|Blood. 2013 May 2;121(18):3682-91. |
|Wogonoside induces cell cycle arrest and differentiation by affecting expression and subcellular localization of PLSCR1 in AML cells.[Pubmed: 23487022 ]|
|Wogonoside is the main flavonoid component derived from the root of Scutellaria baicalensis Georgi. It is a popular Chinese herbal medicine with the potential to treat hematologic malignancies.
METHODS AND RESULTS:
In this study, we investigated the anticancer effects of Wogonoside in acute myeloid leukemia (AML) cell lines and primary patient-derived AML cells. Wogonoside exerted antiproliferative properties both in vitro and in vivo. Furthermore, it efficiently inhibited the proliferation of U937 and HL-60 cells through the induction of G1 phase arrest and the promotion of differentiation. We also demonstrated that Wogonoside significantly increased the transcription of phospholipid scramblase 1 (PLSCR1) due to its influence on the expression of cell cycle- and differentiation-related genes, including the upregulation of p21waf1/cip1 and downregulation of the oncogenic protein c-Myc. Wogonoside also promoted PLSCR1 trafficking into the nucleus and facilitated its binding to the inositol 1,4,5-trisphosphate receptor 1 (IP3R1) promoter, thus increasing the expression of IP3R1. Finally, inhibition of PLSCR1 expression with small interfering RNA partially blocked Wogonoside-induced cell cycle arrest and differentiation and disturbed the Wogonoside-associated molecular events.
The results of this study therefore suggest that Wogonoside may represent a therapeutic candidate for the treatment of AML.
|Fitoterapia. 2014 Oct;98:27-35. |
|Antithrombotic activities of wogonin and wogonoside via inhibiting platelet aggregation.[Pubmed: 25020199 ]|
|Wogonin (WGN), a flavonoid extracted from Scutellaria baicalensis Georgi, has several biological effects including antioxidant, anti-inflammatory, antiviral, neuroprotective, anxiolytic, and anticancer activities, and the flavonoid Wogonoside (WGNS) can be derived from S. baicalensis, as it is a metabolite of wogonin.
METHODS AND RESULTS:
Here, the anticoagulant activities of WGN(S) were examined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of thrombin (factor IIa, FIIa) and activated factor X (FXa), and the effects of WGN(S) on expression of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were evaluated in tumor necrosis factor (TNF)-α activated human umbilical vein endothelial cells (HUVECs). Treatment with WGN(S) resulted in prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, as well as inhibited production of thrombin and FXa in HUVECs. In addition, WGN(S) inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. WGN(S) also elicited anticoagulant effects in mice. In addition, treatment with WGN(S) resulted in significant reduction of the PAI-1 to t-PA ratio.
Collectively, WGN(S) possesses antithrombotic activities and offers a basis for development of a novel anticoagulant.
|Inflammation. 2014 Dec;37(6):2006-12. |
|Wogonoside ameliorates lipopolysaccharide-induced acute lung injury in mice.[Pubmed: 24854163]|
|Wogonoside has been reported to have anti-inflammatory properties. In this study, we evaluated the effect of Wogonoside on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice.
METHODS AND RESULTS:
Male BALB/c mice with ALI, induced by intranasal instillation of LPS, were treated with Wogonoside 1 h prior to LPS exposure. Mice treated with LPS alone showed significantly increased TNF-α, IL-6, and IL-1β levels in the bronchoalveolar lavage fluid (BALF). When pretreated with Wogonoside, the TNF-α, IL-6, and IL-1β levels were significantly decreased. Meanwhile, Wogonoside significantly inhibited LPS-induced increases in the macrophage and neutrophil infiltration of lung tissues and markedly attenuated myeloperoxidase activity. Furthermore, Wogonoside inhibited the TLR4 expression and the phosphorylation of NF-κB p65, and IκB induced by LPS.
In conclusion, our results indicate that Wogonoside exhibits a protective effect on LPS-induced ALI via suppression of TLR4-mediated NF-κB signaling pathways.