Yoshikawa M, Hatakeyama S, Inoue Y, Yamahara J
Kyoto Pharmaceutical University, Japan.
Chem Pharm Bull (Tokyo). 1993 Jan;41(1):214-6. doi: 10.1248/cpb.41.214.
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"-O-beta-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 HCl/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 alpha-methylene gamma-lactone function to amino acid-sesquiterpene adduct has been accomplished by means of Michael type addition reaction.
从藏木香（Saussurea lappa CLARKE）干燥根的中药木香中分离出5种新的氨基酸-倍半萜加合物，即木香胺A、B、C、D和E，以及一种新的木脂素糖苷，(-)-马尾杉醇4″-O-β-D-吡喃葡萄糖苷。它们的结构是根据化学和物理化学证据确定的。在这些化合物中，木香胺A、B、C对大鼠盐酸/乙醇诱导的损伤具有抗溃疡作用，木香胺A对小鼠应激性溃疡形成也具有抑制活性。在这些研究过程中，通过迈克尔型加成反应实现了具有α-亚甲基γ-内酯功能的倍半萜向氨基酸-倍半萜加合物的简便转化。
