Pohanka Miroslav
University of Defense, Hradec Kralove, Czech Republic.
Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2011 Sep;155(3):219-29. doi: 10.5507/bp.2011.036.
Cholinesterases are a group of serine hydrolases that split the neurotransmitter acetylcholine (ACh) and terminate its action. Of the two types, butyrylcholinesterase and acetylcholinesterase (AChE), AChE plays the key role in ending cholinergic neurotransmission. Cholinesterase inhibitors are substances, either natural or man-made that interfere with the break-down of ACh and prolong its action. Hence their relevance to toxicology and pharmacology.
The present review summarizes current knowledge of the cholinesterases and their inhibition. Particular attention is paid to the toxicology and pharmacology of cholinesterase-related inhibitors such as nerve agents (e.g. sarin, soman, tabun, VX), pesticides (e.g. paraoxon, parathion, malathion, malaoxon, carbofuran), selected plants and fungal secondary metabolites (e.g. aflatoxins), drugs for Alzheimer's disease (e.g. huperzine, metrifonate, tacrine, donepezil) and Myasthenia gravis (e.g. pyridostigmine) treatment and other compounds (propidium, ethidium, decamethonium).
The crucial role of the cholinesterases in neural transmission makes them a primary target of a large number of cholinesterase-inhibiting drugs and toxins. In pharmacology, this has relevance to the treatment of neurodegenerative disorders.
胆碱酯酶是一类丝氨酸水解酶，可分解神经递质乙酰胆碱（ACh）并终止其作用。在丁酰胆碱酯酶和乙酰胆碱酯酶（AChE）这两种类型中，AChE在终止胆碱能神经传递中起关键作用。胆碱酯酶抑制剂是天然或人工合成的物质，它们会干扰ACh的分解并延长其作用时间。因此，它们与毒理学和药理学相关。
本综述总结了目前关于胆碱酯酶及其抑制作用的知识。特别关注了与胆碱酯酶相关的抑制剂的毒理学和药理学，如神经毒剂（如沙林、梭曼、塔崩、VX）、农药（如对氧磷、对硫磷、马拉硫磷、马拉氧磷、克百威）、特定植物和真菌次生代谢产物（如黄曲霉毒素）、用于治疗阿尔茨海默病的药物（如石杉碱、美曲膦酯、他克林、多奈哌齐）和重症肌无力（如吡啶斯的明）的药物以及其他化合物（碘化丙啶、溴化乙锭、十烃季铵）。
胆碱酯酶在神经传递中的关键作用使其成为大量胆碱酯酶抑制药物和毒素的主要靶点。在药理学中，这与神经退行性疾病的治疗相关。
