LW-215, a newly synthesized flavonoid, exhibits potent anti-angiogenic activity in vitro and in vivo

• Published in: Gene Vol. 642; pp. 533 - 541
• Main Authors: Zhao, Kai, Yuan, Yang, Lin, Binyan, Miao, Zhaorui, Li, Zhiyu, Guo, Qinglong, Lu, Na
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 05.02.2018
• Subjects: Angiogenesis; EA.hy926 cells; LW-215; VEGFR2; VEGFR2; Angiogenesis; DMSO; EA.hy926 cells; VEGFR; LW-215; MAPK; HUVECs; CAM; ERK
• ISSN: 0378-1119; 1879-0038
• DOI: 10.1016/j.gene.2017.11.065

LW-215 is a newly synthesized flavonoid, which is the derivative of wogonin. Our group has previously confirmed that wogonin has an anti-angiogenic activity, while the anti-angiogenic effect of LW-215 is unclear. In this study, we explored whether LW-215 can inhibit angiogenesis and further probed the potential molecular mechanisms. We found that LW-215 inhibited migration and tube formation in human umbilical vein endothelial cells (HUVECs) and immortalized endothelial EA.hy926 cells without a significant decrease in cell viability. Microvessels sprouting from rat aortic ring and chicken chorioallantoic membrane (CAM) model also revealed that LW-215 could suppress angiogenesis in vivo. Western blot and ELISA analysis indicated that LW-215 could prevent VEGFR2 activation though reducing VEGF autocrine other than VEGFR1. Thus, its downstream kinases, such as Akt, ERK and p38 signaling, were inhibited. Taken together, these results fully showed that LW-215 might be a promising anti-angiogenesis agent. [Display omitted] •LW-215 inhibits angiogenesis in vitro and in vivo.•VEGFR2 signaling contributes to anti-angiogenic activity of LW-215.•Inhibition of VEGF autocrine is crucial for angiogenesis.•LW-215 can be a promising anticancer drug.