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.
Highlights
Since the antimicrobial drug class loses effectiveness over time through bacterial resistance, innovation is needed immediately
The biofilm formation is related to many unsuccessful treatments, based on the fact that bacteria biofilm is difficult to treat with only antibiotics [2]
Betulinic acid was isolated from the Platanus acerifolia bark and ursolic acid (UA) was isolated from waste apple (M. domestica) peels obtained from a local juice factory [13]
Summary
Since the antimicrobial drug class loses effectiveness over time through bacterial resistance, innovation is needed immediately. Biofilm is formed when a bacterial community attaches to a surface and forms a polymeric matrix of hydrated extracellular polymeric substances [3]. Such body surfaces include, for example, skin, lung and teeth [4] where the biofilm persists even after treatment with several antimicrobial agents [5]. For example, skin, lung and teeth [4] where the biofilm persists even after treatment with several antimicrobial agents [5] Another example are the biofilms on medical devices, including artificial heart valves, pacemakers and synthetic joints [6]
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