Dataset Information

A Cyclic Dipeptide from Marine Fungus Penicillium chrysogenum DXY-1 Exhibits Anti-quorum Sensing Activity.

ABSTRACT: 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.

SUBMITTER: Yu X

PROVIDER: S-EPMC7992161 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature

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A Cyclic Dipeptide from Marine Fungus Penicillium chrysogenum DXY-1 Exhibits Anti-quorum Sensing Activity.

Yu Xiaodan X Li Li L Sun Shiwei S Chang Aiping A Dai Xiaoyun X Li Hui H Wang Yinglu Y Zhu Hu H

ACS omega 20210312 11

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 violace ...[more]

PMID: 33778279

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Project description:Simple Summary Besides showing the antibacterial activity of the Preyssler-type polyoxotungstate (POT) P5W30 with the ability to affect MRSA cells, we demonstrated that P5W30 also displays other proprieties, such as anti-quorum sensing and antibiofilm. These are biological activities that are reported for a POT for the first time. Quorum sensing and biofilm facilitate the bacterial colonization, antibiotic resistance and persistence in both the environment and host, and its impairment by POTs can greatly contribute to the control of bacterial infections, such as those caused by multiresistant bacteria. Moreover, antiviral activity was also observed using the enterovirus Qβ. NMR stability studies of P5W30 demonstrate that it remains intact, suggesting its responsibility in the described biological activities. Taken together, our results emphasize the potential biomedical use of POTs, particularly the Preyssler-type POT, to fight antibiotic-resistant MRSA strains and their ability to form biofilm, besides being a promising antiviral agent. Abstract The increase in bacterial resistance to antibiotics has led researchers to find new compounds or find combinations between different compounds with potential antibacterial action and with the ability to prevent the development of antibiotic resistance. Polyoxotungstates (POTs) are inorganic clusters that may fulfill that need, either individually or in combination with antibiotics. Herein, we report the ability of the polyoxotungstates (POTs) with Wells-Dawson P2W18, P2W17, P2W15, and Preyssler P5W30 type structures to differently affect Gram-negative and Gram-positive microorganisms, either susceptible or resistant to antibiotics. The compound P5W30 showed the highest activity against the majority of the tested bacterial strains in comparison with the other tested POTs (P2W15, P2W17 and P2W18) that did not show inhibition zones for the Gram-negative bacteria, A. baumanii I73775, E. coli DSM 1077, E. coli I73194, K. pneumoniae I7092374, and P. aeruginosa C46281). Generally, the results evidenced that Gram-positive bacteria are more susceptible to the POTs tested. The compound P5W30 was the one most active against S. aureus ATCC 6538 and MRSA16, reaching <0.83 mg·mL−1 (100 μM) and 4.96 mg·mL−1 (600 μM), respectively. Moreover, it was verified by NMR spectroscopy that the most promising POT, P5W30, remains intact under all the experimental conditions, after 24 h at 37 °C. This prompted us to further evaluate the anti-quorum sensing activity of P5W30 using the biosensor Chromobacterium violaceum CV026, as well as its antibiofilm activity both individually and in combination with the antibiotic cefoxitin against the methicillin-resistant Staphylococcus aureus 16 (MRSA16). P5W30 showed a synergistic antibacterial effect with the antibiotic cefoxitin and chloramphenicol against MRSA16. Moreover, the antibiofilm activity of P5W30 was more pronounced when used individually, in comparison with the combination with the antibiotic cefoxitin. Finally, the antiviral activity of P5W30 was tested using the coliphage Qβ, showing a dose-dependent response. The maximum inactivation was observed at 750 μM (6.23 mg·mL−1). In sum, P5W30 shows anti-quorum sensing and antibiofilm activities besides being a potent antibacterial agent against S. aureus and to exhibit antiviral activities against enteric viruses.

Dataset Information

A Cyclic Dipeptide from Marine Fungus Penicillium chrysogenum DXY-1 Exhibits Anti-quorum Sensing Activity.

Publications

A Cyclic Dipeptide from Marine Fungus <i>Penicillium chrysogenum</i> DXY-1 Exhibits Anti-quorum Sensing Activity.

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