It is known that procyanidins, which are contained in grape seeds, are antioxidative and have certain biological effects. Antiulcer activities of grape seed extracts (GSE-I and GSE-II) and procyanidins were investigated using rats. GSE-I (with low flavanol content), GSE-II (with high flavanol content), and procyanidins at a dose of 200 mg/kg strongly inhibited the stomach mucosal injury induced by 60% ethanol containing 150 mM hydrochloride. This suppressive effect seems dependent on the content of procyanidin oligomers. Procyanidin oligomers (dimers to hexamers) were prepared and studied for their antiulcer activities at a dose of 200 mg/kg. The gastric protective activity of a series of procyanidins increased with the increasing polymerization of catechin units. Oligomers longer than tetramers showed a strong protective effect against gastric mucosal damage. The binding ability of procyanidin oligomers to bovine serum albumin in the acidified solution was strengthened with the increase of molecules. The mechanism of antiulcer activity may be the protection by radical scavenging activity on the stomach surface against radical injury induced by HCl/EtOH solution and the defense action of procyanidins covering the stomach surface by their strong ability to bind protein. Keywords: Grape seed extract; antiulcer activity; procyanidin; oligomer; radical scavenging activity; HCl/EtOH-induced ulcer
The effect of a single oral administration of proanthocyanidins, oligomeric and polymeric polyhydroxyflavan-3-ol units, on the antioxidative potential of blood plasma was studied in rats. Proanthocyanidin-rich extract from grape seeds was administered by intragastric intubation to fasted rats at 250 mg/kg of body weight. The plasma obtained from water- or proanthocyanidin-administered rats was oxidized by incubation with copper sulfate or 2, 2'-azobis(2-amidinopropane) dihydrochloride (AAPH) at 37 degrees C, and the formation of cholesteryl ester hydroperoxides (CE-OOH) was followed. The plasma obtained from proanthocyanidin-administered rats was significantly more resistant against both copper ion-induced and AAPH-induced formation of CE-OOH than that from control rats. The lag phase in the copper ion-induced oxidation of rat plasma was remarkably increased at 15 min after administration of proanthocyanidins and reached a maximum level at 30 min. When the plasma from proanthocyanidin-administered rat was hydrolyzed by sulfatase and beta-glucuronidase following analysis by high-performance liquid chromatography with electrochemical detection, metabolites of proanthocyanidins occurred in rat plasma at 15 min after administration, three peaks of which were identified as gallic acid, (+)-catechin, and (-)-epicatechin. These results suggest that the intake of proanthocyanidins, the major polyphenols in red wine, increases the resistance of blood plasma against oxidative stress and may contribute to physiological functions of plant food including wine through their in vivo antioxidative ability.
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