Molecular modelling and experimental validation of mangiferin and its related compounds as quorum sensing modulators of Pseudomonas aeruginosa

芒果苷及其相关化合物作为铜绿假单胞菌群体感应调节剂的分子建模和实验验证

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Abstract

The LasR quorum sensing system regulates the virulence factors of Pseudomonas aeruginosa, a multi-drug resistant pathogen. Mangiferin and related compounds have been found to modulate this system as determined by in silico and in vitro experimental procedures. ZINCPharmer was used to compile a library of over 1000 metabolites that were screened to the top five based on shared pharmacophores and drug-like properties with mangiferin. Molecular docking and molecular dynamics simulation (140 ns) showed that ZINC E (- 55.64 ± 2.93 kcal/mol) and ZINC D (- 54.51 ± 2.82 kcal/mol) had significantly lower binding free energy compared to mangiferin-LasR (- 42.24 ± 3.94 kcal/mol) and the reference standard (azithromycin-LasR (- 40.01 ± 6.15 kcal/mol). ZINC D (95.16%) competed favorably with mangiferin (95.77%) as potential QS modulators at sub-minimum inhibitory concentrations relative to ZINC E (85.07%) and azithromycin (85.79%). These observations suggest mangiferin and related lead compounds as potential drug candidates for P. aeruginosa infection management.

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