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.
Keywords: chlorin.; photodynamic therapy; photosensitizer; tumor.