enzymes

Pancreatin (pancrelipase) is a mixture of several digestive enzymes secreted by the exocrine cells of the pancreas. It is composed of amylase, lipase and protease.

Melagatran, a direct and orally active thrombin inhibitor, specifically inhibits thrombin without affecting other enzymes in the coagulation cascade or fibrinolytic enzymes. It does not rely on endogenous co-factors to exert its antithrombin effect, and may alleviate the harmful effects of endotoxemia. As a result, Melagatran offers a promising strategy for the prevention of arterial occlusion.

Isonicotinic acid, a metabolite of isoniazid and a useful isomer of nicotinic acid, is formed from isoniazid by hydrazinolysis and can be catalyzed by cytochrome P450 enzymes, such as CYP2C.

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

Sodium taurocholate (Taurocholate Sodium) hydrate is the main end product of cholesterol catabolism. During enterohepatic circulation, bile taurocholic acid is converted by the microorganisms to taurodeoxycholic acid and deoxycholic acid.[3] These are reabsorbed by the liver via a carrier-mediated process and converted by liver enzymes to taurocholic acid.

Ifosfamide (NSC-109724) alkylates and forms DNA crosslinks, thereby preventing DNA strand separation and DNA replication. Ifosfamide is a synthetic analog of the nitrogen mustard cyclophosphamide with antineoplastic activity. This agent is a prodrug that must be activated through hydroxylation by hepatic microsomal enzymes.

Pyridoxal phosphate (Vitamin B6 phosphate) is the active form of vitamin B6 and a coenzyme for many pyridoxal phosphate (PLP)-dependent enzymes. PLP is involved in numerous enzymatic transamination, decarboxylation and deamination reactions; it is necessary for the synthesis of amino acids and amino acid metabolites, and for the synthesis and or catabolism of certain neurotransmitters, including the conversion of glutamate into gamma-aminobutyric acid (GABA) and levodopa into dopamine. PLP can be used as a dietary supplement in cases of vitamin B6 deficiency. Reduced levels of PLP in the brain can cause neurological dysfunction.

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

Protocatechuic acid (3, 4-Dihydroxybenzoic acid) (3, 4-dihydroxybenzoic acid) is a natural phenolic compound found in many edible and medicinal plants. Recent studies indicate that it could be used as a protective agent against cardiovascular diseases and neoplasms. The mechanism of its action is mostly associated with antioxidant activity, including inhibition of generation as well as scavenging of free radicals and up-regulating enzymes which participate in their neutralization.

Auraptene is a coumarin derived from citrus plants that bears a geranyloxyl moiety at its C-7. It has anti-inflammatory, anti-carcinogenic, anti-bacterial, neuroprotective, and hepatoprotective activities. It inhibits leukocyte activation and induces phas

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.

Adenosylcobalamin (AdoCbl) is a biologically active form of vitamin B12 .It is a cofactor for methylmalonyl CoA mutase. It belongs to the corrinoid group of compounds, which contain a corrin macrocycle, and is produced only by certain bacteria and archaea. It is a cofactor for various enzymes including mutases, eliminases, aminomutases, and a reductase.

Ketorolac tromethamine salt (Ketorolac tris salt) non-selective inhibits the enzymes cyclooxygenase 1 (COX-1) and COX-2with anti-inflammatory, analgesic, and antipyretic activities.

Diammonium Glycyrrhizinate (Glycyrrhizin) , an extensively used anti-inflammatory agent, is isolated from the licorice root. It is metabolized to glycyrrhetinic acid, which inhibits 11-β-hydroxysteroid dehydrogenase and other enzymes involved in the metabolism of corticosteroids. Therefore, glycyrrhizic acid, the main and sweet component of licorice, has been studied for its ability to cause hypermineralocorticoidism with potassium loss and sodium retention, edema, increased blood pressure, as well as inhibited the renin-angiotensin-aldosterone system.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

Flavone (2-Phenyl-4-chromone) have effects on CYP (P450) activity which are enzymes that metabolize most drugs in the body.

Amorolfine hydrochloride (Amorolfine HCl) is an antifungal reagent. It exerts the antifungal activity by selectively interrupting two steps in the pathway of ergosterol synthesis and eventually disrupting the function and structure of fungal cell membrane. Amorolfine hydrochloride , a morpholine antifungal drug, can inhibit D14 reductase and D7-D8 isomerase. These enzymes can deplete ergosterol and cause ignosterol to accumulate in the fungal cytoplasmic cell membranes.

