期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 44, 期 7, 页码 2936-2943出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.12.014
关键词
Andrographolide; Bacteria; Quorum sensing; Biofilm
资金
- Natural Science Fund of China [30772642]
- Science and Technology Plans of Guangzhou City [2006Z3-E4071, 2007Z3-E4071]
- Guangdong Province [2006B35603001, 2006-169]
Andrographolide (Andro), the main active component of the herb Andrographis paniculata, has been used for many years to treat a variety of diseases including bacterial and viral infections. Andro was recently reported to act by inhibiting the bacterial quorum sensing system. We have synthesized several Andro analogues and investigated their antibacterial activity and mechanism of action. The new compounds were found to be much more potent than the parent Andro in inhibiting bacterial growth and quorum sensing system. Compounds 5 and 7 significantly reduced virulence factor production. Compound 7 completely inhibited Pseudomonas aeruginosa (P. aeruginosa) biofilm formation, and exhibited synergistic activity with conventional antibiotics. These findings suggest that compound 7 may be the basis for future drug development to combat the unmet needs of virulence factor production, biofilm formation and antibiotic resistance. (C) 2008 Elsevier Masson SAS. All rights reserved.
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