蜂毒肽C末端片段的反序肽的抗菌活性和溶血活性  

Antibacterial and Hemolytic Activities of the Reverse-sequence Analogs of a Melittin′s C-terminal Segment

作　　者：陈素霞[1] 孙学军[1] 李顺子[1] 阎虎生[1] 

机构地区：[1]南开大学高分子化学研究所吸附与分离功能高分子材料国家重点实验室,天津300071

出　　处：《高等学校化学学报》2005年第12期2233-2236,共4页Chemical Journal of Chinese Universities

基　　金：国家"九五"攻关项目(批准号:9690105154);天津市重点科学基金(批准号:033801811)资助

摘　　要：设计并合成了具有不同碱性氨基酸残基数和不同疏水性片段链长的基于Mel(12～26)的系列反序肽类似物. 结果表明, 反序肽的正电荷和疏水性对于抑菌活性都很重要, N端至少保留3个碱性氨基酸(正电荷>4)和C端的疏水性片段的链长至少为8个氨基酸残基的类似物具有较高的抑菌活性, 具有较大的抑菌活性的最小反序肽类似物为具有11个氨基酸残基的RetroMel(13～23). 这些反序肽的溶血活性都很小.Melittin is an amphipathic a-helical peptide with 26 amino acids. It has high antimicrobial activity and toxicity to eukaryotic cells. C-terminal 15-residue fragment of melittin （ GLPALISWIKRKRQQ-NH2 ）, M（ 12-26）, retained some of the antimicrobial activity but lost most of the hemolytic activitiy. A series of reverse-sequence analogs of M（12-26） with various numbers of basic amino acid residues and various lengths of the hydrophobic segment were synthesized. In the reverse-sequence analogs, the positive charges introduced by the basic residues and the N-terminal amino group were gathered in the N-terminus, while the hydrophobic segment was located in the C-terminus. The results indicate both of the positive charge and the hydrophobicity of the reverse-sequence analogs were necessary for the antimicrobial and hemolytic activities. At least three Nterminal basic animo acids and eight amino acid residues for the hydrophobic segment were required for high antimicrobial activity. A 11-residue peptide, RetroMel （13-23 ） was the shortest peptide retaining the antimi- crobial activity. All these of the reverse-sequence analogs possessed very low hemolysis.

关 键 词：蜂毒肽 反序 抑菌活性 溶血活性 

分 类 号：Q516[生物学—生物化学]