Enzymatic reduction of chloramphenicol and nitrosochloramphenicol by rat liver microsomal preparations

Lori O. Lim, Adel A Yunis

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Chloramphenicol (CAP) and nitrosochloramphenicol (NO-CAP) were metaboli-cally reduced to aromatic amines by rat liver microsomes in vitro. The reduction required anaerobic conditions and was mediated by a NADPH-dependent reductase system. Both CAP and NO-CAP reduction were time and concentration dependent. Compared to CAP, NO-CAP (0.5 mM) reduction was rapid with complete conversion occurring in 90–120 min. At 2.5 mM NO-CAP reduction was depressed. In the presence of NO-CAP (0.05–2.5 mM) CAP metabolism was inhibited from 17 to 91 %. These results indicate that CAP and NO-CAP are metabolized by similar microsomal reductase systems and NO-CAP is unstable, readily reduced further to the aromatic amine.

Original languageEnglish (US)
Pages (from-to)58-64
Number of pages7
JournalPharmacology
Volume27
Issue number1
DOIs
StatePublished - 1983

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Chloramphenicol
Liver
Amines
Oxidoreductases
Liver Microsomes
nitrosochloramphenicol
NADP

Keywords

  • Chloramphenicol
  • Enzymatic reduction
  • Nitrosochloramphenicol
  • Rat liver microsomes

ASJC Scopus subject areas

  • Pharmacology

Cite this

Enzymatic reduction of chloramphenicol and nitrosochloramphenicol by rat liver microsomal preparations. / Lim, Lori O.; Yunis, Adel A.

In: Pharmacology, Vol. 27, No. 1, 1983, p. 58-64.

Research output: Contribution to journalArticle

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AB - Chloramphenicol (CAP) and nitrosochloramphenicol (NO-CAP) were metaboli-cally reduced to aromatic amines by rat liver microsomes in vitro. The reduction required anaerobic conditions and was mediated by a NADPH-dependent reductase system. Both CAP and NO-CAP reduction were time and concentration dependent. Compared to CAP, NO-CAP (0.5 mM) reduction was rapid with complete conversion occurring in 90–120 min. At 2.5 mM NO-CAP reduction was depressed. In the presence of NO-CAP (0.05–2.5 mM) CAP metabolism was inhibited from 17 to 91 %. These results indicate that CAP and NO-CAP are metabolized by similar microsomal reductase systems and NO-CAP is unstable, readily reduced further to the aromatic amine.

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