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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Platinum (II)-coordinated Portulaca oleracea polysaccharides as metal-drug based polymers for anticancer study
Qianqian Han1, Lirong Huang2, Ying Wang1
1Institute of Environmental Toxicology and Environmental Ecology, Yancheng Teachers University, Yancheng City, Jiangsu Province, 224051, People's Republic of China; Chemistry and Chemical Engineering, Nanjing University of Technology, Nanjing City, Jiangsu Province, 210009, People's Republic of China.
Abstract:
Novel polysaccharide-platinum conjugated polymers bearing alendronate on Portulaca oleracea polysaccharides (PPS) were designed and synthesized. Their chemical structures and properties were characterized by Fourier transform infrared spectroscopy (FT-IR), 1H NMR and 31P NMR spectroscopy, Thermogravimetric analysis (TGA), X-ray powder diffraction (XRD), UV-vis spectrophotometer (UV-vis) and other analysis methods. The results demonstrated that alendronate can be used as the linker of Portulaca oleracea polysaccharides and platinum compounds. Portulaca oleracea polysaccharides-alendronate (PPS-ALN) conjugates exhibited stronger antioxidant ability than PPS. The cytotoxicity assay to cancer cells was tested in vitro, and the Portulaca oleracea polysaccharides-alendronate-platinum (PPS-ALN-Pt) conjugates strongly inhibited the proliferation of cancer cells than PPS and PPS-ALN. The evaluation of complexes affinity toward supercoiled plasmid DNA, displayed a high DNA interaction. Interestingly, the platinum conjugates displayed immunological competence in HeLa cells by cellular immunofluorescence assay. Besides, the cellular platinum accumulation of PPS-ALN-Pt conjugates was higher than that of cisplatin in HeLa cells, implying that the polysaccharide-platinum conjugated polymers might have a synergistically therapeutic application in metal anticancer drug delivery.
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