title: Synthesis, characterization and biological evaluation of mixed-ligand ruthenium(II) complexes for photodynamic therapy.
abstract: This study investigated the photodynamic therapy (PDT) and anticancer activity of mixed ligand Ru(ii) terpyridyl complexes (Ru1-Ru3). The photophysical and photochemical properties, hydrophobic properties, DNA binding and DNA transcription inhibition abilities, cell uptake efficiency, cellular localization and photo-cytotoxicity were investigated. Ru1-Ru3 exhibited red luminescence between 670-710 nm and functioned as photo-sensitizers (PSs) by generating both singlet oxygen and radical ions. Without light activation, Ru1-Ru3 were located at the cytoplasm and were nontoxic to cells. However, upon light activation, Ru1-Ru3 exhibited significant photocytotoxicity. After PDT treatment, mitochondria alteration and nuclear membrane disruption occurred, which resulted in relocalization of the complexes from the cytoplasm to the nucleus. Moreover, high cellular oxidative stress caused cell necrocytosis after PDT treatment.
authors.affiliation: MOE Key Laboratory of Bioinorganic and Synthetic Chemistry, School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, P. R. China. cesjln@mail.sysu.edu.cn ceschh@mail.sysu.edu.cn.
authors.forename: Huaiyi
authors.initials: H
authors.lastname: Huang
authors.forename: Pingyu
authors.initials: P
authors.lastname: Zhang
authors.forename: Bole
authors.initials: B
authors.lastname: Yu
authors.forename: Chengzhi
authors.initials: C
authors.lastname: Jin
authors.forename: Liangnian
authors.initials: L
authors.lastname: Ji
authors.forename: Hui
authors.initials: H
authors.lastname: Chao
mesh_terms: D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000494:pharmacology; D004268:DNA-Binding Proteins / Q000378:metabolism; D004353:Drug Evaluation, Preclinical / Q000379:methods; D056945:Hep G2 Cells; D006801:Humans; D008024:Ligands; D010778:Photochemotherapy / Q000379:methods*; D017319:Photosensitizing Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D012428:Ruthenium / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D056831:Coordination Complexes; D004268:DNA-Binding Proteins; D008024:Ligands; D017319:Photosensitizing Agents; D012428:Ruthenium