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抗菌肽 Melectin 通过干扰膜和与 DNA 结合表现出抗菌和抗肿瘤活性。

The Antimicrobial Peptide Melectin Shows Both Antimicrobial and Antitumor Activity via Membrane Interference and DNA Binding.

机构信息

Key Laboratory for Gynecologic Oncology Gansu Province, Department of Obstetrics and Gynecology, The First Hospital of Lanzhou University, Lanzhou, People's Republic of China.

The Precision Medicine Laboratory, The First Hospital of Lanzhou University, Lanzhou, People's Republic of China.

出版信息

Drug Des Devel Ther. 2021 Mar 19;15:1261-1273. doi: 10.2147/DDDT.S288219. eCollection 2021.

DOI:10.2147/DDDT.S288219
PMID:33776423
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7989573/
Abstract

PURPOSE

Increasingly complex diseases require novel drugs for their treatment. Antimicrobial peptides (AMPs) are promising candidate treatments due to their broad existence and special characteristics. However, the current understanding of AMPs is not sufficient to allow them to be produced commercially for clinical use.

MATERIALS AND METHODS

Melectin, from the venom of the cleptoparasitic bee , does not exhibit sequence homology with other wasp venom peptides. To investigate this more deeply, we explored the antibacterial and antitumor activities of Melectin and related mechanisms.

RESULTS

Our results demonstrate that Melectin possesses antimicrobial properties against standard sensitive/clinical drug-resistant bacteria strains as well as antitumor activity. It has an α-helix form and exhibits moderate cytotoxicity. Its action mechanisms are involved with membrane interfering and DNA binding. The membrane interfering effect was distinct between different phospholipid compositions.

CONCLUSION

We found that Melectin may serve as a new potential template in the battle against multidrug resistance, and our study indicated that there are promising prospects for medically applicable drugs based on AMPs.

摘要

目的

越来越复杂的疾病需要新型药物来治疗。由于抗菌肽(AMPs)的广泛存在和特殊特性,它们是很有前途的候选治疗方法。然而,目前对抗菌肽的了解还不足以将其商业化生产用于临床应用。

材料与方法

来自寄生性蜜蜂毒液的 Melectin 与其他黄蜂毒液肽没有序列同源性。为了更深入地研究这一点,我们探索了 Melectin 及其相关机制的抗菌和抗肿瘤活性。

结果

我们的结果表明,Melectin 具有针对标准敏感/临床耐药菌菌株的抗菌特性以及抗肿瘤活性。它具有α-螺旋构象,表现出中等的细胞毒性。其作用机制涉及膜干扰和 DNA 结合。不同磷脂组成的膜干扰作用明显不同。

结论

我们发现 Melectin 可能成为对抗多药耐药性的新潜在模板,我们的研究表明,基于 AMPs 的医学应用药物具有广阔的前景。

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Expert Opin Drug Discov. 2020 Nov;15(11):1343-1354. doi: 10.1080/17460441.2020.1791080. Epub 2020 Aug 4.
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DAPTOMYCIN, its membrane-active mechanism vs. that of other antimicrobial peptides.达托霉素,其与其他抗菌肽的膜活性机制比较。
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Update on targeted cancer therapies, single or in combination, and their fine tuning for precision medicine.
伊朗临床样本分离菌株中毒素对唑类抗真菌耐药性的拮抗作用评估
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Pharmacological effects and mechanisms of bee venom and its main components: Recent progress and perspective.蜂毒及其主要成分的药理作用和机制:最新进展与展望
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Antimicrobial Peptides with Anti- Activity.具有 活性的抗菌肽。
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