Zhang Yun, Song Jingjing, Zhang Wei, Liang Ranran, Ma Yinyun, Zhang Li, Wei Xiaojin, Ni Jingman, Wang Rui
Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, Lanzhou University, Lanzhou, 730000, China; School of Pharmacy, Lanzhou University, Lanzhou, 730000, China.
J Pept Sci. 2014 Oct;20(10):785-93. doi: 10.1002/psc.2667. Epub 2014 Jun 23.
Antimicrobial peptides have been widely recognized as potential candidates for treating tumor, especially for defending against multidrug-resistant cells. Previously, based on the structure of substance P, we have designed a novel class of hybrid antimicrobial peptide NS, which possesses potent antimicrobial activity against a broad spectrum of bacterial pathogens. In this study, we evaluated its cytotoxicity to tumor cells and studied the possible mechanism of action. We showed that NS could efficiently kill tumor cells by rapidly disrupting the tumor cell membrane and inhibiting the DNA synthesis. In addition, we also found that NS could efficiently deliver plasmids into cells and exhibit high transfection efficiency after the introduction of a stearyl moiety to its N-terminus, like many reported cell-penetrating peptides. Taken together, this study revealed the potential multiple functions of NS, providing fundamental support for further therapeutic application as potential antitumor agent.
抗菌肽已被广泛认为是治疗肿瘤的潜在候选物，尤其是用于抵御多药耐药细胞。此前，基于P物质的结构，我们设计了一类新型的杂合抗菌肽NS，它对多种细菌病原体具有强大的抗菌活性。在本研究中，我们评估了其对肿瘤细胞的细胞毒性，并研究了可能的作用机制。我们发现NS可以通过快速破坏肿瘤细胞膜和抑制DNA合成来有效杀死肿瘤细胞。此外，我们还发现，与许多已报道的细胞穿透肽一样，在NS的N端引入硬脂酰部分后，它可以有效地将质粒导入细胞并表现出高转染效率。综上所述，本研究揭示了NS的潜在多种功能，为其作为潜在抗肿瘤药物的进一步治疗应用提供了基础支持。
