Physcion, is an anthraquinone isolated and purified from roots of Rheum officinale Baill, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively[3]. Treatment with physcion (5, 10, and 20 μmol/L) dose-dependently suppressed the cell viability and colony formation in CNE2 cells. Physcion (10 and 20 μmol/L) dose-dependently blocked cell cycle progression at G1 phase and induced both caspase-dependent apoptosis and autophagy in CNE2 cells. In the xenograft murine model, administration of physcion dose-dependently suppressed the tumor growth without affecting the body weight[4]. Physcion application caused reduced lipogenesis and alleviated inflammation in alcohol-induced mice. And the circadian misalignment triggered by ethanol was efficiently reversed by physcion. Physcion attenuated lipogenesis via reprogramming the circadian clock in HepG2 cells[5]. Oral administration of physcion improved the severity of 2,4-dinitrochlorobenzene-induced AD-like lesional skin through reducing infiltration of inflammatory cells and mast cells, and the protein and mRNA levels of TSLP, IL-4, and IL-6 in the lesional skin tissues[6]. Physcion prevents Hcy-induced endothelial dysfunction by activating Ca2+- and Akt-eNOS-NO signaling pathways[7].
Physcion/大黄素甲醚 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Bone-marrow-derived dendritic cells (BMDCs)
1-100 µM
18 hours
To evaluate the cytotoxic effects of Physcion on BMDCs, the results showed that Physcion at concentrations of 1-100 μM had no significant cytotoxicity to BMDCs.
Int J Mol Sci. 2020 Mar 4;21(5):1753
HepG2
5 µM, 10 µM, 20 µM
24 and 48 hours
Physcion induces apoptosis in HCC cells by upregulating miR-370 and modulates the level of miR-370 through AMPK/Sp1/DNMT1 signaling.
Am J Cancer Res. 2016 Dec 1;6(12):2919-2931
SMMC7721
5 µM, 10 µM, 20 µM
24 and 48 hours
Physcion induces apoptosis in HCC cells by upregulating miR-370 and modulates the level of miR-370 through AMPK/Sp1/DNMT1 signaling.
Am J Cancer Res. 2016 Dec 1;6(12):2919-2931
Human colorectal cancer SW620 cells
2.5, 5 µM
24 hours
To evaluate the inhibitory effect of Physcion on migration and invasion of SW620 cells. Results showed that Physcion dose-dependently inhibited cell adhesion, migration, and invasion without affecting cell viability.
Acta Pharmacol Sin. 2016 Feb;37(2):264-75
SH-SY5Y cells
10, 20, 40 µM
24 hours
Physcion significantly increased the viability of SH-SY5Y cells, reduced OGD/R-induced apoptosis, and decreased the levels of pro-inflammatory factors TNF-α, IL-1β, IL-6, and IL-10.
Drug Des Devel Ther. 2021 Jan 25;15:277-287
SK-N-BE(2)-C human neuroblastoma cells
40 µM
24 hours
To investigate the effect of Physcion on hST8Sia VI gene expression, results showed that Physcion significantly increased hST8Sia VI mRNA levels.
Int J Mol Sci. 2016 Aug 2;17(8):1246
RAW 264.7 cells
100 µM
24 hours
To verify the activity of Physcion and measure the expression of surface molecules. The results showed that Physcion at 100 μM increased the expressions of CD40, CD80, CD86, and MHCII.
Int J Mol Sci. 2020 Mar 4;21(5):1753
HepG2 cells
0.125, 0.25 µM
24 hours
To investigate the effects of Physcion on ethanol-induced lipid accumulation and inflammation. Physcion dose-dependently restored ethanol-inhibited cell survival, reduced lipid accumulation, and improved lipid metabolism by modulating BMAL1 and AMPK pathways.
Front Pharmacol. 2020 Nov 23;11:573074
HeLa cells
80–300 µM
48 hours
To evaluate the effect of Physcion on the viability of HeLa cells, the results showed that Physcion inhibited the viability of HeLa cells in a concentration-dependent manner.
Cells. 2021 Aug 8;10(8):2029
Physcion/大黄素甲醚 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 J mice
High-fat diet-induced obesity model
Dietary supplementation
0.002% (w/w)
16 weeks continuously
To investigate the effects of PY on high-fat diet-induced obesity and related metabolic disorders. Results showed that PY supplementation significantly decreased body and white adipose tissue weights, ameliorated plasma lipids, adipokines, cytokines, and fecal lipids, reduced fatty acid synthesis in the liver while increasing fatty acid oxidation, and markedly decreased lipid synthesis while increasing lipolysis and oxidation in white adipose tissue.
Nutr Metab (Lond). 2019 May 15;16:31
Nude mice (BALB/c, nu/nu)
HepG2 xenograft model
Intraperitoneal injection
20 mg/kg/day and 40 mg/kg/day
Once daily, duration not specified
Physcion suppresses tumor growth and induces apoptosis in vivo by upregulating miR-370 and modulating AMPK/Sp1/DNMT1 signaling.
Am J Cancer Res. 2016 Dec 1;6(12):2919-2931
SD rats
Cerebral ischemia-reperfusion injury model
Oral gavage
20 or 40 mg/kg
Once daily for 7 days
Physcion significantly reduced cerebral infarction area, attenuated neuronal injury and apoptosis, and decreased the expressions of TLR4, p-NF-κB p65, and p-IκB.
Drug Des Devel Ther. 2021 Jan 25;15:277-287
C57BL/6N mice
Alcoholic liver fibrosis model
Gavage
20/40 mg/kg
Once a week for 8 weeks
Physcion significantly improved liver inflammation, collagen deposition and lipid accumulation in alcoholic liver fibrosis mice, alleviating liver fibrosis by inhibiting HMGB1/NLRP3/GSDMD pathway
Front Pharmacol. 2025 Mar 27;16:1532590
C57BL/6 mice
Ethanol-induced acute liver injury model
Oral gavage
250 or 500 μg/kg
Once daily for 14 consecutive days
To investigate the protective effects of Physcion on ethanol-induced liver injury. Physcion pretreatment significantly reduced serum ALT, AST, and TG levels, decreased hepatic lipid accumulation and inflammation, and improved liver injury by modulating BMAL1 and AMPK/SREBP1/P2X7R signaling pathways.
Front Pharmacol. 2020 Nov 23;11:573074
Adult mice
LPS-induced neuroinflammation model
Oral
30 mg/kg/day
Once daily for 3 weeks
Physcion mitigates LPS-induced neuroinflammation, oxidative stress, and memory impairments via TLR-4/NF-κB signaling
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