Huperzine A improves muscle contraction; focus boost

Huperzine A (Huperzine Alpha, HupA) is a nootropic alkaloid purified from club moss Huperzia serrata, a herb used in Chinese folk medicine. Huperzine A is especially interesting for its cognitive enhancing and neuroprotective properties. Therefore, this alkaloid is also investigated for treatment of Alzheimer’s disease and dementia. As a bodybuilding supplement, Huperzine A is added to boost focus during workout.

Bioavailability and Absorption

Orally administered huperzine A starts to appear in plasma after 5-10 minutes and reaches a peak concentration at about one hour [1]. This [1] and one other study [2] reported rapid absorption and distribution with moderate elimination rate. Huperzine A has high oral bioavailability (96.9% in mice [24]) [3].

Effects of Huperzine A on Mental Functions

Huperzine A is reversible, potent, and selective anticholinesterase (the enzyme responsible for the breakdown of acetylcholine) inhibitior [4-6,18]. As a result, more acetylcholine is available in the brain, thus increasing the efficacy of the remaining cholinergic neurons.

Significantly improved cognition was reported in 78 patients with mild to moderate vascular dementia when compared to placebo [7]. In 34 adolescent students complaining of memory inadequacy enhanced memory and learning performance was markedly elevated after 4 weeks of 50 mcg of huperzine A administration [8].

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Treatment of Alzheimer’s Disease

A review (6 trials with a total 454 patients) [9] evaluating huperzine A for treatment of Alzheimer’s disease reported that huperzine A is superior to placebo for patients with AD. Huperzine appeares to improve global cognitive function, behavioral disturbance, and functional performance. However, most studies included in a review were of a poor methodological quality. A more recent review (2011) [10] concluded that the current clinical evidence in support of the use of huerzine A in AD is still inconclusive or inadequate.

One high-quality large-scale randomized controlled trial [11] reported remarkably improved cognition, behavior and mood in patients with mild to moderate AD. However, in this study Huperzine A was stacked with Vitamin E which might have triggered a synergistic effect. Furthermore, phase IV clinical trials in China reported significantly improved memory of elderly people and patients with Alzheimer’s disease and vascular dementia [19-22].

Preclinical and clinical findings suggest that HupA is a promising candidate for the treatment of neurodegenerative diseases [18,23].

Antioxidant Action

Studies [12,13,23] even reported that Huperzine A scavenges free radicals in the brain.

Huperzine A as Bodybuilding Supplement

As a bodybuilding supplements huperzine A is used to boost focus during workouts. However, no studies examined its direct effect for this purpose nor were effects of huperzine A (or other anticholinesterase inhibitors [14]) adequately examined in healthy population.

Acetylcholine is also a critical neurotransmitter for muscle contractions [15]. Therefore, huperzine A was reported to significantly increase the amplitude of muscle contraction induced by stimulating nerve [16].

Works Well With…

Huperzine A is often stacked with choline (such as alpha-glyceryl phosphoryl choline [Alpha-GPC]) to further elevate the levels of neurotransmitter acetylcholine.

Dosage

Typical dose of huperzine A in bodybuilding supplements is 50 mcg. This dose also sufices for increased memory and learning [8]. Doses for AD treatment range from 200 to 500 micro g/day [11,17].

Side Effects and Toxicity

No serious adverse effects were reported in patients with AD after huperzine A administration [9]. In a study by Zhang Z et al. [11] huperzine A was regarded as safe. Animal and clinical safety tests showed that HupA had no unexpected toxicity [18].

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(Other common names: Huperzina A, Huperzine, Huperzine-A, Selagine, Huperzia serrata extract, club moss, Huperzia serrata leaf standardized extract, Toothed Clubmoss Extract)

