Synthesis of Ursolic Acid-based Hybrids: In Vitro Antibacterial, Cytotoxicity Studies, In Silico Physicochemical and Pharmacokinetic Properties

Vuyolwethu Khwaza, Samson Olaitan Oselusi, Eric Morifi, Mutshinyalo Nwamadi, Kamogelo S. Hlope, Derek Tantoh Ndinteh, Thabe Moses Matsebatlela, Opeoluwa Oyehan Oyedeji, Blessing Atim Aderibigbe

Research output: Contribution to journalArticlepeer-review

Abstract

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 including1H/13C 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 IC50 value of 43.64 g/mL. 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.

Original languageEnglish
Pages (from-to)232-253
Number of pages22
JournalRecent Advances in Anti-Infective Drug Discovery
Volume19
Issue number3
DOIs
Publication statusPublished - 2024

Keywords

  • antibacterial
  • anticancer
  • cytotoxicity
  • hybrid molecules
  • Synthesis
  • ursolic acid

ASJC Scopus subject areas

  • Drug Discovery
  • Infectious Diseases
  • Pharmacology (medical)

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