Eupatilin (Polymethoxyflavone · Gastroprotective · Anti-inflammatory)
| Compound | Eupatilin (5,7-Dihydroxy-3′,4′,6-Trimethoxyflavone; Stillen® active ingredient) |
| Chemical class | Polyphenol — Flavone (Polymethoxyflavone; Artemisia-type) |
| CAS | 22368-21-4 |
| Primary source | Artemisia asiatica, Artemisia argyi (Korean/Chinese mugwort) |
| Key applications | Gastroprotective (gastric ulcer, GERD); anti-inflammatory; antioxidant |
| Claim strength | High (gastroprotective RCT); Moderate (anti-inflammatory) |
| Typical form | Artemisia asiatica extract standardised to eupatilin ≥0.5%; Stillen® (prescription Korea) |
| Buy from Herbuno | Availability on request — request bulk pricing → |
Name origin: Eupatilin is named after Eupatorium — an early misattribution, as the compound is now primarily associated with Artemisia species. It is a polymethoxyflavone carrying three methoxy groups (3′, 4′, 6-positions) alongside two free hydroxyl groups at C-5 and C-7. Traditional use: Artemisia asiatica (Korean mugwort, Ssuk) is one of the most important medicinal plants in Korean traditional medicine — used for gastrointestinal disorders, gynaecological conditions, and as a warming agent. The fresh juice is consumed for gastritis, peptic ulcer, and intestinal inflammation in Korean folk medicine. Eupatilin was identified as the primary gastric-protective constituent of Artemisia asiatica extracts. Research trajectory: Eupatilin is commercially developed as Stillen® (Dong-A Pharmaceutical, Korea) — a prescription gastroprotective drug — making it one of the very few flavone compounds to achieve drug approval. Multiple Phase III RCTs in gastritis, gastric ulcer, and GERD have been conducted. Commercial source: Eupatilin standardised isolate is not currently in the Herbuno catalogue at compound-specific level; availability on request.
Evidence for Eupatilin Applications
Gastroprotective activity: Multiple Korean RCTs (Stillen® Phase II/III trials) demonstrate eupatilin at 60 mg/day significantly reduces endoscopic gastritis severity scores, improves gastric mucosal integrity, and accelerates gastric ulcer healing versus placebo. Mechanism involves gastric mucus secretion stimulation (via PGE₂ upregulation), inhibition of H. pylori virulence factors (CagA, VacA), and reduction of neutrophil-mediated mucosal damage. Claim strength: High.
Anti-inflammatory: Eupatilin inhibits COX-2 selectively over COX-1 — a gastroprotective profile sparing prostaglandin synthesis needed for mucosal integrity while reducing inflammatory prostaglandins. 5-LOX inhibition and NF-κB suppression are also documented. Claim strength: Moderate.
Anti-cancer: Eupatilin has demonstrated antiproliferative activity in gastric, cervical, and colorectal cancer cell lines via G2/M arrest, caspase activation, and PI3K/Akt pathway inhibition. Research is preclinical. Claim strength: Emerging.
Neuroprotective: In glutamate-induced neurotoxicity and amyloid-β aggregation models, eupatilin at 10–50 μM demonstrates neuroprotective activity via Nrf2 induction and MAPK modulation. Distant from its gastroprotective evidence base; preclinical only. Claim strength: Emerging.
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Dosage & Formulator Specification
Eupatilin's pharmaceutical dosing (Stillen®) is 60 mg/day (30 mg twice daily) as a standardised tablet for gastritis and gastric ulcer treatment in South Korea — prescription-only. Eupatilin itself is not a controlled substance in most markets but is not yet widely available as supplement-grade material.
For formulators seeking Artemisia-based gastroprotective formulas, A. asiatica extract standardised to eupatilin (≥0.5–1.0%) is the appropriate specification. This is distinct from Artemisia annua (artemisinin source) and Artemisia absinthium (absinthin/thujone source). Species verification is essential.
Eupatilin's polymethoxy structure confers higher lipophilicity than unsubstituted flavones, making it a candidate for lipid-based formulation or self-emulsifying delivery systems for improved oral bioavailability. Stable under normal manufacturing conditions (pH 4–8, up to 80 °C for short periods).
Eupatilin's mechanism (mucosal defence strengthening) is complementary to PPIs (acid suppression) — the two approaches may be synergistic for patients with insufficient response to acid suppression alone.
Frequently Asked Questions — Eupatilin
Is eupatilin the same as the drug Stillen?
Stillen® is a registered Korean prescription drug whose active ingredient is eupatilin isolated from Artemisia asiatica — one of the few flavone compounds with Phase III RCT data backing a regulatory drug approval, distinguishing it from most plant polyphenols with only preclinical evidence.
Which Artemisia species is the commercial source of eupatilin?
Artemisia asiatica (Korean mugwort, Ssuk) and Artemisia argyi (Chinese moxa herb, Ai Ye) are the primary eupatilin-yielding species. A. annua (sweet wormwood — artemisinin source) and A. absinthium (absinthin/thujone source) are distinctly different species not used for eupatilin production.
What gastric conditions has eupatilin been clinically validated for?
Korean Phase II and III RCTs have validated eupatilin (Stillen® 60 mg/day) for acute and chronic gastritis, peptic ulcer healing acceleration, and GERD — the strongest clinical evidence base for any flavone compound in gastrointestinal medicine.
How does eupatilin's mechanism differ from PPIs (proton pump inhibitors)?
PPIs reduce gastric acid secretion to limit mucosal exposure. Eupatilin does not inhibit acid secretion; instead it strengthens the gastric mucosal defence layer — stimulating mucus production, increasing PGE₂-mediated mucosal blood flow, and reducing neutrophil infiltration. These complementary mechanisms suggest potential for combination use.
Related compounds: Sinensetin, Nobiletin, Tangeretin, Chrysin
Claim-strength scale – High = multiple human RCTs; Moderate = limited trials or strong preclinical convergence; Emerging = early-stage lab or animal data.
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