(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

设计并合成了新的具有旋光活性的二萜类内酯衍生物2, 并通过NMR, IR, HRMS和X射线单晶衍射等技术分析了其结构和绝对构型.

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

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.