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Huperzine A |
Exciting break through new product to improve your memory, protect against premature brain aging, and even have a positive effect on mood.
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Huperzine A is an alkaloid derived from the chinese club moss,Qian Ceng Ta, scientifically known as Huperzia serrata (or Lycopodium serratum). This alkaloid is also found in Lycopodium selago. It has been an integral part of traditional Chinese medicine for centuries, and usage has included treatment of fevers, inflammation, and blood disorders.
Huperzine A is now gaining importance as a potential treatment for neurodegenerative disorders like Alzheimer's, dementia, and epilepsy. Huperzine A is also an important inhibitor of the neurotransmitter NMDA (N-methyl D-aspartate), which is a potent excitotoxin (brain chemicals (e.g., glutamate) that leads to prolonged excitation of brain neurons and ultimately results in death).
In addition to this, huperzine A also acts as an inhibitor of the enzyme acetylcholinesterase that is responsible for termination of synaptic neurotransmission. Though huperzine A is still not approved by the USFDA for pharmaceutical therapy, it is sold as a dietary supplement in the US. Increasing clinical studies, both in animals and humans, continue to show the many therapeutic benefits of this compound. Huperzine A is currently approved in China for the treatment of Alzheimer's disease.
Huperzine A is the only substance known to cross the blood-brain barrier and inhibit the action of acetylcholinesterase. Acetylcholinesterase acts by breaking down the neurotransmitter acetylcholine, thus terminating synaptic transmission between neurons in the brain. By inhibiting the activity of acetylcholinesterase, huperzine A indirectly leads to an increase in the concentration of acetylcholine, resulting in functional brain activity. This forms the basis for the therapeutic effects of huperzine A in treating dementias and other neurodegenerative diseases like Alzheimer's disease.
Due to its effect on acetylcholine, huperzine A is also used to improve memory and cognitive functions of the brain. Also, by acting as an indirect stimulator of acetylcholine, huperzine A also helps in treatment of the autoimmune muscle disorder, Mysathenia gravis, which is characterized by weak and fatigued muscles.
Additionally, by acting as an inhibitor of the neurotransmitter, NMDA (N-methyl D-aspartate), huperzine A protects the neurons from toxic effects of substances like glutamate, thus preventing occurence of seizures or epilepsy. Hence, it is quite evident that huperzine A helps maintain overall physiology of neurons by protecting them from toxic damage.
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Huperzine A has been an important component of traditional chinese medicine since 1980s. Huperzia serrata, apart from huperzine A, also produces huperzine B which is much less active than huperzine A. Ancient chinese medicine has found profound benefits of huperzine A in treating swellings and inflammations, fevers and blood diseases. It was also used as a stimulant of acetylcholine, thus leading to improved transmission of electrical signals between neurons in the brain. However, much of clinical research in the last 10 years has shown the extremely beneficial use of huperzine A in treating neurodegenerative disorders like Alzheimer's disease and dementias.
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Acetylcholinesterase inhibitor/Acetylcholine stimulator:
Huperzine A acts by inhibiting the activity of acetylcholinesterase that is responsible for breaking down the important neurotransmitter in brain, acetylcholine. Thus, by acting as an indirect stimulator of acetylcholine, huperzine A helps in healthy and proper transmission of nerve impulses or signals in the brain. By doing so, it also helps maintain the physiological balance of neurons in the brain.
Alzheimer's:
Huperzine A is gaining attention as a potential cure for Alzheimer's disease. While it has been approved in China for treatment of Alzheimer's, it is still awaiting approval by the USFDA. The first indication of beneficial effects of huperzine A in treating Alzheimer's disease came from a study done at the Zhejiang Medical University, Hangzhou, China in 1995. A double blind placebo-controlled study was done where Alzheimer's disease patients were administered 200 microgram/day of huperzine A for 8 weeks. About 58% of the subjects showed significant improvement in their cognitive and behavioral functions.
Another study done by the Chinese Academy of Medical Sciences in 2002 on 202 Alzheimer's patients showed that administration of 400 micrograms of huperzine A daily improved their behavioral and cognitive functions, thus leading to a significant improvement in their daily activities. It also seemed to increase the mobility of these patients.
Huperzine A has been found to be better than its chemical counterpart, tacrine (a chemically synthesized drug commonly used to treat Alzheimer's disease), due to the fact that huperzine exhibits fewer side effects than tacrine. Huperzine A also has very few serious side effects, and its dosage can safely be increased depending on the patient’s needs (versus tacrine, where an increase in dosage may lead to an increase in side effects). Recent studies also indicate the protective nature of huperzine against the toxic beta-amyloid plaques in brain, which are precursors to Alzheimer's disease.
