Cholinesterase (ChE)

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.

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

Timosaponin AIII (Timosaponin A3) induces autophagy in HeLa cells followed by apoptotic cell death (IC50: 10 μM). The Timosaponin AIII cellular response is mediated via inhibition of mTORC1 and induction of ER stress (IC50: 2.5 μM, BT474 cells; 6 μM, MDAMB231). The Timosaponin AIII pro-apoptotic response is selective for tumor cells over normal cells but autophagy is induced in both.

Vamicamide (FK 176) is a novel anticholinergic compound. Vamicamide increases spontaneous locomotor activity in mice at 32 mg kg (p.o.) or higher and inhibits cataleptic convulsions in mice at 100 mg kg.

Simpinicline (OC-02) (OC-02) is a highly selective nicotinic acetylcholine receptor (nAChR) agonist that activates the trigeminal parasympathetic pathway and can be used to treat dry eye.

Rovatirelin (S-0373) is a newly synthesized thyrotropin-releasing hormone (TRH) analog that ameliorates cytosine arabinoside-induced motor dysfunction in a rat model of spinal cerebellar degeneration via acetylcholine and dopamine neurotransmission.

Clozapine N-oxide dihydrochloride, a derivative of Clozapine and an agonist of human muscarinic design receptors (DREADDs), crosses the blood-brain barrier and activates DREADD receptors hM3Dq and hM4Di.

Epiberberine chloride, a natural pro-berberine from Coptis chinensis Franch. is an AChE, BChE, and BACE1 inhibitor with IC50 values of 1.07, 6.03, and 8.55 μM, respectively.Epiberberine chloride has antioxidant effects and inhibits the effects of Ca9-22 and Fa2R. Epiberberine chloride has antioxidant effects, inhibits the motility of Ca9-22 and FaDu cell lines, and can be used to study hyperlipidemia, Alzheimer's disease and diabetes.

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.

Kuwanon U (4'-methoxykuwanon E), a compound from Morus alba, is a cholinesterase inhibitor with antimicrobial activity, inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), and exerts its inhibitory effect by preventing ATP binding in the cytoplasmic domain of SERCA1, which can be used in the study of diabetes mellitus and bacterial infections.

Ursolic acid acetate (Acetylursolic acid) has cytotoxic activity, antimalarial activity, antitumor and anticancer activities. Acetylursolic acid has NO production inhibitory activities. Acetylursolic acid has inhibition against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes.

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

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.

Vincosamide is an alkaloid from Psychotria leiocarpa extract, inhibits the acetylcholinesterase (AChE) activity with anti-inflammatory activity. Vincosamide can effect relaxation of the supercoiled pBR322 plasmid DNA in the presence of Cu2+.

Jatrorrhizine chloride (Neprotine chloride) is a potent and orally active uptake-2 transporter inhibitor. It exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of the MAPK pathway in HT22 hippocampal neurons.

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.

Lobetyolinin is a compound from Codonopsis pilosula with acetylcholinesterase (AChE) inhibitory and antiarrhythmic activities.

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

Buntanetap ((+)-Phenserine) is an orally active inhibitor of polyneurotoxic proteins (TINAPs) for the study of neurological disorders, endocrine and metabolic disorders, and cardiovascular diseases.

Loganin (Loganoside), an iridoid glucoside, has been reported to be an inhibitor of Cox-1 and also noted to suppress TNF-α formation. This compound also has displayed potent free-radical-scavenging activity and inhibitory effects on melanogenesis.

Chikusetsusaponin Ib (Chikusetsu saponin Ib) is an inhibitor of AChE and can be used in studies about anti-Alzheimer's diseases.

PE 154 is a potent fluorescent inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 280 pM and 16 nM respectively. PE 154 is commonly used to label β-amyloid plaques in histochemical analysis.

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

CV-6209 is a potent antagonist of the platelet-activating factor (PAF) receptor.