title: Comparative studies of the cellular uptake, subcellular localization, and cytotoxic and phototoxic antitumor properties of ruthenium(II)-porphyrin conjugates with different linkers.
abstract: Six water-soluble free-base porphyrin-Ru(II) conjugates, 1-3, and Zn(II) porphyrin-Ru(II) conjugates, 4-6, with different linkers between the hydrophobic porphyrin moiety and the hydrophilic Ru(II)-polypyridyl complex, have been synthesized. The linear and two-photon-induced photophysical properties of these conjugates were measured and evaluated for their potential application as dual in vitro imaging and photodynamic therapeutic (PDT) agents. Conjugates 1-3, with their high luminescence and singlet oxygen quantum yields, were selected for further study of their cellular uptake, subcellular localization, and cytotoxic and photocytotoxic (under linear and two-photon excitation) properties using HeLa cells. Conjugate 2, with its hydrophobic phenylethynyl linker, was shown to be highly promising for further development as a bifunctional probe for two-photon (NIR) induced PDT and in vitro imaging. Cellular uptake and subcellular localization properties were shown to be crucial to its PDT efficacy.
authors: Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong SAR.
authors: Jing-Xiang
authors: JX
authors: Zhang
authors: Jun-Wei
authors: JW
authors: Zhou
authors: Chi-Fai
authors: CF
authors: Chan
authors: Terrence Chi-Kong
authors: TC
authors: Lau
authors: Daniel W J
authors: DW
authors: Kwong
authors: Hoi-Lam
authors: HL
authors: Tam
authors: Nai-Ki
authors: NK
authors: Mak
authors: Ka-Leung
authors: KL
authors: Wong
authors: Wai-Kwok
authors: WK
authors: Wong
mesh_terms: D000042:Absorption; D000970:Antineoplastic Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D001692:Biological Transport; D006367:HeLa Cells; D006801:Humans; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D042541:Intracellular Space / Q000378:metabolism*; D008665:Metalloporphyrins / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D057054:Molecular Imaging; D017319:Photosensitizing Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D012428:Ruthenium / Q000737:chemistry*; D014867:Water / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D008665:Metalloporphyrins; D017319:Photosensitizing Agents; D014867:Water; D012428:Ruthenium