Facially Amphiphilic Cholic Acid–Lysine Conjugates as Promising Antimicrobials
Poonam Singla, Mahaldeep Kaur, Anjna Kumari, Laxmi Kumari, Sandip V. Pawar, Rachna Singh, Deepak B. Salunke
Abstract
. A pronounced effect of increase in lysine residues was noted on the observed activity. The lead compounds were found to be active against drug-resistant bacterial and fungal clinical isolates and also improved the efficacy of antifungal agents amphotericin B and voriconazole. Membrane-permeability studies demonstrated the ability of these compounds to induce membrane damage in the tested microbes. The active conjugates did not show any hemolytic activity and were also found to be nontoxic to the normal cells as well as the examined cancer cell lines. The observed antimicrobial activity was attributed to the facial amphiphilic conformations, hydrophobic/hydrophilic balance, and the overall charge on the molecules.