橙皮苷半合成香叶木苷及抑癌作用研究

Semi-synthesis of Diosmin from Hesperidin and Anticancer Effect

摘要:

本文首次研究了一种半合成香叶木苷的化学方法，并测定该合成产物对六种常见癌细胞的抗增殖活性。该方法以廉价的橙皮苷为原料，用DDQ作脱氢剂，氧化制备香叶木苷。经sephadex LH-20柱纯化后，HPLC-MS与1H-NMR鉴定确定该产物为香叶木苷，首次证实该转化方法对于黄酮苷类物质的合成是可行的。优化所得合成工艺为：原料质量比为1:0.4，反应温度为110℃（油浴温度），反应时间为6小时。本实验的研究结果为香叶木苷的合成与应用提供新的途径。

Abstract:

A new semi-synthesis method for flavonoid glycosides diosmin was performed. And the antiproliferative activity of the diosmin sample against six common cancer cells was determined. Diosmin was prepared from available and inexpensive hesperidin using DDQ as the dehydrogenating agent. After purified through the Sephadex LH-20 column, diosmin was identified by HPLC-MS and 1H-NMR. It was confirmed that the transformation method is feasible for the synthesis of flavonoid glycosides. The final synthesis process is: raw material ratio 1:0.4, reaction temperature 110℃ (oil bath temperature), and reaction time 6 hours. The results of this study will provide a new idea for the synthesis and application of diosmin.