I1WL5W 多肽

H-WKKIWSKIKKLLK-NH2

H-Trp-Lys-Lys-Ile-Trp-Ser-Lys-Ile-Lys-Lys-Leu-Leu-Lys-NH2

13

95.2

C₈₅H₁₄₄N₂₂O₁₄

1698.19

固相合成

Multidrug resistance among various bacterial strains is leading to worldwide resistance to a wide range of antibiotics. Combination therapy involving current antibiotics and other biological or chemical molecules represents an attractive novel strategy. In this study, we investigated the synergistic antibacterial activity of a series of Trp-containing antimicrobial peptides (AMPs) with four classes of traditional chemical antibiotics that are inactive against multidrug-resistant Staphylococcus epidermidis (MRSE) in vitro and in vivo. Among the antibiotics that we studied, penicillin, ampicillin and erythromycin showed a distinct synergistic effect in combination with all of the Trp-containing AMPs, represented by a fractional inhibitory concentration index (FICI) of <0.5. The antibacterial activities were noticeably improved, with 32-to 64-fold reductions in the MIC values for ampicillin and 16- to 32-fold reductions in the MIC values for erythromycin and penicillin. Tetracycline showed synergistic activity with only I1WL5W but additive activity with L11W, L12W, and I4WL5W. Ceftazidime exhibited additive activity with the Trp-containing peptides. In addition, the antibiotics in combination with the peptide significantly inhibited biofilm formation by MRSE 1208. A mechanistic study demonstrated that the Trp-containing peptides, especially I1WL5W and I4WL5W, which contain two tryptophan residues, disrupted bacterial inner and outer membranes, which promoted antibiotic delivery into the cytoplasm and access to cytoplasmic targets; however, L11W and L12W may have increased intracellular antibiotic concentrations by decreasing blaZ, tet(m) and msrA expression. Importantly, strong synergistic activity against the MRSE 1208 strain was observed for the combination of I1WL5W and penicillin in a mouse infection model. Thus, the combination of AMPs and traditional antibiotics could be a promising option for the prevention of acute and chronic infections caused by MRSE.

一般情况下， I1WL5W 多肽 粉末应该保存在-20甚至-70摄氏度. I1WL5W 多肽 溶解后应该-70摄氏度分装保存，避免反复冻融. 了解更多细节，请查阅手册:多肽溶解及保存指南

• Shang D, Liu Y, Jiang F, Ji F, Wang H, Han X. Synergistic Antibacterial Activity of Designed Trp-Containing Antibacterial Peptides in Combination With Antibiotics Against Multidrug-Resistant Staphylococcus epidermidis. Front Microbiol. 2019;10:2719. Published 2019 Nov 25. doi:10.3389/fmicb.2019.02719

三氟乙酸（Trifluoroacetic acid，简称 TFA）是高效液相色谱（简称 HPLC）纯化过程中常用的反离子。TFA 的存在可能会对肽的净重量、外观及溶解度产生影响，具体如下：

对净重量的影响：TFA 盐会增加产物的总质量。在大多数情况下，肽的含量占总重量的 80% 以上，剩余部分则为 TFA。

对溶解度的影响：TFA 盐通常能提高肽在水溶液中的溶解度。

在生物检测中的影响：对于大多数标准的体外检测，残留的 TFA 水平一般不会造成干扰。但需注意，在高灵敏度的细胞研究或生化研究中，需关注其存在可能带来的影响。

干品多肽的重量中不仅仅包含多肽，还包含有一些非肽的组份，如水、被吸收的溶剂、配位离子和盐等。肽的净含量是指肽在其中的重量百分比，这个百分比的数值范围很大，可能从50%到90%，取决于纯度、序列以及合成和纯化的方法，不要将肽的净含量和肽的纯度混为一谈，他们是两个完全不同的概念。纯度通常是通过HPLC测定的。纯度定义的是多肽样品中含正确序列的组分的百分比，而肽的净含量是指样品中肽类物质相对于总物质所占的百分比，肽的净含量通常是氨基酸组分分析或紫外分光法测定的，这个信息主要是在一些对肽的浓度很敏感的实验中，对计算肽的浓度是很重要的。