Loewenstein-Lichtenstein Y, Schwarz M, Glick D, Nørgaard-Pedersen B, Zakut H, Soreq H
Department of Biological Chemistry, Hebrew University of Jerusalem, Israel.
Nat Med. 1995 Oct;1(10):1082-5. doi: 10.1038/nm1095-1082.
Normal butyrylcholinesterase (BuChE), but not several of its common genetic variants, serves as a scavenger for certain anti-cholinesterases (anti-ChEs). Consideration of this phenomenon becomes urgent in view of the large-scale prophylactic use of the anti-ChE, pyridostigmine, during the 1991 Persian Gulf War, in anticipation of nerve gas attack and of the anti-ChE, tacrine, for improving residual cholinergic neurotransmission in Alzheimer's disease patients. Adverse symptoms were reported for subjects in both groups, but have not been attributed to specific causes. Here, we report on an Israeli soldier, homozygous for 'atypical' BuChE, who suffered severe symptoms following pyridostigmine prophylaxis during the Persian Gulf War. His serum BuChE and recombinant 'atypical' BuChE were far less sensitive than normal BuChE to inhibition by pyridostigmine and several other carbamate anti-ChEs. Moreover, atypical BuChE demonstrated 1/200th the affinity for tacrine of normal BuChE or the related enzyme acetylcholinesterase (AChE). Genetic differences among BuChE variants may thus explain at least some of the adverse responses to anti-ChE therapies.
正常的丁酰胆碱酯酶(BuChE),而非其几种常见的基因变体,可作为某些抗胆碱酯酶(anti-ChEs)的清除剂。鉴于1991年海湾战争期间为预防神经毒气袭击而大规模预防性使用抗胆碱酯酶药物吡啶斯的明,以及为改善阿尔茨海默病患者残余胆碱能神经传递而使用抗胆碱酯酶药物他克林,对这一现象的研究变得紧迫起来。两组受试者均报告出现了不良症状,但尚未明确具体病因。在此,我们报告一名以色列士兵,其“非典型”BuChE为纯合子,在海湾战争期间接受吡啶斯的明预防治疗后出现了严重症状。他的血清BuChE和重组“非典型”BuChE对吡啶斯的明和其他几种氨基甲酸酯类抗胆碱酯酶的抑制作用远不如正常BuChE敏感。此外,非典型BuChE对他克林的亲和力仅为正常BuChE或相关酶乙酰胆碱酯酶(AChE)的1/200。因此,BuChE变体之间的基因差异可能至少部分解释了对抗胆碱酯酶疗法的不良反应。