Wogonin is a powerful flavone found in Chinese skullcap (Scutellaria baicalensis) that provides exceptional anticancer and anti-inflammatory benefits. This specialized plant compound, distinguished by its methoxy group at the C-8 position, helps inhibit cancer cell growth through multiple mechanisms, reduces inflammation by suppressing NF-κB signaling, provides neuroprotective benefits, supports liver health, offers anxiolytic effects through GABA receptor modulation, demonstrates antiviral and antimicrobial properties, provides immune system modulation, and shows antioxidant activity while working synergistically with other skullcap compounds to enhance overall health effects.
Alternative Names: 5,7-dihydroxy-8-methoxyflavone, 5,7-Dihydroxy-8-methoxyflavanone, Scutellaria flavone
Categories: Flavonoid, Phytochemical, Flavone
Primary Longevity Benefits
- Anti-inflammatory
- Antioxidant
- Anticancer
- Neuroprotective
Secondary Benefits
- Immune modulation
- Hepatoprotective
- Anxiolytic
- Antiviral
- Antimicrobial
Mechanism of Action
Wogonin exerts its diverse biological effects through multiple molecular pathways. As a potent anti-inflammatory agent, wogonin inhibits the nuclear factor-kappa B (NF-κB) signaling pathway by preventing the phosphorylation and degradation of IκBα, thereby blocking the nuclear translocation of NF-κB and subsequent expression of pro-inflammatory genes. It also suppresses the production of inflammatory mediators such as tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6), and prostaglandin E2 (PGE2) by inhibiting cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression. Wogonin’s antioxidant properties stem from its ability to scavenge reactive oxygen species (ROS) directly and to enhance the activity of endogenous antioxidant enzymes including superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx).
It activates the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway, leading to increased expression of antioxidant response element (ARE)-dependent genes. In cancer cells, wogonin induces apoptosis through both intrinsic (mitochondrial) and extrinsic (death receptor) pathways. It upregulates pro-apoptotic proteins (Bax, Bad) while downregulating anti-apoptotic proteins (Bcl-2, Bcl-xL), leading to mitochondrial membrane permeabilization, cytochrome c release, and caspase activation. Wogonin also inhibits cancer cell proliferation by arresting the cell cycle at G1/S or G2/M phases through modulation of cyclins, cyclin-dependent kinases (CDKs), and CDK inhibitors.
It suppresses angiogenesis by inhibiting vascular endothelial growth factor (VEGF) expression and signaling. Wogonin’s neuroprotective effects are mediated through multiple mechanisms, including inhibition of glutamate-induced excitotoxicity, reduction of oxidative stress in neuronal cells, and modulation of gamma-aminobutyric acid (GABA) receptors, which contributes to its anxiolytic properties. It enhances brain-derived neurotrophic factor (BDNF) expression and activates the phosphatidylinositol 3-kinase (PI3K)/Akt pathway, promoting neuronal survival and plasticity. In the liver, wogonin protects hepatocytes from oxidative damage and inflammation by inhibiting lipid peroxidation and enhancing the activity of phase II detoxification enzymes.
It also exhibits antiviral properties by interfering with viral replication processes and modulating host immune responses. Additionally, wogonin has immunomodulatory effects, regulating the function of various immune cells including T lymphocytes, B lymphocytes, macrophages, and dendritic cells, which contributes to its therapeutic potential in autoimmune and inflammatory disorders.
Optimal Dosage
Disclaimer: The following dosage information is for educational purposes only. Always consult with a healthcare provider before starting any supplement regimen, especially if you have pre-existing health conditions, are pregnant or nursing, or are taking medications.
Due to limited human clinical trials specifically on isolated wogonin, optimal dosage ranges are not well established. Most studies use Scutellaria baicalensis extracts standardized to contain 5-30% wogonin, with typical daily doses ranging from 300-900 mg of the extract.
