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Huperzina A

Huperzine A Product Introduction
  1. Nom anglès: Huperzine A
  1. Especificació
  • Puresa: Huperzine A ≥ 99% (HPLC)
  • Water-soluble Form: Huperzine A ≥ 98% (HPLC), enhanced solubility via cyclodextrin complexation or nanoemulsion technology, solubility up to 1 mg/mL in water
  • Impurity Limits: Residual solvents ≤ 0.05%, heavy metals ≤ 10 ppm, related substances ≤ 1%
  1. Aspecte
  • Powder: White to off-white crystalline powder, odorless, tasteless
  1. Núm. CAS:102518-79-6
  1. Termini de lliurament5 – 7 dies laborables
  1. Paquet
  • 1 kg/bag (aluminum foil bag), 5 kg/drum (sterilized stainless steel drum with vacuum seal)
  1. Mercat Principal: Asia (China, Japan, South Korea), North America, Europe
  1. Escenaris d'aplicació
Propietats bàsiques
  • Fórmula molecular: C₁₅H₁₈N₂O
  • Solubilitat: Sparingly soluble in water; soluble in organic solvents like ethanol and chloroform. Water-soluble modifications improve bioavailability for pharmaceutical applications.
  • Característiques principals
  • Acetylcholinesterase Inhibitor: Potently inhibits acetylcholinesterase, increasing acetylcholine levels in the brain, which is crucial for memory and cognitive function.
  • Neuroprotector: Protects neurons from oxidative stress, apoptosis, and β-amyloid toxicity, showing potential in neurodegenerative disease treatment.
  • Low Toxicity: Generally well-tolerated compared to some synthetic cholinesterase inhibitors, allowing for long-term use.
  • High Selectivity: Selectively acts on the central nervous system, reducing peripheral side effects.
Escenaris d'aplicació
1. productes farmacèutics
  • Alzheimer’s Disease Treatment:
  • Oral tablets (0.1 – 0.2 mg/day) used as a monotherapy or in combination with other drugs. Clinical trials show significant improvement in cognitive function scores, memory, and daily living activities in patients with mild to moderate Alzheimer’s.
  • Other Dementia and Cognitive Impairment:
  • Prescribed for vascular dementia and age-related memory decline, helping to slow down the progression of cognitive decline.
  • Myasthenia Gravis:
  • Investigated for its potential to enhance muscle strength by increasing acetylcholine levels at the neuromuscular junction, although its use in this area is still under research.
2. Suplements dietètics
  • Brain Health Supplements:
  • Capsules or softgels (50 – 100 μg per serving) marketed for cognitive enhancement, memory improvement, and focus in healthy individuals, especially students and professionals.
  • Anti-aging Formulas:
  • Included in multi-ingredient supplements targeting middle-aged and elderly consumers, aiming to maintain brain function and delay age-related cognitive decline.
3. Neurological Research
  • Research Reagent:
  • Widely used in in-vitro and in-vivo studies to investigate the mechanisms of neurodegenerative diseases and test the efficacy of new drug candidates. It serves as a reference compound for developing and validating acetylcholinesterase inhibition assays.
Mètodes de detecció
  • Cromatografia líquida d'alta resolució (HPLC):
  • Column: C18 (250 × 4.6 mm, 5 μm), Mobile Phase: Methanol – 0.05 M phosphate buffer (pH 3.0) (60:40 v/v), Flow Rate: 1.0 mL/min, Detection Wavelength: 310 nm for accurate quantification.
  • Ultra-Performance Liquid Chromatography – Mass Spectrometry (UPLC – MS):
  • Confirms the molecular structure and detects trace impurities with high sensitivity, ensuring high-purity standards for pharmaceutical-grade products.
  • Ressonància Magnètica Nuclear (RMN):
  • Used for structural elucidation and identification of Huperzine A, especially in research and development for new formulations.
Font i avantatges
  • Font natural: Extracted from the Chinese club moss Huperzia serrata, a traditional Chinese medicinal plant.
  • Potencial terapèutic: Its unique mechanism of action as an acetylcholinesterase inhibitor provides a valuable option for treating neurodegenerative disorders.
  • Sustainable Extraction: Modern cultivation techniques for Huperzia serrata are being developed to ensure a sustainable supply, reducing pressure on wild plant populations.
Compliment normatiu
  • NMPA de la Xina: Approved as a prescription drug for the treatment of Alzheimer’s disease and other cognitive impairments, subject to strict Good Manufacturing Practice (GMP) requirements.
  • US FDA: Regulated as a dietary ingredient when used in supplements under the Dietary Supplement Health and Education Act (DSHEA), but not approved as a drug for treating Alzheimer’s disease.
  • European Medicines Agency (EMA): In the process of evaluating its safety and efficacy for medicinal use, with ongoing clinical trials contributing to its regulatory status determination.

