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Naringin
Natural API

Naringin

Naringin (CAS: 10236-47-2) is a naturally occurring dihydroflavonoid glycoside. As the primary bitter compound in citrus fruits (especially grapefruit), it serves defensive and signaling functions in plants. Modern research has revealed naringin's broad biological activities, making it a hotspot in natural product research.

Product Name: Naringin

CAS No.​: 10236-47-2

Molecular Formula: C₂₇H₃₂O₁₄

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    Naringin

    Basic information

    Product Name: Naringin

    CAS No.​: 10236-47-2

    Molecular Formula: C₂₇H₃₂O₁₄

    Physicochemical Properties:

    Parameter

    Value/Description

    Appearance

    White to pale yellow crystalline powder

    Melting point

    171-174°C

    Solubility

    Poor in water (0.1 mg/mL), soluble in DMSO/methanol

    [α]D²⁰

    -82° (c=1, ethanol)

    pKa

    7.2 (phenolic hydroxyl)

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Naringin (CAS: 10236-47-2)

    98% by HPLC

    Loss on drying

    ≤5.0%

    Ash

    ≤1.0%

    Key Features

    index_10-7

    Abundant source

    Grapefruit peel and pulp (content up to 1-5%)
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    Pleiotropic effects

    Combines antioxidant, anti-inflammatory, and metabolic regulation properties
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    Prodrug characteristic

    Metabolized into more active naringenin in intestines

    Pharmacological Mechanisms

    1.Molecular Target Network

    Molecular Target Network

    2.Pharmacokinetics

    Absorption

    Hydrolyzed to aglycone in gut, bioavailability 5-8%

    Distribution

    92% plasma protein binding, low BBB penetration

    Metabolism

    Significant enterohepatic circulation, mainly UGT1A1/1A9 glucuronidation

    Excretion

    Primarily biliary (>60%), urinary <10%

    Clinical Applications

    Indication

    Mechanism

    Evidence Level

    Type 2 diabetes

    Glycosidase inhibition + insulin sensitization

    Phase II

    NAFLD

    Lipid metabolism + anti-fibrosis

    Animal models

    Chemoadjuvant

    Cisplatin nephrotoxicity mitigation

    Phase I

    Dosage and Administration

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    Diabetes

    500-1000 mg/day (bid)
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    Antioxidant

     250 mg/day
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    MTD

     Single dose ≤2000 mg

    Safety Evaluation

    1. Adverse Effects

    System

    Incidence

    Manifestations

    Gastrointestinal

    15%

    Bloating, diarrhea

    Neurological

    3%

    Mild headache

    Hypersensitivity

    <1%

    Rash

    2. Drug Interactions

    CYP3A4 substrates (e.g., statins): AUC may increase 2-3×

    P-gp inhibitors (e.g., cyclosporine): Bioavailability ↑40%

    Research Progress Green max

    Novel Formulations

    Phospholipid complex: Bioavailability →25%

    Nanocrystals: 8× higher BBB penetration

    Sustained-release microspheres: t₁/₂→12h

    New Indications

    Alzheimer's: 60% higher Aβ clearance (animal)

    COVID-19: 3CL protease inhibition (IC₅₀=32 μM)

    pomelo

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