pyochelin and zingerone

Topics: Animals; Mice; Peritonitis; Phenols; Pseudomonas aeruginosa; Pseudomonas Infections

In this article, we report the chemical synthesis of pyochelin-zingerone conjugate via a hydrolysable ester linkage for drug delivery as a "Trojan Horse Strategy." It is a new therapeutic approach to combat microbial infection and to address the issue of multi drug resistance in Gram-negative, nosocomial pathogen Pseudomonas aeruginosa. Pyochelin (Pch) is a catecholate type of phenolate siderophore produced and utilized by the pathogen P. aeruginosa to assimilate iron when colonizing the vertebrate host. Zingerone, is active component present in ginger, a dietary herb known for its anti-virulent approach against P. aeruginosa. In the present study, zingerone was exploited to act as a good substitute for existing antibiotics, known to have developed resistance by most pathogens. Encouraging results were obtained by docking analysis of pyochelin-zingerone conjugate with FptA, the outer membrane receptor of pyochelin. Conjugate also showed anti-quorum sensing activity and also inhibited swimming, swarming, and twitching motilities as well as biofilm formation in vitro.

Topics: Anti-Bacterial Agents; Biofilms; Drug Design; Drug Resistance, Bacterial; Guaiacol; Microbial Sensitivity Tests; Molecular Docking Simulation; Molecular Structure; Phenols; Pseudomonas aeruginosa; Quorum Sensing; Thiazoles