Department of Pharmaceutical Sciences, Faculty of Pharmacy, Nutrition and Health Sciences, University of Calabria, Rende (CS), Italy.
J Enzyme Inhib Med Chem. 2010 Oct;25(5):622-8. doi: 10.3109/14756360903389856.
This study aimed to investigate the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity of the essential oils from Pinus nigra subsp. nigra, P. nigra var. calabrica, and P. heldreichii subsp. leucodermis. This activity is relevant to the treatment of Alzheimer's disease (AD), since cholinesterase drugs are currently the only drugs available to treat AD. P. heldreichii subsp. leucodermis exhibited the most promising activity, with IC(50) values of 51.1 and 80.6 microg/mL against AChE and BChE, respectively. An interesting activity against AChE was also observed with P. nigra subsp. nigra essential oil, with an IC(50) value of 94.4 microg/mL. Essential oils were analyzed by GC and GC-MS with the purpose of investigating their relationships with the observed activities. Among the identified constituents, terpinolene, beta-phellandrene, linalyl acetate, trans-caryophyllene, and terpinen-4-ol were tested. trans-Caryophyllene and terpinen-4-ol inhibited BChE with IC(50) values of 78.6 and 107.6 microg/mL, respectively. beta-Phellandrene was selective against AChE (IC(50) value of 120.2 microg/mL).
本研究旨在探讨黑松(Pinus nigra subsp. nigra)、卡拉布里亚黑松(P. nigra var. calabrica)和希氏松(P. heldreichii subsp. leucodermis)精油对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)的抑制活性。这种活性与阿尔茨海默病(AD)的治疗有关,因为胆碱酯酶抑制剂类药物是目前唯一可用于治疗 AD 的药物。希氏松(P. heldreichii subsp. leucodermis)表现出最有前途的活性,对 AChE 和 BChE 的 IC50 值分别为 51.1 和 80.6μg/mL。黑松(P. nigra subsp. nigra)精油也表现出有趣的 AChE 抑制活性,IC50 值为 94.4μg/mL。通过 GC 和 GC-MS 对精油进行分析,目的是研究它们与观察到的活性之间的关系。在所鉴定的成分中,松油萜、β-水芹烯、乙酸芳樟酯、反式石竹烯和萜品-4-醇进行了测试。反式石竹烯和萜品-4-醇对 BChE 的抑制 IC50 值分别为 78.6 和 107.6μg/mL。β-水芹烯对 AChE 具有选择性(IC50 值为 120.2μg/mL)。