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Biomolecules 2019, 9(2), 58; https://doi.org/10.3390/biom9020058

Triterpene Derivatives as Relevant Scaffold for New Antibiofilm Drugs

1
Laboratório de Fitoquímica e Síntese Orgânica, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul 90610-000, Brazil
2
Laboratório de Biofilmes e Diversidade, Faculdade de Farmácia and Centro de Biotecnologia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul 91501-970, Brazil
*
Author to whom correspondence should be addressed.
Received: 15 January 2019 / Revised: 30 January 2019 / Accepted: 30 January 2019 / Published: 11 February 2019
(This article belongs to the Special Issue Evaluation and formulation of Bioactive Terpenes)
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Abstract

New medicines for the treatment of bacterial biofilm formation are required. For this reason, this study shows the in vitro activity of betulinic acid (BA), ursolic acid (UA) and their twenty derivatives against planktonic and biofilm cells (gram-positive bacterial pathogens: Enterococcus faecalis, Staphylococcus aureus and Staphylococcus epidermidis). We evaluated the antibiofilm activity (through the crystal violet method), as well as the antibacterial activity via absorbance (OD600) at concentrations of 5, 25 and 100 µM. Likewise, the cytotoxicity of all compounds was evaluated on a kidney African green monkey (VERO) cell line at the same concentration, by MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) methodology. We verified for the first time whether different groups at carbon 3 (C-3) of triterpenes may interfere in the antibiofilm activity with minimal or no antibacterial effect. After the screening of 22 compounds at three distinct concentrations, we found antibiofilm activity for eight distinct derivatives without antibiotic effect. In particular, the derivative 2f, with an isopentanoyl ester at position C-3, was an antibiofilm activity against S. aureus without any effect upon mammalian cells. View Full-Text
Keywords: ursolic acid; betulinic acid; cytotoxicity; pathogenic biofilms; bacterial pathogens ursolic acid; betulinic acid; cytotoxicity; pathogenic biofilms; bacterial pathogens
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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da Silva, G.N.S.; Primon-Barros, M.; Macedo, A.J.; Gnoatto, S.C.B. Triterpene Derivatives as Relevant Scaffold for New Antibiofilm Drugs. Biomolecules 2019, 9, 58.

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