Compound Monograph

Jaceosidin

Jaceosidin (4',5,7-trihydroxy-3',6-dimethoxyflavone) is a 6-methoxyflavone of mugwort (Artemisia) and yerba santa, closely co-studied with eupatilin. Its research is a broad but cell-line-dominated anticancer literature (including HPV-16 E6/E7 inhibition) plus rodent anti-inflammatory work — all preclinical, with no human trials, and one honest counter-signal (it is pro-angiogenic in endothelial cells).

Classification

Jaceosidin is a flavone (6-methoxyflavone), part of the phenolics class. Antioxidant compounds built around one or more phenol rings — the flavonoids, tannins, phenolic acids, coumarins, and pigments behind much of a plant's protective chemistry.

Where Does It Come From? (5)

Jaceosidin is a naturally occurring flavone (6-methoxyflavone), found in Mugwort, Yerba Santa and 3 other sources. It is well tolerated orally (low toxicity).

Artemisia vulgaris and other Artemisia speciesCentaurea species Feverfew Tanacetum parthenium Mugwort Yerba Santa Eriodictyon californicum

Pharmacology & Research

Jaceosidin is a 6-methoxyflavone (a methoxylated relative of luteolin) whose pharmacology is largely Korean Artemisia research, tightly paired with its co-flavone eupatilin. The bulk of its literature is a broad but cell-line-dominated anticancer dataset — its single most-cited result being inhibition of the HPV-16 E6/E7 oncoproteins 1Reference 1Kim MK et al. · 2005Inhibitory effect of jaceosidin from Artemisia argyi on the function of HPV-16 E6/E7 oncoproteinsView study → — alongside rodent anti-inflammatory work. Everything is preclinical, there are no human trials, and one honesty point runs through the page: in endothelial cells jaceosidin is pro-angiogenic 6Reference 62014Jaceosidin promotes angiogenesis via VEGFR2/FAK/PI3K/AKT/NF-κB in endothelial cells (context caution)View study →, which cuts against a naive “anti-tumour” framing.

What the evidence supports
  • Broad preclinical anticancer + anti-inflammatory signals: apoptosis/cell-cycle arrest across several tumour lines and reduced inflammation in mouse models 1,2,8Reference 1Kim MK et al. · 2005Inhibitory effect of jaceosidin from Artemisia argyi on the function of HPV-16 E6/E7 oncoproteinsView study →Reference 2Lee HG et al. · 2013Jaceosidin induces G2/M arrest via ATM–Chk1/2→cdc25C–cdc2 in endometrial cellsView study →Reference 8Min SW et al. · 2009AnimalEupatilin and jaceosidin inhibit carrageenan-induced inflammation in miceView study →.
  • The honest headline: essentially all in-vitro/rodent, with no in-vivo tumour efficacy or human data — and a pro-angiogenic endothelial result 6Reference 62014Jaceosidin promotes angiogenesis via VEGFR2/FAK/PI3K/AKT/NF-κB in endothelial cells (context caution)View study → that argues against self-medication framing in cancer or vascular-sensitive contexts.
Evidence by indicationStrength of support
32%
AntioxidantUnsupported
18%
1. Anticancer

Jaceosidin’s strongest single result is inhibition of HPV-16 E6/E7 oncoprotein function in cervical-cancer cells 1Reference 1Kim MK et al. · 2005Inhibitory effect of jaceosidin from Artemisia argyi on the function of HPV-16 E6/E7 oncoproteinsView study →; other lines show G2/M arrest via ATM–Chk1/2 in endometrial cells 2Reference 2Lee HG et al. · 2013Jaceosidin induces G2/M arrest via ATM–Chk1/2→cdc25C–cdc2 in endometrial cellsView study →, p53-dependent arrest in U87 glioblastoma 3Reference 3Khan M et al. · 2011Jaceosidin induces p53-dependent G2/M arrest in U87 glioblastoma cellsView study →, Bax/Mcl-1/c-FLIP-mediated apoptosis in renal Caki cells 4Reference 4Jeong MS et al. · 2016Jaceosidin induces apoptosis via Bax/Mcl-1/c-FLIP in renal Caki cellsView study → and ROS-driven apoptosis in ras-transformed breast epithelium 5Reference 5Lee HG et al. · 2007Jaceosidin induces apoptosis in ras-transformed breast epithelial cells via ROSView study →.

