Interest of RGD-containing linear or cyclic peptide targeted tetraphenylchlorin as novel photosensitizers for selective photodynamic activity.

摘要: Destruction of the neovasculature is essential for tumor eradication by photodynamic therapy. Since over-expression integrins correlated with angiogenesis, we conjugated a photosensitizer (5-(4-carboxyphenyl)-10,15,20-triphenylchlorin or porphyrin) to αvβ3 integrin specific peptide RGD (H-Arg-Gly-Asp-OH) motif as common sequence. We reported an efficient solid-phase synthesis new family peptidic photosensitizers linear cyclic[RGDfK] and compared conjugates in vitro selectivity activity. The were characterized 1H NMR, MALDI, UV–visible spectroscopy singlet oxygen formation was performed. Chlorins containing constrained incorporated up 98- 80-fold more, respectively, than unconjugated over 24-h exposure human umbilical vein endothelial cells (HUVEC) over-expressing integrin. Peptidic moiety also led non-specific increased cellular uptake murine mammary carcinoma (EMT-6), lacking binding receptors. Survival measurements demonstrated that HUVEC greatly sensitive conjugates-mediated