Journal Article <論文・報告>抗菌ペプチドを用いた薬物送達システムの開発

黒田, 逸月  ,  高橋, 有己

1pp.54 - 57 , 2016-03 , 京都大学学際融合教育研究推進センター高大接続科学教育ユニット
Cell membrane permeability is one of the obstacles that must be overcome during drug development. In the present study, antimicrobial peptides that increase cell membrane permeability were used to overcome this obstacle. In particular, melittin, indolicidin, magainin, and dermcidin were selected. Evaluation of membrane permeability enhancement by calcein-encapsulated liposomes suggested that melittin and indolicidin increase membrane permeability. Therefore, we designed the novel peptides melittinR8, or mellitin fused with R8, and indolicidinRGD, or indolicidin fused with RGD. Evaluation of membrane permeability enhancement by using calcein-encapsulated liposomes and 8 different cell types showed that mellitinR8 exhibits the greatest permeability enhancement among the antimicrobial peptides tested. By using FITC-DNA and FITC-Dextran as model drugs, the enhancement of drug delivery into cells by melittinR8 was evaluated. As a result, high membrane permeability enhancement was observed in the case of delivering FITC-DNA into cancer cells. These results indicate that melittinR8 can be a tool to facilitate the delivery of DNA into cancer cells.

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