Abstract: Endothelial dysfunction induced by hyperlipidemia is recognized as one of the pivotal factors in the pathogenesis of metabolic syndrome and a variety of cardiovascular complications. Mechanisms involved in hyperlipidemia-induced endothelial dysfunction include the imbalance between the secretion of vasoconstrictor and vasodilator, vasculitis and up-regulated oxidative stress in endothelial cells. Many studies have proved that the activation of κ-opioid receptor (κ-OR) has some cardiovascular protective effect. However, the role of κ-OR in hyperlipidemia-induced endothelial dysfunction is still unclear. This paper reviews the current knowledge about hyperlipidemia-induced endothelial dysfunction and the cardiovascular protective effect of κ-OR activation on hyperlipidemia-induced endothelial dysfunction.