Corilagin, a gallotannin, inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL[1]. Cori effectively protects against APAP(Acetaminophen)-induced ALF (acute liver failure) via the upregulation of the AMPK/GSK3β-Nrf2 signaling pathway[2]. Corilagin induced the apoptosis of gastric cancer cells mainly via activating caspase‑8, ‑9, ‑3 and poly ADP‑ribose polymerase proteins. Corilagin triggered autophagy in gastric cancer cells and the inhibition of autophagy improved the activity of corilagin on cell growth suppression. In addition, corilagin significantly increased intracellular reactive oxygen species production, which is important in inhibiting the growth of gastric cancer cells[3]. Corilagin can suppress schistosome egg-induced hepatic fibrosis via inhibition of M2 macrophage polarization in the IL-13Rα1 signaling pathway[4]. In addition, corilagin dose-dependently blocks SARS-CoV-2-RBD binding and abolishes the infectious property of RBD-pseudotyped lentivirus in hACE2 overexpressing HEK293 cells, which mimicked the entry of SARS-CoV-2 virus in human host cells[5].
Corilagin/柯里拉京 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Nrf2−/− HepG2 cells
30 μM
6 h
Corilagin-mediated expression of antioxidant enzymes was blocked in Nrf2−/− HepG2 cells.
Cell Commun Signal. 2019 Jan 10;17(1):2
HepG2 cells
7.5, 15, 30 μM
6 h
Corilagin efficiently decreased APAP-triggered ROS generation and cell death, and induced the expression of several antioxidant enzymes.
Cell Commun Signal. 2019 Jan 10;17(1):2
HEK293
0-100 μM
72 h
Evaluate the effect of Corilagin on cell viability, results showed no cytotoxicity at 100 μM.
Phytomedicine. 2021 Jul;87:153591
LO2
0-100 μM
72 h
Evaluate the effect of Corilagin on cell viability, results showed no cytotoxicity at 100 μM.
Phytomedicine. 2021 Jul;87:153591
Beas-2B
0-100 μM
72 h
Evaluate the effect of Corilagin on cell viability, results showed no cytotoxicity at 100 μM.
Phytomedicine. 2021 Jul;87:153591
GES-1 cells
0-100 µM
24 h
To evaluate the toxicity of Corilagin on normal cells, results showed that Corilagin had low toxicity on GES-1 cells
Int J Mol Med. 2019 Feb;43(2):967-979
BGC823 cells
0, 10, 20, 30, 40, 50 µM
24 h
To evaluate the inhibitory effect of Corilagin on cell proliferation, results showed that Corilagin significantly inhibited the proliferation of BGC823 cells in a concentration-dependent manner
Int J Mol Med. 2019 Feb;43(2):967-979
SGC7901 cells
0, 10, 20, 30, 40, 50 µM
24 h
To evaluate the inhibitory effect of Corilagin on cell proliferation, results showed that Corilagin significantly inhibited the proliferation of SGC7901 cells in a concentration-dependent manner
Int J Mol Med. 2019 Feb;43(2):967-979
Mouse peritoneal macrophages (MPMs)
100 µg/ml, 50 µg/ml, 25 µg/ml
24 h
To study the effect of corilagin on the TLR4 signaling pathway in MPMs. Results showed that corilagin significantly inhibited the expression of TLR4 and its downstream molecules.
Front Immunol. 2020 Aug 6;11:1611
Ana-1 cells
100 µg/ml, 50 µg/ml, 25 µg/ml
24 h
To evaluate the cytotoxicity of corilagin on Ana-1 cells and its effect on the TLR4 signaling pathway. Results showed that corilagin significantly reduced the mRNA and protein expression of TLR4 and its downstream molecules.
Front Immunol. 2020 Aug 6;11:1611
Mouse macrophage RAW 264.7
2 mg/ml
4 days
Corilagin promotes macrophage transformation from pro-inflammatory M1 phenotype to anti-inflammatory M2 phenotype and upregulates the secretion of anti-inflammatory factors IL-10 and TGF-β.
Regen Biomater. 2024 Jul 1;11:rbae074
Human umbilical vein endothelial cells (HUVECs)
2 mg/ml
4 days
Corilagin modification not only enhances ECs adhesion and monolayer function via accelerating VEGF and TGF-β secretion but also promotes macrophage transformation from pro-inflammatory M1 phenotype to anti-inflammatory M2 ones.
Regen Biomater. 2024 Jul 1;11:rbae074
HEK293T cells
3.33 μM (EC50)
24 h
To evaluate the inhibitory effect of Corilagin on SARS-CoV-2 RdRp activity, results showed that Corilagin effectively inhibited RdRp activity.
Acta Pharm Sin B. 2021 Jun;11(6):1555-1567
Huh-7 cells
4.96 μM (EC50)
48 h
To evaluate the inhibitory effect of Corilagin on HCoV-OC43 replication, results showed that Corilagin effectively inhibited viral replication.
Acta Pharm Sin B. 2021 Jun;11(6):1555-1567
Vero cells
0.13 μM (EC50)
48 h
To evaluate the inhibitory effect of Corilagin on SARS-CoV-2 replication, results showed that Corilagin effectively inhibited viral replication.
Acta Pharm Sin B. 2021 Jun;11(6):1555-1567
Corilagin/柯里拉京 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
APAP-induced acute liver failure model
Intraperitoneally
15, 30, 60 mg/kg
Twice (at 12-hour intervals)
Corilagin significantly reduced APAP-induced mortality, ALT and AST levels, and attenuated liver histopathological changes.
Cell Commun Signal. 2019 Jan 10;17(1):2
ApoE−/− mice
High-fat and high-cholesterol diet-induced atherosclerosis model
Intragastric administration
40, 20, 10 mg/kg
Every 2 days for 2 weeks
Corilagin effectively reduced serum lipid levels (TG, TC, and LDL-C), alleviated aortic pathological changes and intimal lipid deposition, and decreased the expression of molecules associated with the Olfr2 signaling pathway (Olfr2 and Adcy3) and NLRP3 inflammasome effectors (NLRP3, Caspase-1, NEK7, and ASC), as well as inflammatory cytokines (IL-1β, IL-18, and TNF-α).
Front Immunol. 2024 May 13;15:1364161
C57BL/6J mice
Con A-induced hepatitis model
Intraperitoneal injection
25 mg/kg
Twice, 12 hours apart
To investigate the protective effect of Corilagin on Con A-induced liver injury. Results showed that Corilagin significantly increased the survival rate of mice, reduced serum ALT and AST levels, improved liver histopathological damage, reduced hepatocyte apoptosis and oxidative stress, and inhibited M1 macrophage activation.
Front Immunol. 2022 Jan 13;12:807509
Sprague-Dawley rats
Peripheral artery disease (PAD) model
Intragastric administration
40 mg/kg·day, 20 mg/kg·day, 10 mg/kg·day
Once daily for 1 month
To evaluate the effect of corilagin on atherosclerotic plaques in PAD model rats. Results showed that corilagin significantly reduced plaque coverage area and inhibited the TLR4 signaling pathway and its downstream molecules.
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