Article ID Journal Published Year Pages File Type
1371706 Bioorganic & Medicinal Chemistry Letters 2012 4 Pages PDF
Abstract

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.

Graphical abstractAtractylenolide II and III isolated from Atractylodes macrocephala were demonstrated to behave as farnesoid X receptor antagonists. Additionally, atractylenolide III also acted as a progesterone receptor agonist.Figure optionsDownload full-size imageDownload as PowerPoint slide

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