Silybin

Silybin: The Premier Hepatoprotective Agent from Nature’s Pharmacy

1. What is Silybin?

Silybin, chemically known as Silibinin, est le primary bioactive flavonolignan constituent isolated from the fruits and seeds of the milk thistle plant (Silybum marianum L. Gaertn.). It represents the most potent and extensively researched component within the standardized mixture known as Silymarine, constituting approximately 50-70% of its total flavonolignan content. Silybin functions as a powerful hepatoprotectant et mitochondrial stabilizer, renowned for its antioxidant, anti-inflammatory, antifibrotic, and potential anticancer properties. Its molecular structure comprises a dihydroflavonol unit (taxifolin) conjugated with a phenylpropanoid unit (coniferyl alcohol), forming a unique benzodioxane ring system crucial for its biological activity.

2. Source du produit, propriétés chimiques et identifiants

• Source: Extrait et purifié à partir du achenes (fruits/seeds) de Silybum marianum (Chardon-Marie).

• Propriétés chimiques :

  • Apparence: Typically a white to off-white crystalline powder.

  • Solubilité: Expositions low water solubility but is soluble in ethanol, acetone, dimethyl sulfoxide (DMSO), et methanol. Often formulated as phospholipid complexes (e.g., Siliphos®) ou glycosides to enhance bioavailability.

  • Stabilité: Sensitive to light, heat, and oxygen. Requires storage under inert conditions (nitrogen atmosphere) at low temperatures (2-8°C) for long-term stability.

• Identifiants clés :

  • Numéro de registre CAS : 22888-70-6 (Silybin A and B mixture)

  • Formule moléculaire (MF) : C25H22O10

  • Poids moléculaire (PM) : 482,44 g/mol

  • Numéro EINECS : 245-302-5

3. Efficacy, Optimal Form, Health Benefits, Dosage & Safety

• “Best” Form & Highest Content: High-Purity Silybin (><｜end▁of▁thinking｜> Isomers A & B), often complexed with phosphatidylcholine (e.g., Siliphos®), is widely regarded as the most effective and bioavailable form. This complexation significantly enhances intestinal absorption and liver targeting compared to uncomplexed silymarin or crude extracts. Products standardized to ><｜end▁of▁thinking｜> Silybin represent the pinnacle of concentration and therapeutic potential. Shaanxi Zhonghong utilizes proprietary purification techniques to achieve this benchmark.

• Avantages et mécanismes pour la santé :

  • Liver Protection & Regeneration: Le cornerstone benefit. Silybin acts as a puissant antioxydant, scavenging free radicals (ROS/RNS) and elevating intracellular glutathione (GSH) levels. It stabilizes hepatocyte membranes, inhibiting toxin uptake. It stimulates hepatocyte ribosomal RNA synthesis, promoting liver regeneration. Demonstrated efficacy against alcoholic liver disease (ALD), non-alcoholic fatty liver disease (NAFLD)/non-alcoholic steatohepatitis (NASH), drug/toxin-induced hepatotoxicity (e.g., acetaminophen, Amanita phalloides), and viral hepatitis support.

  • Anti-inflammatory & Antifibrotic: Module NF-κB, TNF-α, TGF-β1, et autres pro-inflammatory cytokine signaling pathways. Inhibits stellate cell activation, reducing collagen deposition et liver fibrosis progression.

  • Anticancer Potential (Emerging Research): Expositions anti-proliferative, pro-apoptotic, anti-angiogenic, et anti-metastatic effects in various cancer models (e.g., prostate, lung, skin, colon), often through modulation of STAT3, Akt/mTOR, and MAPK pathways. Améliore chemotherapy efficacy while reducing toxicity.

  • Metabolic Support: May improve sensibilité à l'insuline and ameliorate features of syndrome métabolique relevant to NAFLD/NASH.

  • Neuroprotection & Antidepressant Effects (Preclinical): Shows promise in models of neurodegeneration (Alzheimer’s, Parkinson’s) et depression, linked to its anti-inflammatory and antioxidant actions within the CNS.