Gap: essentially all in-vitro (the HPV work extends to docking-only in-silico studies), with no in-vivo tumour efficacy and no human data — and jaceosidin is pro-angiogenic in endothelial cells (VEGFR2/FAK/PI3K/AKT/NF-κB) 6Reference 62014Jaceosidin promotes angiogenesis via VEGFR2/FAK/PI3K/AKT/NF-κB in endothelial cells (context caution)View study →, a counter-signal that must be stated honestly 1,6Reference 1Kim MK et al. · 2005Inhibitory effect of jaceosidin from Artemisia argyi on the function of HPV-16 E6/E7 oncoproteinsView study →Reference 62014Jaceosidin promotes angiogenesis via VEGFR2/FAK/PI3K/AKT/NF-κB in endothelial cells (context caution)View study →.

2. Anti-inflammatory / anti-allergic

Jaceosidin has in-vitro antioxidant and anti-inflammatory activity from A. princeps 7Reference 7Jung UJ et al. · 2008In-vitro antioxidant and anti-inflammatory activities of jaceosidin from Artemisia princepsView study →, reduced carrageenan-induced paw inflammation in mice (with eupatilin) 8Reference 8Min SW et al. · 2009AnimalEupatilin and jaceosidin inhibit carrageenan-induced inflammation in miceView study →, and benefited a mouse atopic-dermatitis model via ubiquitin-mediated JAK1 degradation 10Reference 102026Jaceosidin ameliorates atopic dermatitis via ubiquitin-mediated JAK1 degradationView study →; the mechanism centres on ERK/NF-κB suppression (blocking TPA-induced COX-2 and MMP-9) 9Reference 9Jeong MA et al. · 2007Jaceosidin inhibits TPA-induced COX-2 and MMP-9 via ERK1/2View study →.

Gap: small models, often co-dosed with eupatilin, with no human trials 8,10Reference 8Min SW et al. · 2009AnimalEupatilin and jaceosidin inhibit carrageenan-induced inflammation in miceView study →Reference 102026Jaceosidin ameliorates atopic dermatitis via ubiquitin-mediated JAK1 degradationView study →.

3. Antioxidant

Jaceosidin’s flavone hydroxyl pattern gives in-vitro radical-scavenging activity 7Reference 7Jung UJ et al. · 2008In-vitro antioxidant and anti-inflammatory activities of jaceosidin from Artemisia princepsView study →.

Gap: generic scavenging with no isolate clinical relevance 7Reference 7Jung UJ et al. · 2008In-vitro antioxidant and anti-inflammatory activities of jaceosidin from Artemisia princepsView study →.

4. Bitter-receptor antagonism

Jaceosidin (with other Eriodictyon californicum flavonoids) antagonises the human bitter receptor hTAS2R31 in a cell assay 14Reference 14Fletcher JN et al. · 2011Flavonoids from Eriodictyon californicum as hTAS2R31 bitter-receptor antagonistsView study → — a plausible contributor to yerba santa’s traditional “bitter-blocking” reputation.

Gap: one in-vitro report, and a flavour-science curiosity rather than a health claim — no confirmation that whole-plant exposure produces a meaningful taste effect in people 14Reference 14Fletcher JN et al. · 2011Flavonoids from Eriodictyon californicum as hTAS2R31 bitter-receptor antagonistsView study →.

Mechanisms

Target / pathwayEffectRelevant to
HPV-16 E6 / E7 oncoproteinsinhibits function (cell; docking-predicted binding)anticancer (cervical/HPV)
ATM–Chk1/2; p53; Bax↑/Mcl-1↓/c-FLIP↓cell-cycle arrest and intrinsic apoptosisanticancer (various lines)
ERK1/2 → COX-2, MMP-9; NF-κB / MAPKsuppressedanti-inflammatory / anti-invasion
JAK1ubiquitin-mediated degradationatopic-dermatitis model
VEGFR2/FAK/PI3K/AKT/NF-κBactivated → pro-angiogenic (context caution)endothelial counter-signal
hTAS2R31 (bitter receptor)antagonist (cell assay)taste / bitter-masking

Pharmacokinetics

Jaceosidin shows typical flavone pharmacokinetics — poor. Systemic levels are low enough to require tandem MS for quantitation in rat plasma 11Reference 112009AnimalLC-MS/MS determination of jaceosidin in rat plasmaView study →, and human-liver-microsome work shows it is metabolised by cytochrome P450 with rapid phase-II UGT glucuronidation 12Reference 122010In-vitro metabolism of jaceosidin: CYP and UGT characterisation in human liver microsomesView study →; both jaceosidin and eupatilin also inhibit several CYP activities in vitro, a theoretical herb–drug-interaction signal at high exposure 13Reference 132010Effects of eupatilin and jaceosidin on CYP450 activities in human liver microsomesView study →. The expected profile is low oral bioavailability, extensive first-pass conjugation and short plasma exposure, with no human pharmacokinetics for the isolate.