Dementia:
Owing to its effect on acetylcholinesterase and subsequently, acetylcholine, huperzine A has also been implicated in treatment of dementias. Moreover, huperzine A has been shown to protect the nerve cells from glutamate toxicity, gas poisoning and oxidative stress.
Learning/Memory:
Huperzine A has been shown to protect the brain neuronal cells from oxidative stress, gas poisoning, and glutamate toxicity. These protective effects enhance the learning and memorization abilities of brain neuronal cells. Rat studies have shown that administration of 100-400 micrograms/day of huperzine A can lead to reversal of memory deficits in the brain.
Epileptic seizures:
Huperzine A has been shown to prevent onset of epileptic seizures due to its extensive activity on acetylcholine and acetylcholine receptors in the brain neuronal cells. Studies in rats have shown that huperzine prevents seizures by inhibiting the action of NMDA and thus protects the brain from its excitotoxic effects. Also, huperzine A protects the brain from organophosphorus toxicity, as in soman-induced toxicity and subsequent seizures.
Research on this subject:
Bai DL, Tang XC, He XC. Huperzine A, a potential therapeutic agent for treatment of Alzheimer's disease. Curr Med Chem. 2000;7(3):355–74.
Coleman BR, Ratcliffe RH, Oguntayo SA, et al. [+]-Huperzine A treatment protects against N-methyl-D-aspartate-induced seizure/status epilepticus in rats. Chem Biol Interact. 2008;175(1-3):387-95.
Haigh JR, Johnston SR, Peppernay A, et al. Protection of red blood cell acetylcholinesterase by oral huperzine A against ex vivo soman exposure: next generation prophylaxis and sequestering of acetylcholinesterase over butyrylcholinesterase. Chem Biol Interact. 2008;175(1-3):380-6.
Kelly BJ, Knopman DS. Alternative medicine and Alzheimer disease. Neurologist. 2008;14(5):299-306.
Lallement G, Veyret J, Masqueliez C, et al. Efficacy of huperzine in preventing soman-induced seizures, neuropathological changes and lethality. Fundam Clin Pharmacol. 1997;11(5):387-94.
Li J, Wu HM, Zhou RL, Liu GJ, Dong BR. Huperzine A for Alzheimer's disease. Cochrane Database Syst Rev. 2008;(2):CD005592.
Mazurek A. An open-label trial of huperzine A in the treatment of Alzheimer's disease. Alternat Ther. 2000;5(2):97-98.
Tonduli LS, Testylier G, Masqueliez C, et al. Effects of Huperzine used as pre-treatment against soman-induced seizures. Neurotoxicology. 2001;22(1):29-37.
Ved HS, Koenig ML, Dave JR, Doctor BP. Huperzine A, a potential therapeutic agent for dementia, reduces neuronal death caused by glutamate. Neuroreport. 1997;8(4):963-8.
Wang ZF, Tang LL, Yan H, Wang YJ, Tang XC. Effects of huperzine A on memory deficits and neurotrophic factors production after transient cerebral ischemia and reperfusion in mice. Pharmacol Biochem Behav. 2006;83(4):603-11.
Wang ZF, Wang J, Zhang HY, Tang XC. Huperzine A exhibits anti-inflammatory and neuroprotective effects in a rat model of transient focal cerebral ischemia. J Neurochem. 106(4):1594-603.
Xu SS, Gao ZX, Weng Z, et al. Efficacy of tablet huperzine-A on memory, cognition, and behavior in Alzheimer's disease. Zhongguo Yao Li Xue Bao. 1995;16(5):391-5.
Zangara A. The psychopharmacology of huperzine A: an alkaloid with cognitive enhancing and neuroprotective properties of interest in the treatment of Alzheimer's disease. Pharmacol Biochem Behav. 2003;75(3):675–86.
Zhang HY, Tang XC. Neuroprotective effects of huperzine A: new therapeutic targets for neurodegenerative disease. Trends Pharmacol Sci. 2006;27(12):619-25.
Zhang HY, Zheng CY, Yan H, et al. Potential therapeutic targets of huperzine A for Alzheimer's disease and vascular dementia. Chem Biol Interact. 2008;175(1-3):396-402.
United States National Library of Medicine Drug Information Portal for Huperzine A.
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Sources and Forms of Huperzine A: |
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The most common source of huperzine A is the chinese club moss Huperzia serrata also known as Lycopodium serratum. A study done by Ma and co-workers in 2005 showed that another club moss (belonging to the same family of Huperziaceae) indigenous to the US, Phlegmariurus carinatus, possessed much higher concentrations of huperzine A compared to H.serrata. Moreover, they also concluded that the concentration of huperzine A differed based on the geographical location, species, climatic conditions as well as in different parts of the same plant. The low yield of huperzine A from natural sources led to development of methods that would allow it to be synthesized chemically in the laboratory. Hence much of huperzine A these days is synthesized chemically in laboratories as a racemic mixture which is found to be much more potent than currently marketed drugs for Alzheimer's like physostigmine, but about 3 times less potent than naturally occuring huperzine A.
