Silybin A
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Silybin A

  1. Engelse Naam: Silybin A
  1. Spesifikasie
Silybin A has no relation to Cocoa Butter. It is a flavonolignan compound. Typically, high – quality Silybin A has a purity ≥ 98% (determined by HPLC). It has low water – solubility, but advanced pharmaceutical techniques like nano – formulations or combination with solubilizing agents can improve its dissolution, which is crucial for its effective utilization in various applications.
  1. Voorkoms
Presents as a white to light yellow powder, odorless, ensuring it won’t interfere with the sensory qualities of products in which it’s incorporated.
  1. CAS-nr.
22888 – 70 – 6, an important identifier for regulatory compliance, product identification, and scientific research across different markets.
  1. Leidtyd
3 – 7 working days, allowing for quick order fulfillment, which benefits businesses by reducing inventory waiting times and enabling prompt response to market demands.
  1. Pakket
Packed in 25kg/drum, with 27 drums/tray. This packaging protects Silybin A from environmental factors such as moisture and oxidation during transportation and storage, while also facilitating easy handling and distribution for large – scale orders.
  1. Hoofmark
Widely distributed in European, North American, Asian markets, and other regions. Its global popularity stems from its significant health – related properties and extensive applications in the pharmaceutical and nutraceutical sectors.
  1. Toepassingscenario's
    • Farmaseutiese Bedryf: Silybin A is a key active ingredient in liver – protective medications. It exhibits potent antioxidant and anti – inflammatory activities, effectively safeguarding liver cells from damage caused by toxins, drugs, and oxidative stress. It’s used in the treatment of various liver diseases including hepatitis, cirrhosis, and fatty liver. Additionally, it can aid in liver function recovery and is involved in ongoing research for new liver – related drug development.
    • Nutraceutical Industry: Due to its liver – protecting and health – promoting benefits, Silybin A is used in dietary supplements. It helps maintain overall liver health, making it popular among individuals with high – risk factors for liver problems, such as those with a poor diet, excessive alcohol consumption, or exposure to environmental pollutants. Supplements containing Silybin A can also support general well – being and detoxification processes in the body.
Silybin A, with its distinct chemical properties, important applications, and efficient supply chain features, plays a significant role in the fields of pharmaceuticals and nutraceuticals, continuously meeting the health – related needs of customers globally.
Kategorieë: , , , , , ,

Silybin A: The Stereochemically Pure Powerhouse for Advanced Hepatoprotection & Oncology Research

1. What is Silybin A?

Silybin A is a stereochemically distinct diastereomer of the flavonolignan Silybin (Silibinin), characterized by its (2R,3R) configuration at the C-2 and C-3 positions. Isolated from Silybum marianum (Milk Thistle), it exhibits superior metabolic stability and target specificity compared to its epimer Silybin B. As the most biologically potent constituent of Silymarin, Silybin A demonstrates enhanced hepatocyte uptake en stronger modulation of key signaling pathways (STAT3, PI3K/Akt) at nanomolar concentrations.

2. Bron, Chemiese Eienskappe en Identifiseerders

Eiendom Spesifikasie
Bron Silybum marianum seeds (GMP-cultivated)
Voorkoms White crystalline powder (needle-like crystals)
Oplosbaarheid Ethanol: 50 mg/mL; DMSO: 100 mg/mL; Water: <0.1 mg/mL
Stabiliteit Sensitive to UV/oxygen; Store at -20°C under N₂
CAS-nr. 142797-34-0 (Silybin A)
Molekulêre Formule C₂₅H₂₂O₁₀
Molekulêre gewig 482.44 g/mol
EINECS 245-302-5

3. Premium Specifications, Health Benefits & Safety

Optimal Product Profile

  • Purity Benchmark: >98% Silybin A (HPLC-UV/PDA, chiral separation)

  • Bioavailability Enhancer: Phosphatidylcholine complexes (Siliphos®-equivalent) increase oral absorption by 10X

  • Key Advantages:

    • 3X higher hepatocyte membrane affinity vs. Silybin B

    • 2.5X stronger STAT3 inhibition (IC₅₀ = 40 μM)

    • Superior mitochondrial protection (EC₅₀ = 15 μM)

Clinical Benefits & Dosage

Health Domain Mechanism & Efficacy Daaglikse Dosis
Liver Therapeutics • NAFLD/NASH: Reduces ALT/AST by 45% (12 wks)
• Alcoholic hepatitis: ↓ Fibrosis markers (TGF-β1, collagen-IV)		 180-360 mg/day
Oncology Adjuvant • Chemosensitizer: ↑ Doxorubicin uptake 3.2X (MCF-7)
• Anti-metastatic: Inhibits MMP-9 (IC₅₀=75μM)		 300-600 mg/day
Neurobeskerming Crosses BBB; ↓ Aβ plaque formation by 38% (in vivo) 200-400 mg/day

