INHIBITION OF MURINE MACROPHAGE NITRIC-OXIDE SYNTHASE EXPRESSION BY APIVOXIL PRODRUG OF ANTIVIRAL ACYCLIC NUCLEOTIDE ANALOG 9-(2-PHOSPHONOMETHOXYETHYL)ADENINE

Authors
ZIDEK Z FRANKOVA D HOLY A BOUBELIK M DRABER P
Citation
Z. Zidek et al., INHIBITION OF MURINE MACROPHAGE NITRIC-OXIDE SYNTHASE EXPRESSION BY APIVOXIL PRODRUG OF ANTIVIRAL ACYCLIC NUCLEOTIDE ANALOG 9-(2-PHOSPHONOMETHOXYETHYL)ADENINE, Biochemical pharmacology, 54(8), 1997, pp. 855-861
Citations number
36
Categorie Soggetti
Pharmacology & Pharmacy",Biology
Journal title
Biochemical pharmacology → ACNP
ISSN journal
00062952
Volume
54
Issue
8
Year of publication
1997
Pages
855 - 861
Database
ISI
SICI code
0006-2952(1997)54:8<855:IOMMNS>2.0.ZU;2-O
Abstract
The effect of the acyclic nucleotide analogue, 9-(2-phosphonomethoxyet hyl)adenine (PMEA, Adefovir), and its (bis)pivaloyloxymethyl ester (bi s-POM-PMEA, Adefovir Dipivoxil) on in vitro nitric oxide (NO) producti on by murine peritoneal macrophages was investigated. Bis-POM-PMEA inh ibited in a concentration-dependent manner the formation of NO generat ed by interferon-gamma and lipopolysaccharide, the IC50 being 15 mu M. Suppressed transcription of mRNA for inducible NO synthase (EC 1.14.1 3.39) resulting in decreased synthesis of NO synthase protein was foun d. Parent compound PMEA was virtually ineffective. (C) 1997 Elsevier S cience Inc.