• Apport quotidien : Typical supplemental dosages range from 100 mg to 600 mg of Silybin daily, often divided into 2-3 doses. Dosing for specific conditions (e.g., Amanita poisoning treatment) can be significantly higher (20-50 mg/kg body weight IV) under medical supervision. Always consult a healthcare provider for personalized dosing.

• Précautions et effets secondaires :

  • Generally well-tolerated. The most common side effects are mild gastrointestinal disturbances (e.g., laxative effect, nausea, dyspepsia).

  • Potential Drug Interactions: Silybin may inhibit cytochrome P450 enzymes (notably CYP2C9 and CYP3A4) et UDP-glucuronosyltransferases (UGTs), potentially affecting the metabolism of drugs like diazepam, warfarin, losartan, phenytoin, and certain statins. It may also inhibit efflux transporters (P-glycoprotein, BCRP). Consult a doctor/pharmacist before use if taking medications.

  • Allergies : Contraindicated in individuals with known hypersensitivity to milk thistle or plants in the Asteraceae/Compositae family (ragweed, chrysanthemums, marigolds).

  • Grossesse/Allaitement : Safety not fully established; use only if clearly needed under medical guidance.

4. Premier Source: Shaanxi Zhonghong Investment Technology Co., Ltd.

Shaanxi Zhonghong Investment Technology Co., Ltd. stands as a vertically integrated leader dans le bioactive compound industry, boasting 28 years of specialized expertise. En tant que certified high-tech enterprise, we orchestrate agile R&D, collaborative innovation, precision manufacturing, and global distribution, exclusively serving the demanding needs of chemical, material science, and life science sectors.

• Objectif principal : Advanced extraction, isolation, and purification of plant-derived active pharmaceutical ingredients (APIs) and nutraceuticals, y compris Silybin of exceptional purity.

• Product Spectrum: Comprehensive portfolio encompassing standardized botanical extracts, cosmetic actives, nutraceutical/functional food ingredients, pharmaceutical intermediates, natural pigments (colours), and plant-based sweeteners.

• Scientific Prowess (R&D Barrier):

  • Strategic Alliances: Maintain laboratoires communs de recherche avec 5 universités d'élite, fostering cutting-edge discovery.

  • Portefeuille de propriété intellectuelle : Hold 20+ granted patents covering proprietary extraction methodologies and novel compounds.

  • Bibliothèque de composés exclusive : Possess a globally unique repository of characterized phytochemicals.

• Manufacturing Excellence (Equipment Edge):

  • Deploy instrumentation analytique de pointe y compris U/HPLC (Ultra/High-Performance Liquid Chromatography), GC-MS (Gas Chromatography-Mass Spectrometry), and 600MHz+ NMR (Nuclear Magnetic Resonance Spectrometry).

  • Notre stringent purity specifications exceed industry standards by 20%+, guaranteeing uncompromising quality and batch-to-batch consistency.

• Global Reach (Supply Network): Our meticulously managed supply chain delivers solutions d'ingrédients personnalisées à multinational pharmaceutical corporations, research institutions, and nutraceutical brands across plus de 80 pays en Asie, en Europe et dans les Amériques.

5. Spécifications du produit : Contrôle qualité rigoureux

Shaanxi Zhonghong’s Silybin adheres to the most stringent quality parameters:

6. Flux de production avancé

Notre Conforme aux BPF Silybin production integrates cutting-edge, patent-protected technologies:

1. Qualification des matières premières : Sourcing premium Silybum marianum seeds via agronomic partnerships, subject to rigorous identity and contaminant screening.

2. Prétraitement : Seeds undergo mechanical decortication et cryogenic milling to optimize extraction yield.

3. Extraction sélective : Utilisation dynamic countercurrent multi-stage extraction (DCME) avec mélanges éthanol/eau de qualité alimentaire under controlled temperature/pressure, maximizing flavonolignan recovery while minimizing impurities.

