Acetylcholinesterase
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Acetylcholinesterase is the enzyme that breaks down acetylcholine.
Inhibitors[edit | edit source]
Aceytlcholinesterase inhibitors inhibit acetylcholinesterase from breaking down acetylcholine, resulting in higher circulating levels of the neurotransmitter.
They are used to treat myasthenia gravis and postural orthostatic tachycardia, and to improve cognitive function in Alzheimer's disease[1] and Parkinson's disease.
Examples of potential therapeutic inhibitors[edit | edit source]
Compounds which function as reversible competitive or noncompetitive inhibitors of cholinesterase are those most likely to have therapeutic uses. These include:
- Tetrahydrocannabinol, the main active ingredient in cannabis is a competitive inhibitor of acetylcholinesterase[2]
- Carbamates
- Phenanthrene derivatives
- Caffeine – noncompetitive (also an Adenosine receptor antagonist)[3][4]
- Rosmarinic acid - ester of Caffeic acid. Found in plants species of Lamiaceae family.[5]
- Alpha-Pinene - noncompetitive reversible[6][7][1]
- Piperidines
- Tacrine, also known as tetrahydroaminoacridine (THA')
- Edrophonium
- Huperzine A[8][9]
- Ladostigil
- Ungeremine[10]
- Lactucopicrin
Examples of irreversible inhibitors[edit | edit source]
Irreversible inhibitors can lead to muscular paralysis, convulsion and death by asphyxiation. Organophosphates, some insecticides, and nerve gases for chemical warfare are examples of irreversible inhibitors.[citation needed]
See also[edit | edit source]
Learn more[edit | edit source]
References[edit | edit source]
- ↑ Tabet, N. (July 1, 2006). "Acetylcholinesterase inhibitors for Alzheimer's disease: anti-inflammatories in acetylcholine clothing!". Age and Ageing. 35 (4): 336–338. doi:10.1093/ageing/afl027. ISSN 0002-0729. PMID 16788077. Retrieved November 9, 2016.
- ↑ Eubanks, Lisa M.; Rogers, Claude J.; Beuscher, Albert E.; Koob, George F.; Olson, Arthur J.; Dickerson, Tobin J.; Janda, Kim D. (December 2006). "A molecular link between the active component of marijuana and Alzheimer's disease pathology". Molecular Pharmaceutics. 3 (6): 773–777. doi:10.1021/mp060066m. ISSN 1543-8384. PMC 2562334. PMID 17140265.
- ↑ Karadsheh, N; Kussiel, P; Linthicum, DS (1991). "Inhibition of acetylcholinesterase by caffeine, anabasine, methyl pyrrolidine and their derivatives". Toxicology letters. 55 (3): 335–42. doi:10.1016/0378-4274(91)90015-X. PMID 2003276.
- ↑ Pohanka, M (2014). "The effects of caffeine on the cholinergic system". Mini Reviews in Medicinal Chemistry. 14 (6): 543–549. doi:10.2174/1389557514666140529223436. PMID 24873820.
- ↑ Vladimir-Knežević, Sanda; Blažeković, Biljana; Kindl, Marija; Vladić, Jelena; Lower-Nedza, Agnieszka D.; Brantner, Adelheid H. (January 9, 2014). "Acetylcholinesterase Inhibitory, Antioxidant and Phytochemical Properties of Selected Medicinal Plants of the Lamiaceae Family". Molecules. 19 (1): 767–782. doi:10.3390/molecules19010767. PMID 2003276.
- ↑ Miyazawa, Mitsuo; Yamafuji, Chikako (March 9, 2005). "Inhibition of acetylcholinesterase activity by bicyclic monoterpenoids". Journal of Agricultural and Food Chemistry. 53 (5): 1765–1768. doi:10.1021/jf040019b. ISSN 0021-8561. PMID 15740071.
- ↑ Perry, Nicolette S.L.; Houghton, Peter J.; Theobald, Anthony; Jenner, Peter; Perry, Elaine K. (July 1, 2000). "In-vitro Inhibition of Human Erythrocyte Acetylcholinesterase by Salvia lavandulaefolia Essential Oil and Constituent Terpenes". Journal of Pharmacy and Pharmacology. 52 (7): 895–902. doi:10.1211/0022357001774598. ISSN 2042-7158. PMID 10933142.
- ↑ Bauer, Brent A. Alzheimer's disease. mayoclinic.com
- ↑ Wang, BS; Wang, H; Wei, ZH; Song, YY; Zhang, L; Chen, HZ (2009). "Efficacy and safety of natural acetylcholinesterase inhibitor huperzine A in the treatment of Alzheimer's disease: an updated meta-analysis". Journal of neural transmission. 116 (4): 457–465. doi:10.1007/s00702-009-0189-x. PMID 19221692.
- ↑ Rhee, IK; Appels, N; Hofte, B; Karabatak, B; Erkelens, C; Stark, LM; Flippin, LA; Verpoorte, R (November 2004). "Isolation of the Acetylcholinesterase Inhibitor Ungeremine from Nerine bowdenii by Preparative HPLC Coupled On-Line to a Flow Assay System". Biological & Pharmaceutical Bulletin. 27 (11): 1804–1809. doi:10.1248/bpb.27.1804. PMID 15516727.
