期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 222, 期 -, 页码 -出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2021.111508
关键词
Photodynamic therapy; Antitumor; Valproic acid; Platinum diimine complex; Photocytotoxicity; Singlet oxygen
In this study, a novel VPA-modified platinum diimine complex was synthesized, which could efficiently generate singlet oxygen and release VPA in the presence of esterase, potentially significantly enhancing the cytotoxicity of the complex.
Histone deacetylase inhibitors have often been used in combination treatment of various types of cancers due to their non-genotoxic epigenetic potential. Valproic acid (VPA) is a well-known histone deacetylase inhibitor. Conjugate of VPA with a phtoactive platinum diimine complex through an ester bond has been fabricated to potentiate the photocytotoxicity of the photosensitizer. Its capability to generate singlet oxygen, behavior in the presence of esterase, and photocytotoxicity in tumor cells have also been studied. The results revealed that the novel VPA-modified platinum diimine complex could produce singlet oxygen efficiently and release VPA in the presence of porcine liver esterase. The results also suggested that incorporation of VPA moiety into the platinum diimine complex might significantly enhance the cytotoxicity of the complex.
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