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Antibacterial activity of structural analogs of betulin against Escherichia coli, Staphylococcus aureus, Bacillus subtilis, and methicillin-resistant Staphylococcus aureus



Antibacterial activity of structural analogs of betulin against Escherichia coli, Staphylococcus aureus, Bacillus subtilis, and methicillin-resistant Staphylococcus aureus



Abstracts of the General Meeting of the American Society for Microbiology 101: 39



Betulin, a pentacyclic triterpenoid derived from the outer bark of white "paper" birch, and a few structural analogs have recently shown antiviral activity against herpes simplex viruses. This study was designed to find the in vitro effectiveness of other analogs against potentially infectious bacteria using the minimum inhibitory concentration method. Compounds were dissolved in both water and dimethyl sulfoxide (DMSO), with concentrations of 125 ng/mL and 10 mg/mL, respectively. Controls included penicillin G (10 units), tetracycline (30 mcg), streptomycin (10 mcg), 0.85% saline solution, and DMSO. Compounds inhibiting E. coli growth included betulin 3,28-diphosphate, betulin 3,28-diglutarate, and betulin diglycolate, each at a concentration of 0.265+-.21muM. Betulin 3,28-dimaleate and betulin 3,28-diphthlate, each at a concentration of 2.3+-.11muM, had a bacteriocidal effect against laboratory S. aureus. Methicillin-resistant S. aureus was susceptible to betulin 3,28-dimaleate and suberin at a concentration of 0.263+-.24muM. No compounds were effective against B. subtilis. Due to its bacteriocidal effect on both strains of S. aureus, betulin 3,28-dimaleate has future importance in treating S. aureus infections. Certain structural analogs of betulin, in general, were 70X more effective than the control antibiotics, indicating their high potential in fighting tomorrow's bacterial infections.

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