Huperzine A: Is it an Effective Disease-Modifying Drug for Alzheimer’s Disease?

Abstract

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder for which there is no cure. Huperzine A (HupA) is a natural inhibitor of acetylcholinesterase (AChE) derived from the Chinese folk medicine Huperzia serrata (Qian Ceng Ta). It is a licensed anti-AD drug in China and is available as a nutraceutical in the US. A growing body of evidence has demonstrated that HupA has multifaceted pharmacological effects. In addition to the symptomatic, cognitive-enhancing effect via inhibition of AChE, a number of recent studies have reported that this drug has “non-cholinergic” effects on AD. Most important among these is the protective effect of HupA on neurons against amyloid beta-induced oxidative injury and mitochondrial dysfunction as well as via the up-regulation of nerve growth factor and antagonizing N-methyl-d-aspartate receptors. The most recent discovery that HupA may reduce brain iron accumulation lends further support to the argument that HupA could serve as a potential disease-modifying agent for AD and also other neurodegenerative disorders by significantly slowing down the course of neuronal death.

Natural Products & Complementary Medicines: where are we up to?

“…Moreover, these findings are further supported by clinical studies conducted recently in which G. biloba shows potential benefit in patients with Alzheimer's disease, including the improvement of cognitive function and activities of daily living (Yang, Wang et al 2016). Also, natural compounds antagonizing glutamate receptors are reported such as huperzine A, derived from Huperzia serrata (Qian and Ke 2014).…”

Molecular Evolution and Functional Characterization of a Bifunctional Decarboxylase Involved in Lycopodium Alkaloid Biosynthesis

“…Whole plants from the families Huperziaceae and Lycopodiaceae have been used in Chinese folk medicine for the treatment of various symptoms . Huperzia serrata produces huperzine A (HupA), a promising candidate drug for the treatment of Alzheimer's disease, owing to its function as a potent acetylcholinesterase inhibitor (Wang et al, 2009;Qian and Ke, 2014). HupA and its derivative ZT-1 have been evaluated in clinical trials for the treatment of Alzheimer's disease Jia et al, 2013).…”

Cholinesterase Inhibitors

“…Huperzine A is a cholinesterase inhibitor that is derived from the Chinese folk medicine Huperzia serrata (Qian & Ke, 2014). It is licensed in China as a treatment for Alzheimer' s disease and is available in the US as a nutraceutical (not regulated by the US Food and Drug Administration).…”