cytochrome p450

Cytochrome P450 is a family of monooxygenases that use hydrogen peroxide as a co-substrate to catalyze the conversion of fatty acids into terminal olefins. As a membrane-bound hemoprotein, Cytochrome P450 plays a crucial role in drug detoxification, cellular metabolism, and maintaining homeostasis.

Naringin (Naringoside), a flavanone glycoside, exerts various of pharmacological effects such as blood lipid lowering, antioxidant activity, anticancer activity, and inhibition of cytochrome P450 enzymes.

Methoxsalen (NCI-C55903) is a Photoactivated Radical Generator and Psoralen. The mechanism of action of methoxsalen is as a Photoabsorption. The physiologic effect of methoxsalen is by means of Photosensitizing Activity.

Diosmetin (Luteolin 4-methyl ether) has been found to act as a weak TrkB receptor agonist.

Bergapten (5-Methoxypsoralen), a psoralen, inhibits cell replication.

Apigenin (NSC 83244) is an aromatic oil extracted from the flowers or leaves of the daisy-like plants. Extracts, oils and teas made from chamomile are used for its soothing qualities as a sedative, mild analgesic and sleep medication. Apigenin has not been implicated in causing serum enzyme elevations or clinically apparent liver injury.

Gentiopicroside (Gentiopicrin), a naturally occurring iridoid glycoside, extracted from Gentiana manshurica Kitag, inhibits P450 activity, with an IC50 and a Ki of 61 μM and 22.8 μM for CYP2A6; has antianti-inflammatoryand antioxidative effects.

Phloracetophenone (1-(2,4,6-Trihydroxyphenyl)ethanone) has antiobesity and hypolipidemic effects, may be partly mediated by delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.

Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.

Tetrahydrocurcumin (HZIV 81-2), a major metabolite of curcumin, has strong antioxidant and cardioprotective properties.

2,6-Dimethylquinoline is a natural product extracted from the roots of Peucedantu praeruptorum. 2,6-Dimethylquinoline is an inhibitor of CYP1A2 and CYP2B6 with an IC50 of 3.3 and 480 µM, respectively.

Ginsenoside C-K (Ginsenoside K) is a bacterial metabolite of G-Rb1 exhibiting anti-inflammatory effects by reducing iNOS and COX-2.

Cedrol is a cedrane sesquiterpenoid and a tertiary alcohol,Cedrol inhibits the cytochrome P450 (CYP) isoforms CYP2B6 and CYP3A4 (Kis = 0.9 and 3.4 μM, respectively)

Tetrahydropiperine (Cosmoperine) is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.

Quinidine is a stereoisomer of the antimalarial agent quinine and a class Ia antiarrhythmic agent. for the treatment of abnormal heart rhythms and also malaria.

7-Ethoxycoumarin, a typical human P450 substrate, is catalyzed by both wild-type and mutant forms of CYP102A1.

α-Terpinyl acetate is a natural compound found in several essential oils, is a flavouring agent.

Quinidine sulfate dihydrate (Pitayine Sodium) is a potent and selective cytochrome P450db inhibitor

Piperonylic acid (2H-1,3-benzodioxole-5-carboxylic acid) is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic acid selectively inactivate the CYP73A P450 subpopulation.

ε-Viniferin (epsilon-Viniferin) a dimer of resveratrol, shows the inhibitory effects of epsilon-viniferin on human CYP1A1, CYP1A2, CYP1B1, CYP2A6, CYP2B6, CYP2E1, CYP3A4 and CYP4A activities.

Isoasatone A, a natural product isolated from the plant [Heterotropa takaoi M.], exhibits anti-insect activity.

Phillyrin (Forsythin) is a novel AMPK activator, has anti-obesity effects in nutritive obesity mice, it can prevent lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation. Phillyrin(Forsythin) may be a new preventive agent of acute lung injury in the clinical setting, it potentially contributes to the suppression of the activation of MAPK and NF-κB pathways, it also has protective effects on H2O2-induced oxidative stress and apoptosis in PC12 cells.

Ginsenoside Rd (Gypenoside VIII) may have properties that inhibit or prevent the growth of tumors.

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.