4. Purification primaire : Répartition liquide-liquide et macroporous resin adsorption chromatography (MRAC) to concentrate Silymarin complex and remove sugars, lipids, and pigments.

5. High-Resolution Isolation: Chromatographie liquide préparative à haute performance (Prep-HPLC) employing polar-embedded C18 or phenyl-hexyl stationary phases et optimized mobile phase gradients for baseline separation of Silybin isomers (A & B) from other flavonolignans (Isosilybin, Silychristin, Silydianin).

6. Crystallization & Polymorph Control: Anti-solvent crystallization under strict thermodynamic control to achieve desired crystalline polymorphic form and high purity. Multiple recrystallizations may be employed.

7. Complexation (Optional): Phospholipid complexation via solvent evaporation/spray drying to produce bioavailability-enhanced Silybin-Phosphatidylcholine Complex (e.g., Siliphos® equivalent).

8. Lyophilization (Freeze-Drying): For thermolabile forms or enhanced stability, employing controlled lyophilization cycles.

9. Libération sous contrôle qualité rigoureux : Chaque lot subit full compendial testing (Identity, Assay, Impurities, Residual Solvents, Heavy Metals, Microbiology) using validated methods before release.

7. Scénarios d'application

• Médicaments: Core ingredient in hepatoprotective drugs (oral tablets/capsules, injectables for Amanita poisoning), formulations for NAFLD/NASH therapy, et adjuvant oncology therapeutics.

• Nutraceutiques et compléments alimentaires : Liver support complexes, detox formulations, antioxidant blends, standalone Silybin capsules/tablets (standardized or phospholipid complexed).

• Aliments et boissons fonctionnels : Fortification of health drinks, bars, and foods targeting liver wellness (requires solubility-enhanced forms).

• Cosméceutiques : Incorporé dans anti-aging serums, creams, and lotions pour sa puissance antioxidant, anti-glycation, and anti-inflammatory effects protecting skin from environmental stressors and UV-induced damage.

• Veterinary Medicine: Liver support supplements for companion animals and livestock.

• Recherche: Biochemical reagent for studying liver pathophysiology, oxidative stress mechanisms, apoptosis regulation, and cancer biology.

8. Comprehensive Quality Control (QC) System

Shaanxi Zhonghong met en œuvre un multidimensional QC strategy exceeding pharmacopeial standards (USP, EP, CP) to ensure Silybin API integrity, safety, and efficacy:

• Identité et pureté : HPLC-UV/PDA/DAD is the primary workhorse for quantifying Silybin A+B et related flavonolignans (Isosilybin A/B, Silychristin, Silydianin), alongside detection and quantification of organic impurities. HPLC-ELSD/CAD monitors residual solvents. UPLC-QTOF-MS/MS fournit definitive structural confirmation and screens for trace unknown impurities. High-Resolution NMR (1H, 13C, 2D) confirms molecular structure and stereochemistry.

• Contrôle des contaminants : ICP-MS assure heavy metal compliance at parts-per-billion (ppb) levels. GC-MS/MS et LC-MS/MS achieve ultra-trace detection of pesticides and mycotoxins. Validated microbiological methods (membrane filtration, enrichment cultures) strictly monitor bioburden according to USP/EP.

• Physical Characterization: Dynamic Vapor Sorption (DVS) assesses hygroscopicity. Differential Scanning Calorimetry (DSC) et Thermogravimetric Analysis (TGA) déterminer melting point, polymorphism, and thermal stability. Laser Diffraction Particle Size Analysis (PSD) et Scanning Electron Microscopy (SEM) characterize morphology.

• Stability & Storage: ICH-compliant accelerated (40°C/75% RH) and long-term (25°C/60% RH) stability studies establish retest periods and optimal storage conditions (typically 2-8°C under nitrogen). Forced degradation studies identify potential degradation pathways.

