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 language | English (US) |
|---|---|
| Pages (from-to) | 58-64 |
| Number of pages | 7 |
| Journal | Pharmacology |
| Volume | 27 |
| Issue number | 1 |
| DOIs | |
| State | Published - 1983 |
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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 journal › Article
}
TY - JOUR
T1 - Enzymatic reduction of chloramphenicol and nitrosochloramphenicol by rat liver microsomal preparations
AU - Lim, Lori O.
AU - Yunis, Adel A
PY - 1983
Y1 - 1983
N2 - 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.
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.
KW - Chloramphenicol
KW - Enzymatic reduction
KW - Nitrosochloramphenicol
KW - Rat liver microsomes
UR - http://www.scopus.com/inward/record.url?scp=0020565934&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0020565934&partnerID=8YFLogxK
U2 - 10.1159/000137830
DO - 10.1159/000137830
M3 - Article
C2 - 6611649
AN - SCOPUS:0020565934
VL - 27
SP - 58
EP - 64
JO - Pharmacology
JF - Pharmacology
SN - 0031-7012
IS - 1
ER -