Luteolin (3',4',5,7-Tetrahydroxyflavone) | CAS 4484-88-2 | 98% HPLC | Light Yellow to Yellow Crystalline Powder | Natural Flavone / PI3K-Akt & NF-κB

1. Product Overview

Luteolin (CAS 4484-88-2), systematically named 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-1-benzopyran-4-one (3′,4′,5,7-tetrahydroxyflavone), is a naturally occurring flavone widely distributed in edible plants such as parsley, celery, chamomile, and Perilla frutescens. With the molecular formula C₁₅H₁₀O₆ and a molecular weight of 286.24 g/mol, it appears as a light yellow to yellow crystalline powder. Luteolin exhibits broad bioactivities including potent antioxidant, anti-inflammatory, and antitumor effects. It inhibits PI3K/Akt and NF-κB signaling pathways, suppresses COX-2/iNOS expression, scavenges ROS/RNS, and induces apoptosis in various cancer cell lines via mitochondrial and caspase-dependent mechanisms. It also displays IgE–receptor (FcεRI) antagonism and mast cell stabilization. This product is supplied exclusively for laboratory research use and is not intended for clinical, diagnostic, veterinary, food, or cosmetic applications.

2. Key Features and Advantages

• Multi-target bioactivity: Inhibits PI3K p110α/δ (low µM range), blocks IκBα degradation and NF-κB nuclear translocation, suppresses COX-2/iNOS via MAPK/AP-1 modulation; also inhibits PDE4 (bronchodilatory potential).

• Antioxidant & free radical scavenging: Direct DPPH•, ABTS•+, O₂•⁻, and •OH scavenging (IC₅₀ 5–20 µM in cell-free assays); upregulates Nrf2/ARE-dependent antioxidant enzymes (HO-1, NQO1).

• Pro-apoptotic in cancer cells: Induces caspase-3/8/9 activation, Bax/Bak upregulation, ΔΨm loss, and cell cycle arrest (G2/M or G0/G1 depending on cell type) at 10–50 µM; less toxic to normal cells at equivalent doses.

• High purity: Typically ≥98% by HPLC (suppliers offer 98–99%+), suitable for cell viability (MTT/CCK-8), Western blot (p-Akt, p-IκBα, cleaved caspase), flow cytometry (Annexin V/PI, ROS-DCFDA), and LC-MS quantification.

• Solubility: Soluble in DMSO (≥10 mg/mL with mild warming/sonication; 10–50 mM stock), ethanol, DMF; soluble in dilute alkali (turns yellow→deep yellow); practically insoluble in water (<0.05 mg/mL). Photosensitive — protect from light.

• Well-documented natural product: Referenced in >5,000 publications; stable at -20°C protected from light for 2–3 years.

3. Main Applications

• Antioxidant & anti-inflammatory research: Measuring ROS/RNS scavenging (DPPH, ABTS, ORAC), Nrf2 activation (ARE-luciferase), and suppression of pro-inflammatory cytokines (TNF-α, IL-6, IL-1β) in LPS-stimulated macrophages/Raw264.7.

• Signal transduction studies: Evaluating PI3K/Akt, MAPK, and NF-κB pathway inhibition by Western blot (p-Akt Ser473, p-ERK, p-IκBα) and reporter assays in cancer or immune cells.

• Antitumor mechanism: Assessing luteolin-induced apoptosis, autophagy (LC3-II conversion), cell cycle arrest, and sensitization to chemotherapeutics (e.g., doxorubicin, cisplatin) in HepG2, MCF-7, A549, etc.

• Allergic & mast cell studies: Testing FcεRI signaling inhibition, β-hexosaminidase release suppression, and degranulation blockade in RBL-2H3 or bone marrow–derived mast cells.

• Nutraceutical/botanical research: Quantification in plant extracts/foods by HPLC-DAD or LC-MS/MS; studying flavonoid metabolism (phase II conjugation: luteolin-7-O-glucuronide, etc.) and bioavailability.

4. Technical Specifications

5. Storage and Handling

• Store the powdered compound sealed with desiccant, strictly protected from light (amber vial or foil-wrapped); recommended storage at -20°C (long term 2–3 years) or 4°C (short term ≤6 months). For DMSO or ethanolic stock solutions, aliquot and store at -20°C or -80°C wrapped in foil (6–12 months stable); avoid repeated freeze–thaw cycles. Typical working stocks are 10–50 mM in anhydrous DMSO or absolute ethanol, prepared with gentle warming/sonication if needed.

• Before opening, allow the sealed vial to warm to room temperature to prevent moisture condensation. Keep container tightly closed and wrapped in aluminum foil when not in use.

• Handle in a well-ventilated area or fume hood. Use personal protective equipment including safety glasses, nitrile gloves, and a lab coat. Avoid inhalation of dust and contact with skin or eyes. May stain surfaces yellow.

• Intended exclusively for laboratory research by qualified personnel; not for human or veterinary use, food supplement formulation, or cosmetic applications (despite being a dietary flavonoid—this material is research-grade only).

6. Safety Overview

• Luteolin is a naturally occurring flavonoid with low acute toxicity in animal studies (LD₅₀ oral mouse >2,000 mg/kg) but has significant bioactivity as a kinase/NF-κB inhibitor and estrogen receptor modulator (weak ERβ affinity). Treat as potentially hazardous: may cause irritation to eyes, skin, and respiratory system.

• In case of eye contact, rinse immediately with plenty of running water for at least 15 minutes and seek medical advice. In case of skin contact, wash thoroughly with soap and water.

• If inhaled, move the person to fresh air and keep at rest in a position comfortable for breathing. If ingested, rinse mouth and seek medical attention—do not induce vomiting unless directed by medical personnel.

• Use appropriate engineering controls (fume hood) and personal protective equipment (safety goggles, nitrile gloves, lab coat). Avoid generating dust; work under reduced light if possible due to photosensitivity.

• Dispose of in accordance with local regulations for chemical waste. Do not discharge into drains, waterways, or soil.

• For detailed safety information, refer to the applicable Safety Data Sheet (SDS) prior to handling.

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