Huperzia serrata (Thunb.) Trevis.

Last updated: 06 Apr 2017

Scientific Name

Huperzia serrata (Thunb.) Trevis.

Synonyms

Lycopodium javanicum Sw., Lycopodium sargassifolium Liebm., Lycopodium serratum Thunb., Urostachys javanicus (Sw.) Herter, Urostachys myriophyllifolius (Hayata) Herter, Urostachys serratus (Thunb.) Herter, Urostachys serratus (Thunb.) Herter ex Nessel, Huperzia selago var. serrata (Thunb.) Á. Löve & D. Löve, Huperzia serrata f. intermedia (Nakai) Ching, Huperzia serrata f. longipetiolata (Spring) Ching, Lycopodium serratum f. intermedium Nakai, Lycopodium serratum var. javanicum (Sw.) Makino, Lycopodium serratum var. longipetiolatum Spring, Lycopodium serratum var. myriophyllifolium Hayata, Lycopodium serratum var. thunbergii Makino, Urostachys serratus var. japonicaneotropicus Herter ex Nessel. [1]

Vernacular Name

English Chinese club-moss [2].

Geographical Distributions

Huperzia serrata can be found throughout China except parts of north and northwest China; Bhutan, Cambodia, India, Indonesia, Japan, Korea, Laos, Malaysia, Myanmar, Nepal, Philippines, Russia, Sri Lanka, Thailand, Vietnam; Australia, Central America, and Pacific islands. [3]

Botanical Description

H. serrata is a terrestrial plant that belongs to Lycopodiaceae family. [1][3]

The stem is erect or ascending, 10-30 cm, 1.5-3.5 mm in diameter at middle, together with leaves 1.5-4 cm wide, 2-4 times dichotomously branched, upper portion often with bulbils. [3]

The leaves are sparse, attached at right angles with stem, lustrous, narrowly elliptic, conspicuously contracted toward base, straight, 1-3 cm × 1-8 mm, thinly leathery, both surfaces glabrous, midrib conspicuously raised, base cuneate, decurrent, petiolate, margin straight and not crispate, irregularly toothed, apex acute or acuminate; teeth acute at apex, coarse or slightly small. Sporophylls homomorphic with trophophylls; sporangia visible on both sides of sporophylls, yellowish, reniform. [3]

Cultivation

H. serrata can be found in the forests, shrubs, and along the roadsides, from sea level up to 300-2700 m altitude. [3]

Chemical Constituent

H. serrata extract was found to contain (-)- huperzine A, [4][5] and alkaloid N-oxides (e.g. huperzine J, huperzine K , and huperzine L). [6]

Plant Part Used

No documentation.

Traditional Use

No documentation.

Preclinical Data

Pharmacology

Anticholinesterase activity

Huperzine A isolated from H. serrata has been reported to act as an acetylcholinesterase inhibitor similar to and as effective as pharmaceutical agents such as tacrine [7][8][9][10]. Data indicates that huperzine A binds to the enzyme acylation site in the active site gorge, but interferes slightly with the binding of peripheral site ligands [11].

Huperzine B isolated from H. serrata was found to exhibit higher selectivity in the inhibition of acetylcholinesterase, and lower toxicity in mice than tacrine. [12]

Antioxidative activity

The effects of huperzine A (HupA) isolated from H. serrata on Abeta(25-35)-induced cell lesion, level of lipid peroxidation, antioxidant enzyme activities were investigated in rats PC12 and primary cultured cortical neurons. Following a 48 h exposure of the cells to Abeta(25-35), a significant reduction in cell survival and activities of glutathione peroxidase (GSH-Px) and catalase (CAT), as well as increased production of malondialdehyde (MDA) and superoxide dismutase (SOD) were observed. The results indicate that HupA has protective effects against Abeta-induced cell toxicity, which might be beneficial for the treatment of Alzheimer's disease. [13][14][15]

Neuroprotective activity

Huperzine A was reported to exhibit potent acetylcholinesterase inhibitor, with a potential for reversing organophosphate poisoning and decreasing the seizures seen with this type of poisoning. Huperzine A may be beneficial in treating the seizures associated with organophosphate poisoning in part due to a protective effect of both peripheral and central acetylcholine stores. [16]

Another study reported neuroprotective effects of huperzine A, not only where cholinergic neurons are impaired, but also under conditions in which glutamatergic functions are compromised. [17]

Toxicity

No documentation.

Clinical Data

Clinical findings

Anticholinesterase activity

Huperzine A, an alkaloid that isolated from H. serrata was found to exhibit a significant anticholinesterase activity and has been used on myasthenia gravis patients. The therapeutic effects were studied by random, match and double-blind method on 56 patients of multi-infarct dementia or senile dementia and 104 patients of senile and presenile simple memory disorders. The result showed that the curative effect of huperzine A was significant. Only a few patients felt slight dizziness and this did not affect the therapeutic effects. [18][19]

Human study that has been performed using huperzine A (HupA) showed that both HupA in capsules and tablets have equal efficacy and safety for treating patients with Alzheimer disease (AD). [20]

Human study in China found that pre-treatment of patients before surgery with huperzine A produced a positive benefit on cerebral cholinergic system during recovery. [21]

Pharmacokinetic activity

One study measured the pharmacokinetics of huperzine A isolated from H. serrata in six patients, reporting rapid absorption, wide distribution in the body, and elimination at a moderate rate. [22]

Side effects

Transient side effects such as dizziness may occur. [23]

Interaction & Depletion

Interaction with drug

Studies report that huperzine A may act in the body like some of these medications, which may alter the effects of these medications and possibly the dose needed for treatment. These drugs include tacrine, donepezil, rivastigmine, galantamine. Use with caution. [7][12]

Interaction with other Herbs

No documentation.

