Acetylcholinesterase and butyrylcholinesterase inhibitory activity of Pinus species essential oils and their constituents.
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).
Bonesi
Marco
M
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Nutrition and Health Sciences, University of Calabria, Rende (CS), Italy.
Menichini
Federica
F
Tundis
Rosa
R
Loizzo
Monica R
MR
Conforti
Filomena
F
Passalacqua
Nicodemo G
NG
Statti
Giancarlo A
GA
Menichini
Francesco
F
D000110:Acetylcholinesterase; D000544:Alzheimer Disease / Q000188:drug therapy; D002091:Butyrylcholinesterase; D002800:Cholinesterase Inhibitors / Q000032:analysis* / Q000737:chemistry*; D055808:Drug Discovery; D008401:Gas Chromatography-Mass Spectrometry; D015394:Molecular Structure; D009822:Oils, Volatile / Q000737:chemistry*; D009994:Osmolar Concentration; D008517:Phytotherapy; D028223:Pinus / Q000737:chemistry*; D018515:Plant Leaves / Q000737:chemistry; D013729:Terpenes / Q000032:analysis* / Q000737:chemistry*
D002800:Cholinesterase Inhibitors; D009822:Oils, Volatile; D013729:Terpenes; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase