Open AccessRadiation-induced PEGylated Ethambutol Has Low Antimycobacterial Activity in Vitro
Author(s) -
Maykel GonzálezTorres,
Silvia Guzmán-Beltrán,
Marco A. Mata-Gómez,
Gerardo LeyvaGómez,
Cristina Velasquillo,
Joaquı́n Zúñiga,
Susana Vargas,
Hernán Cortés,
Rogelio Rodríguez-Talavera
Publication year - 2020
Publication title -
biointerface research in applied chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.216
H-Index - 11
ISSN - 2069-5837
DOI - 10.33263/briac112.88848894
Subject(s) - ethambutol , antimycobacterial , polyethylene glycol , chemistry , peg ratio , in vitro , mycobacterium tuberculosis , pharmacology , polymerization , tuberculosis , medicine , biochemistry , organic chemistry , pathology , finance , economics , polymer
Tuberculosis is an airborne disease caused by Mycobacterium tuberculosis and remains one of the leading causes of death worldwide. The rise in multidrug-resistant strains has prompted the search for novel strategies to produce tuberculostatic agents. This research is aimed at developing a derivative of ethambutol by gamma radiation-induced polymerization with polyethylene glycol (PEG). The synthesis was verified by Raman spectroscopy and UV–Vis spectrometry. The results show that PEG can be chemically bonded to ethambutol by amine and alcohol groups. In in vitro biological evaluation, PEGylated and neat ethambutol showed similar cell viabilities, while the modified drug lowered bacterial growth inhibitory activity. A mechanism for the polymerization is proposed. The particle size increased for PEGylated drugs concerning the starting polyether. Despite the low antimycobacterial activity in vitro, the product seems to be a promising tool for the rapid screening of hydrolase activity.