| In vitro: |
| Environ Toxicol. 2014 May;29(7):740-9. | | Chrysophanol-induced cell death (necrosis) in human lung cancer A549 cells is mediated through increasing reactive oxygen species and decreasing the level of mitochondrial membrane potential.[Pubmed: 22848001] | Chrysophanol (1,8-dihydroxy-3-methylanthraquinone) is one of the anthraquinone compounds, and it has been shown to induce cell death in different types of cancer cells. The effects of Chrysophanol on human lung cancer cell death have not been well studied.
METHODS AND RESULTS:
The purpose of this study is to examine Chrysophanol-induced cytotoxic effects and also to investigate such influences that involved apoptosis or necrosis in A549 human lung cancer cells in vitro. Our results indicated that Chrysophanol decreased the viable A549 cells in a dose- and time-dependent manner. Chrysophanol also promoted the release of reactive oxygen species (ROS) and Ca(2+) and decreased the levels of mitochondria membrane potential (ΔΨm ) and adenosine triphosphate in A549 cells. Furthermore, Chrysophanol triggered DNA damage by using Comet assay and DAPI staining. Importantly, Chrysophanol only stimulated the cytocheome c release, but it did not activate other apoptosis-associated protein levels including caspase-3, caspase-8, Apaf-1, and AIF.
CONCLUSIONS:
In conclusion, human lung cancer A549 cells treated with Chrysophanol exhibited a cellular pattern associated with necrotic cell death and not apoptosis in vitro. | | Pest Manag Sci. 2007 May;63(5):511-5. | | Synergistic interaction of physcion and chrysophanol on plant powdery mildew.[Pubmed: 17397111] | The extract of the plant Rheum officinale Baill, mainly containing the anthraquinones physcion and Chrysophanol, is highly active against plant powdery mildew.
METHODS AND RESULTS:
Experiments were conducted in the laboratory and greenhouse to determine the interaction of the two compounds on cucumber powdery mildew [Sphaerotheca fuliginea (Schlecht.) Poll] and on wheat powdery mildew [Blumeria graminis (DC.) Speer f. sp. tritici Marchal]. Physcion was much more bioactive than Chrysophanol against these powdery mildews. There was a significant synergistic interaction between the two compounds on the diseases when the ratios of physcion to Chrysophanol ranged from 1:9 to 5:5. The synergistic degree increased with increase in the Chrysophanol proportion in the combination.
CONCLUSIONS:
The findings indicate that, in order to ensure constant efficacy of the extract on the disease, both the contents and the proportion of the main active ingredients physcion and Chrysophanol have to be determined. | | Biol Pharm Bull. 2008 Nov;31(11):2154-7. | | Anti-diabetic properties of chrysophanol and its glucoside from rhubarb rhizome.[Pubmed: 18981591] | An ethanol extract of rhubarb rhizome exhibited marked glucose transport activity in differentiated L6 rat myotubes. Activity-guided fractionation resulted in the isolation of two anthraquinones, Chrysophanol-8-O-beta-D-glucopyranoside (1) and Chrysophanol (2).
METHODS AND RESULTS:
The anti-diabetic effect was examined by glucose transport activity, glucose transporter 4 (Glut4) expression in myotubes, and the level of insulin receptor (IR) tyrosine phosphorylation as influenced by tyrosine phosphatase 1B, each of which is a major target of diabetes treatment. Chrysophanol-8-O-beta-D-glucopyranoside up to 25 microM dose-dependently activated glucose transport in insulin-stimulated myotubes. Increased tyrosine phosphorylation of IR due to tyrosine phosphatase 1B inhibitory activity with an IC50 value of 18.34+/-0.29 microM and unchanged Glut4 mRNA levels was observed following Chrysophanol-8-O-beta-D-glucopyranoside treatment. Chrysophanol up to 100 microM exerted mild glucose transport activity and elevated the tyrosine phosphorylation of IR via tyrosine phosphatase 1B inhibition (IC50=79.86+/-0.12 microM); Glut4 mRNA expression was also significantly increased by 100 microM. The ED50 values of the two compounds were 59.38+/-0.66 and 79.69+/-0.03 microM, respectively.
CONCLUSIONS:
Therefore, these two anthraquinones from rhubarb rhizome, Chrysophanol-8-O-beta-D-glucopyranoside and Chrysophanol, have mild cytotoxicity and anti-diabetic properties and could play metabolic roles in the insulin-stimulated glucose transport pathway. | | 2016 Dec 8;7:476. | | Chrysophanic Acid Suppresses Adipogenesis and Induces Thermogenesis by Activating AMP-Activated Protein Kinase Alpha In vivo and In vitro[Pubmed: 28008317] | | Chrysophanic acid (CA) is a member of the anthraquinone family abundant in rhubarb, a widely used herb for obesity treatment in Traditional Korean Medicine. Though several studies have indicated numerous features of CA, no study has yet reported the effect of CA on obesity. In this study, we tried to identify the anti-obesity effects of CA. By using 3T3-L1 adipocytes and primary cultured brown adipocytes as in vitro models, high-fat diet (HFD)-induced obese mice, and zebrafish as in vivo models, we determined the anti-obesity effects of CA. CA reduced weight gain in HFD-induced obese mice. They also decreased lipid accumulation and the expressions of adipogenesis factors including peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT/enhancer-binding protein alpha (C/EBPα) in 3T3-L1 adipocytes. In addition, uncoupling protein 1 (UCP1) and peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC1α), the brown fat specific thermogenic genes, were up-regulated in brown adipocytes by CA treatment. Furthermore, when co-treated with Compound C, the AMP-activated protein kinase (AMPK) inhibitor, the action of CA on AMPKα was nullified in both types of adipocytes, indicating the multi-controlling effect of CA was partially via the AMPKα pathway. Given all together, these results indicate that CA can ameliorate obesity by controlling the adipogenic and thermogenic pathway at the same time. On these bases, we suggest the new potential of CA as an anti-obese pharmacotherapy.
Keywords: AMP-activated protein kinase alpha; adipogenesis; chrysophanic acid; obesity; thermogenesis. |
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| In vivo: |
| Neural Regen Res. 2014 May 1;9(9):924-30. | | Chrysophanol attenuates lead exposure-induced injury to hippocampal neurons in neonatal mice.[Pubmed: 25206913] | Previous studies have shown that Chrysophanol protects against learning and memory impairments in lead-exposed adult mice.
METHODS AND RESULTS:
In the present study, we investigated whether Chrysophanol can alleviate learning and memory dysfunction and hippocampal neuronal injury in lead-exposed neonatal mice. At the end of lactation, Chrysophanol (0.1, 1.0, 10.0 mg/kg) was administered to the neonatal mice by intraperitoneal injection for 15 days. Chrysophanol significantly alleviated injury to hippocampal neurons and improved learning and memory abilities in the lead-poisoned neonatal mice. Chrysophanol also significantly decreased lead content in blood, brain, heart, spleen, liver and kidney in the lead-exposed neonatal mice. The levels of malondialdehyde in the brain, liver and kidney were significantly reduced, and superoxide dismutase and glutathione peroxidase activities were significantly increased after Chrysophanol treatment.
CONCLUSIONS:
Collectively, these findings indicate that Chrysophanol can significantly reduce damage to hippocampal neurons in lead-exposed neonatal mice.
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