甲氧基甲醚异戊烯基槲皮素是一个新合成的槲皮素衍生物, 它比槲皮素有更强的细胞保护作用。本文进一步研究了它对大鼠血管内皮细胞的保护作用和可能的机制。甲氧基甲醚异戊烯基槲皮素(2.5-10 μmol/L)可显著提高H2O2损伤的大鼠血管内皮细胞存活率, 其作用强于槲皮素和维生素E。但在无细胞反应体系甲氧基甲醚异戊烯基槲皮素不显示抗氧化作用。甲氧基甲醚异戊烯基槲皮素(5-10 μmol/L)显著提高H2O2损伤大鼠血管内皮细胞的培养液NO水平和SOD活性, 2.5-10 μmol/L可显著增加培养液中GSH-Px活性, 10μmol/L甲氧基甲醚异戊烯基槲皮素显著降低MDA水平。甲氧基甲醚异戊烯基槲皮素(2.5-10 μmol/L)可以非常明显地减少H2O2诱导的RAECs凋亡率。可见甲氧基甲醚异戊烯基槲皮素的细胞保护作用可能归因于它促进内皮细胞NO释放, 增加细胞内SOD和GSH-Px酶生成, 从而减少脂质过氧化; 抑制细胞凋亡也是它的重要机制之一。该发现提示: 甲氧基甲醚异戊烯基槲皮素有可能成为一个对动脉粥样硬化或其它血管损伤相关疾病有益的抗氧化剂。
Methoxyl methyl ether isoamylene quercetin (MIAQ) is one of the newly synthesized quercetin derivatives. The present study investigated the effect of MIAQ on rat aorta endothelial cells (RAECs) injured by hydrogen peroxide (H2O2), as well as the potential mechanisms. We observed that MIAQ at 2.5-10μmol/L significantly enhanced the viability of injured RAECs, and the effect was more potent than quercetin and ct-tocopherol. However, M1AQ at the same concentration failed to show anti-oxidant activity in a cell-free system. In H2O2-injured endothelial cells treated with MIAQ (5-10μmol/L), the level of nitric oxide (NO) and malondialdehyde was decreased, and the activities of superoxide dismutase and glutathione peroxidase was enhanced. In addition, RAECs treated with MIAQ (2.5-10 μmol/L) exhibited significant inhibiting apoptosis. In conclusion, MIAQ had protective effect on RAECs, possibly through increasing NO production and antioxidases activities, as well as inhibiting apoptosis. These findings suggest that MIAQ is possibly beneficial in the prevention of atherosclerosis and other diseases related to endothelial injury.