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Expert Rev Neurother. 2016 Jun;16(6):671-80. doi: 10.1080/14737175.2016.1175303. Epub 2016 Apr 20.

Huperzine A as a neuroprotective and antiepileptic drug: a review of preclinical research.

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a F.M. Kirby Neurobiology Center, Department of Neurology , Boston Children's Hospital, Harvard Medical School , Boston , MA , USA.
b Research and Development - Neurology , Biscayne Pharmaceuticals, Inc ., Miami , FL , USA.
c Departments of Neurology, Beth Israel Deaconess Medical Center, Massachusetts General Hospital , Harvard Medical School , Boston , MA , USA.


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.


GABAergic transmission; Huperzine A; acetylcholinesterase; excitotoxicity; neuroprotection; nicotinic receptors

[Indexed for MEDLINE]

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