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Andrographolide
Natural API

Andrographolide

Andrographolide (CAS: 5508-58-7) is a diterpene lactone compound extracted from Andrographis paniculata (Acanthaceae family). As the primary active component of the traditional Chinese herb Chuanxinlian, it exhibits significant anti-inflammatory, antiviral, immunomodulatory, and hepatoprotective effects. It is included in the pharmacopoeias of China, India, and other countries, and was listed as a WHO-recommended candidate for COVID-19 research in 2020.

Product Name: Andrographolide

IUPAC Name: (3E,4S)-3-[2-[(1R,4aS,5R,6R,8aR)-6-Hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylenedecahydronaphthalen-1-yl]ethylidene]-4-hydroxyfuran-2(3H)-one

CAS No.​: 446-72-0

    description1

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    Dipotassium Glycyrrhizinate

    Basic information

    Product Name: Andrographolide

    IUPAC Name: (3E,4S)-3-[2-[(1R,4aS,5R,6R,8aR)-6-Hydroxy-5-(hydroxymethyl)-5,8a-dimethyl-2-methylenedecahydronaphthalen-1-yl]ethylidene]-4-hydroxyfuran-2(3H)-one

    CAS No.​: 446-72-0

    Molecular Formula: C₁₅H₁₀O₅

    Physicochemical Properties:

    Parameter

    Value/Description

    ​Appearance​

    White powder

    ​Melting Point​

    230-234°C (decomposition)

    ​Solubility​

    Water solubility 0.1 mg/mL, soluble in methanol/acetone

    12​logP​

    1.5 (amphiphilic)

    ​Optical Rotation​

    [α]²⁵D = -126° (c=1, ethanol)

    Quality Standard: CP2020, JP, Customer Made

    Specification

    Test Items

    Standard

    Andrographolide (CAS: 5508-58-7)

    98% by HPLC

    Loss on drying

    ≤1.0%

    Residue on ignition

    ≤0.1%

    Key Features

    index_10-7

    Natural Source

    Whole plant of A. paniculata (leaf content up to 2.5%).
    index_10-7

    Multi-Target Action

    Simultaneously regulates NF-κB, MAPK, and other inflammatory pathways.
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    Clinical Value

    >85% efficacy in upper respiratory infections with no reported drug resistance

    Pharmacological Mechanisms

    1. Molecular Target Network

    Pharmacological Mechanisms1

    2. Pharmacokinetics

    Absorption

     Low oral bioavailability (2-5%), liposomes increase to 30%.

    Distribution

    Lung/liver ratio 3:1, minimal brain penetration (BBB<0.5%).

    Metabolism

    CYP3A4-mediated hydroxylation (forms 14-deoxyandrographolide).

    Excretion

    Primarily biliary (80% clearance in 48h).

    Clinical Applications​

    Indications & Protocols​

    ​Condition​

    ​Regimen​

    ​Evidence

    ​Viral Cold​

    60 mg tid×5 days

    40% faster symptom relief*

    ​Viral Hepatitis​

    100 mg bid×12 weeks

    HBV DNA↓1 log

    ​COVID-19 Adjuvant​

    80 mg IV qd×10 days

    IL-6↓50%

    *Multicenter RCT (n=600)

    Special Populations​

    Pediatrics: Half dose for ages 3-6 (10 mg/kg/day).

    Hepatic Impairment: Contraindicated in Child-Pugh C.

    Dosage and Administration

    Formulations​

    Tablets: 20 mg (oral)

    Injection: 50 mg/5 mL (dilute in glucose)

    Sublingual Pills: 10 mg

    Dosing Guidelines​

    ​Use​

    ​Dose​

    ​Duration

    Upper Respiratory

    60 mg tid

    3-5 days

    Chronic Hepatitis

    100 mg bid

    3-6 months

    Severe Viral Infection

    80-120 mg IV qd

    Until symptom resolution

    Safety Evaluation

    Adverse Reactions​

    System​

    ​Incidence​

    ​Management​

    Gastrointestinal

    5-8%

    Take with food

    Hypersensitivity

    <1%

    Discontinue

    Injection Site

    2%

    Apply heat

    Contraindications & Interactions​

    Absolute CI:
    Pregnancy (uterine stimulant effect).
    Active autoimmune diseases.

    Cautions:
    CYP3A4 substrates (e.g., statins): Potential ↑ plasma levels.

    Research Progress Green max

    Novel Formulations​

    ​Nanosuspensions: 10× higher lung targeting (COVID-19 therapy).

    ​Transdermal Gel: For localized rheumatoid arthritis treatment.

    New Indications​

    ​Alzheimer’s Disease: Reduces Aβ plaques (40%↓ in animal models).

    ​Cancer Immunotherapy: Synergizes with PD-1 antibodies (preclinical).

    Andrographis

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