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  • 标题:Synthesis of Transferrin-Mitomycin C Conjugate as a Receptor-Mediated Drug Targeting System
  • 本地全文:下载
  • 作者:Tetsuro TANAKA ; Yoshiharu KANEO ; Masahide MIYASHITA
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1996
  • 卷号:19
  • 期号:5
  • 页码:774-777
  • DOI:10.1248/bpb.19.774
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Macromolecular conjugates of mitomycin C (MMC) were sunthesized by binding an active ester of glutarylated MMC (MMC-G-OSu) to human holo-transferrin (TF). Water-soluble TF-MMC conjugates (TF-G-MMC) were obtained in a good yield (>95%) by this method. The MMC content of the conjugate increased (0.82-9.49 MMC/w%) with increasing amounts of MMC-G-OSu added to the conjugation mixture. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) analysis showed no aggregation in these conjugates. 125I-TF-G-MMC was bound specifically to the TF receptor on Sarcoma 180 cells; the measurement of equilibrium binding of the 125I-labeled conjugate resulted in a saturation isotherm. The amount of conjugate specifically bound to the TF receptor decreased as the MMC content of the conjugate increased. However, it was found that the conjugate with an MMC content below 10 mol MMC/mol TF still retains a binding activity of more than half that of TF. Therefore, when an optimal chemical modification was chosen, TF could be used as a tumor specific drug carrier.
  • 关键词:tumor targeting;mitomycin C;transferrin;macromolecular conjugate;receptor binding;sarcoma 180
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