Echinatin is a chalcone isolated from the Chinese herbal medicine Gancao with hepatoprotective and anti-inflammatory effects[3]. Administration of echinatin obviously inhibits NLRP3 inflammasome activation and ameliorates LPS-induced septic shock and dextran sodium sulfate-induced (DSS-induced) colitis in mice. Moreover, echinatin exerted favorable pharmacological effects on liver inflammation and fibrosis in a mouse model of nonalcoholic steatohepatitis (NASH)[4]. Echinatin induced apoptosis and autophagy through inactivation of AKT/mTOR signaling pathway, whereas constitutive activation of AKT significantly abrogated these effects. Furthermore, echinatin had a significant antitumor effect in the tumor xenograft model and markedly suppressed cell migration and invasion abilities of ESCC (Esophageal squamous cell carcinoma) cells in a dose-dependent manner[5]. Echinatin exerted its protective effect against MI/R (myocardial ischemic/reperfusion) injury at least partially by suppressing the Hippo/YAP signaling pathway[6]. Echinatin mitigates H2O2-induced oxidative damage and apoptosis in HLECs (Human lens epithelial B3 cells) via the Nrf2/HO-1 pathway, suggesting that Ech may be a potential drug for the treatment of cataracts[7].
Echinatin/刺甘草查尔酮 细胞实验
Cell Line
Concentration
Treated Time
Description
References
THP-1 macrophages
10 μM
48 hours
To evaluate the anti-inflammatory activity of Q-14 compounds. Echinatin demonstrated the most robust anti-inflammation activities (inhibition rate > 90%).
Proc Natl Acad Sci U S A. 2023 May 2;120(18):e2301775120
human liver microsomes
25.86 μM
3 min or 33 min preincubation
To evaluate the inhibitory effect of Echinatin on CYP3A, results showed that Echinatin inhibited CYP3A-catalyzed testosterone 6β-hydroxylation in a time-dependent manner, with IC50 values decreasing from 25.86 μM to 8.08 μM.
Acta Pharmacol Sin. 2022 Apr;43(4):1072-1081
Calu-3 cells
1.1, 3.3, 10, 30 μM
48 hours
To evaluate the inhibition effect of Echinatin on SARS-CoV-2-triggered inflammation. Echinatin reduced SARS-CoV-2-induced IL-1β P17 release in a dose-dependent manner.
Proc Natl Acad Sci U S A. 2023 May 2;120(18):e2301775120
KYSE270 cells
10 μM, 20 μM, 40 μM
24 h and 48 h
To evaluate the effect of echinatin on ESCC cell apoptosis, the results showed that echinatin-induced apoptosis in a dose-dependent way.
Cell Death Dis. 2020 Jul 13;11(7):524
KYSE30 cells
10 μM, 20 μM, 40 μM
24 h and 48 h
To evaluate the effect of echinatin on ESCC cell apoptosis, the results showed that echinatin-induced apoptosis in a dose-dependent way.
Cell Death Dis. 2020 Jul 13;11(7):524
KYSE270 cells
10 μM, 20 μM, 40 μM
5 days
To evaluate the effect of echinatin on ESCC cell proliferation, the results showed that echinatin inhibited cell proliferation substantially in both dose- and time-dependent manner.
Cell Death Dis. 2020 Jul 13;11(7):524
KYSE30 cells
10 μM, 20 μM, 40 μM
5 days
To evaluate the effect of echinatin on ESCC cell proliferation, the results showed that echinatin inhibited cell proliferation substantially in both dose- and time-dependent manner.
Cell Death Dis. 2020 Jul 13;11(7):524
mouse bone marrow-derived macrophages (BMDMs)
below 100 μM
60 minutes
To evaluate the effect of Echinatin on NLRP3 inflammasome activation, results showed that Echinatin significantly inhibited nigericin-induced caspase-1 activation, IL-1β maturation, and LDH release.
JCI Insight. 2021 Jan 25;6(2):e134601
LO2 cells
0, 20, 30, 40, 50 μM
24, 48, 72 hours
To evaluate the toxicity of Echinatin on normal human cells, the results showed that Echinatin had no significant toxicity on LO2 cells
Genes Dis. 2023 May 18;11(2):1050-1065
HS5 cells
0, 20, 30, 40, 50 μM
24, 48, 72 hours
To evaluate the toxicity of Echinatin on normal human cells, the results showed that Echinatin had no significant toxicity on HS5 cells
Genes Dis. 2023 May 18;11(2):1050-1065
HEB cells
0, 20, 30, 40, 50 μM
24, 48, 72 hours
To evaluate the toxicity of Echinatin on normal human cells, the results showed that Echinatin had no significant toxicity on HEB cells
Genes Dis. 2023 May 18;11(2):1050-1065
SV-HUC-1 cells
0, 20, 30, 40, 50 μM
24, 48, 72 hours
To evaluate the toxicity of Echinatin on normal human cells, the results showed that Echinatin had no significant toxicity on SV-HUC-1 cells
Genes Dis. 2023 May 18;11(2):1050-1065
EJ cells
0, 20, 30, 40, 50 μM
24, 48, 72 hours
To evaluate the inhibitory effect of Echinatin on the proliferation of bladder cancer cells, the results showed that Echinatin significantly inhibited the proliferation of T24 and EJ cells
Genes Dis. 2023 May 18;11(2):1050-1065
T24 cells
0, 20, 30, 40, 50 μM
24, 48, 72 hours
To evaluate the inhibitory effect of Echinatin on the proliferation of bladder cancer cells, the results showed that Echinatin significantly inhibited the proliferation of T24 and EJ cells
Genes Dis. 2023 May 18;11(2):1050-1065
MCF-7
>100 μM
48 hours
Evaluated for cytotoxicity, results showed no significant activity
Int J Mol Sci. 2021 Sep 18;22(18):10109
HT-29
>100 μM
48 hours
Evaluated for cytotoxicity, results showed no significant activity
Int J Mol Sci. 2021 Sep 18;22(18):10109
A375P
>100 μM
48 hours
Evaluated for cytotoxicity, results showed no significant activity
Int J Mol Sci. 2021 Sep 18;22(18):10109
Echinatin/刺甘草查尔酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
KYSE270-derived tumor xenograft model
Oral administration
20 mg/kg and 50 mg/kg
Every 2 days
To evaluate the inhibitory effect of echinatin on ESCC tumor growth, the results showed that echinatin significantly suppressed tumor growth without obvious toxicity to animals.
Cell Death Dis. 2020 Jul 13;11(7):524
C57BL/6 mice
LPS-induced septic shock model
Intraperitoneal injection
20 mg/kg and 40 mg/kg
Single dose
To evaluate the protective effect of Echinatin on LPS-induced septic shock, results showed that Echinatin significantly reduced the levels of IL-1β and TNF-α in serum and improved the survival rate of mice.
JCI Insight. 2021 Jan 25;6(2):e134601
BALB/c nude mice
Bladder cancer xenograft model
Oral gavage
0, 20, 40, 60 mg/kg
Once every two days for 21 days
To evaluate the inhibitory effect of Echinatin on tumor growth in a bladder cancer xenograft model, the results showed that Echinatin significantly inhibited tumor growth
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