Synthesis and properties of cell-targeted Zn(II)-phthalocyanine-peptide conjugates.

摘要: Two Zn−Pc−peptide conjugates bearing either a short linker or long PEG−linker between the macrocycle and bifunctional peptide containing nucleoplasmin HIV-1 Tat 48−60 sequences have been synthesized in order to increase Pc cell-targeting ability evaluate effect of linker. The presence chain increased water solubility and, consequently, its fluorescence aqueous solutions. highest quantum yields were observed at low pH (5.0) for both always higher conjugate Both found dark cytotoxicity toward human HEp2 cells (IC50 > 77 μM) but highly phototoxic < 2 μM 1 J cm-2). accumulated most within (26 times more than unconjugated Zn−Pc), followed by (17 Zn−Pc). localized preferentially withi...