Benznidazole and nifurtimox nitroreductase activity in liver microsomes from male rats preinduced with phenobarbital or 3-methylcholanthrene.

Abstract

Liver microsomes from Sprague-Dawley male rats are able to biotransform Benznidazole (Bz) or Nifurtimox (NFX) by nitroreduction. Pretreatment of the rats during three days with phenobarbital (80 mg/kg/day, ip) but not with 3-methylcholanthrene (35 mg/kg/day ip) increased both Bz and NFX nitroreductase activity. Results suggest that cytochrome P-450 but not cytochrome P-448 is involved in the nitroreduction of these two chemotherapeutic agents against Chagas' disease. Possible pharmacological and toxicological implications of these observations are discussed.

• Authors: E G Aguilar, C K de Arranz, E G de Toranzo, J A Castro
• Journal: Research communications in chemical pathology and pharmacology (Res Commun Chem Pathol Pharmacol) Vol. 50 Issue 3 Pg. 443-6 (Dec 1985) ISSN: 0034-5164 [Print] United States
• PMID: 3841223 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Nitrofurans
• Nitroimidazoles
• Methylcholanthrene
• Oxidoreductases
• Nitroreductases
• Nifurtimox
• benzonidazole
• Phenobarbital

Topics

• Animals
• Biotransformation
• Male
• Methylcholanthrene (pharmacology)
• Microsomes, Liver (drug effects, enzymology)
• Nifurtimox (metabolism)
• Nitrofurans (metabolism)
• Nitroimidazoles (metabolism)
• Nitroreductases
• Oxidation-Reduction
• Oxidoreductases (metabolism)
• Phenobarbital (pharmacology)
• Rats
• Rats, Inbred Strains