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目的:初步探讨槲皮苷衍生物3’,4’,5,7-四-(O-甲氧羰甲基)槲皮苷的合成及对心肌缺血的作用。方法:以槲皮苷为原料,N,N-二甲基甲酰胺(DMF)为溶剂,在无水碳酸钾存在下,缓慢滴加氯乙酸甲酯,在3’、4’、5、7位引入醚键,预得到目标产物3’,4’,5,7-四-(O-甲氧羰甲基)槲皮苷。化合物结构经LC-MS、~1H-NMR进行了表征。利用薄膜分散法将产物3’,4’,5,7-四-(O-甲氧羰甲基)槲皮苷制成纳米乳,通过腹腔注射给药,观察其对垂体后叶素诱导的心肌缺血大鼠心血管系统的作用。结果:合成了3’,4’,5,7-四-(O-甲氧羰甲基)槲皮苷,体外代谢试验证明该产物大部分被代谢为末端游离羧基的去甲基产物,极性明显增大。心电图及动物试验结果显示产物对垂体后叶素致心肌缺血大鼠有一定的抗心肌缺血作用。结论:3’,4’,5,7-四-(O-甲氧羰甲基)槲皮苷制成纳米乳腹腔注射对静脉注射垂体后叶素的心肌缺血模型大鼠有明显的对抗作用。
Objective: To investigate the synthesis of quercetin derivative 3 ’, 4’, 5,7-tetrakis (O-methoxycarbonylmethyl) quercetin and its effect on myocardial ischemia. Methods: Quercitrin was used as raw material and N, N-dimethylformamide (DMF) was used as the solvent. Methyl chloroacetate was slowly added dropwise in the presence of anhydrous potassium carbonate. After 3 ’, 4’, 5,7 Position to introduce the target product 3 ’, 4’, 5,7-tetra- (O-methoxycarbonylmethyl) quercitrin. The structures of the compounds were characterized by LC-MS and ~ 1H-NMR. The product 3 ’, 4’, 5,7-tetrakis- (O-methoxycarbonylmethyl) quercitrin was made into nanoemulsion by the film dispersion method and was administered by intraperitoneal injection to observe its effect on vasopressin-induced Cardiovascular system in rats with myocardial ischemia. Results: The 3 ’, 4’, 5,7-tetrakis- (O-methoxycarbonylmethyl) quercitrin was synthesized. Metabolism tests in vitro showed that most of the product was metabolized to the demethylated product of terminal free carboxylate. Sex is obviously increased. ECG and animal test results show that the product of pituitrin-induced myocardial ischemia in rats have a certain role in anti-myocardial ischemia. Conclusion: Nano-milk intraperitoneally injected with 3 ’, 4’, 5,7-tetrakis- (O-methoxycarbonylmethyl) quercitrin has obvious antagonism to intraventricular injection of vasopressin in myocardial ischemia model rats effect.