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KMID : 0043320140370091124
Archives of Pharmacal Research
2014 Volume.37 No. 9 p.1124 ~ p.1129
Cholinesterase inhibitors from the roots of Harpagophytum procumbens
Bae Yoon-Ho

Cuong To Dao
Hung Tran Manh
Kim Jeong-Ah
Woo Mi-Hee
Byeon Jeong-Su
Choi Jae-Sue
Min Byung-Sun
Abstract
Inhibition of cholinesterase has been proposed to be a therapeutic target for the treatment of Alzheimer¡¯s diseases. In our preliminary screening study on the acetylcholinesterase (AChE) inhibitory activity, an ethyl acetate soluble fraction of the roots of Harpagophytum procumbens (Pedaliaceae) was found to inhibit AChE activity at the concentration of 100 ¥ìg/mL. Ten compounds (1?10) were isolated from the active fraction and evaluated for their inhibitory effect on AChE and butyrylcholinesterase (BChE). Among the isolates, verbascosides (5, 6, and 8) containing a caffeoyl and a 3,4-dihydroxyphenethyl groups in their structures, showed effective AChE inhibitory activity and also possessed BChE inhibitory activity. The findings suggest that verbascoside derivatives may be partially related to the anti-Alzheimer effect of this medicinal plant.
KEYWORD
Harpagophytum procumbens, Pedaliaceae, AChE, BChE, Anti-Alzheimer effects
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