葛根素乙酰化衍生物的合成和生物利用度研究

Research on Synthesis and Bioavailability of Puerarin Acetyl Derivatives

本文利用乙酸酐和葛根素反应制备葛根素全乙酰化产物，经碳酸氢钠溶液进行不完全水解，用硅胶层析法对水解产物进行分离，通过紫外、红外、核磁共振和质谱等方法对产物进行鉴定，测定其口服生物利用度。获得四乙酰、五乙酰和六乙酰葛根素，口服生物利用度分别为葛根素的2．24，1．67和1．15倍。结果表明葛根素乙酰化衍生物的口服生物利用度高于葛根素，其中四乙酰葛根素口服生物利用度最高。

To probe into the method of improving oral bioavailability of Puerarin. Prepare the Puerarin derivatives through the way of synthesizing Puerarin and acetic anhydride, and then hydrolyze with liquor of sodium bicarbonate incompletely. Separate the hydrolysate by column chromatography. Confirm the structures of the derivatives by UV, IR, NMR and MS, and measure their bioavailability. The oral bioavailability of the three new resultant derivatives, as tetra-acetyl, pentaacetyl,and hexa-acetyl,is 2.24,1.67 and 1.15 times than Puerarin respectively. There are improvements in oral bioavailability of Puerarin acetylated derivatives, in which tetra-acetyl is the best.