Perry N S, Houghton P J, Theobald A, Jenner P, Perry E K
Department of Pharmacy, King's College London, UK.
J Pharm Pharmacol. 2000 Jul;52(7):895-902. doi: 10.1211/0022357001774598.
Sage (Salvia spp) is reputed in European herbal encyclopaedias to enhance memory, and current memory-enhancing/anti-dementia drugs are based on enhancing cholinergic activity by inhibiting cholinesterase. In this study the effects of Salvia lavandulaefolia Vahl. (Spanish sage) essential oil and some of its constituent terpenes on human erythrocyte acetylcholinesterase were examined in-vitro. The main constituents in the essential oil batch used for analysis of cholinesterase inhibition were camphor (27%), 1,8-cineole (13%), alpha- and beta-pinene (10-15%) and bornyl acetate (10%) with other minor constituents (1% or less) including geraniol, limonene, linalool, terpineol and gamma-terpinene. Using the Ellman spectrophotometric method, kinetic analysis was conducted on the interaction of the essential oil and the main monoterpenoids, camphor, 1,8-cineole and alpha-pinene. IC50 values were obtained for the essential oil, 1,8-cineole and alpha-pinene and were 0.03 microL [corrected] mL(-1), 0.67 mM and 0.63 mM, respectively. Camphor and other compounds tested (geraniol, linalool and gamma-terpinene) were less potent (camphor IC50: >10mM). The essential oil, alpha-pinene, 1,8-cineole and camphor were found to be uncompetitive reversible inhibitors. These findings suggest that if the inhibitory activity of the essential oil is primarily due to the main inhibitory terpenoid constituents identified, there is a major synergistic effect among the constituents. Since no single constituent tested was particularly potent, it remains to be determined whether these in-vitro cholinesterase inhibitory activities are relevant to in-vivo effects of the ingestion of S. lavandulaefolia essential oil on brain acetylcholinesterase activity.
在欧洲草药百科全书中,鼠尾草(鼠尾草属)被认为能增强记忆力,目前的增强记忆/抗痴呆药物是基于通过抑制胆碱酯酶来增强胆碱能活性。在本研究中,体外检测了薰衣草叶鼠尾草(西班牙鼠尾草)精油及其一些萜类成分对人红细胞乙酰胆碱酯酶的影响。用于胆碱酯酶抑制分析的精油批次中的主要成分是樟脑(27%)、1,8-桉叶素(13%)、α-蒎烯和β-蒎烯(10 - 15%)以及乙酸龙脑酯(10%),还有其他微量成分(1%或更少),包括香叶醇、柠檬烯、芳樟醇、松油醇和γ-萜品烯。使用埃尔曼分光光度法,对精油与主要单萜类化合物樟脑、1,8-桉叶素和α-蒎烯的相互作用进行了动力学分析。获得了精油、1,8-桉叶素和α-蒎烯的IC50值,分别为0.03微升[校正后]毫升⁻¹、0.67毫摩尔和0.63毫摩尔。樟脑和其他测试化合物(香叶醇、芳樟醇和γ-萜品烯)的效力较低(樟脑IC50:>10毫摩尔)。发现精油、α-蒎烯、1,8-桉叶素和樟脑是无竞争性可逆抑制剂。这些发现表明,如果精油的抑制活性主要归因于所鉴定的主要抑制性萜类成分,那么这些成分之间存在主要的协同效应。由于所测试的单一成分都不是特别有效,这些体外胆碱酯酶抑制活性是否与摄入薰衣草叶鼠尾草精油对脑乙酰胆碱酯酶活性的体内效应相关,仍有待确定。