Antimicrobial, anti-inflammatory and antioxidant activities of polyoxygenated chalcones

Yesseny A. Vásquez-Martínez, Mauricio E. Osorio, Diego A. San Martín, Marcela A. Carvajal, Alejandra P. Vergara, Elizabeth Sanchez, Marcela Raimondi, Susana A. Zacchino, Carolina Mascayano, Claudia Torrent, Francisco Cabezas, Sophia Mejias, Margarita Montoya, Marcelo Cortez San Martín

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Abstract

©2019 Sociedade Brasileira de Química. It was synthesized nine polyoxygenated chalcones with a potential and safe use as antioxidant, antimicrobial and anti-inflammatory therapies. Chalcones obtained by Claisen-Schmidt condensation were studied as antioxidant, inhibitors of human 5-lipoxygenase, antifungal, antibacterial and antibiotic resistance modifiers. Two chalcones with catecholic moieties were able to strongly decrease the minimum inhibitory concentration (MIC) of methicillin against methicillin-resistant Staphylococcus aureus, increase the antiradical activity and significantly inhibit the human 5-lipoxygenase. Only one of these chalcones was active synergistically with methicillin. Chalcones with methoxyl substituents at different positions displayed the best activities against Cryptococcus neoformans. Only one chalcone showed good activity against the plant pathogenic bacteria Pseudomonas syringae whose half maximal inhibitory concentration (IC50) value (2.5 µg mL-1) was similar to that observed with the antibiotic streptomycin (2.9 µg mL-1). These simple chalcones have safe potential uses in antioxidant, antimicrobial and anti-inflammatory therapies.
Original languageEnglish
Pages (from-to)286-304
Number of pages19
JournalJournal of the Brazilian Chemical Society
DOIs
Publication statusPublished - 1 Jan 2019

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    Vásquez-Martínez, Y. A., Osorio, M. E., San Martín, D. A., Carvajal, M. A., Vergara, A. P., Sanchez, E., Raimondi, M., Zacchino, S. A., Mascayano, C., Torrent, C., Cabezas, F., Mejias, S., Montoya, M., & Martín, M. C. S. (2019). Antimicrobial, anti-inflammatory and antioxidant activities of polyoxygenated chalcones. Journal of the Brazilian Chemical Society, 286-304. https://doi.org/10.21577/0103-5053.20180177