Anti-Tubercular Agents from Glycyrrhiza glabra

Title:Anti-Tubercular Agents from Glycyrrhiza glabra

Volume: 15 Issue: 11

Author(s): Komal Kalani, Vinita Chaturvedi, Sarfaraz Alam, Feroz Khan and Santosh Kumar Srivastava

Affiliation:

Keywords: Drug likeness, GA-1 derivatives, Glycyrrhiza glabra, Molecular docking, Mycobacterium tuberculosis.

Abstract: Bioactivity guided isolation of Glycyrrhiza glabra (Leguminosae / Fabaceae) roots resulted in the characterization of 18β-glycyrrhetinic acid as a major anti-tubercular agent. Further, GA-1 was semi-synthetically converted into its nine derivatives, which were in-vitro evaluated for their antitubercular potential against Mycobacterium tuberculosis H₃₇Rv using BACTEC-460 radiometric susceptibility assay. All the derivatives were active, but the benzylamide (GA-8, MIC 12.5μg/ml) and ethyl oxylate (GA-3, MIC 25.0 μg/ml) derivatives were significantly active against the pathogen. This was further supported by the molecular docking studies, which showed adequate docking (LibDock) scores for GA-3 (120.3) and GA-8 (112.6) with respect to the standard anti-tubercular drug, rifampicin (92.94) on the DNA-directed RNA polymerase subunit beta (rpoB) target site. Finally, the in silico pharmacokinetic and drug-likeness studies showed that GA-3 and GA- 8 possesses drug-like properties. This is the first ever report on the anti-tubercular potential of GA and its derivatives. These results may be of great help in anti-tubercular drug development from a very common, inexpensive, and non toxic natural product.

Cite this article as:

Kalani Komal, Chaturvedi Vinita, Alam Sarfaraz, Khan Feroz and Srivastava Kumar Santosh, Anti-Tubercular Agents from Glycyrrhiza glabra, Current Topics in Medicinal Chemistry 2015; 15 (11) . https://dx.doi.org/10.2174/1568026615666150317223323