CYP-450

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.

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide. It is the S-enantiomer of bupivacaine. Levobupivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Chirocaine. Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 per cent less potent (by molarity) than racemic bupivacaine.Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Adverse drug reactions (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic reactions can rarely occur.

(±)-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.

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

1-Aminobenzotriazole (ABT) (ABT) is a non-specific cytochrome P450 (CYP) inhibitor.

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a reversible neuronal sodium channel inhibitor and the pure S(-)-enantiomer of bupivacaine, used as a long-acting local anesthetic.

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

Liarozole (R75251 dihydrochloride) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.

Paritaprevir free base (ABT-450) is an orally bioavailable, synthetic acylsulfonamide inhibitor of the hepatitis C virus (HCV) protease complex comprised of non-structural protein 3 and 4A (NS3/NS4A), with potential activity against HCV genotype 1. Upon administration, paritaprevir reversibly binds to the active center and binding site of the HCV NS3/NS4A protease and prevents NS3/NS4A protease-mediated polyprotein maturation. This disrupts both the processing of viral proteins and the formation of the viral replication complex, which inhibits viral replication in HCV genotype 1-infected host cells.

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.

(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.

CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50 values of 140 nM and 40 nM, respectively. Extractable from liver and kidney, CYP4A11/CYP4F2-IN-2 has the potential to treat kidney diseases.

Furafylline is a selective inhibitor of human cytochrome P450 (CYP)1A2 (IC50 : 0.07 µM),

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.

1-Ethynylnaphthalene [1-EN] is a selective inhibitor of cytochrome P450 IB1 (CYP1B1).

CYP450-IN-1 (compound 2e) is a potent inhibitor of CYP450.

TMS (2,3',4,5'-Tetramethoxystilbene) is a very selective and potent competitive inhibitor of P450 1B1 (CYP1A1).

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

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.

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.

N-desmethyl Olanzapine is a metabolite of the atypical antipsychotic compound Olanzapinec, which is formed through the oxidative metabolism of olanzapine by the cytochrome 450 (CYP) isoenzyme CYP1A2.

5-Hydroxy-8-methoxypsoralen (5-Hydroxyxanthotoxin) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450) and a metabolite of Xanthotoxin. It is used in the treatment of psoriasis, eczema, vitiligo, and certain cutaneous lymphomas in combination with phototherapy involving exposure to sunlight.

Paritaprevir dihydrate (ABT-450), a highly effective and orally administered antiviral, acts as a non-structural protein 3/4A (NS3/4A) protease inhibitor, displaying EC50 values of 1 and 0.21 nM against HCV genotypes 1a and 1b, respectively. Additionally, it functions as a SARS-CoV 3CL pro inhibitor with an IC50 of 1.31 μM. Primarily metabolized by cytochrome P450 (CYP) 3A, its plasma concentration and half-life are significantly increased when administered with Ritonavir, a CYP450 inhibitor [1] [2] [3] [4].