garcinoic acid

Garcinoic acid is a naturally occurring plant-derived derivative of δ-tocotrienol (a member of the vitamin E family), most notably isolated from Garcinia kola seeds. It is a small molecule best characterized as a selective and efficient agonist of the pregnane X receptor (PXR), a nuclear receptor involved in regulation of xenobiotic, drug metabolism, and inflammation. Garcinoic acid displays distinct pharmacology from other vitamin E analogs, showing specific PXR activation, anti-inflammatory, anti-oxidant, anti-angiogenic effects, and notable activities on nuclear receptors and cell transporters. Mechanistic studies highlight its activity in the reduction of β-amyloid aggregation and deposition in preclinical models of Alzheimer's disease, and as an inhibitor of IL-1β-induced microsomal prostaglandin E2 synthase-1 (mPGES-1) in vitro. Because of its specific, high-affinity engagement of human PXR, garcinoic acid is considered a lead compound for further development of PXR-regulating drugs for immune, inflammatory, and neurodegenerative diseases[1][3][4][5][7][8][9].

Other names

garcinolic acidtrans-delta-tocotrienoloic acidtocotrienoloic acidtrans-(SH)(2E,6E,10E)-13-[(2R)-6-hydroxy-2,8-dimethyl-3,4-dihydrochromen-2-yl]-2,6,10-trimethyltrideca-2,6,10-trienoic aciddelta-garcinoic acidδ-T3-13'COOH