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Platinum(II)–Gadolinium(III) Complexes as Potential Single‐Molecular Theranostic Agents for Cancer Treatment
Author(s) -
Zhu Zhenzhu,
Wang Xiaoyong,
Li Tuanjie,
Aime Silvio,
Sadler Peter J.,
Guo Zijian
Publication year - 2014
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201407406
Subject(s) - gadolinium , cisplatin , chemistry , platinum , in vivo , cytotoxicity , ligand (biochemistry) , cancer treatment , small molecule , chelation , cancer imaging , combinatorial chemistry , cancer , biophysics , cancer research , in vitro , biochemistry , chemotherapy , medicine , inorganic chemistry , organic chemistry , biology , receptor , microbiology and biotechnology , catalysis , surgery
Theranostic agents are emerging multifunctional molecules capable of simultaneous therapy and diagnosis of diseases. We found that platinum(II)–gadolinium(III) complexes with the formula [{Pt(NH 3 ) 2 Cl} 2 GdL](NO 3 ) 2 possess such properties. The Gd center is stable in solution and the cytoplasm, whereas the Pt centers undergo ligand substitution in cancer cells. The Pt units interact with DNA and significantly promote the cellular uptake of Gd complexes. The cytotoxicity of the Pt–Gd complexes is comparable to that of cisplatin at high concentrations (≥0.1 m M ), and their proton relaxivity is higher than that of the commercial magnetic resonance imaging (MRI) contrast agent Gd–DTPA. T 1 ‐weighted MRI on B6 mice demonstrated that these complexes can reveal the accumulation of platinum drugs in vivo. Their cytotoxicity and imaging capabilities make the Pt–Gd complexes promising theranostic agents for cancer treatment.