Table 1.
Table enlisting the documented effect of various natural occurring ligands of pregnane X Receptor
| No | Natural ligand and source | Effective response after binding of ligands with PXR | Ref. |
| 1 | Baicalein from roots of Scutellaria baicalensis Georgi | Attenuated colonic inflammation in DSS induced colitis mice model through stimulation of CDX2. ↓TNFα and IL-6 mRNA levels in intestinal mucosa | Dou et al[122] Plos One 2012 |
| 2 | Forskolin and 1,9 dideoxyforskolin from roots of Coleus forskohlii | ↑CYP3A expression in primary hepatocytes through activation of Protein Kinase A signaling pathway | Ding and Staudinger[151] J Pharmacol Exp Ther 2005 |
| 3 | Z-guggulsterone from Commiphora mukul (Guggul) | ↓CYP7A1 gene in HepG2 cells | Owsley and Chiang[152] Biochem Biophys Res Commun 2003 |
| 4 | E-guggulsterone from Commiphora mukul (Guggul) | ↑CYP3A11 and CYP3A4 mRNA levels only in cultured hepatocytes from PXR +/+ mice and not in PXR KO mice | Brobst et al[153] J Pharmacol Exp Ther 2004 |
| 5 | Hyperforin from Hypericum perforatum (St. John’s wort) | ↑CYP3A4 induction in hepatocytes. Induction of CYP2C9 gene expression was also reported in humans | Moore et al[154] Proc Natl Acad Sci USA 2000 |
| 6 | Colupulone from Humulus lupulus (Hop Extract) | ↑CYP3A4, CYP2B6 and MDR1 gene expression in primary human hepatocytes dose dependently | Teotico et al[155] Mol Pharmacol 2008 |
| 7 | Kava Kava (Piper methysticum) | ↑CYP3A4 mRNA expression in primary human hepatocytes extensively | Raucy[156] Drug Metab Dispos 2003 |
| 8 | Wu Wei Zi [Dibenzocyclooctene lignans: schisandrol B, schisandrin (A and B)] | ↑Transcription of CYP3A4, CYP2C9 and MRP2 genes in primary hepatocytes | Mu et al[157] J Pharmacol Exp Ther 2006 |
| 9 | Ginkgolide A from Gingko Biloba extract | Protection against CCL4 induced acute toxicity model in rats, ↑Iκ-Bα transcription, which in turn inhibited NF-κB | Ye et al[64] Biomol Ther (Seoul) 2016 |
| 10 | Ginkgolide 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 TNFα | Zhou et al[158] Acta Pharmacol Sin 2016 |
↑: Upregulation; ↓: Downregulation; PXR: Pregnane X receptor.