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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
【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.
【Key words】 Stereoselective reduction; 8,12,13,17-Tetrahydroandrographolide; Crystal structure; Glucosidase; Inhibitory activity;
- 【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