Butyryl- and acetyl-cholinesterase inhibitory activities in essential oils of Salvia species and their constituents
Butyryl- and acetyl-cholinesterase inhibitory activities in essential oils of Salvia species and their constituents
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DOI：
10.1002/ptr.1451
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发表时间：
2004-04-01
影响因子：
7.2
通讯作者：
Perry, EK
中科院分区：
文献类型：
--
作者：
Savelev, SU;Okello, EJ;Perry, EK
据报道，鼠尾草提取物具有与阿尔茨海默病治疗相关的胆碱能活性。由于缺乏关于抑制丁酰胆碱酯酶（也被认为是治疗该疾病的目标）的信息，促使对 S. fruticosa、S. lavandulaefolia、S. officinalis 和 S. officinalis var. 的精油进行体外研究。 purpurea 的抗丁酰胆碱酯酶活性。使用 Ellman 的方法测定提取物和成分对人胆碱酯酶的剂量依赖性抑制。 S. fruticosa 和 S. officinalis var. 油对丁酰胆碱酯酶的抑制作用随时间增加。紫斑很明显。 IC50值分别从5分钟后的0.15+/-0.007和0.14+/-0.007mg/mL下降至90分钟孵育时间后的0.035+/-0.016和0.06+/-0.018mg/mL。单个成分（例如 3-蒈烯和 β-蒎烯）也显示出对丁酰胆碱酯酶的缓慢起效。对这些油的化学成分及其成分的抗丁酰胆碱酯酶活性的分析表明，所测试的化合物都不能解释这些油的总活性，并且可能存在协同作用。版权所有 (C) 2004 John Wiley Sons, Ltd.
Extracts of Salvia (sage) species have been reported to have cholinergic activities relevant to the treatment of Alzheimer's disease. A lack of information on the inhibition of the enzyme butyrylcholinesterase, also considered to be a target in the treatment of the disease, prompted this in vitro investigation of the essential oils of S. fruticosa, S. lavandulaefolia, S. officinalis and S. officinalis var. purpurea for anti-butyrylcholinesterase activity.Dose-dependent inhibition of human cholinesterases by the extracts and constituents was determined using the method of Ellman. A time dependent increase in the inhibition of butyrylcholinesterase by the oils of S. fruticosa and S. officinalis var. purpurea was evident. IC50 values decreased from 0.15 +/- 0.007 and 0.14 +/- 0.007 mg/mL after 5 min to 0.035 +/- 0.016 and 0.06 +/- 0.018 mg/mL after 90 min incubation time respectively. The slow onset of inhibition of butyrylcholinesterase was also shown by individual constituents, such as 3-carene and beta-pinene. Analyses of the chemical composition of the oils and anti-butyrylcholinesterase activity of their constituents revealed that none of the compounds tested would account for the total activity of the oils and that synergy is likely. Copyright (C) 2004 John Wiley Sons, Ltd.