhou 341000, PR China.
  • Wang Z; Key Laboratory of Prevention and Treatment of Cardiovascular and Cerebrovascular Disease of the Ministry of Education, Key Laboratory for Tissue Engineering of Jiangxi Province, College of Pharmacy, Gannan Medical University, Ganzhou 341000, PR China.
  • Chen Y; School of Medicine, Hunan University of Chinese Medicine, Changsha 410208, PR China. Electronic address: chenyi@hnucm.edu.cn.
J Inorg Biochem ; 256: 112571, 2024 07.
Article em En | MEDLINE | ID: mdl-38669912
ABSTRACT
In this paper, a series of cyclometalated bismuth(III) complexes bearing C,O-bidentate ligands were synthesized and characterized by techniques such as UV-vis, NMR, HRMS, and single crystal X-ray diffraction. Meanwhile, their cytotoxicities against various human cell lines, including colon cancer cells (HCT-116), breast cancer cells (MDA-MB-231), lung cancer cells (A549), gastric cancer cells (SGC-7901), and normal embryonic kidney cells (HEK-293) were assessed in vitro. Compared with the clinical cisplatin, most of the synthesized complexes possessed significantly higher degrees of anticancer activity and selectivity, giving a selectivity index of up to 71.3. The structure-activity relationship study revealed that the anticancer performance of these bismuth(III) species depends on the factors of coordination environment surrounding the metal center, such as coordination number, coordination bonding strength, lone 6s2 electron pair stereoactivity. The Annexin V-FITC/PI double staining assay results suggested that the coordination environment-dependent cytotoxicity is ascribable to apoptosis. Western blot analysis confirmed the proposal, as evidenced by the down-regulating level of Bcl-2 and the activation of caspase-3. Furthermore, the representative complexes Bi1, Bi4, Bi6, and Bi8 exhibited relatively lower inhibitory efficiency on human ovarian cancer cells (A2780) than on its cisplatin-resistant daughter cells (A2780/cis), thus demonstrating that such compounds are capable of circumventing the cisplatin-induced resistance. This investigation elucidated the excellent anticancer performance of C,O-coordinated bismuth(III) complexes and established the correlation between cytotoxic activity and coordination chemistry, which provides a practical basis for in-depth designing and developing bismuth-based chemotherapeutics.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Bismuto / Complexos de Coordenação / Antineoplásicos Limite: Humans Idioma: En Revista: J Inorg Biochem / J. inorg. biochem / Journal of inorganic biochemistry Ano de publicação: 2024 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Bismuto / Complexos de Coordenação / Antineoplásicos Limite: Humans Idioma: En Revista: J Inorg Biochem / J. inorg. biochem / Journal of inorganic biochemistry Ano de publicação: 2024 Tipo de documento: Article
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