Background: Kaempferol-3-O-sophoroside (KPOS) was isolated from the leaves of cultivated mountain ginseng. Kaempferol (KP) has antitumor, anti-oxidative, anti-allergic and antidiabetic activities but the barrier protective effects and underlying mechanism are not fully identified. In this study, we attempted to determine whether pretreatment with KPOS induced significant barrier protective activities in lipopolysaccharide (LPS)-stimulated human umbilical vein endothelial cells (HUVECs).
Methods: The anti-inflammatory activities of KPOS were determined by measuring solute flux, neutrophil adhesion and migration and activation of pro-inflammatory proteins in LPS-activated HUVECs.
Results: We found that KPOS inhibited LPS-induced barrier disruption, expression of cell adhesion molecules, neutrophil adhesion and transendothelial migration of neutrophils to HUVECs. Further studies revealed that KPOS suppressed the production of tumor necrosis factor-α (TNF-α) and activation of nuclear factor-κB (NF-κB) by LPS, and that anti-inflammatory activities of KPOS were better than those of KP.
Conclusion: Collectively, these results suggest that KPOS possesses barrier integrity activity, inhibitory activity on cell adhesion and migration to endothelial cells by blocking the activation of NF-κB expression and production of TNF-α, thereby endorsing its usefulness as therapy for vascular inflammatory diseases.