By Condition
Condition | Dosage | Notes |
---|---|---|
Inflammation | 400-800 mg of standardized Scutellaria extract (containing approximately 20-40 mg wogonin) daily | Divided into 2-3 doses throughout the day with meals |
Anxiety | 300-600 mg of standardized Scutellaria extract daily | Lower doses may be effective due to GABA receptor modulation |
Neuroprotection | 500-900 mg of standardized Scutellaria extract daily | Higher doses may be required for crossing the blood-brain barrier in sufficient quantities |
Liver protection | 400-800 mg of standardized Scutellaria extract daily | May be more effective when combined with other hepatoprotective compounds |
By Age Group
Age Group | Dosage | Notes |
---|---|---|
Adults (18-65) | 300-900 mg of standardized Scutellaria extract daily | Start with lower doses and gradually increase as needed |
Seniors (65+) | 200-600 mg of standardized Scutellaria extract daily | Lower doses recommended due to potential changes in metabolism and elimination |
Children and adolescents | Not recommended | Safety and efficacy not established in pediatric populations |
Bioavailability
Absorption Rate
Wogonin has relatively poor oral bioavailability, estimated at approximately 1-5% in animal studies, primarily due to its low water solubility, extensive first-pass metabolism, and P-glycoprotein efflux in the intestine.
Enhancement Methods
Combination with piperine (black pepper extract) to inhibit P-glycoprotein efflux and intestinal metabolism, Liposomal encapsulation to improve solubility and intestinal absorption, Nanoparticle formulations to enhance cellular uptake and tissue distribution, Phospholipid complexation to improve lipid solubility and membrane permeability, Co-administration with quercetin or other flavonoids that may compete for metabolic enzymes, Cyclodextrin inclusion complexes to improve solubility, Emulsion-based delivery systems to enhance dissolution rate
Timing Recommendations
Wogonin is best absorbed when taken with meals containing some fat, which can enhance solubility and absorption. Taking divided doses throughout the day may maintain more consistent blood levels due to its relatively short half-life (approximately 2-4 hours in animal studies). For anxiety or sleep benefits, taking a dose in the evening may be beneficial due to its GABA-modulating effects. For anti-inflammatory effects, consistent daily dosing is recommended to maintain therapeutic levels.
Safety Profile
Safety Rating
Side Effects
- Gastrointestinal discomfort (mild to moderate)
- Nausea (uncommon)
- Diarrhea (uncommon)
- Headache (rare)
- Dizziness (rare)
- Potential sedative effects at higher doses
- Allergic reactions (rare)
Contraindications
- Pregnancy and breastfeeding (due to insufficient safety data)
- Scheduled surgery (discontinue 2 weeks before due to potential anticoagulant effects)
- Bleeding disorders (due to potential antiplatelet activity)
- Hormone-sensitive conditions (due to potential phytoestrogenic effects)
- Autoimmune conditions (caution due to immunomodulatory effects)
- Hypotension (may enhance blood pressure-lowering effects)
Drug Interactions
- Anticoagulant and antiplatelet medications (may enhance bleeding risk)
- Sedatives and CNS depressants (may enhance sedative effects)
- Cytochrome P450 substrates (may affect metabolism of drugs metabolized by CYP1A2, CYP2C9, CYP2C19, and CYP3A4)
- P-glycoprotein substrates (may alter drug transport and absorption)
- Immunosuppressants (may interfere with therapeutic effects)
- Antihypertensive medications (may enhance blood pressure-lowering effects)
- Hepatotoxic drugs (potential for additive effects on liver function)
Upper Limit
Due to limited human clinical data, a definitive upper limit has not been established. Based on animal studies and traditional use of Scutellaria baicalensis, doses exceeding 1200 mg of standardized extract (containing approximately 60-120 mg wogonin) daily are not recommended without medical supervision.
