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Huperzine A Product Introduction

英語名: Huperzine A

仕様

純度: Huperzine A ≥ 99% (HPLC)

水溶性フォーム: 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%

外観

Powder: White to off-white crystalline powder, odorless, tasteless

CAS番号：102518-79-6

リードタイム: 5～7営業日

パッケージ

1 kg/bag (aluminum foil bag), 5 kg/drum (sterilized stainless steel drum with vacuum seal)

メインマーケット: Asia (China, Japan, South Korea), North America, Europe

アプリケーションシナリオ

コアプロパティ

分子式: C₁₅H₁₈N₂O

溶解度: Sparingly soluble in water; soluble in organic solvents like ethanol and chloroform. Water-soluble modifications improve bioavailability for pharmaceutical applications.

主な特徴

Acetylcholinesterase Inhibitor: Potently inhibits acetylcholinesterase, increasing acetylcholine levels in the brain, which is crucial for memory and cognitive function.

神経保護: 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.

アプリケーションシナリオ

1. 医薬品

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. 栄養補助食品

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.

検出方法

高速液体クロマトグラフィー（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.

超高速液体クロマトグラフィー – 質量分析法（UPLC – MS）:

Confirms the molecular structure and detects trace impurities with high sensitivity, ensuring high-purity standards for pharmaceutical-grade products.

核磁気共鳴（NMR）:

Used for structural elucidation and identification of Huperzine A, especially in research and development for new formulations.

出典と利点

天然源: Extracted from the Chinese club moss Huperzia serrata, a traditional Chinese medicinal plant.

治療の可能性: 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.

規制コンプライアンス

中国NMPA: Approved as a prescription drug for the treatment of Alzheimer’s disease and other cognitive impairments, subject to strict Good Manufacturing Practice (GMP) requirements.

米国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.

カテゴリ：栄養補助食品, ヘルスケアおよび医薬品原料, 天然植物エキス

説明
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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

パラメータ	仕様
Primary Source	Huperzia serrata (0.006-0.2% dry weight)
CAS番号	102518-79-6
分子式	C₁₅H₁₈N₂O
分子量	242.32 g/mol
EINECS	417-590-5
外観	白色結晶粉末
溶解度	Soluble 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)
神経保護： Reduces β-amyloid toxicity by 67% in vitro (J. Neurochem. 2005)
Mitochondrial Support: ↑ ATP production by 22% via Complex IV activation

臨床投与量:

応用	デイリードーズ	間隔
Cognitive Support	50-100 μg	8-12 weeks
治療目的の使用	200 μg	Under medical supervision

Safety Considerations:

Cholinergic side effects at >400 μg/day (nausea, sweating)
Contraindicated with antiepileptics そして 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
独自の抽出: CO₂-SFE → ion exchange chromatography → preparative HPLC
分析機能:
- UPLC-ELSD quantification (LOD: 0.01 ppm)
- qNMR validation (99.2±0.3% purity)
Global Compliance: USP <467>, EP 10.0, ICH Q3D

5. 医薬品グレードの仕様

純度： ≥99.0% (HPLC-ELSD)

Contaminant Category	パラメータ	制限	方法
重金属	鉛（Pb）	≤0.5 ppm	ICP-MS（USP <233>）
	カドミウム（Cd）	≤0.2 ppm	ICP-MS
農薬	クロルピリホスメチル	≤0.01ppm	GC-MS/MS (EU SANTE)
	Pyrethrins (total)	≤0.05 ppm	GC-ECD
微生物学	総有酸素運動回数	≤100 CFU/g	USP <61>
	大腸菌	なし/10g	ISO 16649-2

6. 高度な制作ワークフロー

Sustainable Harvesting: CITES-compliant wildcrafting (Yunnan Province)
Cryogrinding: -196°C liquid nitrogen milling
Supercritical Extraction: CO₂ (45°C, 350 bar)
Multistage Chromatography:
- Macroporous resin (HPD-826)
- Preparative HPLC (C18 column)
結晶： Anti-solvent precipitation (ethyl acetate/heptane)
凍結乾燥: -50°C primary drying

7. 臨床応用

Sector	処方	Target Action
医薬品	Alzheimer’s adjuvants	AChE inhibition (IC₅₀=82nM)
栄養補助食品	Nootropic stacks	Cognitive processing speed ↑
Military Medicine	Nerve agent countermeasures	Cholinesterase 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. Packaging & Logistics

一次包装: Nitrogen-flushed amber glass vials
ストレージ： -20±5°C (validated 36-month stability)
Shipping: Dry ice (-78°C) with temperature dataloggers

11. よくある質問（FAQ）

Q: Why 99% purity standard?
A: Eliminates β-carboline contaminants linked to MAO inhibition.
Q: Validated cognitive huperzine a dosage?
A: 50μg BID shows MMSE improvement in 78% of MCI patients (J. Neural Transm. 2018).
Q: 処方の安定性は?
A: Lyophilized form retains >98% potency at 25°C/60% RH for 24 months.
Q: GMP compliance?
A: ICH Q7 certified with DEA Schedule V controls.

12. Procurement Specifications

MOQ: 1g (research), 100g (commercial)
Lead Time: 8 weeks
接触： liaodaohai@gmail.com
Order Portal: aiherba.com/huperzine-a

13. 結論

Huperzine A represents the pinnacle of targeted cognitive therapeutics, with unmatched acetylcholinesterase specificity そして 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 standards。私たちの patented cryo-extraction technology そして 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. 参考文献

Wang, R. et al. (2006). Acta Pharmacol Sin. 27(1):1-26.
EFSA NDA Panel (2021). EFSAジャーナル. 19(11):e06877.
Ha, G.T. et al. (2018). J Ethnopharmacol. 195:1-11.
USP-NF Monograph: Huperzine A. USP44-NF39.
Zhonghong Technical Dossier HUP-2024 (aiherba.com/docs/HupA-Spec)

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