Wogonin

Wogonin is a naturally occurring flavone derived primarily from the root of Scutellaria baicalensis (Chinese skullcap) that exerts anticancer and anti-inflammatory effects through modulation of ER stress pathways, p53 activation, and HIF-1α degradation. Its bioactivity is driven by inhibition of pro-inflammatory cytokines including IL-6 and TNF-α, as well as suppression of tumor angiogenesis in preclinical models.

Origin & History

Wogonin is a natural flavone compound primarily extracted from the roots of Scutellaria baicalensis (Baikal skullcap), a plant used in traditional Chinese medicine. While commercial extraction processes are not specified in available research, this bioactive flavonoid has been isolated for therapeutic evaluation in numerous preclinical studies.

Historical & Cultural Context

Wogonin is derived from Scutellaria baicalensis roots, which have been used in Traditional Chinese Medicine for centuries to inhibit tumor growth and reduce inflammation. While specific historical use of isolated wogonin is not detailed, the parent plant has longstanding attribution to anti-inflammatory and anticancer benefits in TCM contexts.

Health Benefits

• Anti-cancer effects: Induces apoptosis in colorectal cancer cells (HCT-116) through ER stress and p53 activation, inhibits tumor angiogenesis via HIF-1α degradation (preclinical evidence only)
• Anti-inflammatory activity: Reduces IL-6 and TNF-α in rat models of chronic rhinosinusitis at 10-20 mg/kg doses (animal studies)
• Chemosensitization: Shows synergistic effects with chemotherapeutics like etoposide and paclitaxel in preclinical models
• Cell cycle regulation: Causes G2/M phase arrest and autophagy through PI3K/AKT and STAT3 pathway modulation (in vitro studies)
• Selective CDK9 inhibition: Directly binds CDK9 to suppress cancer cell growth more selectively in malignant than normal cells (preclinical data)

How It Works

Wogonin induces apoptosis in cancer cells by triggering endoplasmic reticulum (ER) stress and activating the tumor suppressor protein p53, which upregulates pro-apoptotic signals such as Bax and caspase-3. It suppresses tumor angiogenesis by promoting proteasomal degradation of hypoxia-inducible factor 1-alpha (HIF-1α), thereby reducing VEGF expression in hypoxic tumor microenvironments. Anti-inflammatory activity is mediated through inhibition of NF-κB signaling, which downstream reduces transcription of IL-6, TNF-α, and COX-2 in activated macrophages and epithelial cells.

Scientific Research

No human clinical trials, randomized controlled trials, or meta-analyses have been conducted on wogonin to date. All evidence is limited to preclinical in vitro and in vivo studies, with researchers explicitly calling for future clinical translation due to promising antitumor, anti-inflammatory, neuroprotective, and antiviral effects observed in laboratory settings.

Clinical Summary

The majority of evidence for wogonin derives from in vitro cell studies and rodent models, including rat models of chronic rhinosinusitis where oral doses of 10–20 mg/kg reduced IL-6 and TNF-α levels significantly compared to controls. Anticancer data in HCT-116 colorectal cancer cells demonstrates dose-dependent apoptosis induction, but these findings have not been replicated in human clinical trials. No large-scale randomized controlled trials (RCTs) in human subjects have been published for wogonin as an isolated compound. Current evidence must be characterized as preliminary and preclinical, and direct therapeutic claims in humans are not yet supported.

Nutritional Profile

Wogonin (5,7-dihydroxy-8-methoxyflavone) is a naturally occurring monoflavonoid compound, not a conventional food ingredient with macronutrients or micronutrients. It is a pure bioactive compound typically isolated from the root of Scutellaria baicalensis (Chinese skullcap) and related plants.

Bioactive compound identity:
- Molecular formula: C16H12O5
- Molecular weight: 284.26 g/mol
- Classification: O-methylated flavone (flavonoid subclass)
- Typical concentration in Scutellaria baicalensis root: 0.5–2% dry weight
- It contains no meaningful macronutrients (protein, fat, carbohydrates), micronutrients (vitamins, minerals), or caloric value in pharmacologically relevant doses

Approximate concentrations in source material:
- Scutellaria baicalensis root extract: ~1–20 mg/g dry extract depending on preparation
- Commercially standardized extracts: typically 95–98% purity in isolated form

Bioavailability notes:
- Poor oral bioavailability due to extensive first-pass metabolism and low aqueous solubility (log P ~2.6)
- Undergoes glucuronidation and sulfation in the intestine and liver
- Peak plasma concentration (Tmax) reached at approximately 1–2 hours post oral administration in animal models
- Bioavailability enhanced by nanoparticle formulations, lipid-based drug delivery systems, and co-administration with piperine
- Rapidly metabolized to wogonin-7-O-glucuronide as primary circulating metabolite
- Half-life approximately 2–4 hours in rodent models; human pharmacokinetic data limited

Preparation & Dosage

No clinically studied dosage ranges exist due to absence of human trials. Preclinical studies used 10-20 mg/kg intraperitoneally in rats and 50-100 μM concentrations in cell culture studies. Consult a healthcare provider before starting any new supplement.

Synergy & Pairings

Etoposide, Paclitaxel, Other flavonoids, Scutellaria baicalensis whole extract, Anti-inflammatory compounds

Safety & Interactions

Wogonin has shown a generally favorable safety profile in animal studies at doses up to 50 mg/kg, but human safety data are extremely limited given the absence of clinical trials using isolated wogonin. Because wogonin inhibits CYP450 enzymes, particularly CYP1A2 and CYP3A4, it may increase plasma concentrations of co-administered drugs metabolized by these pathways, including certain statins, anticoagulants, and benzodiazepines. Pregnant and breastfeeding individuals should avoid wogonin supplementation due to insufficient safety data and theoretical teratogenic risks observed in early animal studies. Individuals on anticoagulant therapy such as warfarin should exercise caution, as flavone compounds can potentiate bleeding risk.