Saussureamines A, B, C, D, and E, New Anti-Ulcer Principles from Chinese Saussureae Radix

Abstract

Five new amino acid-sesquiterpene adducts, saussureamines A, B, C, D, and E, were isolated from Chinese Saussureae Radix, the dried root of Saussurea lappa clarke, together with a new lignan glycoside, (-)-massoniresinol 4”β-D-glucopyranoside. Their structures were determined on the basis of chemical and physicochemical evidence. Among of these compounds, saussureamines A, B, C showed anti-ulcer effect on HC1 / ethanol-induced lesions in rats, and saussureamine A also exhibited a inhibitory activity on stress-induced ulcer formation in mice. During the course of these studies, facile conversion from sesquiterpene having an a-methylene y-lactone function to amino acid-sesauiterpene adduct has been accomplished by means of Michael type addition reaction. © 1993, The Pharmaceutical Society of Japan. All rights reserved.