Bolt H L, Eggimann G A, Jahoda C A B, Zuckermann R N, Sharples G J, Cobb S L
Department of Chemistry , Durham University , South Road , Durham , DH1 3LE , UK . Email:
School of Biological and Biomedical Sciences , Durham University , Durham DH1 3LE , UK . Email:
Medchemcomm. 2017 Feb 1;8(5):886-896. doi: 10.1039/c6md00648e. eCollection 2017 May 1.
Peptoids are a promising class of antimicrobial agents with reported activities against a range of both Gram-positive and Gram-negative bacteria, fungi and most recently parasites. However, at present the available toxicity data is somewhat limited and as such rationally designing effective antimicrobial peptoids can be challenging. Herein, we present the toxicity profiling of a series of linear peptoids against mammalian cell lines (HaCaT and HepG2). The cytotoxicity of the peptoid library has then been correlated with their antibacterial properties against Gram-positive and Gram-negative bacteria and also to the hydrophobicity of the peptoid sequences. The work presented provides valuable data to aid in the future rational design of antimicrobial peptoids.
类肽是一类很有前景的抗菌剂，据报道对一系列革兰氏阳性菌和革兰氏阴性菌、真菌以及最近发现的寄生虫都有活性。然而，目前可用的毒性数据在一定程度上有限，因此合理设计有效的抗菌类肽可能具有挑战性。在此，我们展示了一系列线性类肽对哺乳动物细胞系（HaCaT和HepG2）的毒性分析。然后将类肽文库的细胞毒性与其对革兰氏阳性菌和革兰氏阴性菌的抗菌特性以及类肽序列的疏水性进行了关联。所呈现的工作提供了有价值的数据，有助于未来合理设计抗菌类肽。
