Lincosamides: Chemical structure, biosynthesis, mechanism of action, resistance, and applications

Publisher Summary Natural lincosamides are produced by several Streptomyces species, mainly by Streptomyces lincolnensis, S. roseolus, and S. caelestis and by Micromonospora halophytica. Lincosamides constitute a relatively small group of antibiotics with a chemical structure consisting of amino acid and sugar moieties. Their mechanism of action is via inhibition of protein synthesis in sensitive micro-organisms. Lincosamides have an unusual antimicrobial spectrum, being active against only Gram-positive and not Gram-negative aerobic bacteria. They exhibit a significant antibiotic activity against some anaerobic bacteria. They are used therapeutically, especially in cases where synergistic effects of a mixed anaerobic and aerobic microflora are anticipated. Lincomycin and clindamycin are also useful alternatives to penicillin and its derivatives in the treatment of upper respiratory tract infections in patients with allergy to penicillin. The chapter also discusses the major route of resistance to lincosamides. Furthermore, with the current knowledge of gene clusters specifying biosynthesis of lincomycin and the related antibiotic celesticetin, production of new derivatives of lincosamides by genetic engineering can be easily imagined, resulting in production of new derivatives of lincosamides.