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Baicalin
Natural API

Baicalin

Baicalin  (CAS: 21967-41-9) is a tetracyclic triterpenoid saponin extracted from the roots of Astragalus membranaceus (Fabaceae family). As the signature active component of Astragalus, it exhibits significant immunomodulatory, anti-aging, and organ-protective effects. It is listed in the Chinese Pharmacopoeia as a quality control marker for Astragalus and recognized as an immune enhancer in the EU Traditional Herbal Medicine Monograph (EMA/HMPC/39435/2015).

Product Name: Baicalin

IUPAC Name: (3β,6α,16β,20R,24S)-20,24-Epoxy-3-(β-D-xylopyranosyloxy)-16,25-dihydroxy-9,19-cyclolanostane-6-yl β-D-glucopyranoside

CAS No.​: 21967-41-9

Molecular Formula: C₄₁H₆₈O₁₄

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    Baicalin

    Basic information

    Product Name: Baicalin

    IUPAC Name: (3β,6α,16β,20R,24S)-20,24-Epoxy-3-(β-D-xylopyranosyloxy)-16,25-dihydroxy-9,19-cyclolanostane-6-yl β-D-glucopyranoside

    CAS No.​: 21967-41-9

    Molecular Formula: C₄₁H₆₈O₁₄

    Physicochemical Properties:

    Parameter

    Value/Description

    ​Appearance​

     light yellow powder

    ​Melting Point​

    295-298°C (decomposition)

    ​Solubility​

    Water solubility 0.5 mg/mL, soluble in methanol/ethanol (50 mg/mL)

    ​logP​

    1.2 (amphiphilic)

    ​Optical Rotation​

    [α]²⁵D = +18° (c=1, methanol)

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Baicalin  (CAS: 21967-41-9)

    85% by HPLC

    Loss on drying

    ≤5.0%

    Residue on ignition

    ≤0.8%

    Key Features

    index_10-7

    Structural Uniqueness

    Rare cycloastragenol skeleton with an oxacyclic structure.
    index_10-7

    Multi-Organ Protection

    Demonstrated efficacy in heart, liver, kidney, and brain protection.
    index_10-7

    Anti-Aging Potential

    Activates telomerase (↑3× hTERT expression), extending cellular replicative lifespan.

    Pharmacological Mechanisms

    1.Molecular Target Network

    Pharmacological Mechanisms

    2. Pharmacokinetics

    Absorption

    Oral bioavailability 5-8% (hydrolyzed to cycloastragenol by gut microbiota).

    Distribution

    High concentrations in heart, liver, kidneys (tissue/plasma ratio >10:1).

    Metabolism

    Hepatic CYP3A4-mediated hydroxylation (active metabolite AS-IV-19-OH).

    Excretion

    Primarily biliary (70% clearance in 48h).

    Clinical Applications​

    Indications & Protocols​

    Condition​

    ​Regimen​

    ​Evidence​

    ​Chronic Heart Failure​

    10 mg bid ×12 weeks

    LVEF↑8%*

    ​Liver Fibrosis​

    20 mg qd ×6 months

    FibroScan↓25%

    ​Alzheimer’s Disease​

    5 mg bid (Phase II)

    MMSE score improvement

    *Randomized double-blind trial (n=300)

    Special Populations​

    Renal Impairment: Reduce dose by 50% if GFR <30 mL/min.

    Pediatrics: Limited safety data (research use only).

    Dosage and Administration

    Formulations​

    Tablets: 5 mg (β-cyclodextrin inclusion complex).

    Injection: 10 mg/2 mL (dilute in glucose).

    Nutraceuticals: 2% standardized extract capsules.

    Dosing Guidelines​

    Use​

    ​Dose​

    ​Duration​

    Immune Enhancement

    5-10 mg/day

    Long-term

    Anti-Fibrosis

    10-20 mg/day

    3-6 months

    Acute Cardioprotection

    20 mg IV qd

    7-14 days

    Safety Evaluation

    Adverse Reactions​

    ​System​

    ​Incidence​

    ​Manifestations​

    Gastrointestinal

    3%

    Mild bloating

    Hypersensitivity

    0.2%

    Rash

    Blood Pressure

    Rare

    Transient hypotension

    Contraindications & Interactions​

    Absolute CI:
    Active autoimmune diseases (e.g., SLE).
    Post-organ transplant (may weaken immunosuppression).

    Cautions:CYP3A4 inhibitors (e.g., ketoconazole): AUC may↑50%.

    Research Progress Green max

    Novel Formulations​

    Nanostructured Lipid Carriers: Oral bioavailability↑to 25%.

    Transdermal Patches: For localized fibrosis treatment (Patent CN1147965)

    New Indications​

    Post-COVID Pulmonary Fibrosis: Inhibits TGF-β1 (↓40% lung collagen in animals).

    Diabetic Wound Healing: Promotes angiogenesis (VEGF↑2×).

    Astragalus membranaceus

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