Huperzine A, a potential therapeutic agent for treatment of Alzheimer's disease

Curr Med Chem. 2000 Mar;7(3):355-74. doi: 10.2174/0929867003375281.


HupA is a potent, reversible and selective inhibitor of AChE with a rapid absorption and penetration into the brain in animal tests. It exhibits memory-enhancing activities in animal and clinical trials. Compared to tacrine and donepezil, HupA possesses a longer duration of action and higher therapeutic index, and the peripheral cholinergic side effects are minimal at therapeutic doses. This review article deals with a comprehensive survey of the progress in chemical and pharmacological studies of HupA including the isolation and structure elucidation, pharmacological actions, total synthesis, SAR studies and the future development of HupA. Recently, it has been reported that HupA could reduce neuronal cell death caused by glutamate. The dual bio-activities of HupA would further enhance its value and potentiality as the therapeutic agent for Alzheimer s disease.

Publication types

  • Review

MeSH terms

  • Acetylcholine / physiology
  • Alkaloids
  • Alzheimer Disease / drug therapy*
  • Animals
  • Brain / drug effects
  • Brain / physiology
  • Cholinesterase Inhibitors / chemical synthesis
  • Cholinesterase Inhibitors / isolation & purification
  • Cholinesterase Inhibitors / pharmacology*
  • Cholinesterase Inhibitors / therapeutic use
  • Cholinesterases / drug effects
  • Cognition / drug effects
  • Cognition / physiology
  • Drugs, Chinese Herbal / isolation & purification
  • Drugs, Chinese Herbal / pharmacology
  • Haplorhini
  • Humans
  • Rats
  • Sesquiterpenes / chemical synthesis
  • Sesquiterpenes / isolation & purification
  • Sesquiterpenes / pharmacology*
  • Sesquiterpenes / therapeutic use
  • Stereoisomerism
  • Structure-Activity Relationship


  • Alkaloids
  • Cholinesterase Inhibitors
  • Drugs, Chinese Herbal
  • Sesquiterpenes
  • huperzine A
  • Cholinesterases
  • Acetylcholine