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中文摘要：
以转铁蛋白（Tf）为靶向载体,与双氢青蒿素（DHA）化学偶联制备一种新的双氢青蒿素衍生物-转铁蛋白靶向药物。以DHA为原料先合成了12β-对甲酰肼苯基双氢青蒿素（DBAH）,并采用紫外、红外、核磁共振及电化学等手段对目标产物的结构进行了表征。利用高碘酸钠氧化Tf的C端的N-糖链上的邻位羟基,其氧化产物和DBAH通过希夫碱偶联合成了DBAH-Tf靶向药物,采用紫外吸收光谱法和电化学方法进行表征。四甲基氮唑蓝法（MTT）分析了DBAH-Tf及DHA对人乳腺癌细胞（MCF-7）和正常乳腺细胞的体外杀伤作用,结果表明,DBAH-Tf对MCF-7的杀伤作用是正常乳腺癌细胞的286倍,体现出良好的靶向性。
英文摘要：
As target-carrier, transferrin（Tf） was conjugated with dihydroartemisinin （DHA） to form a new targeted drug. An analog of artemisinin, 4-（12-dihydroartemisininoxy） benzoic acid hydrazide （DBAH） have been synthesized and characterized by UV/vis absorption spectroscopy, IR spectroscopy, NMR, electroanalytic chemistry. Periodate was used to oxidize hydroxide group on the N-glycoside chains of C-domain, and then DBAH was reacted with the oxidized transferrin to form a covalent conjugate. In addition, this targeted drug was characterized by ultraviolet spectroscopy and electroanalytic chemistry. Methyl thiazolyl tetrazolium （MTT） assay was used to evaluate the killing effect of DBAH-Tf on MCF-7 and human normal breast cells. The results showed that DBAH-Tf was 286 times more potent in killing MCF-7 cancer cells than normal cells, which implied that DBAH-Tf could target to cancer cells.
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