Studies on toxicity of antitubercular drugs namely isoniazid, rifampicin, and pyrazinamide in an in vitro model of HepG2 cell line

Medicinal Chemistry Research
2011.0

Abstract

Antitubercular drugs (ATT) are known to be majorly metabolized and detoxified in liver by both Phase I and Phase II group of drug metabolizing enzymes. These drugs as well as their metabolites are toxic and during this process cause injury to liver. In this study, we have investigated the in vitro hepatotoxic potential of both individual as well as combination ATT drugs using an in vitro model of human hepatocellular carcinoma cell line (HepG2). The cells were treated with varied concentrations of ATT drugs namely isoniazid (INH), rifampicin (RIF), and pyrazinamide (PYZ) for different durations. Cytotoxicity assay using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyltetrazoliumbromide) as well as morphological analysis using phase contrast microscopy have shown that concentrations used were not cytotoxic. However, pretreatment with sub-cytotoxic concentrations of INH and PYZ increased the toxicity with the same drugs. This report corroborates the clinical finding that long-term treatment as well combination drug therapy with ATT induces hepatotoxicity rather than individual drugs.

Knowledge Graph

Similar Paper

Studies on toxicity of antitubercular drugs namely isoniazid, rifampicin, and pyrazinamide in an in vitro model of HepG2 cell line
Medicinal Chemistry Research 2011.0
Occurrence of erythro-docosasphinga-4,8-dienine, as an ester, in anemonia sulcata.
Tetrahedron Letters 1986.0
New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity
European Journal of Medicinal Chemistry 2018.0
Protective effects of the bioactive natural product N-trans-Caffeoyldopamine on hepatotoxicity induced by isoniazid and rifampicin
Bioorganic & Medicinal Chemistry Letters 2015.0
Design, synthesis and in vitro anti-mycobacterial evaluation of gatifloxacin-1H-1,2,3-triazole-isatin hybrids
Bioorganic & Medicinal Chemistry Letters 2017.0
Preparation and antitubercular activities in vitro and in vivo of novel Schiff bases of isoniazid
European Journal of Medicinal Chemistry 2009.0
Novel 1,2,3-Triazole Derivatives for Use against Mycobacterium tuberculosis H37Rv (ATCC 27294) Strain
Journal of Medicinal Chemistry 2011.0
Azide-alkyne cycloaddition towards 1H-1,2,3-triazole-tethered gatifloxacin and isatin conjugates: Design, synthesis and in vitro anti-mycobacterial evaluation
European Journal of Medicinal Chemistry 2017.0
Transferrin conjugates of antitubercular drug isoniazid: Synthesis and in vitro efficacy
European Journal of Medicinal Chemistry 2019.0
Novel isoniazid embedded triazole derivatives: Synthesis, antitubercular and antimicrobial activity evaluation
Bioorganic & Medicinal Chemistry Letters 2020.0