Biomol Ther.
2013 Jul;21(4):277-283.
Inhibitory Effect of an Urotensin II Receptor Antagonist on Proinflammatory Activation Induced by Urotensin II in Human Vascular Endothelial Cells
- Affiliations
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- 1Department of Pathophysiology, College of Pharmacy, Ajou University, Suwon 443-749, Republic of Korea. yisjung@ajou.ac.kr
- 2Brain Korea 21 for Molecular Science and Technology, Ajou University, Suwon 443-749, Republic of Korea.
- 3Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon 305-343, Republic of Korea.
- 4Research Institute of Pharmaceutical Sciences and Technology, Ajou University, Suwon 443-749, Republic of Korea.
Abstract
- In this study, we investigated the effects of a selective urotensin II (UII) receptor antagonist, SB-657510, on the inflammatory response induced by UII in human umbilical vein endothelial cells (EA.hy926) and human monocytes (U937). UII induced inflammatory activation of endothelial cells through expression of proinflammatory cytokines (IL-1beta and IL-6), adhesion molecules (VCAM-1), and tissue factor (TF), which facilitates the adhesion of monocytes to EA.hy926 cells. Treatment with SB-657510 significantly inhibited UII-induced expression of IL-1beta, IL-6, and VCAM-1 in EA.hy926 cells. Further, SB-657510 dramatically blocked the UII-induced increase in adhesion between U937 and EA.hy926 cells. In addition, SB-657510 remarkably reduced UII-induced expression of TF in EA.hy926 cells. Taken together, our results demonstrate that the UII antagonist SB-657510 decreases the progression of inflammation induced by UII in endothelial cells.