作者: Ammar Almaaytah , Shadi Tarazi , Mohammad Al-Fandi , Ahmad Abuilhaija , Nizar Al-shar’i
DOI: 10.1007/S10989-014-9444-6
关键词: Rational design 、 Melittin 、 Multiple drug resistance 、 Microbiology 、 Antimicrobial 、 Therapeutic index 、 Biology 、 Antibiotics 、 Antimicrobial peptides 、 Peptide
摘要: BMAP-27 and melittin are two antimicrobial peptides (AMPs) that display potent activities against a wide range of microbes including multidrug resistant (MDR) strains bacteria. Unfortunately, their significant toxicity eukaryotic cells has hampered development into clinically useful antibiotics. In this study, we have rationally designed novel hybrid AMP aiming to retain the while enhancing therapeutic index. The strategy employed in our design was based on combining individual α-helical fragments each generate with improved characteristics compared parent peptides. Named as BMAP27-Melittin, peptide displayed broad spectrum activity standard representative Gram-positive Gram-negative bacterial 1–7.5 µM. Moreover, managed kill MDR bacteria potency MIC values low 1 BMAP27-Melittin also proved exhibit antibiofilm hemolytic antiproliferative studies revealed is exhibiting minimal at concentrations. Additionally, molecular dynamics simulations folding folded well-defined structure; supporting experimental findings. Overall, work highlights potential rational generating AMPs enhanced specificity could be developed successful therapeutics for treatment infections.