TY - JOUR
T1 - Synthesis of Ursolic Acid-based Hybrids
T2 - In Vitro Antibacterial, Cytotoxicity Studies, In Silico Physicochemical and Pharmacokinetic Properties
AU - Khwaza, Vuyolwethu
AU - Oselusi, Samson Olaitan
AU - Morifi, Eric
AU - Nwamadi, Mutshinyalo
AU - Hlope, Kamogelo S.
AU - Ndinteh, Derek Tantoh
AU - Matsebatlela, Thabe Moses
AU - Oyedeji, Opeoluwa Oyehan
AU - Aderibigbe, Blessing Atim
N1 - Publisher Copyright:
© 2024 Bentham Science Publishers.
PY - 2024
Y1 - 2024
N2 - 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.
AB - 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.
KW - antibacterial
KW - anticancer
KW - cytotoxicity
KW - hybrid molecules
KW - Synthesis
KW - ursolic acid
UR - http://www.scopus.com/inward/record.url?scp=85188429969&partnerID=8YFLogxK
U2 - 10.2174/0127724344272444231114103144
DO - 10.2174/0127724344272444231114103144
M3 - Article
C2 - 38317466
AN - SCOPUS:85188429969
SN - 2772-4344
VL - 19
SP - 232
EP - 253
JO - Recent Advances in Anti-Infective Drug Discovery
JF - Recent Advances in Anti-Infective Drug Discovery
IS - 3
ER -