[Effects of metabolites of mangrove fungus Xylaria sp. from South China Sea Coast on the activity of acetylcholinesterase in vitro].
OBJECTIVE
To investigate the effects of metabolites of mangrove fungus Xylaria sp. from South China Sea Coast, xyloketal A-D, on the activity of acetylcholinesterase (AChE) in vitro.


METHODS
Activity of AChE was determined by a modified method of Ellmen. The selectivity of the compounds for AChE and butyrylcholinesterase (BuChE) was also tested and compared with that of a positive control, velnacrine. The inhibitory properties of xylokets on AChE were characterized as well.


RESULTS
AChE activity was inhibited by xyloketal A-D in a dose-dependent manner, their IC50 were determined to be 29.9, 137.4, 109.3 and 425.6 micromol/L, respectively. At the same time, velnacrine and all the four compounds showed inhibitory effects on BuChE in different degree, and the inhibitory activity of xyloketals on AChE was found to be reversible and noncompetitive.


CONCLUSIONS
Xyloketal A-D can inhibit AChE as well as BuChE activity in vitro. So xyloketal A-D were likely considered as drug candidates against Alzheimer' s disease (AD) for further development.
Jinghui
Luo
L
School of Chemistry and Chemical Engineering, Zhongshan University, Guangzhou 510275.
Yingbao
Yang
Y
Yongcheng
Lin
L
Zhiliang
Chen
C
Xiongyu
Wu
W
D000110:Acetylcholinesterase / Q000378:metabolism*; D001210:Asia, Southeastern; D002091:Butyrylcholinesterase / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005658:Fungi / Q000737:chemistry*; D066298:In Vitro Techniques; D008386:Marine Biology; D015394:Molecular Structure; D011714:Pyrans / Q000302:isolation & purification* / Q000494:pharmacology*
D002800:Cholinesterase Inhibitors; D011714:Pyrans; C438053:xyloketal A; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase