cholinesterase (che)

Pyridostigmine bromide (Mestinon) is a cholinesterase inhibitor with a slightly longer duration of action than NEOSTIGMINE. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants.

Neostigmine methyl sulfate (Syntostigmin) is a reversible inhibitor of acetylcholinesterase, can not cross the blood-brain barrier, used in the treatment of myasthenia gravis.

Neostigmine bromide is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier.

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density volume and mineralization in vivo.

Scopoletin (Esculetin 6-methyl ether) is a plant growth factor derived from the root of Scopolia carniolica, inhibits of acetylcholinesterase (AChE).

sn-Glycero-3-phosphocholine (Choline glycerophosphate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have a potential for the treatment of Alzheimer's disease and dementia. sn-Glycero-3-phosphocholine rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of the acetylcholine neurotransmitter. It is a non-prescription drug in most countries due to its Generally Recognised As Safe (GRAS) status [1]. Studies have investigated its efficacy for cognitive disorders including stroke and Alzheimer's disease. An Italian multicentre clinical trial on 2, 044 patients suffering from recent stroke were supplied Glycerylphosphorylcholine in doses of 1, 000 mg day for 28 days and 400 mg three times per day for the five ensuing months. The trial confirmed the therapeutic role of alpha-GPC on the cognitive recovery of patients based on four measurement scales, three of which reached statistical significance [2].

Donepezil (Aricept) is a piperidine-based, potent, specific, and reversible inhibitor of acetylcholinesterase (AChE). It can be used for the treatment of mild to moderate dementia of the Alzheimer's type.

Methyl tridecanoate is a natural product.

Coumaran (2,3-Dihydrobenzofuran), an acetylcholinesterase (AChE) inhibitor isolated from the leaves of L. camara, can be used as a biopesticide and belongs to the class of 1-benzofurans as the 2,3-dihydro derivative of benzofuran with a role as a metabolite.

Physostigmine, a parasympathomimetic alkaloid, is a reversible cholinesterase inhibitor. It extracts from the Calabar bean.

Protriptyline Hydrochloride is the hydrochloride salt form of protriptyline, a tricyclic secondary amine with an antidepressant property. Protriptyline hydrochloride (Protriptyline HCl) blocks the re-uptake of norepinephrine and serotonin by nerve terminals, thereby increasing available norepinephrine and serotonin. In addition, this agent exhibits anticholinergic activity.

Galanthamine N-Oxide, an alkaloid extracted from Zephyranthes concolor bulbs, effectively inhibits acetylcholinesterase (AChE) from electric eel with an EC50 of 26.2 μM. It acts as a significant inhibitor of substrate accommodation within the active sites of Torpedo californica AChE (TcAChE), human AChE (hAChE), and human BChE (hBChE) enzymes.

Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300 CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively.

Epi-galantamine, a diastereomer of galantamine, is an alkaloid extracted from the bulbs and flowers of the Caucasian snowdrop (Galanthus woronowii). It acts as an AChE inhibitor, featuring an EC50 of 45.7 μM.

Pirimiphos-methyl (AI3-27699) is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, moths, snout beetles and Ephestia cautella during storage of agricultural grains.

Acephate (Orthene) is an anticholinesterase insecticide with a weak inhibitory effect on AChE in rats, but it can effectively inhibit AChE in cockroaches.

Isoimperatorin is an anti-inflammatory agent, exhibits significant inhibitory effects on acetylcholinesterase (AChE).

(-)-Huperzine A (HupA) , an active Lycopodium alkaloid extracted from the traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).

Rhodiosin is a compound with antioxidant activity.

1. Swertianolin (Bellidifolin-8-O-Glucoside), mangiferin, rhodenthoside A-C, isoorientin, isovitexin, and amarogentin would serve as potential chemotaxonomic markers to differentiate Gentianaceae species. 2. Swertianolin and swertiamarin show significant hepatoprotective effect in the liver damage model induced by alpha-naphthylisot hiocyanate. 3. Swertianolin shows anti-acetylcholinesterase activity effects. 4. Swertianolin shows that it can scavenge superoxide and hydroxyl radicals with the studying method of the autoxidation of Pyrogallol and afenton.

Demecarium bromide (BC-48) is a potent cholinesterase inhibitor,and is treatment glaucoma agent.

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.

N-p-trans-Coumaroyltyramine is a natural product and an acetylcholinesterase (AChE) inhibitor with an IC50 of 122 μM. It also exhibits anti-trypanosomal activity with an IC50 of 13.3 μM for T. brucei rhodesiense.

Isomerazin (Isomeranzin) has anti-inflammatory activity, it suppresses inflammation by inhibiting M1 macrophage polarization through the p65, NF-κB and ERK pathway.