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Chemical Structure| 22368-21-4 Chemical Structure| 22368-21-4

Structure of Eupatilin
CAS No.: 22368-21-4

Chemical Structure| 22368-21-4

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Eupatilin is an activiator of PPARα. It is a lipohilic flavonoid extracted from artemisia species with antioxidant, anti-tumor, and anti-inflammatory activities.

Synonyms: NSC 122413

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Product Details of Eupatilin

CAS No. :22368-21-4
Formula : C18H16O7
M.W : 344.32
SMILES Code : O=C1C=C(C2=CC=C(OC)C(OC)=C2)OC3=C1C(O)=C(OC)C(O)=C3
Synonyms :
NSC 122413
MDL No. :MFCD13194819
InChI Key :DRRWBCNQOKKKOL-UHFFFAOYSA-N
Pubchem ID :5273755

Safety of Eupatilin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CCD-18Co cells 200 μM Minimal effect on normal colon cell viability Antioxidants (Basel). 2021 Jun 15;10(6):957.
Diseased human lung fibroblasts from IPF patients (DHLFs) 50 μM 48-72 hours To assess the effect of Eupatilin on proliferation and αSMA expression in DHLFs. Results demonstrated Eupatilin significantly inhibited cell proliferation and completely suppressed αSMA expression. EBioMedicine. 2019 Jan;39:484-496.
Mouse hepatic stellate cell line (ONGHEPA1) 50 μM 24 hours To evaluate the inhibitory effect of Eupatilin on TGF-β-induced transdifferentiation of hepatic stellate cells into myofibroblasts. Results showed Eupatilin completely inhibited TGF-β-induced fibrosis. EBioMedicine. 2019 Jan;39:484-496.
CEP290WT RPE1 cells 20 μM 48 hours Eupatilin promoted ciliogenesis in CEP290WT cells under serum starvation conditions. J Clin Invest. 2018 Aug 1;128(8):3642-3648.
RPE1-Smo-EGFP cells 20 μM 24 hours Eupatilin promoted Smo-EGFP transport to the ciliary membrane and partially restored ciliary length in CEP290null cells. J Clin Invest. 2018 Aug 1;128(8):3642-3648.
LCA5 JB342 patient retinal organoids 10 µM 30 days Reduced CEP290 and IFT88 accumulation along the cilium, improved rhodopsin traffic to the outer segment Acta Neuropathol Commun. 2025 Feb 11;13(1):26.
LCA5 KO retinal organoids 10 µM 30 days Reduced CEP290 and IFT88 accumulation along the cilium, improved rhodopsin traffic to the outer segment Acta Neuropathol Commun. 2025 Feb 11;13(1):26.
RAW264.7 cells 10, 25, 50, 100 μmol/L 24 hours To evaluate the effect of Eupatilin on inflammatory cytokines and ROS in LPS-stimulated RAW264.7 cells. Results showed that Eupatilin significantly reduced the production of NO, IL-6, and ROS. Int J Mol Sci. 2022 Jan 29;23(3):1582.
CEP290 KO and CEP290 LCA10 iPSCs-derived retinal organoids 10 µM or 20 µM 30 days Eupatilin significantly increased cilia incidence and length Cells. 2023 Jun 7;12(12):1575.
CEP290 KO RPE1 cells 20 µM 24 hours Eupatilin significantly increased cilia incidence and length Cells. 2023 Jun 7;12(12):1575.
CEP290 LCA10 patient-derived fibroblasts 20 µM 24 hours Eupatilin significantly increased cilia incidence and length Cells. 2023 Jun 7;12(12):1575.
HK-2 cells 50 µg/ml 24 hours Eupatilin attenuated cisplatin-induced injury in HK-2 cells by activating the PPARα/Nrf2/HO-1/NQO1 pathway, promoting cell proliferation and inhibiting apoptosis. Int J Mol Med. 2021 Feb;47(2):511-522.
LX-2 cells 0, 20, 40, 80 μM 48 hours Eupatilin significantly repressed the levels of fibrotic markers COL1α1 and α-SMA, as well as other collagens in LX-2 cells. Int J Mol Sci. 2023 Mar 21;24(6):5933.
Rat cerebral cortex synaptosomes 0.5, 1, 3, 5, 10 μM 10 min Eupatilin inhibited 4-AP-induced glutamate release with an IC50 of 5.1 μM, by suppressing P/Q-type Ca2+ channels and reducing synapsin I phosphorylation Int J Mol Sci. 2022 Nov 2;23(21):13406.
HT29 cells 50 μM and above 48 hours Inhibits cell proliferation and induces apoptosis Antioxidants (Basel). 2021 Jun 15;10(6):957.
HCT116 cells 25 μM and above 48 hours Inhibits cell proliferation and induces apoptosis Antioxidants (Basel). 2021 Jun 15;10(6):957.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Bleomycin-induced lung fibrosis model (BLM) Forced nasal administration (preventative study) and oral gavage (therapeutic study) 100-200 mg/kg Preventative study: once daily (5 times/week) for 1 week; Therapeutic study: twice daily for 14 days To evaluate the efficacy of Eupatilin in preventing and treating BLM-induced lung fibrosis. Results demonstrated Eupatilin significantly attenuated fibrosis severity, reduced collagen deposition and TGF-β production, and promoted tissue regeneration. EBioMedicine. 2019 Jan;39:484-496.
Mice Rd16 mouse model (harboring Cep290 in-frame deletion) Subcutaneous injection 40 mg/kg Once daily for 3 weeks Eupatilin improved cone photoreceptor function in rd16 mice, partially restoring M-opsin trafficking to the outer segment of cone photoreceptors. J Clin Invest. 2018 Aug 1;128(8):3642-3648.
BALB/c mice OVA-induced asthma model Intraperitoneal injection 15 mg/kg, 30 mg/kg Once daily for 7 days To evaluate the therapeutic effect of Eupatilin in OVA-induced asthmatic mice. Results showed that Eupatilin reduced the numbers of inflammatory cells, especially neutrophils and eosinophils, decreased the levels of IL-5, IL-13 in the BALF and OVA-IgE in the serum, and improved lung inflammation and mucus hypersecretion. Int J Mol Sci. 2022 Jan 29;23(3):1582.
C57BL/6J male mice CCl4-induced hepatic fibrosis model Intragastrical 10, 20, 40 mg/kg/day Once daily for 4 weeks Eupatilin significantly alleviated CCl4-induced hepatic fibrosis in mice, improved liver function, and reduced collagen deposition. Int J Mol Sci. 2023 Mar 21;24(6):5933.
Rats KA-induced glutamate excitotoxicity model Intraperitoneal injection 10, 30 mg/kg Administered 30 min before KA injection, evaluated after 72 h Eupatilin pretreatment prevented KA-induced neuronal degeneration, glutamate elevation, glutaminase increase, EAAT decrease, GluN2A protein decrease, and GluN2B protein increase Int J Mol Sci. 2022 Nov 2;23(21):13406.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.52mL

2.90mL

1.45mL

29.04mL

5.81mL

2.90mL

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