Regulatory Status
Fda Status
Wogonin itself is not approved as a drug by the FDA. Supplements containing wogonin or Scutellaria baicalensis extracts are regulated as dietary supplements under the Dietary Supplement Health and Education Act (DSHEA) of 1994. Manufacturers cannot make specific disease treatment claims but may make general structure/function claims with appropriate disclaimers. The FDA has not evaluated the safety or efficacy of wogonin specifically.
International Status
Eu: In the European Union, wogonin is not approved as a medicinal product. Scutellaria baicalensis extracts containing wogonin may be sold as food supplements, subject to the general food safety regulations. The European Food Safety Authority (EFSA) has not issued specific health claims for wogonin or Scutellaria extracts. Some EU member states may have their own regulations regarding traditional herbal medicinal products containing Scutellaria.
Canada: Health Canada regulates Scutellaria baicalensis extracts containing wogonin as Natural Health Products (NHPs). Several Scutellaria products have been issued Natural Product Numbers (NPNs), allowing them to be sold with specific health claims related to traditional use in Chinese medicine. Isolated wogonin is not specifically approved as a standalone ingredient.
Australia: The Therapeutic Goods Administration (TGA) regulates Scutellaria baicalensis extracts as complementary medicines. Several products containing these extracts are listed on the Australian Register of Therapeutic Goods (ARTG). Traditional use claims are permitted with appropriate evidence of traditional use in Chinese medicine.
China: Scutellaria baicalensis (Huang Qin) is officially listed in the Chinese Pharmacopoeia as a traditional Chinese medicine. Various formulations containing this herb are approved for specific indications based on traditional use and modern research. Isolated wogonin is used in research but is not commonly approved as a standalone pharmaceutical.
Japan: Scutellaria baicalensis is included in the Japanese Pharmacopoeia and is a component of several Kampo medicine formulations approved by the Ministry of Health, Labour and Welfare for specific indications. Pure wogonin is primarily used in research settings rather than as an approved therapeutic agent.
Synergistic Compounds
Compound | Synergy Mechanism | Evidence Rating |
---|---|---|
Baicalein | Both are flavones from Scutellaria baicalensis with complementary anti-inflammatory and antioxidant mechanisms. Baicalein enhances wogonin’s effects on NF-κB inhibition and may improve overall therapeutic outcomes. | 4 |
Baicalin | The glycoside form of baicalein, works synergistically with wogonin in modulating inflammatory pathways and enhancing antioxidant defense systems. | 4 |
Piperine | Enhances wogonin’s bioavailability by inhibiting P-glycoprotein efflux and intestinal metabolism, potentially increasing plasma concentrations. | 3 |
Quercetin | Complementary antioxidant and anti-inflammatory effects. May compete for metabolic enzymes, potentially extending wogonin’s half-life. | 3 |
Curcumin | Synergistic anti-inflammatory effects through complementary inhibition of NF-κB and inflammatory cytokines. Both compounds also show synergistic anticancer potential. | 3 |
EGCG (Epigallocatechin gallate) | Complementary antioxidant mechanisms and potential synergistic effects in cancer cell apoptosis induction. | 2 |
Resveratrol | Synergistic effects on AMPK activation and Nrf2 pathway enhancement, potentially improving antioxidant and metabolic benefits. | 2 |
Vitamin C | May help regenerate wogonin after it acts as an antioxidant, extending its antioxidant capacity. | 2 |
Zinc | Potential synergistic effects on immune modulation and antiviral activity. | 2 |
