Werner-FelmayerzvutsronmlkihgfedcbaUSPMIFCBA et al.: Tetrahydrobiopterin-dependent nitric oxide formation in vitro 53
Pleridines
Vol. 3, pp. 5 3 - 5 4
Short Communication
Tetrahydrobiopterin-Dependent Conversion of L-Arginine to L-Citrulline
and Nitric Oxide in Murine and Human Cells
1 )
G. Werner-Felmayer, E. R. Werner, G. Weiss and H. Wächter
2
'
Institut für Medizinische Chemie und Biochemie, Universität Innsbruck, Fritz-Pregl-Str. 3, A-6020 Innsbruck,
Austria
(Received March 1992)
Introduction
Nitric oxide (NO) synthase converts L-arginine to
NO and L-citrulline. Recent work characterizing this
enzyme shows that there exist at least two forms in
mammalian cells: a constitutive and Ca
2+
-dependent
form which is typically found in endothelium and
brain and a cytokine-induciblc, Ca
2+
-independent
form which can be found in macrophages but also a
variety of other cell types. NO stimulates guanylate
cyclase and thus mediates vasodilation and its effects
in neurotransmission. Via formation of iron nitrosyl
complexes NO inhibits aconitase and ribonucleotide
reductase, leading to cytotoxicity [for review on NO
synthase see (1)].
Both types of NO synthase require NADPH, flavins
and tetrahydrobiopterin as cofactors and it was shown
recently that FAD, FMN and tetrahydrobiopterin
copurify with the enzyme from porcine cerebellum (2,
see also Werner, E. R. et al., this volume).
Here we compare the effect of influencing intracellular
tetrahydrobiopterin levels on cytokine-induced NO
synthase from murine fibroblasts and on the consti-
tutive NO synthase from human endothelial cells.
lf
Support by the Austrian "Bundesministerium für Wissen-
schaft und Forschung, Sektion Forschung" is gratefully
acknowledged.
2)
Author to whom correspondence should be addressed.
Pteridines / Vol.3 / No. 1/2
Copyright © 1992 Walter de Gruyter • Berlin • New York
Material and Methods
Murine fibroblasts isolated from ear dermis of Balb/c
mice were cultured as described (3). Human endoth-
elial cells from umbilical vein were grown on gelatine-
coated surfaces in medium 199 supplemented with
20% (v/v) of heat-inactivated fetal calf serum, 2 mM
L-glutamine, 100 U/ml penicillin, 0.1 mg/ml strepto-
mycin, 50yxwvutsrponmlkihgfedcbaUTRPONMKIHGFDCBA g/ml endothelial cell growth supplement
(Boehringer, FRG), 50 g/ml insulin, 0.1 mg/ml trans-
ferrin and 0.5% (w/v) of bovine serum albumine. Cells
used for experiments were between passage 3 and 12.
In murine fibroblasts formation of NO was deter-
mined as the amount of nitrite accumulated in super-
natants after 48 to 72 hours of cytokine treatment (50
U/ml murine interferon-gamma in combination with
500 U/ml murine tumour necrosis factor-alpha). In
endothelial cells NO was measured via formation of
cGMP upon activation of constitutive NO synthase
by the Ca-ionophore A23187. For this purpose en-
dothelial cells grown in 6-well plates were treated for
15 min with 1 mM 3-isobutyl-l-methyl-xanthine in
10 mM Hepes, pH = 7.5, containing 145 mM NaCl,
5 mM KCl, 1 mM MgCl
2
and 2.5 mM CaCl
2
. The re-
action was started by addition of 1 Μ A23187. After
4 min the reaction mixture was removed and cGMP
levels of individual wells were determined after cell
lysis with 0.01 Ν HCl by radioimmunoassay (Amer-
sham, UK).
Tetrahydrobiopterin synthesis was inhibited by treat-
ment of cells with 5 mM 2,4-diamino-6-hydroxy-py-
rimidine (DAHP) for 24 hours in endothelial cells and
for the period of cytokine induction in murine fibro-
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