• Documentation et traçabilité : Full analytical documentation (CoA, MSDS) accompanies each batch. Dossiers de lots électroniques (EBR) et Laboratory Information Management Systems (LIMS) ensure complete traceability from raw seed to finished Silybin API.

9. Emballage sécurisé et logistique mondiale

• Emballage primaire : Double-sealed, food-grade polyethylene bags placed inside robust, HDPE containers with induction-sealed lids. For highly sensitive material, aluminum foil bags under vacuum or nitrogen purge are utilized.

• Emballage secondaire : Sealed containers securely packed in corrugated export cartons avec desiccant packs.

• Étiquetage : Compliant labeling with product name (Silybin), CAS no., batch no., manufacturing/expiry date, net weight, storage conditions, GMP certification, et hazard symbols (if applicable).

• Logistique: Expertise en global cold chain logistics (2-8°C) via air/sea freight. Real-time temperature monitoring available. Comprehensive export documentation (Commercial Invoice, Packing List, CoA, MSDS, Certificate of Origin, Health Certificate) provided. Customs clearance support ensured.

10. Health Efficacy & Mechanism Research, Applications & Innovation, Research Frontiers

• Mechanistic Depth: Research continuously elucidates Silybin’s molecular targets beyond antioxidant effects: modulation of key signaling pathways (PI3K/Akt, MAPK, JAK/STAT, NF-κB, Nrf2), influence on microRNA expression, epigenetic modifications, regulation of autophagy, et gut-liver axis modulation.

• Expanding Clinical Applications: Active clinical investigation focuses on NASH/NAFLD treatment paradigms, chemoprevention, chemo/radiotherapy sensitization and protection, neurological disorders (Alzheimer’s, Parkinson’s), diabetic complications, et viral hepatitis adjunct therapy.

• Applications industrielles et innovation technologique : Key focus areas include novel drug delivery systems (nanoparticles, liposomes, SNEDDS) to overcome bioavailability limitations, synthetic biology for sustainable production, development of pure Silybin stereoisomers (A vs. B) to understand differential bioactivity, and creation of targeted conjugates.

• Frontières et défis de la recherche : Major challenges include optimizing oral bioavailability without complexation, conducting definitive large-scale human trials for newer indications (cancer, neurodegeneration), fully understanding stereoselective pharmacokinetics and pharmacodynamics, establishing optimal dosing regimens for specific diseases, et ensuring sustainable sourcing and extraction. Metabolomics and microbiome interactions are emerging frontiers.

11. Foire aux questions (FAQ)

• Q: What is the difference between Silymarin and Silybin?

  • A: Silymarin is the extrait standardisé from milk thistle seeds, containing a mixture of flavonolignans (Silybin A & B, Isosilybin A & B, Silychristin, Silydianin) and some flavonoids. Silybin (specifically the isomers Silybin A and Silybin B) is the most biologically active single compound within Silymarin, typically making up 50-70% of a high-quality extract. High-purity Silybin (><｜end▁of▁thinking｜>) isolates this key active.

• Q: Why choose high-purity Silybin over standard Silymarin?

  • UN: High-purity Silybin (><｜end▁of▁thinking｜>) offres precise dosing of the most potent constituent, enabling targeted therapeutic applications et advanced research where the specific effects of Silybin need to be isolated. It allows for development of high-dose formulations (e.g., for NASH or oncology) that might not be feasible with crude extract.

• Q: Is Silybin safe? What are the main side effects?

  • A: Silybin is generally very safe at recommended doses. The most common side effects are mild and gastrointestinal (e.g., loose stools, bloating, nausea). Serious adverse effects are rare. Consult a doctor before use if pregnant, breastfeeding, have a hormone-sensitive condition, or are taking medications (due to potential interactions).

• Q: How does the phospholipid complex improve Silybin?

  • UN: Phosphatidylcholine complexation (e.g., Siliphos®) de manière significative enhances Silybin’s bioavailability – studies show 2-10 fold increases in plasma levels. Phospholipids improve solubility in digestive fluids, facilitate micelle formation, enhance intestinal absorption via passive diffusion and micellar uptake, and may promote direct delivery to liver cells via the lymphatic system and chylomicrons.

