cyp450

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.

Danshensu sodium salt (Sodium Danshensu) is sodium salt of danshensu from the widely used Chinese herb Danshen. It can inhibited phenylephrine- and CaCl2-induced vasoconstriction in Ca2+-free medium.

(E)-Flavokawain A, a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.

N-Acetyl-L-aspartic acid is a derivative of aspartic acid, synthesized in neurons from the amino acid aspartic acid and acetyl coenzyme A. N-Acetyl-L-aspartic acid has antioxidant activity.

Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a/CD18 adhesion molecules. It is commonly used to induce uremia models.

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

Erucin （1-isothiocyanato-4-methylsulfanylbutane） is a dietary isothiocyanate produced by enzymatic hydrolysis of glucoErucin with potential cancer preventive effects, involved in apoptosis and cell cycle blockade through PARP-1 cleavage, p53 and p21，Cyp450, quinone reductase (QR), glutatione transferase (GST) and other pathways.

1. Humantenmine is a toxic compound isolated from Gelsemium elegans Benth . 2. Humantenmine and koumine may inhibit several CYP450 enzyme activities.

Curcumenol ((+)-Curcumenol), one of the major components of Zedoary turmeric oil, is an antibiotic drug which has anti-Y, anti-inflammation activity. Curcumenol may be safely used without inducing metabolic drug-drug interaction through P450 inhibition.

Polygalaxanthone III can significantly inhibit chlorzoxazone 6-hydroxylation catalyzed by CYP2E1.

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

1. Acetylshikonin exhibits weak cytotoxicity against human umbilical vein endothelial cells (HUVECs) with IC5 of over 2 microM, exhibits the antiangiogenic and antitumorigenic effects by suppressing proliferation and angiogenic factors. 2. Acetylshikonin inhibits the generation of NADPH oxidase complex in the activation of respiratory burst of PMNs, but does not directly inhibit the activity of NADPH oxidase already generated. 3. Certain shikonin derivatives(such as Acetylshikonin) act as modulators of the Nur77-mediated apoptotic pathway and identify a new shikonin-based lead that targets Nur77 for apoptosis induction. 4. Acetylshikonin, shikonin, and alkannin have accelerative effect on the proliferation of granulation tissue in rats. 5. Acetylshikonin has inhibitory effect on the edematous response is due neither to the release of steroid hormones from the adrenal gland nor to the glucocorticoid activity, but probably partly to the suppression of mast cell degranulation and partly to protection of the vasculature from mediator challenge. 6. Acetylshikonin induces apoptosis of hepatitis B virus X protein-expressing human hepatocellular carcinoma cells via endoplasmic reticulum stress.

3',4',7,8-Tetramethoxyflavone exhibits inhibitory activity against multiple CYP450 1A2 2C9 2C19 enzymes and can inhibit lipid peroxidation in rat liver microsomes.

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].