cyp3a

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

Schisandrin A, a primary active component extracted from the traditional Eastern medicine Schisandra chinensis, inhibits CYP3A activity, with an IC50 of 6.60 μM and a Ki of 5.83 μM.

1. Dauricine has pulmonary toxicity, can produce pulmonary injury in CD-1 mice by the metabolism of Dauricine mediated by CYP3A. 2. Dauricinec can pass the blood-brain barrier, and that P-glycoprotein has an important role in the transportation of Dauricine across the blood-brain barrier. 3. Dauricine may has anti-tumor effect, can inhibit tumor cells in urinary system and colon cancer cell proliferation, invasion; induce cell apoptosis by suppressing NF-kappaB activity and the expression profile of its downstream genes.

6',7'-Dihydroxybergamottin is a potent inhibitor of CYP3A activity, and may be primarily responsible for the effects of grapefruit juice on cytochrome P450 activity in humans.

1β-Hydroxydeoxycholic acid (1β-OH-DCA), recognized as a secondary bile acid, serves as a biomarker for CYP3A. This compound is metabolized from deoxycholic acid specifically by CYP3A4 and CYP3A7 through recombinant human CYP450 enzymes [1].

1. Schisandrol B (Besigomsin) may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. 2. Schisandrol B has anti-inflammatory property, potentially result from the inhibition of COX-2, iNOS, IL-6, TNF-α and NO through the down-regulation of RIP2 and NF-κB activation. 3. Schisandrol B induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway. 4. Schisandrol B significantly inhibits cell proliferation in a dose-dependent manner, due to cell cycle arrest in the G1 phase with the downregulation of cyclin D1 expression and Retinoblastoma (RB) phosphorylation.

1,3,7-Trimethyluric acid, a purine alkaloid, occurs as a minor metabolite of caffeine in humans. It functions as an antioxidant with the ability to scavenge hydroxyl radicals and offers protective benefits against lipid peroxidation in erythrocyte membranes.

Acetylshikonin can effectively inhibit tumor cells, it can be used to treat hepatocellular carcinoma cells expressing hepatitis B virus X protein (HBX) by inducing ER stress , an oncoprotein from hepatitis B virus. Acetylshikonin inhibits the production of eicosanoid, is due to the attenuation of cytosolic phospholipase A(2) membrane recruitment via the decrease in [Ca(2+)](i) and to the blockade of cyclooxygenase and 5-lipoxygenase activity.