References

1. Li, Y. X., et al. “Pharmacokinetics of huperzine A following oral administration to human volunteers.” European journal of drug metabolism and pharmacokinetics 32.4 (2007): 183-187.
2. Qian, Bo-Chu, et al. “Pharmacokinetics of tablet huperzine A in six volunteers.” Zhongguo yao li xue bao= Acta pharmacologica Sinica 16.5 (1995): 396-398.
3. Cheng, Dong Hang, and Xi Can Tang. “Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities.” Pharmacology Biochemistry and Behavior 60.2 (1998): 377-386.
4. Raves, Mia L., et al. “Structure of acetylcholinesterase complexed with the nootropic alkaloid,(-)-huperzine A.” Nature structural biology 4.1 (1997): 57-63.
5. Ashani, Yacov, James O. Peggins III, and Bhupendra P. Doctor. “Mechanism of inhibition of cholinesterases by huperzine A.” Biochemical and biophysical research communications 184.2 (1992): 719-726.
6. Liu, Jia-Sen, et al. “The structures of huperzine A and B, two new alkaloids exhibiting marked anticholinesterase activity.” Canadian Journal of Chemistry 64.4 (1986): 837-839.
7. Xu, Zhi-Qiang, et al. “Treatment with Hup A improves cognition in vascular dementia patients.” Cell biochemistry and biophysics 62.1 (2012): 55-58.
8. Sun, Qing-Qi, et al. “Huperzine-A capsules enhance memory and learning performance in 34 pairs of matched adolescent students.” Zhongguo yao li xue bao= Acta pharmacologica Sinica 20.7 (1999): 601-603.
9. Li, Jun, et al. “Huperzine A for Alzheimer’s disease.” Cochrane Database Syst Rev 2 (2008).
10. Fu, Li-Min, and Ju-Tzu Li. “A systematic review of single Chinese herbs for Alzheimer’s disease treatment.” Evidence-Based Complementary and Alternative Medicine 2011 (2011).
11. Zhang, Z., et al. “Clinical efficacy and safety of huperzine Alpha in treatment of mild to moderate Alzheimer disease, a placebo-controlled, double-blind, randomized trial.” Zhonghua yi xue za zhi 82.14 (2002): 941-944.
12. Xiao, Xiao Qiu, Jian Wei Yang, and Xi Can Tang. “Huperzine A protects rat pheochromocytoma cells against hydrogen peroxide-induced injury.” Neuroscience letters 275.2 (1999): 73-76.
13. Xiao, Xiao Qiu, et al. “Protective effects of hup A on β-amyloid 25–35 induced oxidative injury in rat pheochromocytoma cells.” Neuroscience letters 286.3 (2000): 155-158.
14. Repantis, Dimitris, Oona Laisney, and Isabella Heuser. “Acetylcholinesterase inhibitors and memantine for neuroenhancement in healthy individuals: a systematic review.” Pharmacological research 61.6 (2010): 473-481.
15. http://meat.tamu.edu/ansc-307-honors/muscle-contraction/
16. Tang, Xi Can, and Yi Fan Han. “Pharmacological profile of huperzine A, a novel acetylcholinesterase inhibitor from Chinese herb.” CNS Drug Reviews 5.3 (1999): 281-300.
17. Wang, Bai-song, et al. “Efficacy and safety of natural acetylcholinesterase inhibitor huperzine A in the treatment of Alzheimer’s disease: an updated meta-analysis.” Journal of neural transmission 116.4 (2009): 457-465.
18. Wang, Rui, and Han Yan. “Progress in studies of hup A, a natural cholinesterase inhibitor from Chinese herbal medicine1.” Acta Pharmacologica Sinica 27.1 (2006): 1-26.
19. Xu, Si-Sun, et al. “Efficacy of tablet huperzine-A on memory, cognition, and behavior in Alzheimer’s disease.” Zhongguo yao li xue bao= Acta pharmacologica Sinica 16.5 (1995): 391-395.
20. Xu, S. S., et al. “Efficacy of tablet huperzine-A on memory and cognition in patients with benign senescent forgetfulness.” Chin J Clin Pharmacol Ther 2.1 (1997): 1.
21. Xu, S. S., et al. “Huperzine-A in capsules and tablets for treating patients with Alzheimer disease.” Zhongguo yao li xue bao= Acta pharmacologica Sinica 20.6 (1999): 486-490.
22. Zhang, Z., et al. “[Clinical efficacy and safety of huperzine Alpha in treatment of mild to moderate Alzheimer disease, a placebo-controlled, double-blind, randomized trial].” Zhonghua yi xue za zhi 82.14 (2002): 941-944.
23. Little, John T., Sally Walsh, and Paul S. Aisen. “An update on huperzine A as a treatment for Alzheimer’s disease.” (2008): 209-215.
24. Wang, Y. E., et al. “Pharmacokinetics of huperzine A in rats and mice.” Zhongguo yao li xue bao= Acta pharmacologica Sinica 9.3 (1988): 193.