title: Photodynamic effects of a novel pterin derivative on a pancreatic cancer cell line.
abstract: 6-Formylpterin (6FP) has the potential to produce singlet oxygen (1O2) under UV-A radiation. In order to apply this potential to anti-cancer photodynamic therapy (PDT), we prepared a novel variant of 6FP, 2-(N,N-dimethylaminomethyleneamino)-6-formyl-3-pivaloylpteridine-4-one (6FP-tBu-DMF), and examined its photodynamic effects on a pancreatic cancer cell line, Panc-1 cells. The study using laser scanning confocal microscopy showed that the drug uptake, the 1O2 generation, and cell death were observed in the 6FP-tBu-DMF-treated cells, while these phenomena were not observed in the 6FP-treated cells. The MTT assay also showed the decrease in cell viability only in the 6FP-tBu-DMF-treated cells. Since 6FP and 6FP-tBu-DMF generate 1O2 to the same extent under UV-A radiation in aqueous solutions, these results indicated that the differences in the photodynamic effects between 6FP and 6FP-tBu-DMF were entirely attributed to the differences in the cell permeability between them. The development of cell permeable pterin derivatives has the potential for application in PDT.
authors.affiliation: Department of Hematology and Oncology, Kyoto University Hospital, Kyoto 606-8507, Japan.
authors.forename: Hiroko
authors.initials: H
authors.lastname: Yamada
authors.forename: Toshiyuki
authors.initials: T
authors.lastname: Arai
authors.forename: Nobuyuki
authors.initials: N
authors.lastname: Endo
authors.forename: Kouhei
authors.initials: K
authors.lastname: Yamashita
authors.forename: Mitsuru
authors.initials: M
authors.lastname: Nonogawa
authors.forename: Keisuke
authors.initials: K
authors.lastname: Makino
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Fukuda
authors.forename: Masataka
authors.initials: M
authors.lastname: Sasada
authors.forename: Takashi
authors.initials: T
authors.lastname: Uchiyama
mesh_terms: D045744:Cell Line, Tumor; D004578:Electron Spin Resonance Spectroscopy; D006801:Humans; D018613:Microscopy, Confocal; D010190:Pancreatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D010778:Photochemotherapy; D011621:Pteridines / Q000627:therapeutic use*
chemical_list: C504029:2-(N,N-dimethylaminomethyleneamino)-6-formyl-3-pivaloylpteridin-4-one; D011621:Pteridines