Development of Glycoconjugated Porphyrin Derivatives for Photodynamic Therapy

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1.Novel Synthetic Strategy for Glycoconjuated Porphyrin DerivativesIn order to improve the yield of glycoconjugated porphyrin derivatives, especially for meta-substituted tetraphenyl porphyrin, Zn2+ ion template methodology had been developed. In addition, demonstrate the RP-TLC purification of glycoconjugated chlorin derivatives to remove concomitant by-product, glycoconjugated porphyrin and bacteriochlorin derivatives. So now glycoconjugated porphyrin and chlorin derivatives can be produced in applicable scale and purity in photodynamic therapy.2.Estimation of Hydrophobicity of Glycoconjugated Porphyrin DerivativesHyrophobicity is fundamental characteristic for pharmakokinetics. We demonstrated the estimation of hydrophobicity of glycoconjugated porphyrin derivatives by means of reversed phase HPLC method. Significant sugedependent hydrophobicity was found clearly.3.Cellular Uptake of Glycoconjugated Porphyrin Derivatives by HeLa cellsPrior to in vitro photocytotoxicity test, the cellular uptake amount of glycoconjugated porphyrin derivatives by HeLa cells was determined by means of fluorometry. The uptake amount significantly depended on sugar unit attached, However, no apprent correlation between hydrophobicity and cellular uptake was found.4.In vitro Photocytotoxicity Test for Glycoconjugated Porphyrin DerivativesPreliminary in vitro photocytotoxicity test was performed for glycoconjugated porphyrin derivatives which exerted higher amount of cellular uptake. Even though the photocytotoxicity was not connected to the cellular uptake amount, photocytotoxicity highly depended on sugar unit attached. These results suggest the possibility of glyco-regulation of photocytotoxicity in PDT.