天然产物研究与开发 ›› 2020, Vol. 32 ›› Issue (4): 627-632.doi: 10.16333/j.1001-6880.2020.4.012

• 研究简报 • 上一篇    下一篇

人参二醇酰化产物的合成及其对大鼠离体胸主动脉的影响

周金娜,张荣平,邹澄*,杨为民,段文越,陈晨,胡建林


  

  1. 昆明医科大学药学院暨云南省天然药物药理重点实验室,昆明 650500

  • 出版日期:2020-04-28 发布日期:2020-06-05
  • 基金资助:
    云南省科技厅-昆明医科大学应用基础研究联合专项重点基金资助项目(2017FE468(-001));NSFC-云南联合基金(U1502226)

Synthesis of panaxadiol acylated products and its effect on isolated rat thoracic aorta

ZHOU Jin-na,ZHANG Rong-ping,ZOU Cheng*,YANG Wei-min,DUAN Wen-yue,CHEN Chen,HU Jian-lin#br#

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  1. School of Pharmaceutical Sciences & Yunnan Key Laboratory of Pharmacology for Natural Products,Kunming Medical University,Kunming 650500,China

  • Online:2020-04-28 Published:2020-06-05

摘要:

本研究旨在探究人参二醇的酰化反应,制备其衍生物,并评价所制备的人参二醇酰化物对SD大鼠离体胸主动脉的舒张活性,通过对人参二醇皂苷3位-羟基基团进行结构改造,与酰氯试剂反应制备其衍生物,采用核磁共振对其结构进行鉴定后,利用Wire Myograph System DMT血管张力测定仪测定其舒张大鼠胸主动脉活性,结果显示所制备的10个人参二醇酰化衍生物均为新化合物,其中化合物PD-3、4、7、9、10具有显著的舒张胸主动脉活性,这些化合物值得进一步深入研究。

关键词: 人参二醇, 衍生物, 酰化反应, 三七, 胸主动脉

Abstract:

The purpose of this study was to explore the acylation of panaxadiol,prepare its derivatives,and evaluated the relaxation activity of the prepared panaxadiol acylates on the isolated thoracic aorta of SD rats.The 3-hydroxyl group of panaxadiol saponins was modified and reacted with acyl chloride reagent to prepare its derivatives.After its structure was identified by nuclear magnetic resonance(NMR),the relaxing activity of rat thoracic aorta was determined by Wire Myograph System DMT vascular tension tester.The results showed that the 10 acylated derivatives of panaxadiol were new compounds,among which compounds PD-3,4,7,9 and 10 had significant relaxing activity of thoracic aorta,which were worthy of further study.

Key words: panaxadiol, derivatives, acylation, notoginseng, thoracic aorta

中图分类号:  R284.3 R965.1