Transferrin conjugates of antitubercular drug isoniazid: Synthesis and in vitro efficacy

Sutar, Yogesh B and Mali, Jaishree K and Telvekar, Vikas N and Rajmani, Raju S and Singh, Amit (2019) Transferrin conjugates of antitubercular drug isoniazid: Synthesis and in vitro efficacy. In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 183 .

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Abstract

Tuberculosis (TB) caused by Mycobacterium tuberculosis (Mtb) has become the world's leading killer disease due to a single infectious agent which survives in the host macrophage for the indefinite period. Hence, it is necessary to enhance the efficacy of the clinically existing antitubercular agents or to discover new anti antitubercular agents. Here, we report the synthesis, characterization and antimycobacterial evaluation of protein-drug conjugates. A carrier protein, Transferrin (Tf) was covalently conjugated to isoniazid (INH) utilizing hydrazone and amide linkers. The purity of the reactions was confirmed by SDS-PAGE while conjugation was confirmed by UV-visible spectrophotometry, MALDI-TOF analysis, and FFIR spectrophotometry. The in vitro antitubercular assay result showed that the inhibitory activity of the parent drug was conserved in both the conjugates. The conjugates were effective against intracellular Mtb H37Rv and were devoid of cytotoxic effect at therapeutic concentration.

Item Type:	Journal Article
Publication:	EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Publisher:	ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Additional Information:	Copyright of this article belongs to ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Keywords:	Transferrin; Isoniazid; Conjugates; Mycobacterium tuberculosis; H37Rv
Department/Centre:	Division of Biological Sciences > Microbiology & Cell Biology
Date Deposited:	10 Jan 2020 10:01
Last Modified:	10 Jan 2020 10:01
URI:	http://eprints.iisc.ac.in/id/eprint/64095

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