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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
HCT116 cells 25 μM and above 48 hours Inhibits cell proliferation and induces apoptosis PMC8232173
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. PMC6355727
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. PMC6355727
CEP290WT RPE1 cells 20 μM 48 hours Eupatilin promoted ciliogenesis in CEP290WT cells under serum starvation conditions. PMC6063470
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. PMC6063470
LCA5 JB342 patient retinal organoids 10 µM 30 days Reduced CEP290 and IFT88 accumulation along the cilium, improved rhodopsin traffic to the outer segment PMC11817871
LCA5 KO retinal organoids 10 µM 30 days Reduced CEP290 and IFT88 accumulation along the cilium, improved rhodopsin traffic to the outer segment PMC11817871
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. PMC8836136
CEP290 KO and CEP290 LCA10 iPSCs-derived retinal organoids 10 µM or 20 µM 30 days Eupatilin significantly increased cilia incidence and length PMC10297203
CEP290 KO RPE1 cells 20 µM 24 hours Eupatilin significantly increased cilia incidence and length PMC10297203
CCD-18Co cells 200 μM Minimal effect on normal colon cell viability PMC8232173
HT29 cells 50 μM and above 48 hours Inhibits cell proliferation and induces apoptosis PMC8232173
CEP290 LCA10 patient-derived fibroblasts 20 µM 24 hours Eupatilin significantly increased cilia incidence and length PMC10297203
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. PMC7797437
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. PMC10054508
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 PMC9657139

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. PMC6355727
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. PMC6063470
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. PMC8836136
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. PMC10054508
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 PMC9657139

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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