Original Article

Anti-cholinesterase activity of huperzine A

Yue-e WANG, Dong-xian YUE, Xi-an TANG


It was studied in vitro that the inhibitory effect of huperzine A (Hup, [(5R,9R,11E)-5-amino-11-ethylidene-5,6,9,10-tetrahydro-7-methyl-5,9-methanocycloocteno[b]pyridine-2(1H)-one]), a new alkaloid extracted from huperzia serrata in 1982 by LIU, on ChE and its mode of action by using Ellman method for determination of ChE activity. Rat erythrocyte membrane and caudate nuclei of pig were used as sources of acetylcholinesterase (AChE) and rat serum was chosen as source of butyrocholinesterase (BuChE),. It was found that Hup exerted a potent inhibitory effect on ChE. The pI50 (negative logarithm of molar concentration causing 50% inhibition of ChE) of Hup towards erythrocyte membrane and caudate nuclei AChE were 7.2 and 7.9, respectively. The inhibitory effect of Hup was about 3 times more potent than that of physostigmine with AChE, but less than that of physostigmine when test with serum (BuChE), so Hup exhibited a more high selectivity towards the true ChE. It demonstrated that Hup belonged to the mixed and reversible ChE inhibitor. The results suggested that Hup might be useful in the treatment of some disease in clinic.

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