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(8R,13R)-8,12,13,17-四氢穿心莲内酯的合成、晶体结构和葡萄糖苷酶抑制活性

Synthesis,Crystal Structure and Glucosidase Inhibitory Activities of (8R,13R)-8,12,13,17-Tetrahydroandrographolide

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【作者】 黄利华徐海伟刘改芝戴桂馥刘宏民

【Author】 HUANG Li-Hua,XU Hai-Wei,LIU Gai-Zhi,DAI Gui-Fu,LIU Hong-Min(New Drug Research & Development Center,Zhengzhou University,Zhengzhou 450052,China)

【机构】 郑州大学化学系郑州大学药学院郑州大学新药研究开发中心郑州大学化学系 郑州大学新药研究开发中心郑州450052郑州大学药学院 郑州大学新药研究开发中心

【Abstract】 Some glucosidase inhibitors show antitumor metastasis and anti-HIV activities and are also clinically useful for the treatment of diabetes,besides andrographolide derivative have been proven to be potent an α-glucosidase inhibitor.In order to investigate the double effect of glucosidase inhibition activity,a new diterpene lactone derivative 2 was synthesized via reduction of compound 1 which was one of the constitutions of Andrographis Pamicutate(Brum) Nees.The structure of compound 2 was confirmed with X-ray diffraction analysis,NMR,IR,HR-MS and so on.Compound 2 shows a selective α-glucosidase inhibitory activity with inhibition of 49.6% at 100 μmol/L,and the mother 1 has no inhibition activity(100 μmol/L).The results indicate that the double bond can affect the α-glucosidase inhibition activity of andrographolide.

【基金】 国家自然科学基金(批准号:20472075)资助
  • 【文献出处】 高等学校化学学报 ,Chemical Journal of Chinese Universities , 编辑部邮箱 ,2007年07期
  • 【分类号】R284
  • 【被引频次】2
  • 【下载频次】341
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