Chrysophanol, a herbaceous perennial plant, belonging to the Polygonaceae family, has anticancer, antiviral, anti-diabetic and anti-inflammatory biological properties. In vivo, the saturation value of drug binding for chrysophanol was 0.53. The obtained LD50 value for oral toxicity of chrsyphanol was 2.5 g/kg[3]. In vitro, chrysophanol inhibited the proliferation of MCF-7 and MDA-MB-231 cells in a dose-dependent manner. In addition, chrysophanol facilitated paclitaxel induced apoptosis and downregulated Bcl-2[4].
Chrysophanol/大黄酚 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HepG2 cells
12.5, 25, 50, 100, 120 μM
48 h
To evaluate the cytotoxicity of chrysophanol on HepG2 cells, results showed that chrysophanol predominantly induced cell death through necrosis.
Chin Herb Med. 2021 Feb 16;13(2):221-227.
H9C2 cells
1, 10, 20 μM
12 h
CHR significantly suppressed the DOX-induced cardiomyocyte injury including the reduction of cell viability, apoptosis and nuclear condensation.
Acta Pharm Sin B. 2019 Jul;9(4):782-793.
human podocytes (AB8/13 cells)
40 μM
48 h
CHR significantly reversed high glucose (HG)-induced growth inhibition in AB8/13 cells and inhibited HG-promoted cell migration and inflammatory responses.
Drug Des Devel Ther. 2020 Nov 16;14:4951-4962.
Caco-2 cells
0.025, 0.05, 0.1 mg/mL SKE
To investigate the bidirectional transport characteristics of chrysophanol in the Caco-2 cell monolayer model, results showed higher transport rates in RAI than in SKE, with ER values close to or above 1.5, suggesting it may be a substrate for ATP-binding cassette membrane transporters.
Chin Herb Med. 2022 Dec 5;15(1):117-122.
PC12 cells
10, 25, 50 μM
12 h
To investigate the neuroprotective effect of chrysophanol (CHR) on PC12 treated with Aβ25-35. Results showed that CHR pretreatment significantly increased cell viability and reduced apoptosis.
Drug Des Devel Ther. 2020 Jul 13;14:2715-2723.
Human sebocytes
0–100 μM
48 h
To investigate the inhibitory effect of Chrysophanol on heat-induced lipogenesis, results showed that Chrysophanol concentration-dependently suppressed the expression of PPARγ and FAS and reduced lipid accumulation.
Lipids Health Dis. 2019 Jun 7;18(1):135.
Chrysophanol/大黄酚 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
DOX-induced cardiomyopathy model
Intragastric administration
5, 20, 40 mg/kg
Once daily for 7 days
Both CHR and 3AB significantly suppressed DOX-induced cardiac apoptosis, mitochondrial impairment and heart dysfunction.
Acta Pharm Sin B. 2019 Jul;9(4):782-793.
C57BL/6 mice
Diabetic nephropathy model
Oral
50 mg/kg or 100 mg/kg
Once daily for 4 weeks
CHR significantly alleviated the symptoms of diabetic nephropathy, including reduced blood glucose, decreased renal inflammation and fibrosis, and inhibited the expression of TGF-β signaling pathway-related proteins.
Drug Des Devel Ther. 2020 Nov 16;14:4951-4962.
Sprague-Dawley rats
Single-pass intestinal perfusion model
Intestinal perfusion
0.94 µg/mL
Perfusion rate 0.2 mL/min, duration 120 minutes
To study the absorption characteristics of chrysophanol in different intestinal segments, results showed the highest absorption coefficient in the colon, and higher Peff values in RAI than in SKE.
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