Sesquiterpenoids from Atractylodes macrocephala act as farnesoid X receptor and progesterone receptor modulators

被引：33

作者：

Tsai, Chia-Jui ^{[1
]}

Liang, Jui-Wei ^{[1
]}

Lin, Hsiang-Ru ^{[1
]}

机构：

[1] Natl Kaohsiung Normal Univ, Dept Chem, Coll Sci, Kaohsiung 82446, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 06期

关键词：

Atractylodes macrocephala (Asteraceae); Farnesoid X receptor; Progesterone receptor; SALT EXPORT PUMP; NUCLEAR RECEPTOR; BILE-ACID; MOLECULAR-BASIS; FXR; TRANSCRIPTION; CHOLESTEROL; GUGGULSTERONE; ANTAGONIST;

D O I：

10.1016/j.bmcl.2012.01.048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two sesquiterpenoids, atractylenolide II and III, were isolated and identified from Atractylodes macrocephala (Asteraceae) to be subsequently evaluated for their activity against farnesoid X receptor (FXR) and progesterone receptor (PR) by transient transfection reporter assays. These sesquiterpenoids did not exert significant agonistic effect but antagonized the activity of chenodeoxycholic acid (CDCA), an endogenous FXR agonist, for FXR driven SHP promoter transactivation. Additionally, they transactivated CYP7A1 gene promoter activity by antagonizing FXR. Apart from acting as a FXR antagonist, atractylenolide III also showed agonistic activity against PR. All these results demonstrated that atractylenolide II and III are the active components of Atractylodes macrocephala to exert specific pharmacologic effects. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：2326 / 2329

页数：4

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