オリゴアルギニンペプチドの細胞内移行におけるTrp 残基導入の影響

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  • Effect of substituting tryptophan for arginine on the cellular uptake of oligo-arginine peptides
  • オリゴアルギニンペプチド ノ サイボウ ナイ イコウ ニ オケル Trpザンキ ドウニュウ ノ エイキョウ

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Oligo-arginine peptides are short cationic peptides capable of traversing the plasma membranes of cells. In order to explore the effective substitutes Trp for Arg on the cellular uptake of oligo-arginine peptides, we designed and synthesized a series of Trp-containing analogues. All synthetic peptides did not show cytotoxicity on Jurkat cells at final concentration of 10μM.［Trp5］- and［Trp6］analogues exhibited moderate cellular uptake（about 75% of octaarginine, R8C）, and［Trp6,8］analogue exhibited similar or even slightly increased cellular uptake as compared to R8C. The other synthetic peptides were showed poor cellular uptake（less than 50%）. A clear relationship was not observed between hydrophobicity and cellular uptake of the synthetic peptides. These results indicated that oligo-arginine pepitde was relatively tolerant to Trp insertion in the middle position but not in the N-terminal position.

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