gramicidin-a and Tuberculosis

Gramicidin S (GS) is a cyclic cationic antimicrobial peptide (CAP) with a wide spectrum of antibiotic activities whose usage has been limited to topical applications owing to its cytotoxic side effects. We have synthesized tetrahydrofuran amino acid (Taa)-containing GS analogues, and we have carried out conformational analysis and explored their structure activity relationships by evaluating their antitubercular, antibacterial and cytotoxic properties. Two of these analogues showed impressive as well as selective activity against Mycobacterium tuberculosis (MTB) without toxicity towards mammalian Vero cells or human RBCs, and are promising as potential leads.

Topics: Animals; Anti-Bacterial Agents; Antitubercular Agents; Bacteria; Bacterial Infections; Chlorocebus aethiops; Erythrocytes; Furans; Gramicidin; Humans; Microbial Sensitivity Tests; Molecular Dynamics Simulation; Mycobacterium tuberculosis; Tuberculosis; Vero Cells