Protective effects of polygodial and related compounds on ethanol-induced gastric mucosal lesions in rats: Structural requirements and mode of action

被引：56

作者：

Matsuda, H ^{[1
]}

Pongpiriyadacha, Y ^{[1
]}

Morikawa, T ^{[1
]}

Kashima, Y ^{[1
]}

Nakano, K ^{[1
]}

Yoshikawa, M ^{[1
]}

机构：

[1] Kyoto Pharmaceut Univ, Yamashina Ku, Kyoto 6078412, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(01)00781-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The methanolic extract from the leaves of Tasmannia lanceolata was found to potently inhibit ethanol-induced gastric lesions in rats. Through bioassay-guided separation, three known sesquiterpenes, polygodial, polygodial 12alpha-acetal, and polygodial 12beta-acetal, and a new sesquiterpene. methyl isodrimeninol, were isolated as the active constituents. Among them, polygodial showed very potent gastroprotective effects (ED50=0.028 mg/kg, po). From the gastroprotective effects of various reduction and oxidation derivatives of polygodial, the dialdehyde or diacetal structure was found to be essential for the strong activity. Since the gastroprotection of polygodial was attenuated by pretreatment with indomethacin, N-ethylmaleimide, N-G-nitro-L-arginine methyl ester and ruthenium red, endogenous prostaglandins, sulfhydryl compounds, nitric oxide and vanilloid receptors may be involved in the protective activity. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：477 / 482

页数：6

共 47 条

[1] RUTHENIUM RED AS A CAPSAICIN ANTAGONIST [J].