Rutin, an active
flavonoid compound, is well known to possess potent antiplatelet,
antiviral and
antihypertensive properties. In this study, we first investigated the possible barrier protective effects of
rutin against pro-inflammatory responses in human umbilical vein endothelial cells (HUVECs) induced by
lipopolysaccharide (LPS) and the associated signaling pathways. The barrier protective activities of
rutin were determined by measuring permeability, monocytes adhesion and migration, and activation of pro-inflammatory
proteins in LPS-activated HUVECs. We found that
rutin inhibited LPS-induced barrier disruption, expression of
cell adhesion molecules (CAMs) and adhesion/transendothelial migration of monocytes to human endothelial cells.
Rutin also suppressed
acetic acid induced-hyperpermeability and
carboxymethylcellulose-induced leukocytes migration in vivo. Further studies revealed that
rutin suppressed the production of
tumor necrosis factor-α (TNF-α) and activation of nuclear factor-κB (NF-κB) by LPS. Collectively, these results suggest that
rutin protects vascular barrier integrity by inhibiting hyperpermeability, expression of CAMs, adhesion and migration of leukocytes, thereby endorsing its usefulness as a
therapy for vascular inflammatory diseases.