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).
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 1Inhibitory 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 6Jaceosidin promotes angiogenesis via VEGFR2/FAK/PI3K/AKT/NF-κB in endothelial cells (context caution)View study →, which cuts against a naive “anti-tumour” framing.
- Broad preclinical anticancer + anti-inflammatory signals: apoptosis/cell-cycle arrest across several tumour lines and reduced inflammation in mouse models 1,2,8Reference 1Inhibitory effect of jaceosidin from Artemisia argyi on the function of HPV-16 E6/E7 oncoproteinsView study →Reference 2Jaceosidin induces G2/M arrest via ATM–Chk1/2→cdc25C–cdc2 in endometrial cellsView study →Reference 8AnimalEupatilin 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 6Jaceosidin 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.
1. Anticancer
Jaceosidin’s strongest single result is inhibition of HPV-16 E6/E7 oncoprotein function in cervical-cancer cells 1Reference 1Inhibitory 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 2Jaceosidin induces G2/M arrest via ATM–Chk1/2→cdc25C–cdc2 in endometrial cellsView study →, p53-dependent arrest in U87 glioblastoma 3Reference 3Jaceosidin induces p53-dependent G2/M arrest in U87 glioblastoma cellsView study →, Bax/Mcl-1/c-FLIP-mediated apoptosis in renal Caki cells 4Reference 4Jaceosidin induces apoptosis via Bax/Mcl-1/c-FLIP in renal Caki cellsView study → and ROS-driven apoptosis in ras-transformed breast epithelium 5Reference 5Jaceosidin 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 6Jaceosidin 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 1Inhibitory effect of jaceosidin from Artemisia argyi on the function of HPV-16 E6/E7 oncoproteinsView study →Reference 6Jaceosidin 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 7In-vitro antioxidant and anti-inflammatory activities of jaceosidin from Artemisia princepsView study →, reduced carrageenan-induced paw inflammation in mice (with eupatilin) 8Reference 8AnimalEupatilin and jaceosidin inhibit carrageenan-induced inflammation in miceView study →, and benefited a mouse atopic-dermatitis model via ubiquitin-mediated JAK1 degradation 10Reference 10Jaceosidin 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 9Jaceosidin 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 8AnimalEupatilin and jaceosidin inhibit carrageenan-induced inflammation in miceView study →Reference 10Jaceosidin ameliorates atopic dermatitis via ubiquitin-mediated JAK1 degradationView study →.
3. Antioxidant
Jaceosidin’s flavone hydroxyl pattern gives in-vitro radical-scavenging activity 7Reference 7In-vitro antioxidant and anti-inflammatory activities of jaceosidin from Artemisia princepsView study →.
Gap: generic scavenging with no isolate clinical relevance 7Reference 7In-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 14Flavonoids 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 14Flavonoids from Eriodictyon californicum as hTAS2R31 bitter-receptor antagonistsView study →.
Mechanisms
| Target / pathway | Effect | Relevant to |
|---|---|---|
| HPV-16 E6 / E7 oncoproteins | inhibits function (cell; docking-predicted binding) | anticancer (cervical/HPV) |
| ATM–Chk1/2; p53; Bax↑/Mcl-1↓/c-FLIP↓ | cell-cycle arrest and intrinsic apoptosis | anticancer (various lines) |
| ERK1/2 → COX-2, MMP-9; NF-κB / MAPK | suppressed | anti-inflammatory / anti-invasion |
| JAK1 | ubiquitin-mediated degradation | atopic-dermatitis model |
| VEGFR2/FAK/PI3K/AKT/NF-κB | activated → 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 11AnimalLC-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 12In-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 13Effects 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.
| Completed | Planned | Terminated | Preclinical |
|---|---|---|---|
| —(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 13Effects of eupatilin and jaceosidin on CYP450 activities in human liver microsomesView study →, and the pro-angiogenic endothelial finding 6Reference 6Jaceosidin 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
- 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/
- 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/
- 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/
- 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/
- 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/
- (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/
- 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/
- Min SW, et al. (2009). Eupatilin and jaceosidin inhibit carrageenan-induced inflammation in mice. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/19505561/
- 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/
- (2026). Jaceosidin ameliorates atopic dermatitis via ubiquitin-mediated JAK1 degradation. Phytomedicine. https://pubmed.ncbi.nlm.nih.gov/42341525/
- (2009). LC-MS/MS determination of jaceosidin in rat plasma. Journal of Pharmaceutical and Biomedical Analysis. https://pubmed.ncbi.nlm.nih.gov/19070985/
- (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/
- (2010). Effects of eupatilin and jaceosidin on CYP450 activities in human liver microsomes. Molecules. https://pubmed.ncbi.nlm.nih.gov/20877236/
- 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/