2004 Fiscal Year Final Research Report Summary
Development of Glycoconjugated Porphyrin Derivatives for Photodynamic Therapy
| Project/Area Number |
13557211
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (B)
|
| Allocation Type | Single-year Grants |
|---|
| Section | 展開研究 |
|---|
| Research Field |
医薬分子機能学
|
|---|
| Research Institution | Nara Women's University |
|---|
Principal Investigator |
YANO Shiganobu Nara Women's University, Grad.Sch.of Human Culture, Professor, 大学院・人間文化研究科, 教授 (60011186)
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
覚知 豊次 北海道大学, 大学院・工学研究科, 教授 (80113538)
KAKUCHI Toyoji Hokkaido Univ., Grad.Scho.of Engineering, Professor, 大学院・工学研究科, 教授 (80113538)
KINOSHITA Isamu Osaka City Univ., Grad.Scho.of Science, Professor, 大学院・理学研究科, 教授 (80128735)
FUJIOKA Kenji Formulation Research Lab., Sumitomo Pharmaceutical Research Div., Research Director, 製剤技術研究所, 研究所所長
|
|---|
| Project Period (FY) |
2001 – 2004
|
| Keywords | Sugar / Photosensitizer / Photodynamic Therapy |
|---|
| Research Abstract |
1.Novel Synthetic Strategy for Glycoconjuated Porphyrin Derivatives
In 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 Derivatives
Hyrophobicity 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 cells
Prior 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 Derivatives
Preliminary 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.
|
