AI Article Synopsis
- A series of carbohydrate-conjugated platinum(IV) complexes were developed based on cisplatin and oxaliplatin, showing dual pH and redox responsiveness.
- The new compounds exhibited greater cytotoxic effects against various human cancer cell lines while being less toxic to normal cells compared to existing drugs like cisplatin and oxaliplatin.
- In vivo tests confirmed that these platinum(IV) compounds effectively inhibited tumor growth with better safety profiles than oxaliplatin.
Article Abstract
A serious of carbohydrate-conjugated platinum(IV) complexes in the form Pt(L2)(A2)(OH)R based on the clinical drug cisplatin and oxaliplatin were designed, synthesized and evaluated as antitumor agents in vitro and in vivo. The conjugates possessing both pH and redox dual-responsive properties exhibited more potent cytotoxicity in seven different human cancer cell lines and lower toxicity to the normal 3T3 cells than cisplatin, oxaliplatin and even the reported bis-functionalized glycosylated platinum(IV) complexes indicating the enhanced safety of the sugar conjugates. Cellular drug uptake and DNA platination were also superior to cisplatin, oxaliplatin and the reported bis-functionalized ones. Peak current of B7 and B8 with the scan rate of 200mv/s at the concentration of 0.08 mM was 5-fold higher at pH 6.4 than the pH 7.4, indicating that carbohydrate-conjugated mono-functionalized platinum(IV) complexes possessed both pH and redox dual-responsive properties in the cancer cells. The in vivo assays demonstrated that the Pt(IV) compounds could inhibit the growth of MCF-7 tumour and exert more safety than oxaliplatin.
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| http://dx.doi.org/10.1016/j.ejmech.2017.01.032 | DOI Listing |
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