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Sarpogrelate inhibits the expression of ICAM-1 and monocyte-endothelial adhesion induced by high glucose in human endothelial cells.

Abstract
Hyperglycemia is the major cause of diabetic angiopathy. Sarpogrelate hydrochloride is an antiplatelet drug, and expected to be useful in the treatment of chronic arterial occlusive diseases. The aim of our study was to evaluate the possible effects of sarpogrelate hydrochloride on adhesion molecule expression and its underlying mechanism in the prevention and treatment of cardiovascular disorders. Intercellular adhesion molecule-1 (ICAM-1) expression and superoxide dismutase (SOD) activity were determined after endothelial cells were exposed to high glucose in the absence and presence of sarpogrelate hydrochloride. Coincubation of endothelial cells with high glucose for 24 h resulted in a significant increase of monocyte-endothelial cell adhesion and the expression of ICAM-1 (P < 0.01). These effects were abolished by sarpogrelate hydrochloride and sarpogrelate hydrochloride significantly increased SOD activities (40 ± 8 vs. 47 ± 7, n = 8, P < 0.01). The low dose sarpogrelate group (0.1 μM) had significantly higher monocyte-endothelial cell adhesion and the expression of ICAM-1 than medium dose sarpogrelate group (1.0 μM) and high dose sarpogrelate group (10.0 μM) (P < 0.05 for comparison among three groups and P < 0.01 for difference between low and high dose sarpogrelate groups). These findings suggested that sarpogrelate hydrochloride was able to protect vascular endothelium from dysfunction induced by high glucose.
AuthorsYing Su, Nan Mao, Min Li, Xia Dong, Fan-Zhen Lin, Ying Xu, Yan-Bo Li
JournalMolecular and cellular biochemistry (Mol Cell Biochem) Vol. 373 Issue 1-2 Pg. 195-9 (Jan 2013) ISSN: 1573-4919 [Electronic] Netherlands
PMID23111892 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Serotonin 5-HT2 Receptor Antagonists
  • Succinates
  • Intercellular Adhesion Molecule-1
  • sarpogrelate
  • Superoxide Dismutase
  • Glucose
Topics
  • Cell Adhesion (drug effects)
  • Cells, Cultured
  • Coculture Techniques
  • Gene Expression (drug effects)
  • Glucose (pharmacology, physiology)
  • Human Umbilical Vein Endothelial Cells (drug effects, physiology)
  • Humans
  • Intercellular Adhesion Molecule-1 (genetics, metabolism)
  • Leukocytes, Mononuclear (drug effects, physiology)
  • Serotonin 5-HT2 Receptor Antagonists (pharmacology)
  • Succinates (pharmacology)
  • Superoxide Dismutase (metabolism)

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