Rac-Belinostat (PX-105684) is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase.

BenzeneazoMalononitrile inhibits the growth of many types of cells, including therapeutic cells. It has also been shown to inhibit the activity of several enzymes, including those involved in drug metabolism. It has also been shown to inhibit the activity of several hormones, including those involved in the regulation of blood sugar levels.

Glycoursodeoxycholic acid (Ursodeoxycholylglycine) is an acyl glycine and a bile acid-glycine conjugate. It is a secondary bile acid produced by the action of enzymes existing in the microbial flora of the colonic environment. In hepatocytes, both primary and secondary bile acids undergo amino acid conjugation at the C-24 carboxylic acid on the side chain, and almost all bile acids in the bile duct, therefore, exist in a glycine conjugated form. Bile acids are steroid acids found predominantly in bile of mammals.

Ofloxacin (Oxaldin) is a fluoroquinolone antibacterial antibiotic. Ofloxacin binds to and inhibits bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, enzymes involved in DNA replication and repair, resulting in cell death in sensitive bacterial species.

L-SelenoMethionine (L-(+)-Selenomethionine) is a naturally occurring amino acid. It promotes cell cycle progression and elevates the expression of the antioxidant enzymes thioredoxin reductase, glutathione reductase.

Phenidone (1-phenyl-3-pyrazolidinone) is a dual inhibitor of cyclooxygenases and lipoxygenases that ameliorates rat paralysis in experimental autoimmune encephalomyelitis by suppressing its target enzymes[1]. The lipoxygenase inhibitor phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[2].

Divalproex Sodium (Valproate semisodium) binds to and inhibits gamma-aminobutyric acid (GABA) transaminase and its anticonvulsant activity may be exerted by increasing brain concentration of GABA and by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. It also is an HDAC inhibitor， Comprised of sodium valproate and valproic acid with anticonvulsant and antiepileptic activities. Divalproex may also work by suppressing repetitive neuronal firing through the inhibition of voltage-sensitive sodium channels.

Cefoperazone (Medocef) binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. It can inhibit rMrp2-mediated [3H]E217βG uptake (IC50: 199 μM).

Nabumetone (BRL14777)(BRL14777) is a non-steroidal anti-inflammatory drug and its active metabolite 6MNA inhibits the enzymes cyclo-oxygenase I and II.

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

2-Phenylethylamine hydrochloride (benzeneethanamine hydrochloride) acts as neuromodulator in the central nervous system. It stimulates the release of norepinephrine and dopamine and is metabolized by monoamine oxidases as well as other enzymes.

Proteinases are enzymes that catalyse the breakdown of proteins. Proteinases are involved in many biological functions, including the digestion of ingested proteins, the breakdown of old proteins, and cell signalling. They also facilitate the formation of new protein products.

3-Chloropropiophenone (CPP) is a synthetic compound that is used in the synthesis of organic reagents, pharmaceuticals, and other products. It has the ability to inhibit certain enzymes (e.g. cytochrome P450) and inhibit the growth of certain tumor cells.

Cholesteryl sulfate sodium (Sodium Cholesteryl Sulfate) is a sterol sulfate in human plasma. Cholesteryl sulfate sodium is a component of cell membrane and has a regulatory function. Cholesteryl sulfate sodium also activates multiple protein kinase C (PKC) iso-enzymes, especially the ε, η and ζ isoforms.

Naringin dihydrochalcone (Naringin DC) is an inhibitor of CYP enzymes, used as an artificial sweetener.

Flumequine (R-802) is a broad-spectrum antibiotic effective against both Gram-positive and Gram-negative bacteria. It operates by inhibiting DNA gyrase (a type II topoisomerase) and topoisomerase IV, enzymes crucial for separating bacterial DNA, thereby preventing cell division.

1. Linalool (Linalol), a natural compound of the essential oils, has been shown to have antinociceptive, antimicrobial, and anti-inflammatory properties. 2. Linalool was protected against LPS/GalN-induced liver injury through induction of antioxidant defense via Nrf2 activating and reduction inflammatory response via NF-κB inhibition. 3. Linalool biosynthesis and accumulation might be involved in plant defense against bacterial and fungal pathogens and be associated with field resistance to citrus canker. 4. Linalool significantly increased the expression of antioxidant enzymes regulated by Nrf-2 and diminished lung tissue levels of several pro-inflammatory cytokines, including tumor necrosis factor α (TNF-α) and interleukin (IL)-6.

