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

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posted on 2022-03-11, 17:20 authored by Halil Şenol, Rabia Büşra Şahin, Berre Mercümek, Halil Burak Kapucu, Ebru Hacıosmanoğlu, Harika Öykü Dinç, Pelin Yüksel Mayda

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 µM, 0.31 µM, and 0.26 µM, 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.

Funding

This study financially supported by Bezmialem Vakif University, Scientific Research Project Number: BAP 20200207. Spectral data were recorded at Bezmialem Vakif University Drug Application and Research Centre (ILMER).

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