Analysis of DNA protection, interaction and antimicrobial activity of isatin derivatives

International Journal of Biological Macromolecules
Mohamed Abdulhamid GanimFatih Sen

Abstract

Isatin, thiosemicarbazone and their derivatives have been widely used in biological applications such as antimicrobial, antiviral and anticancer therapies. Herein, eight isatin and thiosemicarbazone derivative compounds were re-synthesized and evaluated for DNA binding analysis including DNA protection studies using plasmid DNA (pUC19) and DNA interaction experiments using calf thymus DNA (CT-DNA). All compounds were also utilized in vitro assay to assess the antimicrobial activity of compounds against different pathogenic bacterial strains. All isatin and thiosemicarbazone derivative compounds exhibited DNA protection activity which ranged from 23.5 to 59.5%. Among them, I3-(N-2-MP)-TSC had the greatest DNA protective activity. For DNA binding analysis, all compounds had the same constant concentration (40 μM), which interacts with CT-DNA. It was also observed that DNA interactions gave a high intrinsic binding constant (Kb = 1.72 × 104 M-1-9.73 × 105 M-1). Besides, several derivatives of isatin thiosemicarbazone exhibited significant and selective antibacterial activity with low concentration. These compounds primarily affected Gram-positive bacteria, but were not effective against P. vulgaris and E. coli. The Gram-positive m...Continue Reading

Citations

Oct 21, 2019·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·Alireza HabibiZeinab Moradi-Shoeili
Apr 4, 2021·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Run ChengYanqing Wang
Oct 24, 2020·Current Topics in Medicinal Chemistry·Ana I MatesanzAdoración G Quiroga

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