Tetradecapeptide, Mastoparan B(MP B) and its [$Ala^2$]-, [$Ala^4$]-, [$Ala^6$]-, [$Ala^9$]-MP B derivatives were synthesized, and then their antibacterial and hemolytic activities were assayed to examine the effect of hydrophobicity and amphiphilicity...
Tetradecapeptide, Mastoparan B(MP B) and its [$Ala^2$]-, [$Ala^4$]-, [$Ala^6$]-, [$Ala^9$]-MP B derivatives were synthesized, and then their antibacterial and hemolytic activities were assayed to examine the effect of hydrophobicity and amphiphilicity on the MP B-induced those activities. MP B and more hydrophobic [$Ala^2$]-, [$Ala^4$]-MP B showed stronger antibacterial activity and less hydrophobic [$Ala^6$]-MP B than MP B did similar or weaker activity, so more hydrophobic [Ala]-MP B derivative had stronger activity. But more hydrophobic [$Ala^9$]-MP B than MP B showed weaker activity because of its Trp substitution by Ala. On the other hand, [$Ala^2$]- and [$Ala^4$]-MP B showed 100.0% and 69.4% hemolytic activity, but [$Ala^6$]-MP B did the weakest activity(6.1%) and [$Ala^9$]-MP B, weaker activity(26.0%) than MP-B. Therefore, more hydrophobic [Ala]-MP B derivative had stronger activity and the effect of amphiphilicity on the activity was weak.