title: Huperzine A as a neuroprotective and antiepileptic drug: a review of preclinical research.
abstract: Huperzine A (HupA) is an acetylcholinesterase (AChE) inhibitor extracted from Huperzia Serrata, a firmoss, which has been used for various diseases in traditional Chinese medicine for fever and inflammation. More recently, it has been used in Alzheimer's disease and other forms of dementia with a presumed mechanism of action via central nicotinic and muscarinic receptors. HupA is marketed as a dietary supplement in the U.S. This article reviews newly proposed neuroprotective and anticonvulsant HupA properties based on animal studies. HupA exerts its effects mainly via α7nAChRs and α4β2nAChRs, thereby producing a potent anti-inflammatory response by decreasing IL-1β, TNF-α protein expression, and suppressing transcriptional activation of NF-κB signaling. Thus, it provides protection from excitotoxicity and neuronal death as well as increase in GABAergic transmission associated with anticonvulsant activity.
authors.affiliation: a F.M. Kirby Neurobiology Center, Department of Neurology , Boston Children's Hospital, Harvard Medical School , Boston , MA , USA.
authors.forename: U
authors.initials: U
authors.lastname: Damar
authors.affiliation: a F.M. Kirby Neurobiology Center, Department of Neurology , Boston Children's Hospital, Harvard Medical School , Boston , MA , USA.
authors.forename: R
authors.initials: R
authors.lastname: Gersner
authors.affiliation: b Research and Development - Neurology , Biscayne Pharmaceuticals, Inc ., Miami , FL , USA.
authors.forename: J T
authors.initials: JT
authors.lastname: Johnstone
authors.affiliation: c Departments of Neurology, Beth Israel Deaconess Medical Center, Massachusetts General Hospital , Harvard Medical School , Boston , MA , USA.
authors.forename: S
authors.initials: S
authors.lastname: Schachter
authors.affiliation: a F.M. Kirby Neurobiology Center, Department of Neurology , Boston Children's Hospital, Harvard Medical School , Boston , MA , USA.
authors.forename: A
authors.initials: A
authors.lastname: Rotenberg
mesh_terms: D000470:Alkaloids / Q000627:therapeutic use; D000818:Animals; D000927:Anticonvulsants / Q000627:therapeutic use; D002800:Cholinesterase Inhibitors / Q000494:pharmacology; D004827:Epilepsy / Q000188:drug therapy*; D006801:Humans; D018696:Neuroprotective Agents / Q000627:therapeutic use; D012717:Sesquiterpenes / Q000627:therapeutic use
chemical_list: D000470:Alkaloids; D000927:Anticonvulsants; D002800:Cholinesterase Inhibitors; D018696:Neuroprotective Agents; D012717:Sesquiterpenes; C050426:huperzine A
keywords: GABAergic transmission; Huperzine A; acetylcholinesterase; excitotoxicity; neuroprotection; nicotinic receptors