Effect of 4-(12-Dihydroartemisininoxy) Benzoic Acid hydrazide Transferrin Tagged Drug on Human Breast Cancer Cells

As target-carrier, holotransferrin (Tf) was conjugated with dihydroartemisinin (DHA) to form a new targeted drug. An analog of DHA, 4-(12-dihydroartemisininoxy) benzoic acid hydrazide (DBAH) have been synthesized and characterized by UV/vis spectroscopy, IR spectroscopy, NMR, and electrochemistry. Periodate was used to oxidize hydroxy groups on the N-glycoside chains of C-domain on Tf surface, and then DBAH reacted with the oxidized Tf to form a covalent conjugate. In addition, this targeted drug was characterized by UV/vis spectroscopy and electrochemistry. 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 cells than normal cells, which implied that DBAH-Tf could target the cancer cells.