posted on 2021-03-12, 20:15authored byXiaodan Yu, Li Li, Shiwei Sun, Aiping Chang, Xiaoyun Dai, Hui Li, Yinglu Wang, Hu Zhu
Bacterial quorum
sensing (QS) is anticipated as a new potential
target for the development of antimicrobial drugs. An anti-QS substance
against Chromobacterium violaceum CV026
and Pseudomonas aeruginosa PA01 has
been isolated and purified from the crude extracts of the marine fungus Penicillium chrysogenum DXY-1, and the accurate structure
was identified as cyclo(l-Tyr-l-Pro). This cyclic
dipeptide at sub-minimum inhibitory concentration can decrease the
QS-regulated violacein production of C. violaceum CV026 by 79% and QS-mediated pyocyanin production, proteases, and
elastase activity of P. aeruginosa PA01
by 41%, 20%, and 32%, respectively. In addition, it can also destroy
the biofilm formation and decrease QS gene expression of P. aeruginosa PA01. Molecular docking was further
performed, and the obtained data indicated that this dipeptide blocks
the effect of QS autoinducers through competitive binding to the same
pocket of the receptor proteins. We expect this anti-QS cyclic dipeptide
to be a potential pro-drug treating drug-resistant P. aeruginosa infections, and these findings could
relieve the alarming problem of microbial resistance to antimicrobial
drugs.