Journal
JOURNAL OF NATURAL PRODUCTS
Volume 81, Issue 12, Pages 2621-2629Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jnatprod.8b00315
Keywords
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Funding
- National Natural Science Foundation of China [81673336]
- Pearl River SAMP
- T Nova Program of Guangzhou [201806010116]
- Fundamental Research Funds for the Central University [21617478]
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The quorum sensing (QS) system inhibitors of Pseudomonas aeruginosa are thought to attenuate bacterial pathogenicity and drug resistance by inhibiting biofilm formation and the production of virulence factors. In this study, a synthetic approach to the natural products cajaninstilbene acid (1) and amorfrutins A (2) and B (3) has been developed and was characterized by the Heck reaction, which was used to obtain the stilbene core and a Pinick oxidation to give the O-hydroxybenzoic acid. The biological activities of these compounds against the P. aeruginosa quorum sensing systems were evaluated. Amorfrutin B (3) showed promising antibiofilm activity against P. aeruginosa PAO1 with a biofilm inhibition ratio of 50.3 +/- 2.7. Three lacZ reporter strains were constructed to identify the effects of compound 3 on different QS systems. Suppression efficacy of compound 3 on the expression of lasB-lacZ and pqsA-lacZ as well as on the production of their corresponding virulence factors elastase and pyocyanin was observed.
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