靶向多肽偶联酞菁锌光敏剂的制备及生物学评价

In recent decades, photodynamic therapy has been rapid developed. In the process of photodynamic therapy, photosensitizer plays a vital role. Here we reported our synthestic studies and activitiy test of two new peptide conjugates zinc phthalocyanine photosensitizers for targeted cancer ohotodynamic therapy, Synthesis asymmetric phthalocyanine PCZN2 by introducing glycol structure and asymmetric phthalocyanine PCZN5 by introducing a hydrophilic group hydroxyl. By introducing hydrophilic functional groups, it can greatly increase the solubility of phthalocyanine. The two highly soluble phthalocyanine PCZN2 and phthalocyanine PCZN5By were conjugated to EGFR targeting peptide D4 on resin through solid phase synthesis, which solve the problem of separation and purification about phthalocyanine coupled. Optical experiments show the product has a high quantum yield and singlet oxygen yield. The maximum absorption wavelength is at 685nm with good penetration depth. Cytotoxicity test (MTT) showed targeting peptide conjugate phthalocyanine PCZN3 and PCZN6 are toxic selectively to tumor cells. Confocal microscopic experiments showsed they are able to be selectively recognized by tumor cells. In vivo imaging show both materials PCZN3 and PCZN6 are able to concentrate in tumors in mice with strong targeting. These new targeting photosensitizers show good potential for cancer photodynamic therapy.