Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside can dose-dependently reduce phosho-LRP6, total LRP6, phosho-Dvl2, active β-catenin, and total β-catenin protein expression level in MDA-MB-231 and MDA-MB-468 cells[3]. Echinacoside shows both anti-apoptotic and anti-inflammatory properties, characterized by a substantial inhibition of hepatocyte apoptosis and a significant reduction in the inflammatory markers[4]. Echinacoside (30 - 270 mg/kg body weight; p.o.; daily for 12 weeks) significantly reverses the increases of body weight, serum hydroxyproline (HOP) levels, and the decreases of uterus wet weight and bone mineral density (BMD) in in ovariectomized (OVX) rats[5]. Echinacoside could increase viability of rat pheochromocytoma PC12 cells injured by Aβ (β-amyloid protein) and suppress the increase in intracellular reactive oxygen species (ROS) triggered by Aβ[6]. Moreover, transient treatment with echinacoside inhibits cytochrome c release and caspase-3 activation caused by ensuing rotenone exposure via activating Trk-extracellular signal-regulated kinase (ERK) pathway in neuronal cells[7].
Echinacoside/松果菊苷 细胞实验
Cell Line
Concentration
Treated Time
Description
References
N9 microglial cells
5–20 μM
24 h
To investigate the effect of Echinacoside on LPS-induced N9 microglial cell activation, results showed that Echinacoside reduced the secretion of inflammatory factors and inhibited M1 polarization.
Front Pharmacol. 2023 Jan 4;13:993483.
rat pituitary cells
10^-6 M to 10^-5 M
15 and 30 min
To evaluate if echinacoside could be an agonist of growth hormone secretagogue receptor (GHSR), it was subjected to examination of the induction of growth hormone secretion from primary rat anterior pituitary cells. The results showed that echinacoside was able to significantly stimulate the secretion of growth hormones from rat pituitary cells, and this stimulation was inhibited by a GHSR inverse agonist.
Molecules. 2019 Feb 17;24(4):720.
Hepatic Stellate Cells (HSC-T6)
125, 250, 500 μg/mL
48 h
Inhibited HSC proliferation, blocked TGF-β1/smad signaling pathway, reduced mRNA and protein expression of smad2 and smad3, and increased expression of smad7.
Molecules. 2016 Jan 18;21(1):102.
Human umbilical vein endothelial cells (HUVECs)
30 µM
24 h
Echinacoside inhibited LPS-induced pathological activation and mitochondrial pathway apoptosis of endothelial cells by activating SIRT1 and promoting its expression, inhibiting NOX4 activation, and facilitating NOX4 ubiquitination degradation.
Antioxidants (Basel). 2023 Oct 29;12(11):1925.
lipoxygenase isolated from rat lung cytosol fraction
296 μM
30 min
Ineffective against LOXs in lower concentrations, while higher concentration showed similar inhibition on 8-LOX and 12-LOX (28.7% and 27%, respectively). 15-LOX was more sensitive, and the presence of echinacoside decreased its activity to 47%.
leaves and some of its constituents. Molecules.
Human SW480 colorectal cancer cells
25, 35, 45, 55, 65, 75, 85, 95 μM
24, 48 h
Echinacoside dose-dependently inhibited the growth of SW480 cells, with IC50 values of 55.39 and 35.05 μM for 24 and 48 h, respectively.
Int J Mol Sci. 2015 Jun 29;16(7):14655-68.
Human SW480 colorectal cancer cells
60, 80 μM
10 days
Echinacoside dose-dependently inhibited the colony formation of SW480 cells.
Int J Mol Sci. 2015 Jun 29;16(7):14655-68.
Human SW480 colorectal cancer cells
60, 80 μM
24 h
Echinacoside induced G1 phase cell cycle arrest in SW480 cells and upregulated the G1/S-CDK blocker CDKN1B (p21).
Int J Mol Sci. 2015 Jun 29;16(7):14655-68.
Human SW480 colorectal cancer cells
60, 80 μM
24 h
Echinacoside induced apoptosis in SW480 cells, increasing the levels of active caspase 3 and cleaved PARP proteins.
Int J Mol Sci. 2015 Jun 29;16(7):14655-68.
Human SW480 colorectal cancer cells
60, 80 μM
24 h
Echinacoside increased the level of oxidized guanine 8-oxoG in SW480 cells, indicating induction of oxidation in the nucleotide pool and/or DNA molecules.
Int J Mol Sci. 2015 Jun 29;16(7):14655-68.
Human SW480 colorectal cancer cells
60, 80 μM
24 h
Echinacoside caused extensive DNA damage in SW480 cells, as evidenced by a significant increase in 53BP1 protein.
Int J Mol Sci. 2015 Jun 29;16(7):14655-68.
Echinacoside/松果菊苷 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Exercise-induced injury model
Oral gavage
100 mg/kg
Once daily for 1 week
Echinacoside significantly reduced the infiltration rate of natural killer cells (NK cells) in peripheral blood post-exercise and decreased the expression levels of key genes (GZMB, PRF1, FASLG, and CCL4).
Front Nutr. 2022 Sep 16;9:987545
C57BL/6 mice
Chronic unpredictable mild stress (CUMS) induced depression model
Gavage
15 and 60 mg/kg
Once daily for 21 days
To investigate the effect of Echinacoside on CUMS-induced depressive-like behaviors, results showed that Echinacoside reversed CUMS-induced behavioral changes, reduced levels of inflammatory factors, and increased p-CREB/CREB ratio and BDNF levels in the hippocampus.
Front Pharmacol. 2023 Jan 4;13:993483.
C57BL/6 mice
Sepsis-induced acute lung injury model
Intraperitoneal injection
1 mg/kg, 5 mg/kg, 25 mg/kg
Single injection, lasting 24 hours
Echinacoside alleviated sepsis-induced acute lung injury through the SIRT1-mediated NOX4-Nrf2 axis, inhibited oxidative stress, and preserved endothelial cell function.
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