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Huperzine

from the Pharmacology of Chinese Herbs (2e)

by Kee Chang Huang (CRC, 1999)

 

An alkaloid isolated from the root of Hyperzia serrata (Thunb.) Trev.

 

Chemistry: Several alkaloids have been isolated from Hyperzia.

Huperzine A is the one mostly used. A synthetic product has just been

introduced to replace the natural product.

 

Actions: Huperzine A is a novel potent reversible and selective AChE

inhibitor. The antiAChE activity of huperzine A is more potent than

that of physostigmine and galanthamine, with an IC50, of 0.11 uM/l.

Synthetic racemic huperzine A is 3 times less potent than the natural

product, huperzine A. Huperzine A can penetrate the blood brain

barrier (BBB) rapidly and protect nerve tissue against nerve gas

poisoning. The protective effect lasts at least 6 h after a single

injection.

 

In experiments with rats receiving an intracerebroventricular

injection of AF64A, an anticholine acetyltransferase agent, they

subsequently exhibited an Alzheimerlike syndrome. Xiong et al.z2

treated these animals with huperzine A at a dose of 0.4 to 0.5 mg/kg

intraperitoneally. It significantly ameliorates the AF64A induced

memory deficit in these animals. The authors also reported that

huperzine A can reverse the scopolamine induced deficit in memory

function of rats. Huperzine A, both the natural and synthetic racemic

analogs, is found to be an active cognition enhancer; it can

facilitate memory and motor activity in aged persons.

 

Xu et al gave huperzine A tablets to 56 patients with AD at a dose of

one 0.2 mg tablet 4 times daily for 2 weeks, as compared with the

placebo group. Patients who received huperzine A showed a definite

improvement in memory, cognition, and behavior, with no serious side

effects.

 

Studies of the effect of huperzine A on the endplate potential of the

neuromuscular junction have shown that this agent can increase the

endplate potential and prolong the potential rise time. " The potency

of such an effect is in the following order: E2020 is greater than

huperzine A, which is then greater than tacrine. In microdialysis

studies, huperzine A administration can increase norepinephrine,

dopamine, and acetylcholine levels in the brain tissues

significantly, but with little change in the 5HT level.

 

Pharmacokinetic Studies: Huperzine A is absorbed rapidly from the

intestine, distributed widely in the holy, and eliminated at a

moderate rate from the kidney.

 

Adverse Effects: Similar to other cholinergic mimetic agents,

Huperzine A causes gastrointestinal disturbances and dizziness.

Unline tacrine, no hepatic damage has been reported in patients

taking Huperzine A or its synthetic analog.

 

Therapeutic Uses: Huperzine A has been recommended in the treatment

of senile dementia, including Alzeheimer disease and multi-infarct

dementia. A definite improvement has been observed. it is also

claimed that Huperzine A is effective in patients suffering from

myasthenia gravis.

 

 

 

 

 

 

 

 

 

, " Luke Klincewicz "

<l.klincewicz@w...> wrote:

> TY,

>

> luke

>

>

> , Philip Riviere

<riviere@p...>

> wrote:

> > At 11:33 PM 5/11/00 -0000, Luke Klincewicz wrote:

> > hello all,

> >

> > is anyone here familiar with the use of Huperzia serrata in East

> > Asian herbal medicine? It's in a Physiologics formula combined

> with

> > Vinpocetine, as is purported to be a memory enhancer.

> >

> >

> > To All members,

> >

> >

> > Translated from: Precise of <Chinese Materia Medica> (Xinhua

Bencao

> Gangyao)

> > 3rd volume (Shanghai kexue jishu chubanshe> 1st edition 1990

> (p.620)

> >

> > QIAN CENG TA (Zhiwu mingshi tukao, Qing dynasty) =

> >

> > Huperzia serrarta (Thunb.) Trev. ______ Lycopodium serratum

Thunb.

> >

> > Flavor (wei):bitter (ku) astringent (se)

> > Nature (xing): cool (liang)

> >

> > " toxic " (youdu)

> >

> > Functions (gongneng):

> > dissipate stasis(sanyu) disperse swelling (xiaozhong),

> > sta(u)nch bleeding (zhixue) engender flesh (shengji)

> > disperse inflammation (xiaoyan) resolve toxins (jiedu)

> > anesthetize (mazui) settle pain (zhentong)

> > destroy fleas (mieshi)

> >

> > (Internal) Use: in " knocks and falls " (dieta)/ traumas

(sunshang)/

> stasis

> > pain with swelling (yuxue zhongtong), sciatica pain

(zuogushenjing

> tong),

> > nervous headaches (shenjingxing toutong)and all severe pain

related

> to

> > biliary calculi (danjieshi jutong)

> >

> > External use:for treatment of abscesses (yongju)/ sores and boils

> > (chuangjie)/ scalds (tanghuo shang)

> > anti-fleas (mieshi) and anti-cimices (bedbugs) (chouchong).

> >

> > Internal use, don't overdose (neifu buyi guoliang)

> > Don't use during pregnancy (funu jifu)

> >

> >

> > PS

> > Last year(?),the American Botanical Council Journal reported some

> research

> > done in the treatment of Alzheimer's disease using Huperzia.

> >

> >

> >

> > Philippe Riviere

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