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标题：Isoliquiritigenin, One of the Antispasmodic Principles of Glycyrrhiza Ularensis Roots, Acts in the Lower Part of Intestine
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作者：Yuji Sato ; Ju-Xiu He ; Hidemasa Nagai 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2007
卷号：30
期号：1
页码：145-149
DOI：10.1248/bpb.30.145
出版社：The Pharmaceutical Society of Japan
摘要：Glycyrrhizae Radix is used to treat abdominal pain as a component of Shakuyakukanzoto (Shaoyao-Gancao-tang), a traditional Chinese medicine formulation. Previously, we have reported the isolation of glycycoumarin as a potent antispasmodic with an IC₅₀ value of 2.93±0.94 μ M for carbamylcholine (CCh)-induced contraction of mouse jejunum from an aqueous extract of Glycyrrhizae Radix (licorice), and clarified that its mechanism of action involves inhibition of phosphodiesterase 3. The purpose of the present study was to examine an antispasmodic principle of licorice other than glycycoumarin. Isoliquiritigenin was isolated from an aqueous extract of licorice as a potent relaxant, which inhibited the contraction induced by various types of stimulants, such as CCh, KCl, and BaCl₂ with IC₅₀ values of 4.96±1.97 μ M , 4.03±1.34 μ M and 3.70±0.58 μ M , respectively, which are close to those of papaverine. However, the amount of isoliquiritigenin in the aqueous extract of licorice was very small. When the aqueous licorice extract was treated with naringinase, the amounts of glycosides such as isoliquiritin, which were abundant but had much less potent relaxant activity, were decreased while isoliquiritigenin was increased. At the time, the relaxant activity of the treated sample was increased significantly, shifting the IC₅₀ from 358±104 to 150±38 μg/ml for CCh-induced contraction. Isoliquiritigenin also showed the most potent inhibition of mouse rectal contraction induced by CCh with an IC₅₀ value of 1.70±0.07 μ M . These results suggest that isoliquiritigenin acts as a potent relaxant in the lower part of the intestine by transformation from its glycosides.
关键词：Shakuyakukanzoto;Glycyrrhiza uralensis;antispasmodic;isoliquiritigenin;naringinase;davidigenin