Gastric-mucous membrane protection activity of coptisine derivatives.
Coptisine and 8-oxocoptisine were isolated as principles of the gastric-mucous membrane protection from Coptidis rhizoma. The two compounds showed stronger activity than cimetidine and sucralfate. We prepared several derivatives having a partial structure of coptisine from commercially available starting materials. The compounds obtained were tested for gastric-mucous membrane protective activity and a correlation between activity and structure was studied. Our results suggest that the partial charge of the catechol skeleton is related to activity.
Hirano
H
H
Faculty of Pharmaceutical Sciences and High-Technology Research Center, Kobe-Gakuin University Hyogo, Japan.
Osawa
E
E
Yamaoka
Y
Y
Yokoi
T
T
D000818:Animals; D001599:Berberine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D000089042:Coptis chinensis; D004365:Drugs, Chinese Herbal / Q000138:chemical synthesis / Q000494:pharmacology; D000431:Ethanol / Q000633:toxicity; D005753:Gastric Mucosa / Q000187:drug effects* / Q000473:pathology; D008297:Male; D018517:Plant Roots / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship
D004365:Drugs, Chinese Herbal; C034384:coptisine; D001599:Berberine; D000431:Ethanol; C103789:8-oxoberberine; C107393:Coptidis rhizoma extract