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Green tea polyphenols: novel and potent inhibitors of squalene epoxidase.

Abstract：

:The green tea gallocatechins, (-)-epigallocatechin-3-O-gallate (EGCG) (IC(50) = 0.69 microM), (-)-gallocatechin-3-O-gallate (GCG) (IC(50) = 0.67 microM), (-)-epicatechin-3-O-gallate (ECG) (IC(50) = 1.3 microM), and theasinensin A (IC(50) = 0.13 microM), were found to be potent and selective inhibitors of rat squalene epoxidase (SE), a rate-limiting enzyme of cholesterol biogenesis. On the other hand, flavan-3-ols without galloyl group at C-3 did not show significant enzyme inhibition. It was demonstrated for the first time that the cholesterol lowering effect of green tea may be attributed to their potent SE inhibition activities. Inhibition kinetics revealed that EGCG inhibited SE in noncompetitive (K(I) = 0.74 microM), and non-time-dependent manner. The potent enzyme inhibition would be caused by specific binding to the enzyme, and by scavenging reactive oxygen species required for the monooxygenase reaction.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Abe I,Seki T,Umehara K,Miyase T,Noguchi H,Sakakibara J,Ono T

doi

10.1006/bbrc.2000.2217

subject

Has Abstract

pub_date

2000-02-24 00:00:00

pages

767-71

issue

3

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(00)92217-4

journal_volume

268

pub_type

杂志文章

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