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Molecules 2014, 19(1), 1317-1327;

Antibacterial and Antioxidant Activities of Ursolic Acid and Derivatives

Departamento de Química Orgânica e Inorgânica, Universidade Federal do Ceará, Fortaleza-CE 60451-970, Brazil
Departamento de Farmácia, Universidade Federal do Ceará, Fortaleza-CE 60430-370, Brazil
Laboratório de Ciências Químicas (LCQUI)-CCT-UENF/PPGQO-DEQUIM-UFRRJ, Campos dos Goytacazes-RJ 28013-602, Brazil
Laboratório de Pesquisa de Produtos Naturais, Universidade Regional do Cariri, Crato-CE 63105-000, Brazil
Author to whom correspondence should be addressed.
Received: 7 November 2013 / Revised: 11 December 2013 / Accepted: 20 December 2013 / Published: 21 January 2014
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Ursolic acid, an important bioactive compound, was isolated from ethanol extract of aerial parts of Sambucus australis. In order to develop bioactive ursolic acid derivatives, two semi-synthetic compounds were obtained through modification at C-3. The antibacterial activity of the ursolic acid and its derivatives was investigated. The microdilution method was used for determination of the minimal inhibitory concentration (MIC), against twelve bacterial strains. The influence of ursolic acid and its derivatives on the susceptibility of some bacterial pathogens to the aminoglycosides antibiotics neomycin, amikacin, kanamycin and gentamicin was evaluated. The most representative synergistic effect was observed by 3β-formyloxy-urs-12-en-28-oic acid at the concentration of 64 μg/mL in combination with kanamycin against Escherichia coli (27), a multidrug-resistant clinical isolate from sputum, with reduction of MIC value from 128 μg/mL to 8 μg/mL. Ursolic acid and its derivatives were examined for their radical scavenger activity using the DPPH assay, and showed significant activity. View Full-Text
Keywords: Sambucus australis; ursolic acid; antioxidant activity; antibacterial activity Sambucus australis; ursolic acid; antioxidant activity; antibacterial activity

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do Nascimento, P.G.; Lemos, T.L.; Bizerra, A.M.; Arriaga, Â.M.; Ferreira, D.A.; Santiago, G.M.; Braz-Filho, R.; Costa, J.G.M. Antibacterial and Antioxidant Activities of Ursolic Acid and Derivatives. Molecules 2014, 19, 1317-1327.

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