米托蒽醌-胰岛素偶联物的制备

Synthesis of mitoxantrone-insulin conjugates

目的 探讨以胰岛素为抗癌药物导向载体的米托蒽醌 -胰岛素偶联物的合成方法。方法 直接偶联以及通过间隔基连接米托蒽醌和胰岛素。结果 中间产物及偶联产物经1HNMR、IR、MS、HPLC等确证。结论 直接偶联产物的溶解性不好 ,通过间隔基连接的偶联产物溶解性良好。

OBJECTIVE To synthesize mitoxantrone-insulin conjugates through covalent bond,where mitoxantrone will be an anticancer model drug and insulin acted as a vector.METHODS To direct coupling,spacer was used to join insulin and mitoxantrone.RESULTS The intermediate and final conjugates were characterized by IR, 1HNMR,MS and HPLC.CONCLUSION Compared with the direct coupling product,the product by using a spacer has better solubility.