From the methanolic extract of the dried roots of Saussurea lappa Clarke, Saussureae Radix, five amino acid–sesquiterpene conjugates, saussureamines A, B, C, D and E, were isolated together with a lignan glycoside, (−)-massoniresinol 4″-O-β-d-glucopyranoside. Their stereostructures were determined on the basis of chemical and physicochemical evidence. In addition, saussureamines and the related amino acid–sesquiterpene conjugates were synthesized using a Michael type addition reaction of amino acid to the α-methylene-γ-lactone moiety of sesquiterpenes. Saussureamines A, B and C, costunolide and dehydrocostus lactone showed a gastroprotective effect on acidified ethanol-induced gastric mucosal lesions in rats. Saussureamines A also exhibited an inhibitory effect on gastric mucosal lesions induced by water-immersion stress in mice.
Saussurea lappa, saussureamines, gastroprotective effect, (-)-massoniresinol glucoside
Publication DOI: 10.1016/S0040-4020(00)00696-7Journal NLM ID: 2984170RPublisher: Pergamon Press
Correspondence: Yoshikawa M
Institutions: Kyoto Pharmaceutical University, Kyoto, Japan
Found