Review
Copyright ©The Author(s) 2017.
World J Hepatol. Nov 18, 2017; 9(32): 1210-1226
Published online Nov 18, 2017. doi: 10.4254/wjh.v9.i32.1210
Table 1 Table enlisting the documented effect of various natural occurring ligands of pregnane X Receptor
NoNatural ligand and sourceEffective response after binding of ligands with PXRRef.
1Baicalein from roots of Scutellaria baicalensis GeorgiAttenuated colonic inflammation in DSS induced colitis mice model through stimulation of CDX2. ↓TNFα and IL-6 mRNA levels in intestinal mucosaDou et al[122] Plos One 2012
2Forskolin and 1,9 dideoxyforskolin from roots of Coleus forskohlii↑CYP3A expression in primary hepatocytes through activation of Protein Kinase A signaling pathwayDing and Staudinger[151] J Pharmacol Exp Ther 2005
3Z-guggulsterone from Commiphora mukul (Guggul)CYP7A1 gene in HepG2 cellsOwsley and Chiang[152] Biochem Biophys Res Commun 2003
4E-guggulsterone from Commiphora mukul (Guggul)↑CYP3A11 and CYP3A4 mRNA levels only in cultured hepatocytes from PXR +/+ mice and not in PXR KO miceBrobst et al[153] J Pharmacol Exp Ther 2004
5Hyperforin from Hypericum perforatum (St. John’s wort)↑CYP3A4 induction in hepatocytes. Induction of CYP2C9 gene expression was also reported in humansMoore et al[154] Proc Natl Acad Sci USA 2000
6Colupulone from Humulus lupulus (Hop Extract)CYP3A4, CYP2B6 and MDR1 gene expression in primary human hepatocytes dose dependentlyTeotico et al[155] Mol Pharmacol 2008
7Kava Kava (Piper methysticum)↑CYP3A4 mRNA expression in primary human hepatocytes extensivelyRaucy[156] Drug Metab Dispos 2003
8Wu Wei Zi [Dibenzocyclooctene lignans: schisandrol B, schisandrin (A and B)]↑Transcription of CYP3A4, CYP2C9 and MRP2 genes in primary hepatocytesMu et al[157] J Pharmacol Exp Ther 2006
9Ginkgolide A from Gingko Biloba extractProtection against CCL4 induced acute toxicity model in rats, ↑Iκ-Bα transcription, which in turn inhibited NF-κBYe et al[64] Biomol Ther (Seoul) 2016
10Ginkgolide B from Gingko Biloba extract↑Nuclear translocation of PXR, and protected HUVEC cells from drug induced apoptosis. Anti-inflammatory role by reducing VCAM-1 and E-selectin induced by TNFαZhou et al[158] Acta Pharmacol Sin 2016