[Frontiers in Bioscience 17, 1861-1881, January 1, 2012]

Antimycobacterials from natural sources: ancient times, antibiotic era and novel scaffolds

Juan D. Guzman1,2, Antima Gupta1, Franz Bucar3, Simon Gibbons2, Sanjib Bhakta1

1Institute of Structural and Molecular Biology, Department of Biological Sciences, Birkbeck, University of London, London WC1E 7HX, UK, 2Department of Pharmaceutical and Biological Chemistry,The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, UK, 3Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Karl Franzens University Graz, Universitatsplatz 4, A-8010 Graz, Austria


1. Abstract
2. Introduction
3. Ancient times
4. Discovery of antibiotics
5. Novel antimycobacterial scaffolds from natural products
6. Perspective
7. Acknowledgments
8. References


Mycobacteria are a group of aerobic, non-motile, acid fast bacteria that have a characteristic cell wall composed of a mycolyl-arabinogalactan-peptidoglycan complex. They display different phenotypic attributes in their growth, color and biochemistry. Tuberculosis (TB) is defined as the infection with Mycobacterium tuberculosis complex and was declared a global health emergency principally because of the appearance of multidrug-resistant strains and the associated risk of infection in immune-compromised population. There is an urgent clinical need for novel, potent and safe anti-TB drugs. Natural products have been used since antiquity for treating diverse complaints and novel pharmacophores are discovered every year. Two of the most potent used antimycobacterials, the rifamycins and streptomycin, were first detected in Streptomyces bacteria. Plants are also the source of an exquisite variety of antimicrobials that can lead to useful therapeutics in the future. In this review, natural preparations used since antiquity for treating tuberculosis are described, together with a rapid view of the 20th century antibiotic development against TB. Finally a summary of the most potent recent natural antimycobacterials is displayed.