PDF(Pubmed)
Abstract：
(1) Background: Antimicrobial resistance is growing at an extreme pace and has proven to be an urgent topic, for research into alternative treatments. Such a prospective possibility is hidden in antimicrobial peptides because of their low to no toxicity, effectiveness at low concentrations, and most importantly their ability to be used for multiple treatments. This work was focused on the study of the effect of the modification in position 7 of Temporin A on its biological activity; (2) Methods: The targeted peptides were synthesized using Fmoc/Ot-Bu SPPS. The antibacterial activity of the analogs was determined using the broth microdilution method and disk-diffusion method. In vitro tests were performed to determine the cytotoxicity, phototoxicity, and antiproliferative activity of the peptide analogs on a panel of tumor and normal cell lines; (3) Results: All analogs except DTCit showed good antibacterial activity, with DTDab having the best activity according to the disk-diffusion method. However, DTCit had an acceptable cytotoxicity, combined with good selectivity against the test MCF-7 cell line; (4) Conclusions: The obtained results revealed the importance of the basicity and length of the side chain at position 7 in the Temporin A sequence for both tested activities.
摘要：
（1）背景：抗菌素耐药性正以极端的速度增长，已被证明是一个紧迫的话题，研究替代疗法。这种潜在的可能性隐藏在抗菌肽中，因为它们具有低到没有毒性，在低浓度下的有效性，最重要的是它们能够用于多种治疗。这项工作的重点是研究TemporinA的7位修饰对其生物学活性的影响。（2）方法：使用Fmoc/Ot-BuSPPS合成靶向肽。使用肉汤微量稀释法和圆盘扩散法确定类似物的抗菌活性。进行体外测试以确定细胞毒性，光毒性，和肽类似物对一组肿瘤和正常细胞系的抗增殖活性；（3）结果：除DTCit外，所有类似物均显示出良好的抗菌活性，根据圆盘扩散方法，DTDab具有最好的活性。然而,DTCit具有可接受的细胞毒性，结合针对测试MCF-7细胞系的良好选择性;(4)结论:所获得的结果揭示了在TemporinA序列中第7位侧链的碱性和长度对于两种测试活性的重要性。
