Design and synthesis of acyldepsipeptide-1 analogues: antibacterial activity and cytotoxicity screening

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dc.contributor.authorSibuyi, Nicole R.S
dc.contributor.authorCobongela, Sinazo Z.Z
dc.contributor.authorMakatini, Maya M
dc.date.accessioned2023-06-06T14:02:33Z
dc.date.available2023-06-06T14:02:33Z
dc.date.issued2023
dc.description.abstractAcyldepsipeptides (ADEPs) are receiving more attention as prospective antimicrobial agents due to their unique mode of action and chemical properties. However, their therapeutic potential is limited by their poor pharmacokinetic properties. Chemical modifications have been successful in improving the biocompatibility and bioavailability of ADEPs. In the current study, ADEP1 was modified by introducing a disulphide linkage, replacement of the octa-2,4,6-trienoic acid (OTEA) with either adamantane (Ada) or palmitic acid (Pal), and lastly, comparing the use of D versus L amino acids. The antibacterial effects of the ADEP1 analogues were investigated in Gram-positive and Gram-negative strains using agar well diffusion and microdilution assays. Cytotoxicity was evaluated in human embryonic kidney (HEK)-293 and colon cancer (Caco-2) cells by the MTS assay. Using solid phase peptide synthesis (SPPS), the percentage yield of the synthetic peptides was increased to > 37% with > 96% purity.en_US
dc.identifier.citationCobongela, S.Z., Makatini, M.M., Njengele-Tetyana, Z., Sikhwivhilu, L.M. and Sibuyi, N.R., 2023. Design and synthesis of Acyldepsipeptide1 analogues: Antibacterial activity and cytotoxicity screening. Arabian Journal of Chemistry, p.105000.en_US
dc.identifier.urihttps://doi.org/10.1016/j.arabjc.2023.105000
dc.identifier.urihttp://hdl.handle.net/10566/9047
dc.language.isoenen_US
dc.publisherArabian Journal of Chemistryen_US
dc.subjectAcyldepsipeptidesen_US
dc.subjectAdamantaneen_US
dc.subjectAntimicrobial peptidesen_US
dc.subjectCaseinolytic proteaseen_US
dc.subjectPalmitic aciden_US
dc.titleDesign and synthesis of acyldepsipeptide-1 analogues: antibacterial activity and cytotoxicity screeningen_US
dc.typeArticleen_US

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