A novel compound, NP-184, inhibits the vascular endothelial growth factor induced angiogenesis

作者：Lin Kuan Ting; Lien Jin Cherng; Chung Ching Hu; Kuo Sheng Chu; Huang Tur Fu^*

来源：European Journal of Pharmacology, 2010, 630(1-3): 53-60.

DOI：10.1016/j.ejphar.2009.12.036

• Angiogenesis
• VEGF
• HUVEC
• Benzimidazole

Angiogenesis is observed in many diseases, such as tumor progression, diabetes and rheumatoid arthritis, it is a process that involves proliferation, migration, differentiation and tube formation of endothelial cells Vascular endothelial growth factor (VEGF) plays an important role in angiogenesis by induction of these endothelial functions. Thus, inhibition of these critical angiogenic steps is a practical therapeutic strategy for those diseases NP-184 is a substituted benzimidazole analogue which exhibits a potent anti-thrombotic activity. In this report, NP-184 inhibited the viability of human umbilical vascular endothelial cells (HUVEC) in a concentration-dependent manner, and caused cell apoptosis as examined by cell-cycle analysis and Annexin V staining with flow cytometry NP-184 also concentration-dependently inhibited the HUVEC migration, tube formation on Matrigel. and rat aortic ring sprouting stimulated by VEGF Regarding the intracellular signal transduction, NP-184 concentration-dependently interfered with the activation of AKT. ERK and the nuclear translocation of NF-kappa B. In vivo study showed that NP-184 close-dependently reduced angiogenesis in Matrigel plug assay.

• 出版日期2010-3-25
• 单位中国医科大学