Scutellarin Isolated from <i>Erigeron multiradiatus</i> Inhibits High Glucose-mediated Vascular Inflammation

Abstract

Erigeron multiradiatus (Lindl.) Benth is a traditional Tibetan medicine herb long used to treat various diseases related to in‰ammation. Our previous phytochemical studies on E. multiradiatus resulted in the isolation of scutellarin, which is a known ‰avone glucuronide with comprehensive pharmacological actions. In present study, we investigated the inhibition action of scutellarin on high glucose-induced vascular in‰ammation in human endothelial cells (ECV304 cells). Consistent with previous reports, exposure of ECV304 cells to high glucose for 24 h caused an increase of intercellular adhesion molecule-1 (ICAM-1) and monocyte chemoattractant protein 1 (MCP-1), and promoted cell adhesion between monocyte and ECV304 cells. However, pretreatment with scutellarin (0.1 and 1 mM) reversed these eŠects in a concentration-dependent manner. Scutellarin was able to inhibit the activation of NF-kB induced by high glucose in ECV304 cells. Furthermore, although oral administration of scutellarin (10 and 50 mg/kg) did not produce signiˆcant antihyperglycemic action, it lowered the serum MCP-1 levels signiˆcantly in alloxan-induced diabetic mice. Therefore, our results suggest that scutellarin has anti-in‰ammation eŠect that may aŠord some protection against hyperglycemiainduced vascular in‰ammatory both in vitro and in vivo.

Monocyte Chemoattractant Protein 1 (MCP-1) in obesity and diabetes

“…Up to 7 days of chronic incubation of human umbilical vein endothelial cells (HUVEC) with high glucose increased mRNA expression and production rate of MCP-1 in a time- and concentration (10-35 mM)-dependent manner, through upregulation of reactive oxygen species (ROS) generation and subsequent activation of p38 MAPK [106]. Consistent with previous reports, exposure of human endothelial ECV304 cells to high glucose for 24 h caused an increase of MCP-1 and intercellular adhesion molecule-1 (ICAM-1), and promoted cell adhesion between monocyte and ECV304 cells [107]. Furthermore, high glucose treatment on human acute monocytic leukemia THP-1 cells increased both mRNA and protein levels of MCP-1, enhanced the adhesion of THP-1 cells to endothelial cells, and the pathways reportedly involved oxidative stress, protein kinase C, ERK1/2, and p38 MAPK [108].…”

Scutellarin inhibits cell migration by regulating production of αvβ6 integrin and E-cadherin in human tongue cancer cells

“…It has been shown that extract of Scutellaria barbata specifically targets tumor tissue. Recently, its anti-inflammatory and anti-tumor activities have been revealed (26,27).…”

Scutellarin inhibits translocation of protein kinase C in diabetic thoracic aorta of the rat

“…This causal relationship is currently being investigated. Moreover, others have suggested that Scu can protect against high glucose‐induced vascular inflammation, 29 which is also beneficial for the prevention of diabetic complications.…”