Ma X, Tan C, Zhu D, Gang DR. Is there a better source of huperzine A than Huperzia serrata? Huperzine A content of Huperziaceae species in China. J Agric Food Chem. 2005;53(5):1393-8.
Tang XC, Kindel GH, Kozikowski AP, Hanin I. Comparison of the effects of natural ans synthetic huperzine A on rat brain cholinergic function in vitro and in vivo. J Ethnopharmacol. 44(3):147-55.
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Recommended Dosage of Huperzine A: |
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While there is no clearcut dosage for huperzine A (since it is not yet approved by the USFDA), clinical trials show that 100 to 400 micrograms per day is sufficient in the treatment of Alzheimer's disease, Myasthenia gravis and dementias. However, just 200 micrograms/day is enough for enhancing learning and memorizing abilities.
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Safety and Side Effects of Huperzine A: |
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While there are few serious side effects, care must still be taken during the administration of huperzine A. Some individuals may have allergic reactions ranging from itchy skin, rashes, or hives. Huperzine has also been known to cause diarrhea, hyperactivity, and insomnia. Children and pregnant or lactating women should not take huperzine A as effects have not yet been studied.
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Frequently Asked Questions on Huperzine A: |
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Is a daily supplementary dose of huperzine A necessary?
There is currently no recommended dietary allowance (RDA) for huperzine A, and there are also no studies on the effects of long-term daily supplementation in healthy individuals. The majority of research on huperzine A has focused on the treatment of neurodegenerative disorders. Due to the small incidence of side effects, it may be safe for elderly persons at risk for neurodegenerative disorders to supplement with a minimum daily dosage. Consultation with a medical professional is always advised before starting any supplement regimen.
Can Huperzine A be used in the treatment of Alzheimer's disease?
Huperzine A is currently approved in China for the treatment of Alzheimer's and clinical studies have shown that administration of up to 400 micrograms/day of huperzine A improves mobility, cognitive and behavioral functions in Alzheimer's patients. Huperzine A has not yet been approved by the USFDA for treating Alzheimer’s in the United States, and is as present being marketed as a dietary supplement.
Bai DL, Tang XC, He XC. Huperzine A, a potential therapeutic agent for treatment of Alzheimer's disease. Curr Med Chem. 2000;7(3):355–74.
Ved HS, Koenig ML, Dave JR, Doctor BP. Huperzine A, a potential therapeutic agent for dementia, reduces neuronal death caused by glutamate. Neuroreport. 1997;8(4):963-8.
Xu SS, Gao ZX, Weng Z, et al. Efficacy of tablet huperzine-A on memory, cognition, and behavior in Alzheimer's disease. Zhongguo Yao Li Xue Bao. 1995;16(5):391-5.
Which is a better source of huperzine A - natural or synthetic?
Several studies have shown that there exists almost no significant difference in the efficacy and potency established by both synthetic and natural huperzine A. An in vitro (study conducted outside a living body, usually in laboratory ware) and in vivo (study comducted in a living body so that the exact effect in biologically active or physiological condition is known) study conducted by Tang and colleagues has shown that synthetic huperzine A is three times less potent than natural huperzine A but still much more potent than any of the current drugs being marketed for Alzheimer's treatment. Hanin’s study similarly demonstrated that synthetic huperzine A is less potent than natural huperzine A in treating dementias.
Hanin I, Tang XC, Kindel GL, Kozikowksi AP. Natural and synthetic huperzine A: effect on cholinergic function in vitro and in vivo. Ann N Y Acad Sci. 1993 Sep 24;695:304-6.
Tang XC, Kindel GH, Kozikowski AP, Hanin I. Comparison of the effects of natural and synthetic huperzine A on rat brain cholinergic function in vitro and in vivo. J Ethnopharmacol. 1994 Dec;44(3):147-55.
How does huperzine A work to treat dementias? How does it work to enhance learning and memorization abilities?
Huperzine A acts by blocking the action of acetylcholinesterase, preventing the degradation of specific neurotransmitters in the brain’s neuronal cells. By doing so, it increases the concentration of neurotransmitter acetylcholine, which then enhances the transmission of nerve impulses and signals between neurons in the brain. By facilitating active signal transmission between nerve synapses, huperzine A activates brain cells, thus allowing for treatment of dementias, as well as enhancement of learning and memorization skills.
Ved HS, Koenig ML, Dave JR, Doctor BP. Huperzine A, a potential therapeutic agent for dementia, reduces neuronal death caused by glutamate. Neuroreport. 1997;8(4):963-8.
