New insights into huperzine A for the treatment of Alzheimer's disease

Acta Pharmacol Sin. 2012 Sep;33(9):1170-5. doi: 10.1038/aps.2012.128. Epub 2012 Sep 3.


Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD). Accordingly, some new mechanisms of action for huperzine A have been discovered over the past decades. In addition to its AChE inhibitory effect, potent multifaceted neuroprotective effect through activating cholinergic system and directly acting on mitochondria have been explored. Moreover, in order to maximize the efficacy and safety of huperzine A therapy, great efforts have been made to optimize drug delivery system. In the present article, an attempt is made to discuss the current progress and future perspective for huperzine A therapy in AD.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / isolation & purification
  • Alkaloids / pharmacology*
  • Alkaloids / therapeutic use
  • Alzheimer Disease / drug therapy*
  • Alzheimer Disease / physiopathology
  • Animals
  • Cholinesterase Inhibitors / isolation & purification
  • Cholinesterase Inhibitors / pharmacology
  • Cholinesterase Inhibitors / therapeutic use
  • Drug Delivery Systems
  • Drugs, Chinese Herbal / pharmacology
  • Drugs, Chinese Herbal / therapeutic use
  • Humans
  • Lycopodium / chemistry*
  • Mitochondria / drug effects
  • Mitochondria / metabolism
  • Neuroprotective Agents / isolation & purification
  • Neuroprotective Agents / pharmacology
  • Neuroprotective Agents / therapeutic use
  • Sesquiterpenes / isolation & purification
  • Sesquiterpenes / pharmacology*
  • Sesquiterpenes / therapeutic use


  • Alkaloids
  • Cholinesterase Inhibitors
  • Drugs, Chinese Herbal
  • Neuroprotective Agents
  • Sesquiterpenes
  • huperzine A