| Description: |
Isorhamnetin 3-O-galactoside shows antioxidant, anti-inflammatory, neuroprotective,and barrier protective activities, it could be used as a candidate therapeutic for treatment of severe vascular inflammatory diseases.It has potential anticoagulant activity, it possesses antithrombotic and profibrinolytic activity and offers bases for development of a novel anticoagulant. Isorhamnetin 3-O-galactoside is also a 5-lipoxygenase inhibitor, it may have therapeutic potential in skin inflammatory disorders in traditional medicine. |
| Targets: |
NF-kB | TNF-α | ERK | JNK | p38MAPK | LOX |
| In vitro: |
| Food Chem Toxicol. 2013 Mar;53:197-204. | | Antithrombotic and profibrinolytic activities of isorhamnetin-3-O-galactoside and hyperoside.[Pubmed: 23220618] | The potential anticoagulant activities of two single compounds, Isorhamnetin 3-O-galactoside (IMG) and hyperoside, from Oenanthe javanica, were tested.
METHODS AND RESULTS:
The anticoagulant activities were investigated by measuring activated partial thromboplastin time (aPTT) and prothrombin time (PT), and the ability to inhibit production of thrombin and activated factor X (FXa) was investigated in human umbilical vein endothelial cells (HUVECs). And, the effects of the compounds on expression of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were tested in tumor necrosis factor-(TNF)-α activated HUVECs. Treatment with IMG and hyperoside resulted in significantly prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and IMG or hyperoside inhibited production of thrombin and FXa in HUVECs. In accordance with these anticoagulant activities, both agents elicited anticoagulant effects in mouse. In addition, treatment with IMG and hyperoside resulted in inhibition of TNF-α-induced production of PAI-1, and treatment with IMG resulted in significant reduction of the PAI-1 to t-PA ratio.
CONCLUSIONS:
The anticoagulant and profibrinolytic effects of IMG were greater than those of hyperoside, indicating positive regulation of its anticoagulant function by the methoxy group of IMG. IMG and hyperoside possess antithrombotic activities and offer bases for development of a novel anticoagulant. |
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| In vivo: |
| Journal of Cellular Biochemistry, 2012, 114(2):336-345. | | Anti-inflammatory activities of isorhamnetin-3-O-galactoside against HMGB1-induced inflammatory responses in both HUVECs and CLP-induced septic mice.[Pubmed: 22930571] | High mobility group box 1 (HMGB1) protein is a crucial nuclear cytokine that elicits severe vascular inflammatory diseases. Oenanthe javanica (water dropwort) extract has anti-arrhythmic, neuroprotective and anti-diabetic activity. However, Isorhamnetin 3-O-galactoside (I3G), an active compound from O. javanica, is not researched well for its biological activity.
METHODS AND RESULTS:
Here, we investigated the anti-inflammatory activities of I3G by monitoring the effects of I3G on the lipopolysaccharide (LPS) or cecal ligation and puncture (CLP)-mediated release of HMGB1 and HMGB1 or CLP-mediated modulation of inflammatory responses. I3G potently inhibited the release of HMGB1 and down-regulated HMGB1-dependent inflammatory responses in human endothelial cells. I3G also inhibited HMGB1-mediated hyperpermeability and leukocyte migration in mice. Further studies revealed that I3G suppressed the production of tumor necrosis factor-α and activation of nuclear factor-κB by HMGB1. In addition, I3G reduced CLP-induced HMGB1 release and sepsis-related mortality.
CONCLUSIONS:
Given these results, I3G should be viewed as a candidate therapeutic agent for the treatment of severe vascular inflammatory diseases such as sepsis or septic shock via inhibition of the HMGB1 signaling pathway. |
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Cell. 2018 Jan 11;172(1-2):249-261.e12. doi: 10.1016/j.cell.2017.12.019.IF=36.216(2019)
Cell Metab. 2020 Mar 3;31(3):534-548.e5. doi: 10.1016/j.cmet.2020.01.002.IF=22.415(2019)
Mol Cell. 2017 Nov 16;68(4):673-685.e6. doi: 10.1016/j.molcel.2017.10.022.IF=14.548(2019)
ACS Nano. 2018 Apr 24;12(4): 3385-3396. doi: 10.1021/acsnano.7b08969.IF=13.903(2019)
Nature Plants. 2016 Dec 22;3: 16206. doi: 10.1038/nplants.2016.205.IF=13.297(2019)
Sci Adv. 2018 Oct 24;4(10): eaat6994. doi: 10.1126/sciadv.aat6994.IF=12.804(2019)
