DESIGN, SYNTHESIS AND VALIDATION OF CqsS RECEPTOR AGONIST TO MODULATE THE QUORUM SENSING CIRCUIT OF VIBRIO CHOLERAE–A MOLECULAR MIMIC THERAPY

2015 
Objective: Our earlier studies have characterized a compound from Melia dubia leaves, 4-ethyl resorcinol as an agonist of the Quorum Sensing (QS) receptor, CqsS agonist that had reverse engineered the QS circuit of V. cholerae from low-density to high-density state to effectively inhibit biofilm and enhance the production of protease to detach itself form the host tissue. So, the objective of this study was to synthesize structural derivatives of 4-ethyl resorcinol, to enhance its activity and to down regulate the host cell toxicity was validated. Methods: The antimicrobial (cell-density) and anti-virulent (protease, hemolysis, stress responds and biofilm inhibition) properties of the structural derivatives of 4-ethyl resorcinol were performed. Results: The results indicate that the compound has up surged protease expression along with a remarkable decrease in hemolytic activity at the 7 th hour. The stress responds in treated culture has a higher survival rate while the bacterial cells in the control succumb to stress stating the potential of the drug to induce HCD (high cell density) condition in the LCD (low cell density) state. From CLSM analysis we state that there was significant amount of dead colonies and disrupted biofilm in the respective treated culture Conclusion : This could possibly open up a direction to curb the bacterial biofilm formation and may also turn out to be a potent drug against treating Vibrio cholerae infection at an early point
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