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

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Fifteen new N-containing maltooligosaccharides were obtained using the chemoenzymatic method. Among these compounds, maltooligosaccharides having 6-amino-6-deoxy-D-sorbitol residue, (3R,4R,5R,6S)-hexahydro-3,4,5,6-tetrahydroxy-1H-azepine residue, and (3R,5R)-3,4,5-trihydroxypiperidine residue at the reducing end showed strong inhibitory activities for human pancreatic alpha-amylase (HPA) (EC 3.2.1.1) and human salivary alpha-amylase (HSA). The administration of (3R,4R,5R,6S)-hexahydro-3,5,6-trihydroxy-1H-azepine-4-yl O-alpha-D-glucopyranosyl-(1-->4)-alpha-D-glucopyranoside (13, IC50 = 4.3 x 10(-5) M for HPA, IC50 = 8.2 x 10(-5) M for HSA) and (3R,5R)-3,5-dihydroxypiperidine-4-yl O-alpha-D-glucopyranosyl-(1-->4)-alpha-D-glucopyranoside (18, IC50 = 3.4 x 10(-5) M for HPA, IC50 = 4.6 x 10(-5) M for HSA) to ICR mice suppressed postprandial hyperglycemia.

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