WOGONIN

Wogonin is an O-methylated flavone isolated from Scutellaria baicalensis with a broad spectrum of pharmacological activities including anticancer, anti-inflammatory, and neuroprotective effects. It induces apoptosis, inhibits angiogenesis, and modulates multiple cellular signaling pathways.

Wogonin is a natural flavonoid compound extracted from Scutellaria baicalensis (Chinese skullcap) and related species. It functions primarily through anti-inflammatory, anti-oxidative, and anti-cancer mechanisms, including modulation of MAPK signaling pathways, inhibition of COX-2 expression, and induction of ferroptosis in cancer cells. Research suggests potential applications in cancer treatment, pulmonary conditions, and inflammatory diseases.

Research

Reported Effects

Cancer Applications:: Shows promising results in preclinical studies for pancreatic and lung cancer through ferroptosis induction and PI3K/AKT pathway modulation. Pulmonary Conditions:: Demonstrates effectiveness in reducing pulmonary fibrosis and inflammation in animal models. Cardiac Protection:: Provides significant protection against septic cardiomyopathy in experimental settings. Limited Human Data:: Most evidence comes from in vitro and animal studies; clinical human trials are lacking

  • Shows promising results in preclinical studies for pancreatic and lung cancer through ferroptosis induction and PI3K/AKT pathway modulation
  • Demonstrates effectiveness in reducing pulmonary fibrosis and inflammation in animal models
  • Provides significant protection against septic cardiomyopathy in experimental settings
  • Most evidence comes from in vitro and animal studies; clinical human trials are lacking

Safety Profile

Safety Profile: Wogonin

Common Side Effects

  • Limited human clinical data; most safety information derived from in vitro and animal studies
  • Mild gastrointestinal discomfort including nausea and stomach upset at typical supplement doses
  • Potential sedative effects and drowsiness due to GABAergic activity (wogonin is a positive allosteric modulator of GABA-A receptors)
  • Mild headache reported by some users
  • Dizziness and lightheadedness, potentially related to anxiolytic effects

Serious Adverse Effects

  • Hepatotoxicity: High-dose wogonin has shown hepatotoxic effects in some animal studies; monitor liver function with prolonged use
  • Pro-apoptotic activity: Wogonin induces apoptosis in various cancer cell lines in vitro; while potentially therapeutic, effects on healthy cells at high doses are not fully characterized
  • Bleeding risk: Wogonin and related flavones from Scutellaria baicalensis may have antiplatelet and anticoagulant properties
  • Limited pharmacokinetic data in humans; bioavailability, half-life, and dose-response relationships not well established
  • Potential immunomodulatory effects could theoretically worsen autoimmune conditions

Contraindications

  • Known hypersensitivity to wogonin, Scutellaria baicalensis (Chinese skullcap), or related Lamiaceae family plants
  • Active liver disease or hepatic impairment (hepatotoxicity risk)
  • Concurrent use of CNS depressants (additive sedation via GABA modulation)
  • Active bleeding disorders or upcoming surgery (discontinue 2 weeks prior)
  • Pregnancy and lactation (insufficient safety data; pro-apoptotic activity is a concern)

Drug Interactions

  • Benzodiazepines and other GABAergic drugs: Additive sedation and CNS depression; wogonin binds GABA-A receptors at the benzodiazepine site
  • Anticoagulants/Antiplatelets: Potential additive bleeding risk
  • CYP1A2 and CYP3A4 substrates: Wogonin may inhibit these enzymes in vitro; clinical significance uncertain but caution warranted with narrow therapeutic index drugs
  • Hepatotoxic drugs (acetaminophen, statins, methotrexate): Additive liver injury risk
  • Chemotherapy agents: Wogonin has shown synergistic cytotoxicity with some chemotherapeutics in vitro; consult oncologist

Population-Specific Considerations

  • Elderly: Higher susceptibility to sedative effects; start with lowest dose; monitor for falls and drowsiness
  • Pediatric: No safety data; not recommended
  • Anxiety patients: Potential therapeutic benefit via GABA modulation, but should not replace evidence-based anxiolytics
  • Cancer patients: Investigational anticancer properties; do not use as a substitute for standard therapy; consult oncologist
  • Liver disease patients: Avoid due to potential hepatotoxicity

Pharmacokinetic Profile

Molecular Structure

2D Structure
WOGONIN molecular structure
Molecular Properties
Formula
C16H12O5
Weight
284.26 Da
PubChem CID
5281703
Exact Mass
284.0685 Da
LogP
3
TPSA
76 Ų
H-Bond Donors
2
H-Bond Acceptors
5
Rotatable Bonds
2
Complexity
426
Identifiers (SMILES, InChI)
InChI
InChI=1S/C16H12O5/c1-20-15-12(19)7-10(17)14-11(18)8-13(21-16(14)15)9-5-3-2-4-6-9/h2-8,17,19H,1H3
InChIKeyXLTFNNCXVBYBSX-UHFFFAOYSA-N

Safety Profile

Common Side Effects

  • Limited Safety Data:: Few reported side effects in research studies, but long-term human safety data is minimal
  • Interaction Potential:: As a COX-2 inhibitor and MAPK modulator, may interact with medications affecting these pathways
  • Metabolic Considerations:: Converts to oroxylin A metabolite which may have different activity profile than parent compound
  • Red Blood Cell Effects:: While protective against eryptosis in some conditions, effects on normal red blood cell function require further study

References (6)

  1. [2]
    Wogonin Attenuates Bleomycin-Induced Pulmonary Fibrosis and Oxidative Stress Injury via the MAPK Signaling Pathway

    Wogonin significantly reduced pulmonary fibrosis and oxidative stress in a rat model by modulating the MAPK pathway, showing potential as a therapeutic agent for idiopathic pulmonary fibrosis.

  2. [3]
    Wogonin, a bioactive flavonoid in herbal tea, inhibits inflammatory cyclooxygenase-2 gene expression in human lung epithelial cancer cells

    Wogonin inhibited PMA-induced COX-2 expression in lung cancer cells at the transcriptional level through the MEK1/2 pathway and AP-1 activity, demonstrating anti-inflammatory and anti-cancer properties.

  3. [4]
    Antiproliferative Wnt inhibitor wogonin prevents eryptosis following ionophoric challenge, hyperosmotic shock, oxidative stress, and metabolic deprivation

    Wogonin protected red blood cells from premature death (eryptosis) under various stress conditions including calcium overload and oxidative stress, suggesting potential in preventing chemotherapy-related anemia.

  4. [5]
    Detection of baicalin metabolites baicalein and oroxylin-a in mouse pancreas and pancreatic xenografts

    Study demonstrated that baicalin from Scutellaria baicalensis undergoes significant methylation to oroxylin A during absorption, with substantial amounts detected in pancreatic tissue and tumors, showing tissue-specific distribution patterns.

  5. [6]
    Comparison of the major flavonoid content of S. baicalensis, S. lateriflora, and their commercial products

    Analysis of Scutellaria species found significant variations in wogonin and baicalin content between roots and aerial parts, with roots containing substantially higher levels of active flavonoids.

  6. [1]
    Wogonin attenuates septic cardiomyopathy by suppressing ALOX15-mediated ferroptosis

    Wogonin protected against septic cardiomyopathy in mice by directly binding to and inhibiting ALOX15, preventing cardiomyocyte ferroptosis and improving cardiac function. The cardioprotective effects were mediated through suppression of ALOX15-initiated ferroptosis.

Updated 2026-03-08Sources: peptidebay, pubchem

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