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Inhibition of constitutive endothelial NO-synthase activity by tannin and quercetin.

Abstract：

:The effect of natural polyphenols on three isoforms of NO-synthase was investigated. Among the compounds tested, tannin was the most potent, inhibiting endothelial constitutive NO synthase (eNOS) with an IC50 of 2.2 microM. Other NOS isoforms (i.e. neuronal constitutive NOS and smooth muscle inducible NOS) were also inhibited but at much higher concentrations (selectivity ratio of approx. 20-30). Quercetin was also an effective but less potent inhibitor of eNOS (IC50 = 220 microM). The kinetics of tannin inhibition were investigated to gather information on the mechanism of action. Tannin did not interfere with the interaction of the enzyme with the co-substrates L-arginine and NADPH nor with the cofactor tetrahydrobiopterin. The inhibition level was also independent of free Ca2+ concentration as well as of the presence of high exogenous calmodulin concentrations.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Chiesi M,Schwaller R

doi

10.1016/0006-2952(94)00433-m

subject

Has Abstract

pub_date

1995-02-14 00:00:00

pages

495-501

issue

4

eissn

0006-2952

issn

1873-2968

pii

0006-2952(94)00433-M

journal_volume

49

pub_type

杂志文章

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