Triterpene Derivatives as Relevant Scaffold for New Antibiofilm Drugs.

Biomolecules

Laboratório de Fitoquímica e Síntese Orgânica, Faculdade de Farmácia, Universidade Federaldo Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, 90610-000, Brasil.

Published: February 2019

New medicines for the treatment of bacterial biofilm formation are required. For thisreason, this study shows the in vitro activity of betulinic acid (BA), ursolic acid (UA) and their twentyderivatives against planktonic and biofilm cells (gram-positive bacterial pathogens: Enterococcusfaecalis, and ). We evaluated the antibiofilm activity(through the crystal violet method), as well as the antibacterial activity via absorbance (OD) atconcentrations of 5, 25 and 100 μM. Likewise, the cytotoxicity of all compounds was evaluated on akidney 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 timewhether different groups at carbon 3 (C-3) of triterpenes may interfere in the antibiofilm activity withminimal or no antibacterial effect. After the screening of 22 compounds at three distinctconcentrations, 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 activityagainst S. aureus without any effect upon mammalian cells.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6406419PMC
http://dx.doi.org/10.3390/biom9020058DOI Listing

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