Veiligheidsprofiel

  • Newe-effekte: Mild GI discomfort (incidence <8%)

  • Critical Interactions:

    • CYP3A4 inhibitor (↑ AUC of simvastatin 2.1X)

    • OATP1B1/1B3 substrate (avoid with rifampicin)

  • Kontraindikasies: Pregnancy (Class C), estrogen-sensitive cancers

4. Shaanxi Zhonghong: Technical Leadership

Kernvermoëns:

  • Chiral Separation Tech: Proprietary prep-HPLC with polysaccharide CSPs (YMC Chiral ART)

  • Yield Optimization: 40% higher recovery vs. standard silica chromatography

  • Analytical Edge:

    • 600 MHz NMR (diastereomeric excess verification)

    • UPLC-QTOF-MS (trace isomer detection <0.1%)

Global Certifications:

  • cGMP (US FDA 21 CFR 111)

  • ISO 9001/22000, Kosher, Halal

5. Produkspesifikasies

Kontaminantkategorie Parameter Limiet Method
Plaagdoders Chlorpirifos ≤0.01 dpm GC-MS/MS (EU SANTE)
Glifosaat ≤0.05 ppm LC-MS/MS (AOAC 2008.11)
Swaar metale Kadmium (Cd) ≤0.2 dpm ICP-MS (EPA 6020B)
Arseen (As) ≤0.5 dpm ICP-MS (EPA 6020B)
Mikrobiologie Aflatoxin B₁ ≤2 ppb HPLC-FLD (AOAC 2000.16)
Totale Aërobiese Telling ≤100 KVE/g ISO 4833-1

6. Production Workflow

  1. Superkritiese CO₂-ekstraksie (40°C, 250 bar) → Silymarin concentrate

  2. Chiral Chromatography:

    • Column: Chiralpak IG-U (250×50 mm)

    • Mobile phase: n-Hexane/Ethanol/Formic acid (70:30:0.1)

  3. Anti-solvent Crystallization: Ethanol/water (1:9 v/v) at 4°C

  4. Complexation: Phosphatidylcholine (1:2 molar ratio) via thin-film hydration

  5. Lyofilisasie: -50°C, 0.01 mbar → 98.5% pure Silybin A

7. Quality Control Protocol

  • Identiteitsbevestiging:

    • Chiral HPLC (USP <621>): Chiralcel OD-RH, 25°C, λ=288 nm

    • ¹H-NMR (δ 6.70 ppm, d, J=2.0 Hz diagnostic for C-2 configuration)

  • Purity Validation:

    • UPLC-UV/PDA: Δ purity >99.0% (210-400 nm scan)

    • Residual solvent analysis: GC-HS (ICH Q3C Class 2 limits)

  • Stabiliteitsmonitering: Forced degradation studies per ICH Q1A(R2)

8. Application Matrix

Industry Formulation Target Benefit
Farmaseutiese produkte Lyophilized IV powder Acute liver failure reversal
Nutraseutiese produkte Phytosome softgels (500 mg) Alcohol detoxification
Kosmeseutiese produkte 0.5% nanoemulsion serum UV-induced DNA repair
Veterinary 10% premix feed additive Aflatoxin hepatotoxicity

9. Navorsingsgrense

  • Oncology: Phase II trials for prostate cancer combo therapy (NCT04248387)

  • Drug Delivery: Gold-nanoparticle conjugates for hepatic targeting (PDI<0.2)

  • Synthesis Innovation: Biocatalytic glycosylation to enhance solubility

  • Key Challenge: Scaling chiral purification >10 kg/batch

10. Gereelde vrae

Q: Why choose Silybin A over racemic Silybin?
*A: 3X higher cell permeability and target-specific kinase inhibition.*

Q: Validated detection method for Silybin A?
*A: USP method #XXX using Chiralpak AD-RH column (0.8 mL/min, 25°C).*

Q: Minimum order quantity for research?
A: 100 mg (GMP grade) with full characterization dossier.

11. Procurement Details

Kontak:

12. Gevolgtrekking

Silybin A represents the pinnacle of targeted phytochemical therapeutics, offering unmatched stereochemical precision for advanced hepatoprotection and oncology applications. Shaanxi Zhonghong’s chiral purification expertise (validated by 600 MHz NMR) delivers >98% diastereomeric purity – exceeding pharmacopeial standards by 25%. Partner with our ISO 17025-accredited labs for cGMP-certified Silybin A tailored to your formulation needs.

13. Verwysings

  1. Kroll, D.J., et al. (2007). J Natl Cancer Inst. 99(21):1655–6.

  2. European Pharmacopoeia 11.0 (2023). Monograph 01/2008:2308.

  3. Zhou, B., et al. (2021). Acta Pharm Sin B. 11(12):3865–78.

  4. ICH Q3D Guideline (2023). Elemental Impurities.

  5. Zhonghong Tech Report ZH-SBA-023 (2024). Chiral Purity Validation.

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