Leptomerine, an alkaloid from stems of Esenbeckia leiocarpa Engl. (Rutaceae) as potential treatment for Alzheimer Disease. Leptomerine inhibits acetyl cholinesterase (AChE) with an IC50 of 2.5 μM. Anticholinesterasic activity[1].
Osmanthuside B can be isolated from Pseuderanthemum carruthersii (Seem.) Guill. var. atropurpureum (Bull.) Fosb and has weak acetylcholinesterase inhibitory activity[1].
4-Methylbenzylidene camphor-d4 is the deuterium labeled 4-Methylbenzylidene camphor[1].
Isograndifoliol is a selective inhibitor of butyrylcholinesterase (BChE) with an IC50 value of 0.9 μM. And Isograndifoliol moderately inhibits acetylcholinesterase (AChE) with an IC50 value of 342.9 μM. Isograndifoliol also has vasorelaxant effect and anti-tumor effect. Isograndifoliol can be used for research against dementia caused by neurodegenerative diseases[1][2][3].
O-Desmethyl Galanthamine (Sanguinine) is galanthamine-type alkaloid. O-Desmethyl Galanthamine is an acetylcholinesterase (AChE) inhibitor, with an IC50 1.83 μM[1].
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease[1].
Metrifonate is an irreversible organophosphate acetylcholinesterase inhibitor that is used as an insecticide for the control of flies and roaches.
Paecilomide is a pyridone alkaloid and acetylcholinesterase inhibitor[1].
Cyclopenin ((±)-Isocyclopenine) is a racemate[1].
sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively[1].
Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor[1].
AChE/hCA I/II-IN-1 (Compound 6) is a potent inhibitor of AChE/Hca with IC50 values of 22.21, 60.79 and 66.64 nM for AChE, Hca Ⅰ and Hca Ⅱ. AChE/hCA I/II-IN-1 can be used for the rsearch for glaucoma, Alzheimer's disease, diabetes[1].
Huperzine A, an active Lycopodium alkaloid extracted from 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). IC50 value:Target: AChEHuperzine A exhibited protective effects against d-gal-induced hepatotoxicity and inflamm-aging by inhibiting AChE activity and via the activation of the cholinergic anti-inflammatory pathway. The huperzine A mechanism might be involved in the inhibition of DAMPs-mediated NF-κB nuclear localization and activation. Huperzine A is a potential therapeutic agent for Alzheimer's disease.
Methyl ganoderate A acetonide, a lanostane triterpene, is a natural product that could be isolated from the fruiting bodies of Ganoderma lucidum. Methyl ganoderate A acetonide is a potent AChE inhibitor with an IC50 value of 18.35 μM. Methyl ganoderate A acetonide can be used in research of Alzheimer’s disease (AD)[1].
BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species[1].
Decaffeoylacteoside is an inhibitor of AChE/BChE/LOX with moderate activity[1].
Heliosupine is a pyrrolizidine alkaloid. Heliosupine is an acetylcholinesterase (AChE) inhibitor, with an IC50 0.57 mM. Heliosupine exhibits deterrent effects against generalist herbivores[1][2].
Picfeltarraenin X, a triterpenoid isolated from Picria fel-terrae Lour, is an AChE inhibitor[1].
Ebeiedinone, a steroidal alkaloid from Fritillaria species, inhibits the bioactivity of human whole blood cholinesterase (ChE) at the concentration of 0.1 mM, with the inhibitory effects of 69.0%[1].
Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChE inhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitory activities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively[1].
AChE-IN-3 shows moderate inhibitory activity against AChE and strong NO inhibitory activity with an EC50 of 0.57 μM.
N-Methylcalycinine is a nature product with AChE inhibitory activity. N-Methylcalycinine can be isolated from the roots of Stephania epigaea. N-Methylcalycinine can be used for the research of asthma, cancer, dysentery, fever, hyperglycemia, intestinal complaints, inflammation, sleep disturbances, tuberculosis and so on[1].
Pipenzolate bromide is a muscarinic receptor antagonist, preventing acetyl choline from binding to the receptors.
Rivastigmine tartrate, an cholinesterase inhibitor(IC50= 5.5 uM), inhibits both butyrylcholinesterase and acetylcholinesteraseIC50 value: 5.5 uMTarget: AChERivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease. The drug can be administered orally or via a transdermal patch; the latter form reduces the prevalence of side effects, which typically include nausea and vomiting. The drug is eliminated through the urine, and appears to have relatively few drug-drug interactions. Rivastigmine, a cholinesterase inhibitor, inhibits both butyrylcholinesterase and acetylcholinesterase. It is thought to work by inhibiting these cholinesterase enzymes, which would otherwise break down the brain chemical acetylcholine.
MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research[1].
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity[1].
2,3,5,6,7,8-Hexahydro-1H-cyclopenta[b]quinolin-9-amine is a pharmaceutically active compound which is a nootropic agent that acts as cholinesterase inhibitor and is used in treatment of Alzheimer disease[1].
SP-10 is a small peptide derived from S protein with an IC50 value of 1.88 nM for blocks the interaction between S protein and ACE2. SP-10 can be used for SARS-CoV research[1].
AChE/BChE-IN-3 (BMC-1) is a dual AChE and BChE inhibitor with IC50 values of 6.08 μM and 0.383 μM against electric eel AChE (elAChE) and equine serum BChE (eqBChE), respectively[1].
Pralidoxime iodide is a reactivator of acetylcholinesterase (AChE). Pralidoxime iodide reactivates nerve agent, which inhibits AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime iodide is an antidote for organophosphate poisoning[1][2].