Recent Advances in Methodologies for the Discovery of Antimycobacterial Drugs

Abstract

Mycobacteria, especially M. tuberculosis, have remained a worldwide dominant cause for human morbidity (~10 million annual cases) and mortality (3 million deaths annually) since ancient times. An estimated one-third of living humans are latently infected with M. tuberculosis. Despite this, there have been no new drugs specifically developed against mycobacteria since the 1960s. Because of a slow growth rate, biosafety concerns, and other issues, drug discovery by in vitro screening of natural and synthetic compounds has been limited in the past. However, a number of new techniques and technologies for whole cell antimycobacterial screening have been developed recently. This review examines and compares these methods, discusses common issues in screening with mycobacteria, and considers potential future developments in the field.

Ruthenium (II) phosphine/picolinate complexes as antimycobacterial agents

“…The rise of multidrug resistance (MDR) in MTB has complicated and prolonged the treatment [2]. No new drugs have been developed specifically against mycobacteria since the 1960s [3] and only within the last few years some promising drug candidates have emerged [4,5]. Thus, there is a great need to develop new therapeutic agents to treat tuberculosis, so as to reduce the total duration of treatment and to provide more effective treatment against MDR TB and latent tuberculosis infection [6].…”

Copper-Boosting Compounds: a Novel Concept for Antimycobacterial Drug Discovery

“…Then, 40 l alamarBlue dye mixture (50% alamarBlue, 5% [vol/vol] Tween 80) was added, and incubation was continued for another 24 h before plates were analyzed. Conversion of the indicator dye resazurin into resorufin with a fluorescence emission peak at 590 nm served as a marker for bacterial growth and viability (7)(8)(9).…”

In vitro Antibacterial Activity of Chitosan Nanoparticles against Mycobacterium tuberculosis

“…21,22 For the treatment, each of 0; 150; 300; 600; 1200; 2400 μg/mL chitosan nanoparticles solutions were slowly absorbed into the sterilized paper disc (diameter: 8 mm, Watman, England) and adhered to the surface of the plate on which Mycobacterium tuberculosis strains H37Rv at a concentration of 10 6 CFU/ml had been inoculated in Middlebrook 7H9 broth. Sterilized distilled water was used as a control.…”