Clinical trials

There are no human clinical trials of isolated jaceosidin (efficacy, PK or safety); all evidence is in-vitro or rodent.

CompletedPlannedTerminatedPreclinical
(none, isolate)Moderate(cell-line-dominated)

Last checked: July 2026.

Toxicity & Safety

Jaceosidin has a low isolate-toxicity signal on thin data — no isolated-compound toxicology of concern surfaced, and it shows the usual flavone preference for transformed over normal cells in several studies. Two discipline points: do not import wormwood/thujone toxicity onto this molecule — thujone is a chemically and toxicologically unrelated monoterpene ketone from Artemisia, and jaceosidin carries none of that convulsant profile; and two honest caveats belong on the page — in-vitro CYP inhibition flags a possible herb–drug interaction at high doses 13Reference 132010Effects of eupatilin and jaceosidin on CYP450 activities in human liver microsomesView study →, and the pro-angiogenic endothelial finding 6Reference 62014Jaceosidin promotes angiogenesis via VEGFR2/FAK/PI3K/AKT/NF-κB in endothelial cells (context caution)View study → argues against self-medication framing in cancer or vascular-sensitive contexts.

Pregnancy & lactation

Avoid. No reproductive or developmental data exist for the isolate, and its major botanical source (mugwort/Artemisia) carries a traditional emmenagogue/uterine-stimulant reputation at the whole-herb level — so it is not recommended in pregnancy or lactation.

Dosage

There is no established human dose — jaceosidin has never been given to humans as an isolate. All dosing is preclinical (µM in vitro; mg/kg in rodent models) and not translatable, so no human figure should be inferred.

References

  1. Kim MK, et al. (2005). Inhibitory effect of jaceosidin from Artemisia argyi on the function of HPV-16 E6/E7 oncoproteins. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/15814270/
  2. Lee HG, et al. (2013). Jaceosidin induces G2/M arrest via ATM–Chk1/2→cdc25C–cdc2 in endometrial cells. Food and Chemical Toxicology. https://pubmed.ncbi.nlm.nih.gov/23274058/
  3. Khan M, et al. (2011). Jaceosidin induces p53-dependent G2/M arrest in U87 glioblastoma cells. Asian Pacific Journal of Cancer Prevention. https://pubmed.ncbi.nlm.nih.gov/22471459/
  4. Jeong MS, et al. (2016). Jaceosidin induces apoptosis via Bax/Mcl-1/c-FLIP in renal Caki cells. Chemico-Biological Interactions. https://pubmed.ncbi.nlm.nih.gov/27729209/
  5. Lee HG, et al. (2007). Jaceosidin induces apoptosis in ras-transformed breast epithelial cells via ROS. Annals of the New York Academy of Sciences. https://pubmed.ncbi.nlm.nih.gov/17404061/
  6. (2014). Jaceosidin promotes angiogenesis via VEGFR2/FAK/PI3K/AKT/NF-κB in endothelial cells (context caution). Experimental Biology and Medicine. https://pubmed.ncbi.nlm.nih.gov/24939823/
  7. Jung UJ, et al. (2008). In-vitro antioxidant and anti-inflammatory activities of jaceosidin from Artemisia princeps. Archives of Pharmacal Research. https://pubmed.ncbi.nlm.nih.gov/18449499/
  8. Min SW, et al. (2009). Eupatilin and jaceosidin inhibit carrageenan-induced inflammation in mice. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/19505561/
  9. Jeong MA, et al. (2007). Jaceosidin inhibits TPA-induced COX-2 and MMP-9 via ERK1/2. Annals of the New York Academy of Sciences. https://pubmed.ncbi.nlm.nih.gov/17404058/
  10. (2026). Jaceosidin ameliorates atopic dermatitis via ubiquitin-mediated JAK1 degradation. Phytomedicine. https://pubmed.ncbi.nlm.nih.gov/42341525/
  11. (2009). LC-MS/MS determination of jaceosidin in rat plasma. Journal of Pharmaceutical and Biomedical Analysis. https://pubmed.ncbi.nlm.nih.gov/19070985/
  12. (2010). In-vitro metabolism of jaceosidin: CYP and UGT characterisation in human liver microsomes. Archives of Pharmacal Research. https://pubmed.ncbi.nlm.nih.gov/21191764/
  13. (2010). Effects of eupatilin and jaceosidin on CYP450 activities in human liver microsomes. Molecules. https://pubmed.ncbi.nlm.nih.gov/20877236/
  14. Fletcher JN, et al. (2011). Flavonoids from Eriodictyon californicum as hTAS2R31 bitter-receptor antagonists. Journal of Agricultural and Food Chemistry. https://pubmed.ncbi.nlm.nih.gov/22059530/