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제109회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Antibacterial and anti-inflammatory activities of enantiomeric 9-mer peptide analogs derived from protaetiamycine

2012년 2월 17일 17시 50분 04초
BIO.P-696 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
4월 25일 (수요일) 18:00~21:00
저자 및
이은정, 김진경, 정기웅, 김양미
건국대학교 생명공학과, Korea
Protaetiamycine is an insect defensin, derived from the larvae of the beetle Protaetia brevitarsis. We designed four 9-mer peptide analogues based on the sequence of RLWLAIGRG-NH2, in which Gly or Ile was substituted with Arg, Lys, or Trp to optimize the balance between the hydrophobicity and cationicity of the peptides and to increase bacterial cell selectivity. We investigated their toxicities to bacteria and mammalian cells as well as inflammatory activities. The results suggest that the bactericidal action of our potent antibacterial peptides, namely 9Pbw2 (RLWLAIKRR-NH2) and 9Pbw4 (RLWLAWKRR-NH2), may be attributed to the inhibition of the functions of intracellular components after penetration of the bacterial cell membrane. However, the results of anti-inflammatory activities showed that only 9Pbw3 (RLWLAIWRR-NH2) has strong inhibition of NO production, implying that Trp7 as well as optimum level of hydrophobicity may play key roles in the anti-inflammatory activity of 9Pbw3. Furthermore enantiomeric 9Pbw3-D which is the all-D-amino acid analog of 9Pbw3, showed considerably stronger inhibition of NO production and inflammation-induced cytokine production in LPS-stimulated RAW264.7 cells than 9Pbw3. 9Pbw3-D can be a potent non-cytotoxic antibiotic candidate. The results suggest that our peptides having anti-bacterial and anti-inflammatory activities may be contributed to the potent short antibiotics without cytotoxicity.