LIPPSO, Departament de Química, University of Girona, Maria Aurèlia Capmany 69, 17003 Girona, Spain.
Institut de Química Computacional i Catàlisi i Departament de Química, University of Girona, Maria Aurèlia Capmany 69, 17003 Girona, Spain.
Molecules. 2017 Oct 26;22(11):1817. doi: 10.3390/molecules22111817.
A library of 66 cyclic decapeptides incorporating a Trp residue was synthesized on solid phase and screened against the phytopathogenic bacteria pv. , pv. , and The hemolytic activity of these peptides was also evaluated. The results obtained were compared with those of a collection of Phe analogues previously reported. The analysis of the data showed that the presence of the Trp improved the antibacterial activity against these three pathogens. In particular, 40 to 46 Trp analogues displayed lower minimum inhibitory concentration (MIC) values than their corresponding Phe counterparts. Interestingly, 26 Trp-containing sequences exhibited MIC of 0.8 to 3.1 μM against pv. , 21 peptides MIC of 1.6 to 6.2 μM against pv. and six peptides MIC of 6.2 to 12.5 μM against . Regarding the hemolysis, in general, Trp derivatives displayed a percentage of hemolysis comparable to that of their Phe analogues. Notably, 49 Trp-containing cyclic peptides showed a hemolysis ≤ 20% at 125 μM. The peptides with the best biological activity profile were c(LKKKLWKKLQ) () and c(LKKKKWLLKQ) (), which displayed MIC values ranging from 0.8 to 12.5 μM and a hemolysis ≤ 8% at 125 μM. Therefore, it is evident that these Trp sequences constitute promising candidates for the development of new agents for use in plant protection.
一个包含一个色氨酸残基的 66 个环状十肽库在固相上合成，并针对植物病原菌 pv. pv. 和 进行了筛选。这些肽的溶血活性也进行了评估。将所得结果与先前报道的一组苯丙氨酸类似物的结果进行了比较。数据分析表明，色氨酸的存在提高了这些三种病原体的抗菌活性。特别是，40 到 46 个色氨酸类似物显示出比其相应的苯丙氨酸类似物更低的最小抑菌浓度 (MIC) 值。有趣的是，26 个含有色氨酸的序列对 pv. 的 MIC 值为 0.8 到 3.1 μM，对 pv. 的 MIC 值为 1.6 到 6.2 μM，对 的 MIC 值为 6.2 到 12.5 μM。关于溶血，一般来说，色氨酸衍生物的溶血百分比与它们的苯丙氨酸类似物相当。值得注意的是，在 125 μM 时，49 个含有色氨酸的环状肽的溶血率 ≤ 20%。具有最佳生物学活性谱的肽是 c(LKKKLWKKLQ) () 和 c(LKKKKWLLKQ) (), 其 MIC 值范围为 0.8 到 12.5 μM，在 125 μM 时的溶血率 ≤ 8%。因此，显然这些色氨酸序列是开发用于植物保护的新型药剂的有前途的候选物。