Fumaric acid (2-Butenedioic acid) attenuates the eotaxin-1 expression in TNF-α-stimulated fibroblasts by suppressing p38 MAPK-dependent NF-κB signaling. Fumaric acid has recently been identified as an oncometabolite or an endogenous, cancer-causing metabolite. High levels of this organic acid can be found in tumors or biofluids surrounding tumors. Its oncogenic action appears due to its ability to inhibit prolyl hydroxylase-containing enzymes.

Tris(benzyltriazolylmethyl)amine (TBTA) is a tertiary amine with three 1,2,3-triazole groups that complexes with and stabilizes copper(I), thereby accelerating azide-alkyne cycloadditions used in click chemistry.

Sodium 4-aminosalicylate dihydrate (4-Amino-salicylic acid sodium salt) is the sodium salt form of aminosalicylic acid, an analog of para-aminobenzoic acid (PABA) with antitubercular activity. Sodium 4-aminosalicylate dihydrate exerts its bacteriostatic activity against Mycobacterium tuberculosis by competing with PABA for enzymes involved in folate synthesis, thereby suppressing growth and reproduction of M. tuberculosis, eventually leading to cell death.

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

Antipyrine (Phenazone), an antipyretic and analgesic, has been given as ear drops and by mouth. Antipyrine is frequently used to test the effects of other diseases or drugs on drug-metabolizing enzymes in the liver.

N-Nitrosodiethylamine (NDEA) is a potent hepatocarcinogenic dialkylnitrosoamine primarily found in water, tobacco smoke, cheddar cheese, cured and fried meals, and many alcoholic beverages. NDEA is responsible for changes in nuclear enzymes related to DNA repair replication and induces various tumors in all animal species, targeting mainly the liver, nasal cavity, trachea, lung, and esophagus.

Pyridoxal 5'-phosphate hydrate (PLP)(1:x), the active form of vitamin B6, is a cofactor for many different enzymes involved in transamination reactions, including mitochondrial cysteine desulfurase, cystathionine γ-synthase, various aminotransferases, and a d-serine dehydratase.

Uracil is a common naturally occurring pyrimidine found in RNA, it base pairs with adenine and is replaced by thymine in DNA. Methylation of uracil produces thymine. Uracil's use in the body is to help carry out the synthesis of many enzymes necessary for cell function through bonding with riboses and phosphates. Uracil serves as allosteric regulator and coenzyme for many important biochemical reactions.

Amylase (Diastase) is any one of a group of enzymes which catalyses the breakdown of starch into maltose.

1,1-Bis(Methylthio)-2-Nitroethylene (1,1-BMNE) has a variety of biochemical and physiological effects. It inhibits the activity of enzymes involved in the metabolism of drugs and other compounds, such as cytochrome P450 and acetylcholinesterase.

Thiamine disulfide (Algoneurina) , also known as thiamin or vitamin B1, is a vitamin found in food and manufactured as a dietary supplement and medication. Thiamine also acts as a cofactor for many centrally metabolizing enzymes.

L-Glutathione reduced (Glutathione) is a naturally occurring tripeptide found in cells as an endogenous antioxidant that scavenges oxygen free radicals. L-Glutathione reduced is a cofactor for certain enzymes and is involved in the rearrangement of protein disulfide bonds and the reduction of peroxides.

(CL227193) )binds to and inactivates penicillin-binding proteins (PBPs), enzymes located on the inner membrane of the bacterial cell wall, resulting in the weakening of the bacterial cell wall and cell lysis. Piperacillin Sodium is the sodium salt of piperacillin, a broad-spectrum semisynthetic, ampicillin-derived ureidopenicillin antibiotic with bactericidal activity. PBPs participate in the terminal stages of assembling the bacterial cell wall, and in reshaping the cell wall during cell division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity.

L-Cystine (Cystine Acid) is not considered one of the 20 amino acids, L-Cystine (Cystine Acid) is a sulfur-containing derivative obtained from oxidation of cysteine amino acid thiol side chains. It functions as an antioxidant and protects tissues against radiation and pollution, slowing the aging process. It also aids protein synthesis. L-Cystine (Cystine Acid) is abundant in many proteins of skeletal tissues and skin, and found in insulin and digestive enzymes chromotrypsinogen A, papain, and trypsinogen.

Diperodon hydrochloride (Diperocaine) is a local anesthetic that can be broken down by serolytic enzymes to produce local anesthetic effects.