| Description: |
Angoroside C has anti-inflammatory effect , it can significantly inhibit LPS-induced PGE(2), NO and TNF-alpha in a concentration-dependent manner; it also exhibits cytotoxic and cytostatic activities against several kinds of cancer cells. Angoroside C has beneficial effects against ventricular remodeling, the mechanism is likely to be related to decreasing the level of Ang Ⅱ, attenuating the mRNA expressions of ET-1 and TGF-β1. |
| Targets: |
COX | LOX | NO | TNF-α | PGE | MMP(e.g.TIMP) | TGF-β/Smad |
| In vitro: |
| Life Sci. 2004 Apr 2;74(20):2515-26. | | Phenylpropanoid glycosides from Scrophularia scorodonia: in vitro anti-inflammatory activity.[Pubmed: 15010262] | Five phenylpropanoid glycosides isolated from Scrophularia scorodonia L. (Scrophulariaceae), namely angoroside A (1), Angoroside C (2), angoroside D (3), acteoside (4) and isoacteoside (5), had been evaluated as potential inhibitors of some macrophage functions involved in the inflammatory process.
METHODS AND RESULTS:
These compounds have been tested in two experimental systems: ionophore-stimulated mouse peritoneal macrophages and human platelets serve as source of COX-1 and 5-LOX, and mouse peritoneal macrophages stimulated with E. coli LPS are the means of testing for COX-2, NO and TNF-alpha activity. None of compounds assayed had a significant effect on LTC(4)-release from calcium ionophore-stimulated mouse peritoneal macrophages. However, the release of PGE(2) by mouse peritoneal macrophages stimulated with calcium ionophore was inhibited by most of these compounds. In the TXB(2)-release assay, acteoside (4), angoroside A (1) and Angoroside C (2) showed a significant effect. These five compounds, except Angoroside C (2) significantly inhibited LPS-induced PGE(2), NO and TNF-alpha in a concentration-dependent manner. In LPS-stimulated macrophages, the phenylpropanoid glycoside Angoroside C (2) only had activity on NO.
CONCLUSIONS:
These results indicate that the pharmacology of these compounds may participate in the anti-inflammatory effect of Scrophularia scorodonia. |
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| In vivo: |
| Phytomedicine. 2015 Jul 15;22(7-8):705-12. | | The effect of angoroside C on pressure overload-induced ventricular remodeling in rats.[Pubmed: 26141756 ] | Our previous study reveals that total rough extract of Radix Scrophulariae has a beneficial effect on ventricular remodeling.
HYPOTHESIS:
After carrying out a series of preliminary experiments, we speculated that Angoroside C may be the effective agent.
STUDY DESIGN:
After oral administration, the effect of Angoroside C on ventricular remodeling was evaluated by using a pressure-overloaded rat model, some related indexes were detected in vivo.
METHODS AND RESULTS:
A model of pressure overloaded ventricular remodeling was produced by abdominal aortic constriction (AAC) in rats. The sham-operated rats underwent an identical surgical procedure except for AAC. AAC rats were randomly divided into five groups: model control group, three Angoroside C treated groups (7.5, 15 and 30 mg·kg(-1)) and captopril treated group (40 mg·kg(-1)). The rats were orally administered with the corresponding drugs or drinking water for 4 weeks. The levels of blood pressure (BP), left ventricular weight index (LVWI) and heart weight index (HWI) were detected. Myocardium tissue was stained with hematoxylin and eosin or picric acid/sirius red for cardiomyocyte cross-section area or collagen content measurements respectively. The concentrations of angiotensin Ⅱ (Ang Ⅱ), hydroxyproline (Hyp), matrix metalloproteinase 2 (MMP-2), MMP-9 and tissue inhibitor of metalloproteinase-1 (TIMP-1) in myocardium or serum were determined. Real-time RT-PCR was performed to detect the mRNA expressions of endothelin 1 (ET-1), transforming growth factor β1 (TGF-β1).
Angoroside C significantly reduced the BP, LVWI and HWI, decreased the content of Ang Ⅱ, Hyp, diminished cross sectional area of cardiomyocytes and ameliorated collagen deposition. Additionally, it markedly reduced collagen I and III expressions and regulated matrix metalloproteinase-2, 9 and inhibitors of metalloproteinase expressions. Angoroside C also down regulated the gene expressions of ET-1 and TGF-β1mRNA in myocardium.
CONCLUSIONS:
Angoroside C has beneficial effects against ventricular remodeling. The mechanism is likely to be related to decreasing the level of Ang Ⅱ, attenuating the mRNA expressions of ET-1 and TGF-β1. |
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