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Zerumbone, Sesquiterpene Photochemical from Ginger, Inhibits Angiogenesis.

Park JH, Park GM, Kim JK - Korean J. Physiol. Pharmacol. (2015)

Bottom Line: Zerumbone inhibited HUVECs proliferation, migration and tubule formation, as well as angiogenic activity by rat aorta explants.In particular, zerumbone inhibited phosphorylation of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1, which are key regulators of endothelial cell function and angiogenesis.Overall, these results suggest that zerumbone inhibits various attributes of angiogenesis, which might contribute to its reported antitumor effects.

View Article: PubMed Central - PubMed

Affiliation: Department of Biomedical Science, Catholic University of Daegu, Gyeongsan 712-702, Korea.

ABSTRACT
Here, we investigated the role of zerumbone, a natural cyclic sesquiterpene of Zingiber zerumbet Smith, on angiogenesis using human umbilical vein endothelial cells (HUVECs). Zerumbone inhibited HUVECs proliferation, migration and tubule formation, as well as angiogenic activity by rat aorta explants. In particular, zerumbone inhibited phosphorylation of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1, which are key regulators of endothelial cell function and angiogenesis. In vivo matrigel plug assay in mice demonstrated significant decrease in vascularization and hemoglobin content in the plugs from zerumbone-treated mice, compared with control mice. Overall, these results suggest that zerumbone inhibits various attributes of angiogenesis, which might contribute to its reported antitumor effects.

No MeSH data available.


Related in: MedlinePlus

Effects of zerumbone on VEGFR2- and FGFR1-mediated signaling pathways. (A) HUVECs were treated with various concentrations of zerumbone and stimulated with human VEGF (10 ng/ml) for 15 min. Phosphorylation of VEGFR2 by VEGF was determined using Western blot. (B) HUVECs were treated with zerumbone and stimulated with human bFGF (50 ng/ml) for 15 min. Phosphorylation of of FGFR by bFGF were determined using Western blot. The bands were quantified using image analysis software and their relative intensity was expressed as fold against the image of the VEGF- or bFGF- stimulated cells. ***p<0.001 versus VEGF or bFGF+0 µM zerumbone-treated cells.
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Figure 4: Effects of zerumbone on VEGFR2- and FGFR1-mediated signaling pathways. (A) HUVECs were treated with various concentrations of zerumbone and stimulated with human VEGF (10 ng/ml) for 15 min. Phosphorylation of VEGFR2 by VEGF was determined using Western blot. (B) HUVECs were treated with zerumbone and stimulated with human bFGF (50 ng/ml) for 15 min. Phosphorylation of of FGFR by bFGF were determined using Western blot. The bands were quantified using image analysis software and their relative intensity was expressed as fold against the image of the VEGF- or bFGF- stimulated cells. ***p<0.001 versus VEGF or bFGF+0 µM zerumbone-treated cells.

Mentions: To investigate the molecular mechanism of the anti-angiogenic effect of zerumbone, the essential signal pathways of angiogenesis were explored. VEGFR2 is the primary receptor for VEGF that mediates angiogenic activity, endothelial cell proliferation, migration, differentiation and tube formation [23]. Appropriately we tested whether zerumbone interacted with the VEGF/VEGFR2 signaling pathway. VEGFR2 was phosphorylated by exogenous VEGF in HUVECs and zerumbone blocked this phosphorylation in a concentration-dependent manner (Fig. 4A).


Zerumbone, Sesquiterpene Photochemical from Ginger, Inhibits Angiogenesis.

Park JH, Park GM, Kim JK - Korean J. Physiol. Pharmacol. (2015)

Effects of zerumbone on VEGFR2- and FGFR1-mediated signaling pathways. (A) HUVECs were treated with various concentrations of zerumbone and stimulated with human VEGF (10 ng/ml) for 15 min. Phosphorylation of VEGFR2 by VEGF was determined using Western blot. (B) HUVECs were treated with zerumbone and stimulated with human bFGF (50 ng/ml) for 15 min. Phosphorylation of of FGFR by bFGF were determined using Western blot. The bands were quantified using image analysis software and their relative intensity was expressed as fold against the image of the VEGF- or bFGF- stimulated cells. ***p<0.001 versus VEGF or bFGF+0 µM zerumbone-treated cells.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4499645&req=5

Figure 4: Effects of zerumbone on VEGFR2- and FGFR1-mediated signaling pathways. (A) HUVECs were treated with various concentrations of zerumbone and stimulated with human VEGF (10 ng/ml) for 15 min. Phosphorylation of VEGFR2 by VEGF was determined using Western blot. (B) HUVECs were treated with zerumbone and stimulated with human bFGF (50 ng/ml) for 15 min. Phosphorylation of of FGFR by bFGF were determined using Western blot. The bands were quantified using image analysis software and their relative intensity was expressed as fold against the image of the VEGF- or bFGF- stimulated cells. ***p<0.001 versus VEGF or bFGF+0 µM zerumbone-treated cells.
Mentions: To investigate the molecular mechanism of the anti-angiogenic effect of zerumbone, the essential signal pathways of angiogenesis were explored. VEGFR2 is the primary receptor for VEGF that mediates angiogenic activity, endothelial cell proliferation, migration, differentiation and tube formation [23]. Appropriately we tested whether zerumbone interacted with the VEGF/VEGFR2 signaling pathway. VEGFR2 was phosphorylated by exogenous VEGF in HUVECs and zerumbone blocked this phosphorylation in a concentration-dependent manner (Fig. 4A).

Bottom Line: Zerumbone inhibited HUVECs proliferation, migration and tubule formation, as well as angiogenic activity by rat aorta explants.In particular, zerumbone inhibited phosphorylation of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1, which are key regulators of endothelial cell function and angiogenesis.Overall, these results suggest that zerumbone inhibits various attributes of angiogenesis, which might contribute to its reported antitumor effects.

View Article: PubMed Central - PubMed

Affiliation: Department of Biomedical Science, Catholic University of Daegu, Gyeongsan 712-702, Korea.

ABSTRACT
Here, we investigated the role of zerumbone, a natural cyclic sesquiterpene of Zingiber zerumbet Smith, on angiogenesis using human umbilical vein endothelial cells (HUVECs). Zerumbone inhibited HUVECs proliferation, migration and tubule formation, as well as angiogenic activity by rat aorta explants. In particular, zerumbone inhibited phosphorylation of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1, which are key regulators of endothelial cell function and angiogenesis. In vivo matrigel plug assay in mice demonstrated significant decrease in vascularization and hemoglobin content in the plugs from zerumbone-treated mice, compared with control mice. Overall, these results suggest that zerumbone inhibits various attributes of angiogenesis, which might contribute to its reported antitumor effects.

No MeSH data available.


Related in: MedlinePlus