Wang ZF, Tang LL, Yan H, Wang YJ, Tang XC. Effects of huperzine A on memory deficits and neurotrophic factors production after transient cerebral ischemia and reperfusion in mice. Pharmacol Biochem Behav. 2006;83(4):603-11.
Xu SS, Gao ZX, Weng Z, et al. Efficacy of tablet huperzine-A on memory, cognition, and behavior in Alzheimer's disease. Zhongguo Yao Li Xue Bao. 1995; (5):391-5.
Can huperzine A be used to treat epileptic seizures?
Though there are no human clinical trials to date - significant clinical evidence in rats and mice has shown that huperzine A is capable of preventing epileptic seizures. Studies in mice have shown that huperzine A acts by blocking another important brain neurotransmitter, NMDA, which is responsible for inducing seizures and epilepsy.
Coleman BR, Ratcliffe RH, Oguntayo SA, et al. [+]-Huperzine A treatment protects against N-methyl-D-aspartate-induced seizure/status epilepticus in rats. Chem Biol Interact. 2008;175(1-3):387-95.
Lallement G, Veyret J, Masqueliez C, Aubriot S, Burckhart MF, Baubichon D. Efficacy of huperzine in preventing soman-induced seizures, neuropathological changes and lethality. Fundam Clin Pharmacol. 1997;11(5):387-94.
Tonduli LS, Testylier G, Masqueliez C, et al. Effects of Huperzine used as pre-treatment against soman-induced seizures. Neurotoxicology. 2001;22(1):29-37.
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Additional Research on Huperzine A: |
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Huperzine A and Alzheimer's Disease
Kelley BJ, Knopman DS. Alternative medicine and Alzheimer disease. Neurologist. 2008 Sep;14(5):299-306.
Li J, Wu HM, Zhou RL, Liu GJ, Dong BR. Huperzine A for Alzheimer's disease. Cochrane Database Syst Rev. 2008 Apr 16;(2):CD005592.
Lin HQ, Ho MT, Lau LS, Wong KK, Shaw PC, Wan DC. Anti-acetylcholinesterase activities of traditional Chinese medicine for treating Alzheimer's disease. Chem Biol Interact. 2008 Sep 25;175(1-3):352-4.
Ma X, Gang DR. In vitro production of huperzine A, a promising drug candidate for Alzheimer's disease. Phytochemistry. 2008 Jul;69(10):2022-8.
Zhang HY, Zheng CY, Yan H, Wang ZF, Tang LL, Gao X, Tang XC. Potential therapeutic targets of huperzine A for Alzheimer's disease and vascular dementia. Chem Biol Interact. 2008 Sep 25;175(1-3):396-402.
Zhao JK, Wang DS. Progress of study on treatment of Alzheimer's disease with active ingredients of Chinese herbal medicines. Zhongguo Zhong Xi Yi Jie He Za Zhi. 2008 Feb;28(2):177-81.
Huperzine A and Memory
Chu D, Tian J, Liu W, Li Z, Li Y. Poly(lactic-co-glycolic acid) microspheres for the controlled release of huperzine A: in vitro and in vivo studies and the application in the treatment of the impaired memory of mice. Chem Pharm Bull (Tokyo). 2007 Apr;55(4):625-8.
Wang C, Zhang T, Ma H, Liu J, Fu F, Liu K. Prolonged effects of poly(lactic-co-glycolic acid) microsphere-containing huperzine A on mouse memory dysfunction induced by scopolamine. Basic Clin Pharmacol Toxicol. 2007 Mar;100(3):190-5.
Wang LS, Zhou J, Shao XM, Tang XC. Huperzine A attenuates cognitive deficits and brain injury after hypoxia-ischemic brain damage in neonatal rats. Zhonghua Er Ke Za Zhi. 2003 Jan;41(1):42-5.
Zhang SQ, Wang G, Luo GJ, Zhan H, Chen HW. Effects of huperzine A on cognitive function of rats recovering from general anesthesia. Nan Fang Yi Ke Da Xue Xue Bao. 2008 Feb;28(2):225-7.
Huperzine A and Epilepsy
Bialer M, Johannessen SI, Levy RH, Perucca E, Tomson T, White HS. Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX). Epilepsy Res. 2009 Jan;83(1):1-43.
Coleman BR, Ratcliffe RH, Oguntayo SA, Shi X, Doctor BP, Gordon RK, Nambiar MP. [+]-Huperzine A treatment protects against N-methyl-D-aspartate-induced seizure/status epilepticus in rats. Chem Biol Interact. 2008 Sep 25;175(1-3):387-95.
Tonduli LS, Testylier G, Masqueliez C, Lallement G, Monmaur P. Effects of Huperzine used as pre-treatment against soman-induced seizures.
Neurotoxicology. 2001 Feb;22(1):29-37.
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