Cholinesterase inhibitors from Cleistocalyx operculatus buds.
Five flavonoids, myricetin-3'-methylether 3-O-β-D: -galactopyranoside (1), myricetin-3',5'-dimethylether 3-O-β-D: -galactopyranoside (2), quercetin (3), kaempferol (4), and tamarixetin (5) were isolated from the buds of Cleistocalyx operculatus (Myrtaceae). The chemical structures of these compounds were determined on the basis of spectroscopic analyses, including 2D NMR. Their anti-Alzheimer effects were evaluated via acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity assays. All five compounds 1-5 showed potential inhibitory activities against AChE with IC(50) values of 19.9, 37.8, 25.9, 30.4 and 22.3 μM, respectively, while compounds 1, 3, 4 and 5 also possessed BChE inhibitory activity with IC(50) values of 152.5, 177.8, 62.5, and 160.6 μM, respectively.
College of Pharmacy, Catholic University of Daegu, Gyeongsan, Korea. bsmin@cu.ac.kr
Byung Sun
BS
Min
To Dao
TD
Cuong
Joo-Sang
JS
Lee
Beom-Soo
BS
Shin
Mi Hee
MH
Woo
Tran Manh
TM
Hung
D000544:Alzheimer Disease / Q000188:drug therapy; D002091:Butyrylcholinesterase; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D055808:Drug Discovery; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D035264:Flowers / Q000737:chemistry*; D005690:Galactose / Q000032:analysis / Q000737:chemistry; D006027:Glycosides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009904:Optical Rotation; D009994:Osmolar Concentration; D021241:Spectrometry, Mass, Electrospray Ionization; D013056:Spectrophotometry, Ultraviolet; D017550:Spectroscopy, Fourier Transform Infrared; D027842:Syzygium / Q000737:chemistry*
D002800:Cholinesterase Inhibitors; D005419:Flavonoids; D006027:Glycosides; D002091:Butyrylcholinesterase; D005690:Galactose