Synthesis and Pharmacological Activities of a Quercetin Derivative
- VernacularTitle:槲皮苷衍生物的合成及药理作用研究
- Author:
Xiaoping TANG
;
Zhelong MA
;
Ningchuan SHI
;
Zhishan DING
;
Fusheng JIANG
- Publication Type:Journal Article
- Keywords:
Quercetin;
Synthesis;
Pharmacological activities
- From:
China Pharmacist
2016;19(2):251-254
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To preliminarily explore the synthesis of a quercetin derivative 3′,4′,5,7-four-(O-methoxy carbonyl meth-yl) quercetin and its pharmacological activities. Methods:Quercetin as the reactant and N,N-dimethyl-formamide ( DMF) as the sol-vent, the target product 3′,4′,5,7-four-(O-methoxy carbonyl methyl) quercetin was obtained by the slow addition of methyl chloroace-tate in the presence of anhydrous K2 CO3 to introduce ether bond at 3′,4′,5,7- bit. The structure was characterized by LC-MS, 1 H-NMR and element analysis. The nanoemulsion of the product was prepared using a film dispersion method, and with intraperitoneal in-jection, the effect on pituitrin-induced myocardial ischemia cardiovascular system in rats was observed. Results:3′,4′,5,7-Four-(O-methoxy carbonyl methyl) quercetin was successfully synthesized, and could be metastasized to a demethylation product containing dis-tal free carboxyl with increased polarity proved by metabolic tests in vitro. The results of electrocardiogram and animal experiments showed that the compound had improving effects on pituitrin-induced myocardial ischemia in rats. Conclusion: The nanoemulsion of 3′,4′,5,7-four-(O-methoxy carbonyl methyl) quercetin with intraperitoneal injection shows significant antagonism against pituitrin-in-duced myocardial ischemia in rats.
