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Blockade of cell adhesion by a small molecule selectin antagonist attenuates myocardial ischemia/reperfusion injury.

Abstract
Reperfusion injury is related closely to inflammatory reactions such as the activation and accumulation of neutrophils. We investigated the efficacy of a novel small molecule selectin antagonist (bimosiamose) in a rat model of transient left coronary artery occlusion (30 min) and reperfusion (24 h). Treatment with bimosiamose (25 mg/kg, intravenously at reperfusion) showed a significant reduction in infarction area/area at risk of approximately 41% compared to vehicle control (P=0.01) and preserved the left ventricular function. The accumulation of polymorphonuclear neutrophils at the site of area at risk was decreased significantly, accompanied by 78% reduction of the myeloperoxidase activity. Parallel-plate flow chamber analysis revealed that bimosiamose showed a significant inhibition in rolling (62%, P<0.001) and adhesion (38%, P<0.05) of HL-60 cells to activated human umbilical vein endothelial cells compared with vehicle control. This study demonstrates for the first time that bimosiamose, a novel small molecule selectin antagonist, attenuates significantly ischemia/reperfusion injury.
AuthorsYasuyuki Onai, Jun-ichi Suzuki, Yasunobu Nishiwaki, Ryo Gotoh, Kurt Berens, Richard Dixon, Masayuki Yoshida, Hiroshi Ito, Mitsuaki Isobe
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 481 Issue 2-3 Pg. 217-25 (Nov 28 2003) ISSN: 0014-2999 [Print] Netherlands
PMID14642789 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Biphenyl Compounds
  • Mannosides
  • Selectins
  • bimosiamose disodium
  • Mannose
Topics
  • Animals
  • Biphenyl Compounds (pharmacology, therapeutic use)
  • Cells, Cultured
  • HL-60 Cells
  • Humans
  • Male
  • Mannose (analogs & derivatives)
  • Mannosides (pharmacology, therapeutic use)
  • Myocardial Ischemia (pathology, prevention & control)
  • Myocardial Reperfusion Injury (pathology, prevention & control)
  • Neutrophils (drug effects)
  • Rats
  • Rats, Sprague-Dawley
  • Selectins (physiology)

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