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葛根素衍生物的合成及其对心肌缺血再灌注损伤的保护作用。

The synthesis of puerarin derivatives and their protective effect on the myocardial ischemia and reperfusion injury.

作者信息

Feng Zhi-Qiang, Wang Ying-Yu, Guo Zong-Ru, Chu Feng-Ming, Sun Piao-Yang

机构信息

Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education & Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.

出版信息

J Asian Nat Prod Res. 2010 Oct;12(10):843-50. doi: 10.1080/10286020.2010.505563.

Abstract

Puerarin is a naturally occurring isoflavone and is frequently used for the treatment of cardiovascular symptoms in China. By the structural modification of the puerarin molecule at different positions, seven new puerarin derivatives were obtained, and their cardioprotective activities (in vitro and in vivo) were respectively evaluated. The finding that the activities of 3 and 8 markedly exceeded puerarin suggested that the acylated modification of phenolic hydroxyl at C-7 in the puerarin molecule may improve the cardioprotective activity, which will be an important reference for further structural optimization.

摘要

葛根素是一种天然存在的异黄酮,在中国常用于治疗心血管症状。通过在不同位置对葛根素分子进行结构修饰,获得了七种新的葛根素衍生物,并分别评估了它们的心脏保护活性(体外和体内)。3号和8号衍生物的活性明显超过葛根素这一发现表明,葛根素分子中C-7位酚羟基的酰化修饰可能会提高心脏保护活性,这将为进一步的结构优化提供重要参考。

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