TY - JOUR
T1 - Inhibition of the Quorum Sensing System, Elastase Production and Biofilm Formation in Pseudomonas aeruginosa by Psammaplin A and Bisaprasin
AU - Oluwabusola, Emmanuel T
AU - Katermeran, Nursheena Parveen
AU - Poh, Wee Han
AU - Goh, Teo Min Ben
AU - Tan, Lik Tong
AU - Diyaolu, Oluwatofunmilayo
AU - Tabudravu, Jioji
AU - Ebel, Rainer
AU - Rice, Scott A
AU - Jaspars, Marcel
N1 - Funding: The facilities and equipment support were provided partially by the National Institute of Education, Singapore. This research is funded by the National Research Foundation, Prime Minister’s Office, Singapore under its Marine Science Research and Development Program (Award Nos. MSRDP-P15 and MSRDP-P34). In addition, we acknowledge the E.U. Seventh Framework
Programme Project PharmaSea (grant agreement no-312184) for financial support for the collection of the marine sample.
Acknowledgments: E.T.O. and J.T. wish to thank the resource owners of the district of Wainunu, Bua, Fiji Islands, for the marine sponge used in this study. M.J. wishes to thank Russell Gray of Marine Biodiscovery Centre, Aberdeen, for running the NMR spectrometry.
PY - 2022/3/6
Y1 - 2022/3/6
N2 - Natural products derived from marine sponges have exhibited bioactivity and, in some cases, serve as potent quorum sensing inhibitory agents that prevent biofilm formation and attenuate virulence factor expression by pathogenic microorganisms. In this study, the inhibitory activity of the psammaplin-type compounds, psammaplin A (1) and bisaprasin (2), isolated from the marine sponge, Aplysinellarhax, are evaluated in quorum sensing inhibitory assays based on the Pseudomonas aeruginosa PAO1 lasB-gfp(ASV) and rhlA-gfp(ASV) biosensor strains. The results indicate that psammaplin A (1) showed moderate inhibition on lasB-gfp expression, but significantly inhibited the QS-gene promoter, rhlA-gfp, with IC50 values at 14.02 μM and 4.99 μM, respectively. In contrast, bisaprasin (2) displayed significant florescence inhibition in both biosensors, PAO1 lasB-gfp and rhlA-gfp, with IC50 values at 3.53 μM and 2.41 μM, respectively. Preliminary analysis suggested the importance of the bromotyrosine and oxime functionalities for QSI activity in these molecules. In addition, psammaplin A and bisaprasin downregulated elastase expression as determined by the standard enzymatic elastase assay, although greater reduction in elastase production was observed with 1 at 50 μM and 100 μM. Furthermore, the study revealed that bisaprasin (2) reduced biofilm formation in P. aeruginosa.
AB - Natural products derived from marine sponges have exhibited bioactivity and, in some cases, serve as potent quorum sensing inhibitory agents that prevent biofilm formation and attenuate virulence factor expression by pathogenic microorganisms. In this study, the inhibitory activity of the psammaplin-type compounds, psammaplin A (1) and bisaprasin (2), isolated from the marine sponge, Aplysinellarhax, are evaluated in quorum sensing inhibitory assays based on the Pseudomonas aeruginosa PAO1 lasB-gfp(ASV) and rhlA-gfp(ASV) biosensor strains. The results indicate that psammaplin A (1) showed moderate inhibition on lasB-gfp expression, but significantly inhibited the QS-gene promoter, rhlA-gfp, with IC50 values at 14.02 μM and 4.99 μM, respectively. In contrast, bisaprasin (2) displayed significant florescence inhibition in both biosensors, PAO1 lasB-gfp and rhlA-gfp, with IC50 values at 3.53 μM and 2.41 μM, respectively. Preliminary analysis suggested the importance of the bromotyrosine and oxime functionalities for QSI activity in these molecules. In addition, psammaplin A and bisaprasin downregulated elastase expression as determined by the standard enzymatic elastase assay, although greater reduction in elastase production was observed with 1 at 50 μM and 100 μM. Furthermore, the study revealed that bisaprasin (2) reduced biofilm formation in P. aeruginosa.
KW - marine sponge
KW - psammaplin
KW - marine natural products
KW - quorum sensing inhibitor
KW - Pseudomonas aeruginosa
KW - inhibitor of biofilm formation
KW - elastase inhibitor
U2 - 10.3390/molecules27051721
DO - 10.3390/molecules27051721
M3 - Article
C2 - 35268822
VL - 27
JO - Molecules
JF - Molecules
SN - 1420-3049
IS - 5
M1 - 1721
ER -