Conventional chemotherapeutic agents (e.g., etoposide, cisplatin) | Wogonin has been shown to enhance the apoptotic effects of certain chemotherapeutic agents in cancer cells while potentially reducing their toxicity to normal cells. | 3 |
Antagonistic Compounds
Compound | Interaction Type | Evidence Rating |
---|---|---|
Iron supplements | Wogonin may chelate iron, potentially reducing its absorption when taken simultaneously. | 2 |
Immunosuppressive drugs | Wogonin’s immunomodulatory effects may potentially interfere with the therapeutic action of immunosuppressants. | 2 |
Sedatives and CNS depressants | Wogonin’s GABA-modulating effects may potentiate the effects of sedatives, potentially leading to excessive sedation. | 3 |
Anticoagulant and antiplatelet medications | Wogonin may enhance the anticoagulant effects, potentially increasing bleeding risk. | 3 |
Cytochrome P450 substrates | Wogonin may inhibit certain CYP enzymes (particularly CYP1A2, CYP2C9, CYP2C19, and CYP3A4), potentially affecting the metabolism of drugs that are substrates for these enzymes. | 3 |
P-glycoprotein substrates | Wogonin may inhibit P-glycoprotein, potentially altering the transport and absorption of drugs that are P-gp substrates. | 2 |
Antihypertensive medications | Wogonin may enhance blood pressure-lowering effects, potentially leading to hypotension. | 2 |
Hepatotoxic drugs | While wogonin is generally hepatoprotective, high doses combined with hepatotoxic medications could potentially have additive effects on liver function. | 2 |
Hormone replacement therapy | Wogonin’s potential phytoestrogenic effects may interfere with hormone therapies. | 1 |
Cost Efficiency
Relative Cost
Medium to high
Cost Per Effective Dose
For standardized Scutellaria baicalensis extracts (typically containing 5-30% wogonin): $0.50-$2.00 per day for basic extracts; $2.00-$5.00 per day for premium, highly standardized, or enhanced bioavailability formulations. Pure isolated wogonin for research purposes is significantly more expensive, ranging from $200-$500 per gram.
Value Analysis
The cost-effectiveness of wogonin supplementation varies depending on the intended use and formulation quality. Standard Scutellaria extracts offer reasonable value for general anti-inflammatory and antioxidant benefits, comparable to other botanical anti-inflammatories like curcumin. However, the relatively low bioavailability of standard formulations may limit therapeutic potential, making enhanced delivery systems (liposomal, nanoparticle, etc.) potentially more cost-effective despite their higher price point. For specific conditions like anxiety or cognitive support, wogonin-containing extracts may offer good value compared to pharmaceutical alternatives, with potentially fewer side effects.
The highest value is likely found in high-quality, standardized extracts that specify exact wogonin content and employ bioavailability-enhancing technologies. These provide more predictable therapeutic effects, justifying their premium price. For research purposes, the cost of pure wogonin is high but necessary for controlled studies. For general consumers seeking health benefits, Scutellaria extracts standardized for total flavonoid content (including wogonin, baicalin, and baicalein) may offer the best overall value, as these compounds work synergistically.
Stability Information
Shelf Life
Pure wogonin powder is relatively stable for 2-3 years when properly stored. Standardized Scutellaria extracts typically have a shelf life of 2 years from the date of manufacture.
Storage Recommendations
Store in a cool, dry place away from direct sunlight in airtight containers. Refrigeration can extend shelf life, particularly for liquid formulations. Protect from moisture, heat, and light exposure, which can accelerate degradation. For research-grade pure wogonin, storage under inert gas (nitrogen or argon) at -20°C is recommended for maximum stability.
