Discovery that theonellasterol a marine sponge sterol is a highly selective FXR antagonist that protects against liver injury in cholestasis

• Main Authors: Renga B., Mencarelli A., D'Amore C., Cipriani S., D'Auria M.V., Sepe V., Chini M.G., Monti M.C., Bifulco G., Zampella A., Fiorucci S.
• Other Authors: NUSHS PROJECT
• Format: Article
• Published: 2019
• Subjects: alanine aminotransferase; bile acid; estrogen receptor; glucocorticoid receptor; liver protective agent; multidrug resistance protein 4; peroxisome proliferator activated receptor; progesterone receptor; protein LXR; protein PXR; receptor protein; theonellasterol; thyroid receptor; unclassified drug; vitamin D receptor; 7 hydroxytheonellasterol; 7-hydroxytheonellasterol; cell receptor; farnesoid X receptor; farnesoid X-activated receptor; hormone antagonist; sterol; alanine aminotransferase blood level; animal experiment; animal model; article; bioassay; BSEP gene; cell strain HepG2; controlled study; drug effect; drug isolation; drug mechanism; drug receptor binding; drug structure; extrahepatic bile duct obstruction; histopathology; in vivo study; liver cell; liver histology; liver injury; liver necrosis; liver protection; microarray analysis; molecular docking; mouse; multidrug resistance associated protein 4 gene; nonhuman; OSTalpha gene; protein expression; regulator gene; SHP gene; transactivation; animal; aquatic species; cell protection; chemistry; disease model; drug antagonism; drug development; drug screening; enzyme specificity; feasibility study; human; injury; intrahepatic cholestasis; isolation and purification; liver; pathology; sponge (Porifera); Mus; Rodentia; Theonella swinhoei; Animals; Aquatic Organisms; Cholestasis, Intrahepatic; Cytoprotection; Disease Models, Animal; Drug Discovery; Drug Evaluation, Preclinical; Feasibility Studies; Hep G2 Cells; Hormone Antagonists; Humans; Liver; Mice; Porifera; Receptors, Cytoplasmic and Nuclear; Sterols; Substrate Specificity
• Online Access: https://scholarbank.nus.edu.sg/handle/10635/162005
• Institution: National University of Singapore

10.1371/journal.pone.0030443