pxr

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as cholagogue and choleretic.

Lynestrenol is a synthetic progestational hormone, is the progesterone receptor agonist

7α-Hydroxy-4-cholesten-3-one is an intermediate in bile acid synthesis from cholesterol, a PXR agonist, and a biomarker for bile acid loss and diseases related to defective bile acid biosynthesis. It is also the physiological substrate for [CYP8B1].

Helicid (Helicide) is a medicine available in a number of countries worldwide.

BYAKANGELICIN,a main furanocoumarin constituent isolated and characterized as an aldose reductase inhibitor,and is effective for the treatment of sugar cataracts and diabetic neuropathy and hence might be useful as a lead compound for the development of new type drugs for clinical use.

Isopteropodine (Uncarine E) is an isoyohimbine-type octindole alkaloid isolated from Hamelia patens micropropagated and has antimicrobial activity and stimulates the immune system. Isopteropodine has antimicrobial activity and stimulates the immune system.Isopteropodine is a positive modulator of muscarinic M1 and 5-HT2 receptors and a PXR activator that induces contraction of the rat myometrium.

1. Desmethoxyyangonin (5,6-Dehydrokavain) protects LPS or LPS D-GalN-induced damages in cell or liver tissues mainly through de-regulating IKK NFκB and Jak2 STAT3 signaling pathways. 2. The induction of CYP3A23 by dihydromethysticin and Desmethoxy yangonin involves transcription activation, probably through a PXR-independent or PXR-involved indirect mechanism.

Isosilybin (Isosilibinin) and Silybin might be suitable candidates to design potent PXR antagonists to prevent drug-drug interactions via CYP3A4 in cancer patients.