Huperzine A

Huperzine A (HupA), extracted from a club moss (Huperzia
serrata), is a sesquiterpene alkaloid and a powerful and
reversible inhibitor of acetylcholinesterase (AChE) with on- and
off-rates. [6,8] Huperzia has been used in China for centuries for
the treatment of swelling, fever and blood disorders. It has
demonstrated both memory enhancement in animal and clinical
trials and neuroprotective effects.

Huperzine A has been found to have benefits of reversing or
attenuating cognitive deficits in a broad range of animal models.
Clinical trials have demonstrated that Huperzine A relieves
memory deficits in aged subjects, patients with benign senescent
forgetfulness, Alzheimer's disease and vascular dementia, with
minimal peripheral cholinergic side effects compared with other
AChEIs in use.

L-Huperzine-A was administered systemically or locally through
the microdialysis probe into the rat cortex. In both cases,
acetylcholine, norepinephrine and dopamine levels were
increased significantly. Thus, L-Huperzine-A is a potent inhibitor
of cholinesterase which penetrates into the brain and produces a
dose-dependent increase of acetylcholine, morepinephrine, and
dopamine in rat cortex.

Huperzine A has undergone double-blind, placebo-controlled
clinical trials in patients with Alzheimer's disease (AD), with
significant improvements both to cognitive function and the
quality of life.

Safety and Side Effects of Huperzine A

Animal and clinical safety tests showed that Huperzine A had no
unexpected toxicity, particularly the dose-limiting hepatotoxicity
induced by tacrine. The phase IV clinical trials in China have
demonstrated that Huperzine A significantly improved memory
deficits in elderly people with benign senescent forgetfulness,
and patients with Alzheimer disease and vascular dementia, with
minimal peripheral cholinergic side effects and no unexpected
toxicity. Huperzine A can also be used as a protective agent
against organophosphate intoxication.

Medications that prevent acetylcholine breakdown often produce
side effects, including nausea, vomiting, excess saliva and tear
production, and sweating. In a study of 56 patients suffered from
dementia, a few patients felt slight dizziness.

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Huperzine A

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"Victoria crater" Image Credit: NASA/JPL/Cornell SPACE

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