Inhibition of xanthine oxidase by catechins from tea (Camellia sinensis).
Some epidemiological studies have associated tea drinking with several health benefits, while other such studies have been inconclusive. The liver enzyme, xanthine oxidase (XO) produces uric acid and reactive oxygen species (ROS) during the catabolism of purines. Excess of the former can lead to gout and of the latter to increased oxidative stress, mutagenesis and possibly cancer. Polyphenols are antioxidants, and it has been suggested that they can reduce oxidative stress by their antioxidant properties. We report here on the inhibition of XO by five tea catechins and two flavones. The Ki values (microM) and types of inhibition were catechin (C) (Ki = 303.95, uncompetitive), epicatechin (EC) (Ki = 20.48, mixed), epigallocatechin (EGC) (Ki = 10.66, mixed), epicatechin gallate (ECg) (Ki = 2.86, mixed) and epigallocatechin gallate (EGCg) (Ki = 0.76, competitive). The Ki of EGCg was similar to that of allopurinol (Ki = 0.30, mixed), the drug of choice for inhibition of XO in gout patients. Thus, tea catechins may act at.an earlier stage than has previously been suspected, by inhibiting ROS production, rather than only neutralizing the already formed ROS. This suggests a new mechanism whereby tea drinking may prevent oxidative stress related diseases, e.g. atherosclerosis and cancer.
Aucamp
J
J
Department of biochemistry, University of Pretoria, South Africa.
Gaspar
A
A
Hara
Y
Y
Apostolides
Z
Z
D000970:Antineoplastic Agents / Q000494:pharmacology; D002392:Catechin / Q000031:analogs & derivatives / Q000302:isolation & purification / Q000494:pharmacology*; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D016166:Free Radical Scavengers / Q000494:pharmacology; D007700:Kinetics; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013662:Tea; D014969:Xanthine Oxidase / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D005419:Flavonoids; D016166:Free Radical Scavengers; D013662:Tea; D002392:Catechin; C062669:epicatechin gallate; C045651:epigallocatechin gallate; D014969:Xanthine Oxidase; C057580:gallocatechol