Studies on Synthesis and Biological Activities of Analogues of Melittin

Abstract

Abstract: Melittin(GIGAVLKVLTTGLPALISWIKRKRQQ-NH₂), a 26-residue peptide, is the major component of the venom of the honey bee Apis mellifera, exhibits highly potent antibacterial activity in addition to its hemolytic activity. A peptide corresponding to Melittin′s C-terminal 15 residues and 4 analogues with 15 residues, respectively, were designed and synthesized. The pure peptides were obtained by semi-preparative RP-HPLC. Analytical RP-HPLC showed a single peak and amino acid analysis showed that the peptides had expected amino acid compositions. Antibiotic activities, hemolytic activities, hydrophobicities and secondary structures of the peptides were studied. All these analogues exhibited potent antibacterial activities and had much decreased abilities to lyse human red blood cells. The antibiotic activities were roughly correlated with the hydrophobicities. The hydrophobicities of the residues farther from the basic cluster(KRKR), however, contributed more to the antibiotic activities. While the mechanism of hemolysis of peptides is not the same as antibacterial action. No clear correlation between the hydrophobicities or the hemolytic activities and the secondary structures(α-helical structures) was found.

Key words: Melittin, Antibacterial activity, Hemolytic activity, CD spectrum

CLC Number:

Q516

TrendMD:

LI Shun-Zi, YAN Hu-Sheng, LIU Guo-Dong, HE Bing-Lin, JIANG Lu . Studies on Synthesis and Biological Activities of Analogues of Melittin[J]. Chem. J. Chinese Universities, 2003, 24(3): 449.

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Studies on Synthesis and Biological Activities of Analogues of Melittin

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