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Structure-activity relationship on DNA binding and anticancer activities of a family of mixed-ligand oxidovanadium(V) hydrazone complexes
DEBASHIS PATRA, SUBHABRATA PAUL, NAYIM SEPAY, , TAPAS GHOSH
Published in TAYLOR & FRANCIS INC
2018
PMID: 29171343
Volume: 36
   
Issue: 16
Pages: 4143 - 4155
Abstract
The title family of mixed-ligand oxidovanadium(V) hydrazone complexes are [(VO)-O-V(HL1)(hq)] (1) and [(VO)-O-V(HL2)(hq)] (2), where (HL1)(2-) and (HL2)(2-) are the dinegative form of 2-hydroxybenzoylhydrazone of acetylacetone (H3L1) and benzoylacetone (H3L2), respectively, and hq(-) is the mononegative form of 8-hydroxyquinoline (Hhq). Complexes were used to determine their binding constant with CT DNA using various spectroscopic techniques namely, electronic absorption, fluorescence and circular dichroism spectroscopy. The binding constant values suggest the intercalative mode of binding with the CT DNA and follow the order: 2 > 1. The bulky size as well as electron withdrawing property of the phenyl group (which is present in the beta-diketone part of the hydrazone moiety in complex 2 in place of a CH3 group in complex 1) is responsible for the higher activity of 2 than 1. Complexes were screened for cytotoxic activity on cervical cancer cells and were found to be potentially active (IC50 value for 1 and 2 is 33 and 29 mu M, respectively), even better than the widely used cis-platin (IC50 = 63.5 mu M) and carboplatin (IC50 = > 200 mu M) which is evident from the respective IC50 value. Nuclear staining experiment suggests that these complexes kill the SiHa cancer cells through apoptotic mode. The molecular docking study also suggested the intercalative mode of binding of these complexes with CT DNA and HPV 18 DNA.
About the journal
JournalJournal of Biomolecular Structure and Dynamics
PublisherTAYLOR & FRANCIS INC
ISSN0739-1102
Open AccessNo