• Q: What quality certifications does Shaanxi Zhonghong hold?

  • A: We operate under strict cGMP (Current Good Manufacturing Practice) guidelines. Certifications include ISO 9001 (Quality Management), ISO 22000 / FSSC 22000 (Food Safety Management System), et Casher/Halal options. Specific product certifications (e.g., USP verification, organic) are batch-dependent.

• Q: Can you provide custom Silybin formulations?

  • A: Yes. We specialize in solutions d'ingrédients personnalisées. This includes specific purity grades (e.g., >98%), complexes phospholipidiques, solubility-enhanced forms, particle size optimization (micronization), et private labeling. Contact us to discuss your requirements.

12. Where to Buy High-Purity Silybin

Pour premium Silybin API (><｜end▁of▁thinking｜>), Silymarin extract, ou bioavailability-enhanced Silybin-Phosphatidylcholine Complex, contact Shaanxi Zhonghong Investment Technology Co., Ltd.:

• E-mail: liaodaohai@gmail.com

• Site web: https://aiherba.com

• Contact: Inquire via email or our website for technical dossiers, sample requests, quotes, and custom manufacturing opportunities.

13. Conclusion

Silybin, the preeminent hepatoprotective flavonolignan from Milk Thistle, stands at the forefront of natural bioactive compounds avec robust scientific validation for liver health and expanding therapeutic potential. Shaanxi Zhonghong Investment Technology Co., Ltd., leveraging 28 years of expertise, cutting-edge technology, and unwavering commitment to quality, livre high-purity Silybin API (><｜end▁of▁thinking｜>) and advanced formulations that meet the exacting standards of global pharmaceutical, nutraceutical, and research markets. Notre vertically integrated approach, from sustainable sourcing to cGMP manufacturing and global logistics, ensures a reliable supply of superior Silybin, empowering innovation in health and wellness products worldwide.

14. Références

1. Abenavoli, L., et al. (2018). Milk thistle (Silybum marianum): A concise overview on its chemistry, pharmacological, and nutraceutical uses in liver diseases. Recherche en phytothérapie, 32(11), 2202-2213.

2. Polyak, S. J., et al. (2013). Identification of hepatoprotective flavonolignans from silymarin. Proceedings of the National Academy of Sciences, 110(18), 7150-7155.

3. Loguercio, C., & Festi, D. (2011). Silybin and the liver: From basic research to clinical practice. Journal mondial de gastroentérologie, 17(18), 2288-2301.

4. Deep, G., & Agarwal, R. (2013). Targeting tumor microenvironment with silibinin: Promise and potential for a translational cancer chemopreventive strategy. Current Cancer Drug Targets, 13(5), 486-499.

5. European Pharmacopoeia (Ph. Eur.) 11th Edition. Milk Thistle Fruit Dry Extract, Refined and Standardized.

6. United States Pharmacopeia-National Formulary (USP-NF). General Chapters: <561> Articles of Botanical Origin, <2021> Identification of Articles of Botanical Origin by HPTLC, <1061> Color—Instrumental Measurement, <467> Residual Solvents.

7. Kroll, D. J., et al. (2007). Milk Thistle Nomenclature: Why It Matters in Cancer Research and Pharmacokinetic Studies. Journal of the National Cancer Institute, 99(21), 1655-1656. (Highlights isomer differences).

8. Tian, X., et al. (2020). Recent advances in the development of delivery systems of silymarin. Journal de libération contrôlée, 327, 689-705. (Discusses bioavailability enhancement tech).

9. ICH Guidelines: Q1A(R2) Stability Testing of New Drug Substances and Products, Q2(R1) Validation of Analytical Procedures, Q3C(R8) Impurities: Guideline for Residual Solvents.

10. Shaanxi Zhonghong Internal Quality Control Documentation & Analytical Method Validation Reports.