Lathyrane Diterpenoids as Novel hPXR Agonists: Isolation, Structural Modification, and Structure–Activity Relationships

Pregnane X receptor (PXR) that orchestrates the intricate network of xeno- and endobiotic metabolism is considered as a promising therapeutic target for cholestasis. In this study, the human PXR (hPXR) agonistic bioassay-guided isolation of Euphorbia lathyris followed by the structural modification led to the construction of a lathyrane diterpenoid library (1–34). Subsequent assay of this library led to the identification of a series of potent...