Savelev S, Okello E, Perry N S L, Wilkins R M, Perry E K
School of Biology, University of Newcastle, Ridley building, Newcastle upon Tyne, NE1 7RU, UK.
Pharmacol Biochem Behav. 2003 Jun;75(3):661-8. doi: 10.1016/s0091-3057(03)00125-4.
In vitro anticholinesterase activities of eight commercially available terpenoid constituents of Salvia lavandulaefolia have been investigated. These included 1,8-cineole, camphor, alpha-pinene, beta-pinene, borneol, caryophyllene oxide, linalool and bornyl acetate. Dose-dependent inhibition of acetylcholinesterase (AChE) by these chemical constituents was determined using the method of Ellman [Biochem. Pharmacol. 7 (1961) 88]. The IC50 value of 1,8-cineole was 0.06+/-0.01 mg/ml similar to that of the essential oil (0.05+/-0.01 mg/ml). Analyses of the expected inhibitions based on the prediction of a zero interactive response of a combination at its naturally occurring ratios were carried out in comparison with observed inhibition. Minor synergy was apparent in 1,8-cineole/alpha-pinene and 1,8-cineole/caryophyllene oxide combinations, with interaction indexes not exceeding 0.5. In contrast, a combination of camphor and 1,8-cineole was antagonistic with an interaction index of 2. A combination of all eight compounds was zero interactive. A combination of six constituents, excluding 1,8-cineole and camphor, was used to compare the method of expected response of a combination with a method of summation. These findings reveal that the inhibitory activity of the oil results from a complex interaction between its constituents, which produce both synergistic and antagonistic responses between the component terpenes. Understanding such interactions is important in comparing species on the basis of chemical composition.
已对8种市售薰衣草叶鼠尾草萜类成分的体外抗胆碱酯酶活性进行了研究。这些成分包括1,8-桉叶素、樟脑、α-蒎烯、β-蒎烯、冰片、氧化石竹烯、芳樟醇和乙酸龙脑酯。采用埃尔曼法[《生物化学与药理学》7 (1961) 88]测定了这些化学成分对乙酰胆碱酯酶(AChE)的剂量依赖性抑制作用。1,8-桉叶素的IC50值为0.06±0.01 mg/ml,与精油的IC50值(0.05±0.01 mg/ml)相似。基于各成分按自然比例组合时零相互作用反应的预测,对预期抑制作用进行了分析,并与观察到的抑制作用进行了比较。1,8-桉叶素/α-蒎烯和1,8-桉叶素/氧化石竹烯组合中存在轻微协同作用,相互作用指数不超过0.5。相比之下,樟脑和1,8-桉叶素的组合具有拮抗作用,相互作用指数为2。所有8种化合物的组合零相互作用。使用排除1,8-桉叶素和樟脑的6种成分的组合,将组合预期反应方法与加和方法进行比较。这些发现表明,该精油的抑制活性源于其成分之间的复杂相互作用,这些成分在萜类成分之间产生协同和拮抗反应。了解此类相互作用对于基于化学成分比较不同物种很重要。