4.4 Article

Synthesis of ursolic acid arylidene-hydrazide hybrid compounds and investigation of their cytotoxic and antimicrobial effects

Journal

NATURAL PRODUCT RESEARCH
Volume 37, Issue 15, Pages 2500-2507

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2022.2051170

Keywords

Ursolic acid; arylidene-hydrazide; hybrid molecules; cytotoxicity; antimicrobial; A549; BEAS-2B

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In this study, 13 new hybrid compounds were synthesized from ursolic acid and their cytotoxic activities and antimicrobial properties were evaluated. The results showed that certain compounds exhibited low cytotoxicity against specific cell lines, with compound 7k demonstrating high selectivity against A549 cells. Additionally, compound 7c showed effective antimicrobial activity against Staphylococcus aureus.
In this study, 13 new hybrid compounds (7a-m) were synthesised starting from ursolic acid, and their cytotoxic activities were investigated on the BEAS-2B and A549 cell lines. In addition, the synthesised compounds were tested against Staphylococcus aureus, Escherichia coli, and Candida albicans to determine their anti-microbial properties. The hybrid compounds that exhibited the lowest cytotoxicity against the BEAS-2B were 7k, 7b, and 7g. The cytotoxicity of the compounds against A549 was evaluated, the IC50 value of 7k, 7b, and 7g are found as 0.15 mu M, 0.31 mu M, and 0.26 mu M, respectively. The results showed that the selectivity of 7k was 7 times higher than doxorubicin against the A549 cells. According to the antimicrobial activity studies 7c is found as the most effective compound against S. aureus. Almost all compounds showed a similar inhibition potential against E. coli and C. albicans.

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