Triterpenes from Alisma orientalis act as farnesoid X receptor agonists

Alisol B 23-acetate protects against ANIT-induced hepatotoxity and cholestasis, due to FXR-mediated regulation of transporters and enzymes involved in bile acid homeostasis

“…Since Cyp7a1, Cyp8b1 and genes including Bsep, Mrp2 and Ntcp involved in regulating hepatic bile acid transport are downstream target genes of FXR, as well as the analogues of AB23A have been shown to be the FXR agonists recently (Lin, 2012), we hypothesized that AB23A may activate FXR to regulate expression level of genes in bile acid homeostasis. To verify this hypothesis, we blocked FXR by use of the FXR antagonist GS in mice.…”

“…Therefore, an important and intriguing question arises whether AB23A has hepatoprotective effect on cholestatic liver injury such as ANIT-induced intrahepatic cholestasis. It has been recently reported that analogues of AB23A are the agonists of farnesoid X receptor (FXR), which is a member of the nuclear receptor superfamily of ligand-activated transcription factors (Forman et al, 1995;Lin, 2012). In addition, FXR has been shown to play a critical role in ANIT-induced liver injury (Cui et al, 2009).…”

Beyond Bile Acids: Targeting Farnesoid X Receptor (FXR) with Natural and Synthetic Ligands

“…Alisma orientalis is used in Chinese and Japanese herbal traditional medicine to treat kidney stones, pelvic infections, nephritisabdominal bloating, diarrhea, diabetes and urinary diseases [46]. The chemical composition of this herb mainly includes prostane-type triterpenes like alisol M 23-acetate (11) and alisol A 23-acetate (12) (Fig.…”

Alisma orientalis (Sam.) Juzep. 泽泻 (Zexie, Alismatis Rhizoma)

“…The triterpenes, alisol M 23-acetate and alisol A 23-acetate, were isolated from A. orientalis and found against the Farnesoid X receptor (FXR), which is a member of nuclear receptor superfamily and viewed as one of the essential target proteins to develop antidiabetic treatments. A. orientalis might exert anti-hyperglycemic effect through the FXR pathway [11].…”