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Sesquiterpenoids from Atractylodes macrocephala act as farnesoid X receptor and progesterone receptor modulators
Chia-Jui Tsai1, Jui-Wei Liang, Hsiang-Ru Lin
1Department of Chemistry, College of Science, National Kaohsiung Normal University, Yanchao District, Kaohsiung City, Taiwan, ROC.
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.
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