Contraindications

No documentation.

Dosage

Dosage Range

Huperzine A has been studied at oral dosages of 0.2 to 0.4 mg/day for Alzheimer disease. [24]

Poisonous Management

No documentation.

Line drawing

No documentation.

References

  1. The Plant List. Ver1.1. Huperzia serrata (Thunb.) Trevis. [homepage on the Internet]. c2013 [updated 2012 April 18; cited 2017 Apr 06]. Available from: http://www.theplantlist.org/tpl1.1/record/tro-26621719.
  2. Quattrocchi U. CRC world dictionary of plant names: common names, scientific names, eponyms, synonyms, and etymology. Volume III E-L. Boca Raton, FL: CRC Press LLC, 1999; p. 510.
  3. Flora of China. Huperzia serrata (Thunberg) Trevisan. [homepage on the Internet]. No date [cited 2017 Apr 06]. Available from: http://www.efloras.org/florataxon.aspx?flora_id=2&taxon_id=200002712.
  4. Raves ML, Harel M, Pang YP, Silman I, Kozikowski AP, Sussman JL. Structure of acetylcholinesterase complexed with the nootropic alkaloid, (-)-huperzine A. Nat Struct Biol. 1997;4;57-63.
  5. Pepping J. Huperzine A. Am J Health Syst Pharm. 2000;57(6):530-534.
  6. Gao W, Li Y, Jiang S, Zhu D. Three lycopodium alkaloid N-oxides from Huperzia serrata. Planta Med. 2000;66(7):664-667.
  7. Cheng DH, Ren H, Tang XC. Huperzine A, a novel promising acetylcholinesterase inhibitor. Neuroreport. 1996;8(1):97-101.
  8. Carlie PR, Du DM, Han Y, Liu J, Pang YP. Potent, easily synthesized huperizne A-tacrine hybrid acetylcholinesterase inhibitors. Bioorg Med Chem Lett. 1999;9(16):2335-2338.
  9. Barril X, Orozco M, Luque FJ. Predicting relative binding free energies of tacrine-huperzine A hybrids as inhibitors of acetylcholinesterase. J Med Chem. 1999;42(45):5110-5119.
  10. Carlier PR, Du DM, Han Y, Liu J, Pang YP. Potnt, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors. Bioorg Med Chem Lett. 1999;9(16):2335-2338.
  11. Champs P, Cusack B, Mallnder WD, et al. Huprine X is a novel high-affinity inhibitor of acetylcholinesterase that is of interest for treatment of Alzheimer’s disease. Mol Pharmacol. 2000;57(2):409-417.
  12. Liu J, Zhang HY, Wang LM, Tang XC. Inhibitory effects of huperzine B on cholinesterase activity in mice. Zhongguo Yao Li Xue Bao. 1999;20(2):141-145.
  13. Xiao XQ, Wang R, Han YF, Tang XC. Protective effects of huperzine A on beta-amyloid(25-35) induced oxidative injury in rat pheochromocytoma cells. Neurosci Lett. 2000;286(3):155-158.
  14. Xiao XQ, Wang R, Tang XC. Huperzine A and tacrine attenuate beta-amyloid peptide-induced oxidative injury. J Neurosci Res. 2000;61(5):564-569.
  15. Xiao WQ, Zhang HY, Tang XC. Huperzine A attenuates amyloid beta-peptide fragment 25-35-induced apoptosis in rat cortical neurons via inhibiting reactive oxygen species formation and caspase-3 activation. J Neurosci Res. 2002;67(1):30-36.
  16. Lallement G, Veyret J, Masqueliez C, Aubriot S, Burchhart MF, Baubichon D. Efficacy of huperzine in preventing soman-induced seizures, neuropathological changes and lethality. Fundam Clin Pharmacol. 1997;11(5):387-394.
  17. Ved HS, Koenig ML, Dave JR, Doctor BP. Huperzine A, a potential therapeutic agent for dementia, reduces neuronal cell death caused by glutamate. Neuroreport. 1997;8(4):963-968.
  18. Zhang RW, Tang XC, Han YY, et al. [Drug evaluation of huperzine A in the treatment of senile memory disorders]. Zhongguo Yao Li Xue Bao. 1991;12(3):250-252.
  19. Pilotaz F, Masson P. [Huperzine A: An acetylcholinesterase inhibitor with high pharmacological potential]. Ann Pharm Fr. 1999;57(5):363-367.
  20. Xu SS, Cai ZY, Qu ZW, et al. Huperzine A in capsules and tablets for treating patients with Alzheimer disease. Zhongguo Yao Li Xue Bao. 1999;20(6):486-490.
  21. Wang G, Zhang SQ, Zhan H. [Effect of huperzine A on cerebral cholinesterase and acetylcholine in elderly patients during recovery from general anesthesia]. Nan Fang Yi Ke Da Xue Bao. 2006;26(11):1660-1662.
  22. Qian BC, Wang M, Zhou ZF, Chen K, Zhou RR, Chen GS. Pharmacokinetics of tablet huperzine A in six volunteers. Zhongguo Yao Li Xue Bao. 1995;16(5):396-398.
  23. Skolnick AA. Old Chinese herbal medicine used for fever yields possible new Alzheimer disease therapy. JAMA. 1997;277(10):776.
  24. Drug.com. Know More. Be Sure. Huperzine A. [homepage on the Internet]. c2000-2017 [cited 06 Apr 2017]. Available from: https://www.drugs.com/npp/huperzine-a.html.