Assessing the Solubility and Antibiotic Activity of Yanglingmycin/Coumarin Hybrids
Brave, Amelia C. J.
With the emergence of antibiotic resistance and infections plaguing the global population, it is imperative to focus research on the development of antibacterial agents designed to prevent bacteria from developing resistance. Two biologically active natural products, yanglingmycin and coumarin, were previously hybridized in an attempt to create a multi-target drug able to slow development of antibiotic resistance. Hybrids were predicted to have greater antimicrobial activity than the isolated pharmacophoric components. Initial studies found yanglingmycin-coumarin hybrids to be aqueous insoluble. This investigation aimed to maximize the solubility of these hybrids using a nonlethal polar solvent and to then assess the antibiotic activity of the hybrids. Successful solubilization of lipophilic compounds has previously been achieved through use of cyclodextrins as drug carriers; this study evaluated the solubility of yanglingmycin-coumarin hybrids using methyl β-cyclodextrin and β-cyclodextrin. The most effective solvent for dissolving yanglingmycin-coumarin hybrids was found to be methyl-β-cyclodextrin. Antibacterial assays testing maximum achieved concentrations of hybrid/methyl-β-cyclodextrin solutions with E. coli, S. aureus, B. cereus, and P. aeruginosa did not show evidence of antimicrobial activity. Future research should assess the hybrids’ antibiotic activity with different strains of bacteria to further evaluate their potential as antibiotics.
viii, 24 p.
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