cholinesterase

Trimethylammonium chloride is a product of the breakdown of plants and animals and is a non-competitive acetylcholinesterase inhibitor.

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.

Desoxypeganine (Deoxypeganine) is an inhibitor of cholinesterase. It acting preferentially on butyrylcholinesterase, and as a selective inhibitor of monoamine oxidase A but not monoamine oxidase B.Desoxypeganine is being developed for its potential utility in the pharmacological treatment of alcohol abuse to reduce craving and depression in alcohol abusers, and might also be useful as a smoking cessation aid.

Galanthamine hydrobromide (Galantamine hydrobromide), a long-acting and centrally active AChE inhibitor (IC50:410 nM), is an allosteric potentiator at neuronal nicotinic ACh receptors.

Tacrine (CS 12602) is an indirect cholinergic agonist and centrally acting anticholinesterase. It is approved for the treatment of Alzheimer's disease.

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.

DL-Menthol ((±)-Menthol) is a racemic mixture of the monoterpene alcohols (–)-menthol and (+)-menthod, which have been found in Cannabis. (–)-Menthol is more common than (+)-menthol in nature and exhibits analgesic, antibacterial, and anticancer properties, as well as inhibits cholinesterase.2 (+)-Menthol inhibits the growth of F. verticillioides (MIC: 1.5 mM) but, unlike (–)-menthol, does not exhibit analgesic, antibacterial, anticancer, or cholinesterase inhibitory activities.

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

1. Isoeugenol acetate (Acetylisoeugenol) shows good antifungal activities against R. solani and F. oxysporum. 2. Isoeugenol acetate is a mild sensitizer in vivo.

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].

Methyl tridecanoate is a natural product.

1. Sinapine, an alkaloid from seeds of the cruciferous species, can be used as an effective natural compound for chemo-resistance. 2. Sinapine has antioxidant and radio-protective activities.

Nodakenin ((+)-Marmesinin) is a compound with anti-allergic and anti-inflammatory activities.

Jatrorrhizine (neprotin) is a protoberberine alkaloid isolated from Enantia chlorantha (Annonaceae) and other species. It was found to have antimicrobial and antifungal activity. It binds and noncompetitively inhibits monoamine oxidase (IC50 4 micromolar for MAO-A and 62 for MAO-B).

Galanthamine (Galantamine) is an acetylcholinesterase (AChE)inhibitor(IC50 : 500 nM), can reduce brain damage induced by hypoxia-ischemia.

1. Linarin (Acacetin-7-O-rutinoside) (acacetin-7-O-β-d-rutinoside) shows selective dose dependent inhibitory effect on acetylcholinesterase. 2. Linarin alleviates GalN LPS-induced liver injury by suppressing TNF-α-mediated apoptotic pathways. 3. Linarin prevents A beta-induced neurotoxicity through the activation of PI3K Akt, which subsequently inhibits GSK-3b and up-regulates Bcl-2. 4. The piperine significantly enhanced the oral absorption of Linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of Linarin.

Neoeriocitrin is a natural product isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor.

Leptomerine (IC50 = 2.5 mM) shows potent anticholinesterasic activity.

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

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.

Violanthin is a natural product isolated from the aerial parts of Piper bavinum and inhibits acetylcholinesterase (AChE) (IC50: 79.80 μM). It has potent antioxidant and antibacterial activities.

(±)-Huperzine A is an active Lycopodium alkaloid extracted from traditional Chinese herbs. (±)-Huperzine A is a selective and reversible inhibitor of AChE and can be used in studies about the treatment of Alzheimer's disease.

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.