Degradation Factors
Exposure to UV light and sunlight – causes photodegradation and structural changes, High temperatures (above 30°C) – accelerates oxidation and decomposition, Moisture – can promote hydrolysis and microbial growth, Oxygen exposure – leads to oxidation of the flavonoid structure, pH extremes – wogonin is most stable at slightly acidic to neutral pH (5-7), Metal ions (particularly iron and copper) – can catalyze oxidation reactions, Enzymatic activity – may occur in improperly processed plant extracts
Sourcing
Synthesis Methods
- Semi-synthetic methods starting from chrysin or other flavonoid precursors
- Total chemical synthesis through chalcone intermediates followed by cyclization and methoxylation
- Biotechnological production using engineered microorganisms or plant cell cultures
Natural Sources
- Scutellaria baicalensis (Chinese skullcap) root – primary source, containing approximately 0.1-0.5% wogonin
- Scutellaria lateriflora (American skullcap) – contains lower concentrations
- Scutellaria barbata – contains varying amounts
- Andrographis paniculata – contains trace amounts
- Oroxylum indicum – contains small amounts
Quality Considerations
High-quality wogonin supplements should be standardized to contain a specific percentage of wogonin, typically verified by HPLC analysis. Look for products that specify the exact content of wogonin (not just total flavonoids) and provide third-party testing results. Scutellaria baicalensis extracts should be sourced from mature roots (at least 3-4 years old) as these contain higher concentrations of active flavonoids. Organic cultivation is preferred to minimize pesticide residues. Extraction methods significantly impact quality – alcohol-water extractions typically preserve more of the active compounds than water-only extractions. Avoid products with artificial fillers, preservatives, or excessive excipients. Some manufacturers use proprietary extraction technologies to enhance bioavailability, which may provide better therapeutic outcomes. For research purposes, high-purity isolated wogonin (>98%) is available from specialized chemical suppliers.
Historical Usage
Wogonin is a bioactive flavonoid primarily found in Scutellaria baicalensis (Huang Qin or Chinese skullcap), a plant that has been used in traditional Chinese medicine (TCM) for over 2,000 years. While wogonin itself was not isolated and identified until the modern era, the herb containing it has a rich historical usage. In TCM, Scutellaria baicalensis root is classified as a cooling herb that clears heat, dries dampness, and eliminates toxins. It was traditionally used to treat fevers, inflammation, respiratory infections, diarrhea, jaundice, and bleeding disorders.
The herb appears in numerous classical TCM formulations, including Huang-Lian-Jie-Du-Tang and Xiao-Chai-Hu-Tang. The first documented medicinal use of Scutellaria baicalensis appears in the Shennong Bencao Jing (Divine Farmer’s Materia Medica), compiled around 200-250 CE, where it was recommended for treating abscesses, sores, and inflammatory conditions. During the Ming Dynasty (1368-1644 CE), the famous physician Li Shizhen included detailed descriptions of Scutellaria baicalensis in his monumental work, the Compendium of Materia Medica (Bencao Gangmu), noting its effectiveness for ‘clearing heat from the upper burner’ and treating coughs with yellow phlegm, thirst, and irritability. In Japanese Kampo medicine, which evolved from TCM, Scutellaria baicalensis (called Ogon) is a component of important formulations such as Sho-saiko-to, used for liver disorders.
In Korean traditional medicine, the herb (known as Hwanggeumgol) was used similarly to its applications in China. Native American healers used the related species Scutellaria lateriflora (American skullcap) for nervous disorders, anxiety, and as a sedative, though this species contains lower concentrations of wogonin than its Asian counterpart. Modern scientific interest in wogonin began in the mid-20th century, with its isolation and structural characterization in the 1960s. Research intensified in the 1990s and 2000s as studies revealed its anti-inflammatory, antioxidant, and potential anticancer properties.
Today, wogonin is recognized as one of the key bioactive components responsible for many of the therapeutic effects traditionally attributed to Scutellaria baicalensis.
Scientific Evidence
Evidence Rating
Key Studies
Meta Analyses
Limited meta-analyses specifically on wogonin; most analyses focus on Scutellaria baicalensis extracts containing multiple flavonoids including wogonin, baicalin, and baicalein.
Ongoing Trials
Several preclinical studies investigating wogonin’s potential in cancer therapy, particularly in combination with conventional chemotherapeutic agents, Research on nanoparticle delivery systems to enhance wogonin’s bioavailability and targeted delivery, Investigations into wogonin’s neuroprotective effects in models of neurodegenerative diseases
Disclaimer: The information provided is for educational purposes only and is not intended as medical advice. Always consult with a healthcare professional before starting any supplement regimen, especially if you have pre-existing health conditions or are taking medications.