title: In vitro and in vivo antitumor activity of a novel chlorin derivative for photodynamic therapy.
abstract: In presented paper, a new chlorin derivative 5,10,15,20-tetrakis[(5-N-morpholino)pentyl] chlorin (TMC) was investigated as a photosensitizer in photodynamic therapy (PDT). Cellular uptake, cytotoxicity, intracellular location, biodistribution and antitumor effects were studied using human esophageal cancer cells (Eca-109) and human cervical cancer cells (Hela) in vitro and an esophageal cancer model in BALB/c nude mice. Cellular uptake and biodistribution of TMC were measured by fluorescence spectrophotometer. Cytotoxicity of TMC against Eca-109 and Hela cells was determined by MTT assay. The intracellular location of TMC was detected with a confocal microscopy. It was showed that TMC could rapidly accumulate in tumor cells and localize in cytoplasm. TMC was found to be low-toxic in dark but extensively photosensitive in vitro. A fast clearance rate of TMC was observed in Eca-109-bearing mice. In particular, TMC could significantly inhibit the tumor growth and exhibit a notable antitumor efficacy for PDT in vivo.
authors.forename: C Y
authors.initials: CY
authors.lastname: Zhang
authors.forename: L J
authors.initials: LJ
authors.lastname: Zhang
authors.forename: J W
authors.initials: JW
authors.lastname: Li
authors.forename: J H
authors.initials: JH
authors.lastname: Li
authors.forename: Z M
authors.initials: ZM
authors.lastname: Wu
authors.forename: L X
authors.initials: LX
authors.lastname: Zhang
authors.forename: N
authors.initials: N
authors.lastname: Chen
authors.forename: Y J
authors.initials: YJ
authors.lastname: Yan
authors.forename: Z L
authors.initials: ZL
authors.lastname: Chen
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D004938:Esophageal Neoplasms / Q000188:drug therapy*; D005260:Female; D006367:HeLa Cells; D006801:Humans; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000494:pharmacology*; D011166:Porphyrins / Q000737:chemistry / Q000494:pharmacology*; D014018:Tissue Distribution; D002583:Uterine Cervical Neoplasms / Q000188:drug therapy*
chemical_list: D017319:Photosensitizing Agents; D011166:Porphyrins; C006969:chlorin
keywords: chlorin.; photodynamic therapy; photosensitizer; tumor