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来自苹果绒蚁蜂(膜翅目:蚁蜂科)毒液的合成肽类似物揭示了它们的抗生素和农药活性潜力。

Synthesized peptide analogs from Eumenes pomiformis (Hymenoptera: Eumenidae) venom reveals their antibiotic and pesticide activity potential.

作者信息

Bea Roberto de la Salud, Frawley Elaine, Shen Qian, Moyo Sydney, Thelven Jeremy M, North Lily

机构信息

Department of Chemistry, Rhodes College, Memphis, TN 38112, USA.

Department of Biology, Rhodes College, Memphis, TN 38112, USA.

出版信息

Toxicon. 2023 Mar 1;224:107032. doi: 10.1016/j.toxicon.2023.107032. Epub 2023 Jan 21.

Abstract

One natural antimicrobial peptide (EpVP2a, Eumenes pomiformis Venom Peptide 2a) found in the venom of a potter wasp (Eumenes pomiformis) and six analogs were synthesized and tested to compare their antimicrobial, antifungal, pesticide, and hemolytic activity with the wild type. Our results indicated that while the original peptide and the synthetic analogs had no antifungal activity or anti-bacterial activity against Pseudomonas aeruginosa, the original peptide and the analog with substitution of the aspartic acid on the sequence by a lysine (EpVP2a-D2K2) had activity against Escherichia coli, Staphylococcus aureus and Bacillus subtilis. This same analog also shows significant insecticide activity. The analog with substitution of lysine with a slightly smaller ornithine had activity against E. coli and B. subtilis. All analogs show low hemolytic activity compared to the natural peptide. The peptide with a reverse sequence to the natural one (EpVp2a Retro) shows low helix structure which can also explain why it has no antibacterial activity and low hemolytic activity. Circular dichroism spectra show that these peptides form an alpha helix structure and their amino acid positions predict an amphipathic nature.

摘要

在陶工黄蜂(Eumenes pomiformis)毒液中发现的一种天然抗菌肽(EpVP2a,梨形蜾蠃毒液肽2a),合成了六种类似物并进行测试,以比较它们与野生型的抗菌、抗真菌、杀虫和溶血活性。我们的结果表明,虽然原始肽和合成类似物对铜绿假单胞菌没有抗真菌活性或抗菌活性,但原始肽和序列中天冬氨酸被赖氨酸取代的类似物(EpVP2a-D2K2)对大肠杆菌、金黄色葡萄球菌和枯草芽孢杆菌有活性。同一类似物也显示出显著的杀虫活性。用稍小的鸟氨酸取代赖氨酸的类似物对大肠杆菌和枯草芽孢杆菌有活性。与天然肽相比,所有类似物的溶血活性都较低。与天然序列相反的肽(EpVp2a Retro)显示出低螺旋结构,这也可以解释为什么它没有抗菌活性和低溶血活性。圆二色光谱表明,这些肽形成α螺旋结构,其氨基酸位置预测具有两亲性。

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