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包封型LyeTx III肽:从蜘蛛毒液中分离出的细胞毒性剂。

Encapsulated LyeTx III Peptide: Cytotoxic Agent Isolated from Spider Venom.

作者信息

Santos Daniel Moreira Dos, Santiago Livia Ramos, Santos Nayara Araújo Dos, Romão Wanderson, Resende Jarbas Magalhães, de Lima Maria Elena, Borges Márcia Helena, Ribeiro Rosy Iara Maciel de Azambuja

机构信息

Department of Experimental Pathology, Federal University of São João del-Rei, Divinópolis 36301-158, Brazil.

Petroleomics and Forensics Laboratory, Federal University of Espírito Santo, Vitória 29075-910, Brazil.

出版信息

Toxins (Basel). 2025 Jan 10;17(1):32. doi: 10.3390/toxins17010032.

Abstract

The discovery of novel cytotoxic drugs is of paramount importance in contemporary medical research, particularly in the search for treatments with fewer side effects and higher specificity. Antimicrobial peptides are an interesting class of molecules for this endeavor. In this context, the LyeTx III, a new peptide extracted from the venom of the spider, stands out. The peptide exhibits typical antimicrobial traits: a positive net charge and amphipathic α -helix structure in lipid-like environments. Its unique sequence (GKAMKAIAKFLGR-NH), identified via mass spectrometry and Edman degradation, shows limited similarity to existing peptides. Significantly, when liposome-encapsulated, LyeTx III demonstrates selective activity against tumor cells in culture. Our MTT results showed that the cytotoxicity of the peptide increased against HN13 cells when administered as liposomes, with their viability in HN13 cells alone being 98%, compared to 38% in liposome-encapsulated form. This finding underscores that the LyeTx III peptide may be a good candidate for the development of new drugs against cancer. Its activity when encapsulated is promising, as it can increase its half-life in the body and can also be targeted to specific tumors.

摘要

新型细胞毒性药物的发现在当代医学研究中至关重要,尤其是在寻找副作用更少、特异性更高的治疗方法方面。抗菌肽是这类研究中一类有趣的分子。在此背景下,从蜘蛛毒液中提取的新肽LyeTx III脱颖而出。该肽具有典型的抗菌特性:在类脂环境中带正净电荷且具有两亲性α -螺旋结构。通过质谱和埃德曼降解法鉴定出的其独特序列(GKAMKAIAKFLGR-NH)与现有肽的相似性有限。值得注意的是,当LyeTx III被脂质体包裹时,在培养中对肿瘤细胞表现出选择性活性。我们的MTT结果表明,当以脂质体形式给药时,该肽对HN13细胞的细胞毒性增加,单独的HN13细胞的活力为98%,而脂质体包裹形式的活力为38%。这一发现强调LyeTx III肽可能是开发新型抗癌药物的良好候选物。其被包裹时的活性很有前景,因为它可以延长其在体内的半衰期,还可以靶向特定肿瘤。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cfe4/11768708/4b7c0c7f8e46/toxins-17-00032-g001.jpg

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