anti-acetylcholinesterase

O-Desmethyl Galanthamine (Sanguinine) is a galanthamine-type alkaloid and an acetylcholinesterase (AChE) inhibitor with an IC50 of 1.83 μM.

1. Corydaline (Corydalin), an isoquinoline alkaloid, is one of the major active constituents in a new prokinetic botanical agent. 2. Corydaline promotes gastric emptying and small intestinal transit and facilitates gastric accommodation. 3. Corydaline exhibits the anti-acetylcholinesterase, antiallergic, and antinociceptive activities. 4. Corydaline has potent inhibition of CYP2C19 and CYP2C9.

β-NETA (α-NETA) is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. β-NETA has anti-cancer activity[1][2]. β-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM).

ACHE-IN-38 is a potent Acetylcholinesterase inhibitor that can be used for the synthesis of compounds with anti-inflammatory, anti-tumor, and antibacterial activities.

Kokusaginine is a furoquinoline alkaloid that inhibits acetylcholinesterase (AChE) with an IC50 of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptosis-inducing effects in MCF-7/ADR cells and is utilized in biochemical research focused on cholinesterase inhibition, apoptosis regulation, and multidrug-resistant cancer cell signaling pathways.

Neuroprotective agent 5 (compound 28) acts as a brain-penetrating agent with anti-neuroinflammatory, antioxidant, and neuroprotective properties. It exhibits potent inhibition of nitric oxide (NO) with an EC50 of 0.49 μM and suppresses the release of pro-inflammatory mediators PGE2 and TNF-α. Additionally, it downregulates the expression of iNOS and COX-2 proteins, facilitating the polarization of BV-2 cells from a pro-inflammatory M1 phenotype to an anti-inflammatory M2 phenotype. Neuroprotective agent 5 also dose-dependently inhibits acetylcholinesterase (AChE) activity and the aggregation of Aβ42. This compound is useful for research into Alzheimer's disease.

Imidazole-D4 is an isotope-labeled variant of imidazole, which is a heterocyclic aromatic compound. Imidazole (T5202) molecules serve as inhibitors for acetylcholinesterase (AChEI) and xanthine oxidase (XO) and have been utilized as corrosion inhibitors. They display a range of biological activities, including antifungal, antitubercular, anti-inflammatory, antioxidant, and analgesic properties. Imidazole (T5202) inhibits platelet microsomes from converting endoperoxides (PGG2 and PGH2) into thromboxane A2. Additionally, imidazole derivatives show inhibitory effects on the SARS-CoV-2 3CLpro enzyme, offering potential for research in Alzheimer’s disease, gout, COVID-19, and thrombotic disorders.

AChE-IN-85 (Compound 7k) is an acetylcholinesterase inhibitor with an IC50 of 0.083 μM. It reduces nitric oxide (NO) release, the production of TNF-α and IL-1β, as well as levels of LDH and ROS, and inhibits Aβ42 aggregation. AChE-IN-85 exhibits anti-inflammatory and neuroprotective effects and is applicable for research on diseases such as Alzheimer's.

AChE-IN-54 (compound 3c) is an inhibitor of acetylcholinesterase (AChE) and exhibits anti-lipid peroxidation activity.

Myrtenal is a natural monoterpene. It is found to attenuate diethylnitrosamine-induced hepatocellular carcinoma in rats by stabilizing intrinsic antioxidants and modulating apoptotic and anti-apoptotic cascades. Myrtenal also inhibits acetylcholinesterase

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

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.

Sinapine Thiocyanate, is a derivative of Sinapine (S486605), an alkaloidal amine found in black mustard seeds. It is the choline ester of Sinapic Acid (S486800). It is also a phenolic-chloine conjugates, acting as anti-oxidants and acetylcholinesterase inhibitors, that can be used for the treatment of Alzheimer's disease (AD).

Isonaringin exhibits anti-Alzheimer's activity by inhibiting acetylcholinesterase (AChE).

Sinapine hydroxide, an alkaloid derived from the seeds of cruciferous plants, demonstrates a variety of beneficial properties including anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic, and radio-protective effects. Additionally, it acts as an inhibitor of acetylcholinesterase (AChE), making it valuable for researching neurodegenerative conditions such as Alzheimer's disease, ataxia, myasthenia gravis, and Parkinson's disease[4].

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

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.

H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor antagonist with inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B) with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. With a Ki of 170 nM for hH3R, it demonstrates favorable anti-neuropathic pain and memory-enhancing effects and can cross the blood-brain barrier (BBB) [1].

Ladostigil hydrochloride (TV-3326), an orally active compound, acts as a dual inhibitor targeting both cholinesterase and brain-selective monoamine oxidase (MAO), demonstrating inhibition constants (IC50s) of 31.8 μM for acetylcholinesterase (AChE) and 37.1 μM for MAO-B. This compound exhibits neuroprotective, antioxidant, and anti-inflammatory properties, making it useful for research into depression and Alzheimer's disease.

Isograndifoliol is a chemical compound that acts as a selective inhibitor of butyrylcholinesterase (BChE) with an IC50 value of 0.9 μM and exhibits moderate inhibition of acetylcholinesterase (AChE) with an IC50 value of 342.9 μM. Additionally, it demonstrates vasorelaxant and anti-tumor effects. This compound is utilized in research targeting dementia associated with neurodegenerative diseases.

TZ4M, a 2,4-thiazolidinedione (TZD)-based anti-ADV agent, exhibits neuroprotective effects and acetylcholinesterase (AChE) inhibition in human plasma. It enhances memory and cognitive function in adult rats within a scopolamine-induced Alzheimer-type model [1].

Coumarinic acid serves as a brain-penetrating inhibitor of AChE (acetylcholinesterase) and β-amyloid, with applications in anti-Alzheimer's drug research [1].

S-(-)-N-trans-Feruloyl normetanephrine, a natural product with weak anti-acetylcholinesterase activity, can be isolated from the aerial parts of Bassia indica Wight [1].

hAChE-IN-5 (compound 49) is a dual inhibitor of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBuChE), showing IC50 values of 0.17 μM for both enzymes. It also potently inhibits glycogen synthase kinase 3 beta (GSK3β) with an IC50 of 0.21 μM. Furthermore, it effectively inhibits tau protein and Aβ1-42 peptide self-aggregation, and can bind the peripheral anionic site (PAS) to prevent amyloid-beta (Aβ)-induced neurotoxicity. hAChE-IN-5's ability to cross the blood-brain barrier (BBB) supports its potential in developing multitargeted anti-Alzheimer's agents [1].