In vitro and in vivo antitumor activity of anovel chlorin derivative for photodynamic therapy.

Abstract

In presented paper, anew chlorin derivative 5,10,15,20-tetrakis[(5-N-morpholino)pentyl] chlorin (TMC) was investigated as aphotosensitizer 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 aconfocal 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. Afast clearance rate of TMC was observed in Eca-109-bearing mice. In particular, TMC could significantly inhibit the tumor growth and exhibit anotable antitumor efficacy for PDT in vivo.