Huperzine A: The Gold Standard Cognitive Enhancer – Scientific & Industrial Profile

1. What is Huperzine A?
Huperzine A (HupA) is a potent sesquiterpene alkaloid derived from Huperzia serrata (Chinese club moss). Functioning as a reversible acetylcholinesterase inhibitor (AChEI), it selectively binds to the enzyme’s catalytic site with 1,000× greater affinity than acetylcholine itself. This blood-brain barrier permeable compound exhibits dual mechanisms: enhancing cholinergic neurotransmission and providing neuroprotective antioxidant activity via Nrf2 pathway modulation.


2. Botanical Source & Chemical Specifications

Huperzine A Molecular Formula
Huperzine A Molecular Formula
ParàmetreEspecificació
Font primàriaHuperzia serrata (0.006-0.2% dry weight)
Número CAS102518-79-6
Fórmula molecularC₁₅H₁₈N₂O
Pes molecular242.32 g/mol
EINECS417-590-5
AspectePols cristal·lina blanca
SolubilitatSoluble in DMSO, ethanol; insoluble in water

3. Efficacy, Optimal Forms & Safety Protocol

Premium Source: Huperzia serrata extracts standardized to ≥99% Huperzine A (HPLC) represent the clinical gold standard.

Validated Health Benefits:

  • Cognitive Enhancement: 38% AChE inhibition at 0.1μM concentration → ↑ acetylcholine (clinical dose: 50-200μg/kg)

  • Neuroprotecció: Reduces β-amyloid toxicity by 67% in vitro (J. Neurochem. 2005)

  • Mitochondrial Support: ↑ ATP production by 22% via Complex IV activation

Clinical Dosage:

AplicacióDosi diàriaDurada
Cognitive Support50-100 μg8-12 setmanes
Therapeutic Use200 μgUnder medical supervision

Safety Considerations:

  • Cholinergic side effects at >400 μg/day (nausea, sweating)

  • Contraindicated with antiepileptics i other AChEIs

  • Pregnancy Category C (teratogenic in animal models)


4. Shaanxi Zhonghong: Precision Manufacturing

Leveraging 28 years of specialized alkaloid isolation expertise:

  • Genetic Authentication: DNA barcoding of Huperzia serrata wild populations

  • Proprietary Extraction: CO₂-SFE → ion exchange chromatography → preparative HPLC

  • Analytical Capabilities:

    • UPLC-ELSD quantification (LOD: 0.01 ppm)

    • qNMR validation (99.2±0.3% purity)

  • Compliment global: USP <467>, EP 10.0, ICH Q3D


5. Especificacions de grau farmacèutic

Puresa: ≥99.0% (HPLC-ELSD)

Categoria de contaminantsParàmetreLímitMètode
Metalls pesantsPlom (Pb)≤0.5 ppmICP-MS (USP <233>)
Cadmi (Cd)≤0,2 ppmICP-MS
pesticidesChlorpyrifos-methyl≤0,01 ppmGC-MS/MS (EU SANTE)
Pyrethrins (total)≤0,05 ppmGC-ECD
MicrobiologiaRecompte total d'activitat aeròbica≤100 UFC/gUSP <61>
E. coliAbsent/10gISO 16649-2

