Ursolic, oleanolic and betulinic acids: Antibacterial spectra and selectivity indexes

• Published in: Journal of ethnopharmacology Vol. 120; no. 2; pp. 272 - 276
• Main Authors: Fontanay, Stéphane, Grare, Marion, Mayer, Joséphine, Finance, Chantal, Duval, Raphaël Emmanuel
• Format: Journal Article
• Language: English
• Published: Shannon Elsevier Ireland Ltd 20-11-2008; Amsterdam; New York: Elsevier; Elsevier
• Subjects: Anti-Bacterial Agents - pharmacology; Anti-Bacterial Agents - toxicity; Antibacterial; antibacterial properties; antibiotic resistance; Bacteriology; Betulinic Acid; Biological and medical sciences; Cell Line; cell lines; Cell Survival - drug effects; chemical constituents of plants; Cytotoxicity; Drug Resistance, Bacterial; Enterococcus faecalis; Escherichia coli; Eukaryotic Cells - drug effects; Eukaryotic Cells - metabolism; General pharmacology; Gram-Negative Bacteria - drug effects; Gram-positive bacteria; Gram-Positive Bacteria - drug effects; Humans; Life Sciences; Medical sciences; Medication; Microbial Sensitivity Tests; Microbiology and Parasitology; minimum inhibitory concentration; Oleanolic acid; Oleanolic Acid - pharmacology; Oleanolic Acid - toxicity; Pentacyclic Triterpenes; Pharmaceutical sciences; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; Pseudomonas aeruginosa; Selectivity index; Staphylococcus aureus; structure-activity relationships; toxicity testing; Toxicity Tests; Triterpenes - pharmacology; Triterpenes - toxicity; Ursolic Acid; Virology; Cytotoxicity; Ursolic acid; Selectivity index; Antibacterial; Betulinic acid; Oleanolic acid; Terpenoid; Ursane derivatives; Pharmacognosy; Medicinal plant; Oleanane derivatives; Plant origin; Triterpene; Antibacterial agent
• ISSN: 0378-8741; 1872-7573
• DOI: 10.1016/j.jep.2008.09.001

Ursolic acid (UA), oleanolic acid (OA) and betulinic acid (BA), three hydroxyl pentacyclic triterpenoic acids (HPTAs) naturally found in a large variety of vegetarian foods, medicinal herbs and plants have been investigated for antibacterial activity.
To determine the antibacterial activity of UA, OA and BA, as well as the toxic impact on eukaryotic cells.
Minimum inhibitory concentrations were determined against five reference strains (
Escherichia coli ATCC 25922,
Staphylococcus aureus ATCC 25923 & ATCC 29213,
Enterococcus faecalis ATCC 29212 and
Pseudomonas aeruginosa ATCC 27853), as well as five antibiotic-resistant clinical isolates. Toxicity was evaluated against MRC-5 and HaCaT cell lines.
No antibacterial activity was observed for BA; while OA and more particularly UA, did show a moderate to good antibacterial activity, but limited to Gram-positive bacteria. Nevertheless, OA and UA were devoid of antibacterial activities against clinical isolates. Moreover, viability and cytotoxic assays demonstrated that the three compounds induced a significant cytotoxicity.
Despite of a relative similar chemical structure; UA, OA and BA harboured different antibacterial activities, with more significant ones for UA. However, considering both viability and toxicity values, these compounds seem to have a significant impact on eukaryotic cell viability.