Inhibition of the bacterial surface protein anchoring transpeptidase sortase by isoquinoline alkaloids.
The inhibitory activity of Coptis chinensis rhizome-derived material was evaluated against sortase, a bacterial surface protein anchoring transpeptidase, from Staphylococcus aureus ATCC 6538p and compared to that of four commercially available isoquinoline alkaloids. The biologically active constituent of C. chinensis extract was characterized as the isoquinoline alkaloid, berberine chloride, by spectral analysis. The isolate was a potent inhibitor of sortase, with an IC50 value of 8.7 microg/ml and had antibacterial activity against Gram-positive bacteria with a minimum inhibitory concentration (MIC) in the range of 50-400 microg/ml. Among the four isoquinoline alkaloids tested, berberine chloride had strong inhibitory activity. These results indicate that berberine is a possible candidate for the development of a bacterial sortase inhibitor.
Natural Products Research Institute, Seoul National University, Korea.
Soo-Hwan
SH
Kim
Dong-Sun
DS
Shin
Mi-Na
MN
Oh
Soon-Chun
SC
Chung
Jang-Suk
JS
Lee
Ki-Bong
KB
Oh
D019881:Aminoacyltransferases / Q000037:antagonists & inhibitors*; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D001426:Bacterial Proteins; D001599:Berberine / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D001681:Biological Assay; D039323:Coptis / Q000737:chemistry*; D003546:Cysteine Endopeptidases; D004791:Enzyme Inhibitors; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007546:Isoquinolines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007723:Korea; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D018517:Plant Roots / Q000737:chemistry; D013056:Spectrophotometry, Ultraviolet; D013211:Staphylococcus aureus / Q000187:drug effects / Q000201:enzymology
D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D004791:Enzyme Inhibitors; D007546:Isoquinolines; D001599:Berberine; D019881:Aminoacyltransferases; C120542:sortase A; D003546:Cysteine Endopeptidases