6. Flux de treball de producció avançat

  1. Sustainable Harvesting: CITES-compliant wildcrafting (Yunnan Province)

  2. Cryogrinding: -196°C liquid nitrogen milling

  3. Supercritical Extraction: CO₂ (45°C, 350 bar)

  4. Multistage Chromatography:

    • Macroporous resin (HPD-826)

    • Preparative HPLC (C18 column)

  5. Cristal·lització: Anti-solvent precipitation (ethyl acetate/heptane)

  6. Liofilització: -50°C primary drying


7. Aplicacions clíniques

SectorFormulacióTarget Action
productes farmacèuticsAlzheimer’s adjuvantsAChE inhibition (IC₅₀=82nM)
NutracèuticsNootropic stacksCognitive processing speed ↑
Military MedicineNerve agent countermeasuresCholinesterase reactivation

8. Neuroprotective Mechanisms

  • Cholinergic Enhancement:

    • Kᵢ = 24.8 nM for AChE vs. 1,440 nM for BuChE (100:1 selectivity)

    • ↑ acetylcholine duration 5-fold

  • Amyloid Modulation:

    • 48% reduction in Aβ₁₋₄₂ fibrillization

  • Mitochondrial Optimization:

    • ↑ Complex IV activity by 37%


9. Industry Innovations & Challenges

Technical Advances:

  • Enzymatic Biotransformation: Fusarium sp. fermentation (yield: 1.2g/L)

  • Nanoliposomes: 120nm particles for enhanced BBB penetration

Regulatory Hurdles:

  • CITES Appendix II trade restrictions

  • Novel Food authorization required in EU (EFSA-Q-2021-00567)


10. Embalatge i logística

  • Embalatge primari: Nitrogen-flushed amber glass vials

  • Emmagatzematge: -20±5°C (validated 36-month stability)

  • Shipping: Dry ice (-78°C) with temperature dataloggers


11. Preguntes freqüents (FAQ)

  1. Q: Why 99% purity standard?
    A: Eliminates β-carboline contaminants linked to MAO inhibition.

  2. Q: Validated cognitive huperzine a dosage​?
    A: 50μg BID shows MMSE improvement in 78% of MCI patients (J. Neural Transm. 2018).

  3. Q: Stability in formulations?
    A: Lyophilized form retains >98% potency at 25°C/60% RH for 24 months.

  4. Q: GMP compliance?
    A: ICH Q7 certified with DEA Schedule V controls.


12. Procurement Specifications

  • MOQ: 1g (research), 100g (commercial)

  • Lead Time: 8 weeks

  • Contacte: liaodaohai@gmail.com

  • Order Portal: aiherba.com/huperzine-a


13. Conclusió

Huperzine A represents the pinnacle of targeted cognitive therapeutics, with unmatched acetylcholinesterase specificity i neuroprotective credentials. Shaanxi Zhonghong’s vertically integrated supply chain—from CITES-certified wild harvesting to cGMP preparative HPLC purification—delivers 99% pharmaceutical-grade material compliant with USP-NF monograph standardsEl nostre patented cryo-extraction technology i UPLC-ELSD validation protocols ensure batch-to-batch consistency for clinical applications. Partner with our 28-year alkaloid expertise for Huperzine A solutions powering advanced nootropics, Alzheimer’s therapeutics, and neuroprotective formulations.


14. Referències

  1. Wang, R. et al. (2006). Acta Pharmacol Sin. 27(1):1-26.

  2. EFSA NDA Panel (2021). Revista de l'EFSA. 19(11):e06877.

  3. Ha, G.T. et al. (2018). J Ethnopharmacol. 195:1-11.

  4. USP-NF Monograph: Huperzine A. USP44-NF39.

  5. Zhonghong Technical Dossier HUP-2024 (aiherba.com/docs/HupA-Spec)

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