This invention is in the field of bio-pharmaceutical technology, specifically involving the new derivatives of puerarin, the biological conversion methods and their pharmaceutical applications. This invention published a new type fructosylated puerarin with structure as shown in Formula (I) below, its preparation method being converting puerarin into fructosyl and fructose oligosaccharyl puerarin in a aqueous phase or nonaqueous phase system by bioconversion method, and at a puerarin concentration of 107.5g/L, the monofructosyl-² (2,6)-puerarin concentration can reach 111.7g/L, and conversion rate of fructosylated puerarin is 90%. By adsorption with AB-8 macroporous resin and gradient elution, product with purity over 97% and complying drug specification can be obtained, with extraction rate over 80%. Tests have shown that fructosylated puerarin is effective to acute myocardio ischemia, and can markedly suppress in vitro the proliferation of human breast cancer cell strain MDA-MB-23 and human chronmyelogenors leukemia cell strain K562, and such oligosaccharylated puerarin has low toxicity, with good application prospects in making drugs to treat cardio-cerebral vascular diseases and/or tumour diseases.式（Ｉ）で表される新規なフルクトシル化プエラリンおよびその製造方法、並びに脳心血管疾病および／または癌関連疾病の治療用薬物の製造における使用。式（Ｉ）中、Ｒ１とＲ２はそれぞれ独立して水素、メチル基、エチル基、ホルミル基、アセチル基、メチルアミノ基及び硫酸基から選択され、Ｒはフルクトースモノグリコシルまたは２～５のフルクトースが接続したオリゴサッカリルである。フルクトシル基化プエラリンの製造方法は、水系または非水系におけるプエラリンからフルクトシル化プエラリンおよびオリゴサッカリルプエラリンへの生物学的変換を含む。【化１】
