Glucose-modification of cisplatin to facilitate cellular uptake, mitigate toxicity to normal cells, and improve anti-cancer effect in cancer cells

Cisplatin has been considered an effective anticancer drug clinically. However, drug resistance and side effects of toxicity on normal cells greatly diminish the anti-cancer outcome of cisplatin. In this study, glucose modification was conducted to improve cisplatin anti-cancer efficacy. Firstly, cisplatin was oxidized to c,c,t-[Pt(NH3)2Cl2(OH)2] and then a carboxyl group was introduced to obtain c,c,t-[Pt(NH3)2Cl2(OOCCH2CH2COOH)2] (Pt(IV)–COOH), and finally glucose was grafted onto Pt(IV)–COOH. The glucose modification of cisplatin opens the glucose transport channels (GTC) on the cell membrane for Pt drug. The opening of GTC increases the uptake of Pt drug for cells. This simple and effective modification strategy may not only mitigate toxicity to normal cells, but also increase the anti-cancer effect of Pt drugs.