Eupatilin (5,7-dihydroxy-3',4',6-trimethoxyflavone) is the main lipophilic flavonoid obtained from the Artemisia species. Eupatilin has been reported to have anti-apoptotic, anti-oxidative and anti-inflammatory activities. Eupatilin increases transcriptional activity and expression of peroxisome proliferator-activated receptor α (PPARα) in a keratinocyte cell line and acts as an agonist of PPARα. PPARα agonists ameliorate atopic dermatitis (AD) and restore the skin barrier function. Eupatilin (10, 30, 100 μM) suppresses IL-4 expression and degranulation in RBL-2H3 cells[3]. Eupatilin inhibits TNFα(tumor necrosis factor-alpha)-induced MMP-2/-9 expression by suppressing NF-κB and MAPK⁄AP-1 pathways via PPARα[4]. Eupatilin protected against H2O2-induced oxidative stress and apoptosis through the activation of PI3K/Akt signaling pathway in ARPE-19 cells[5]. Eupatilin can inhibit IL-1β-induced apoptosis via sestrin2-dependent autophagy in chondrocytes[6]. Eupatilin alleviated LPS(lipopolysaccharide)-induced ALI (acute lung injury) through inhibiting inflammation and oxidative stress in a concentration-dependent way, which was likely to be closely related with the activation of PPAR-alpha[7].
Eupatilin/泽兰林素 细胞实验
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.
Eupatilin/泽兰林素 动物实验
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
搜索
