Synthesis of Ursolic Acid-based Hybrids: In Vitro Antibacterial, Cytotoxicity Studies, In Silico Physicochemical and Pharmacokinetic Properties.
| Autor: | Khwaza V; Department of Chemistry, University of Fort Hare, Alice Campus, Alice, Eastern Cape, South Africa., Oselusi SO; School of Pharmacy, University of the Western Cape, Bellville, Cape Town 7535, South Africa., Morifi E; School of Chemistry, Mass Spectrometry Division, University of Witwatersrand, Johannesburg, South Africa., Nwamadi M; Department of Chemistry, University of Johannesburg, Auckland Park Campus, Johannesburg, South Africa., Hlope KS; Department of Biochemistry, Microbiology and Biotechnology, Faculty of Science and Agriculture, University of Limpopo, South Africa., Ndinteh DT; Department of Applied Chemistry, University of Johannesburg, Doornfontein Campus, Johannesburg, South Africa., Matsebatlela TM; Department of Biochemistry, Microbiology and Biotechnology, Faculty of Science and Agriculture, University of Limpopo, South Africa., Oyedeji OO; Department of Chemistry, University of Fort Hare, Alice Campus, Alice, Eastern Cape, South Africa., Aderibigbe BA; Department of Chemistry, University of Fort Hare, Alice Campus, Alice, Eastern Cape, South Africa. |
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| Jazyk: | angličtina |
| Zdroj: | Recent advances in anti-infective drug discovery [Recent Adv Antiinfect Drug Discov] 2024; Vol. 19 (3), pp. 232-253. |
| DOI: | 10.2174/0127724344272444231114103144 |
| Abstrakt: | Background: There is a critical need for the discovery of novel and effective antibacterial or anticancer molecules. Objectives: Amine-linked ursolic acid-based hybrid compounds were prepared in good yields in the range of 60-68%. Methods: Their molecular structures were successfully confirmed using different spectroscopic methods including 1 H/ 13 C NMR, UHPLC-HRMS and FTIR spectroscopy. The in vitro cytotoxicity of some of these hybrid molecules against three human tumour cells, such as MDA-MB23, MCF7, and HeLa was evaluated using the MTT colorimetric method. Result: Their antibacterial efficacy was evaluated against eleven bacterial pathogens using a serial dilution assay. Majority of the bacterial strains were inhibited significantly by compounds 17 and 24, with the lowest MIC values in the range of 15.3-31.25 μg/mL. Compound 16 exhibited higher cytotoxicity against HeLa cells than ursolic acid, with an IC Conclusion: The in vitro antibacterial activity and cytotoxicity of these hybrid compounds demonstrated that ursolic acid-based hybrid molecules are promising compounds. Further research into ursolic acid-based hybrid compounds is required. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.) |
| Databáze: | MEDLINE |
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