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短抗菌肽的批判性评价:来自蝎毒液的短抗菌肽、它们的物理化学特性,以及开发新药的潜力。

A Critical Review of Short Antimicrobial Peptides from Scorpion Venoms, Their Physicochemical Attributes, and Potential for the Development of New Drugs.

机构信息

Ecology and Survival of Microorganisms Group (ESMG), Laboratorio de Ecología Molecular Microbiana (LEMM), Centro de Investigaciones en Ciencias Microbiológicas (CICM), Instituto de Ciencias (IC), Benemérita Universidad Autónoma de Puebla (BUAP), Puebla, México.

Facultad de Ciencias Químicas, Benemérita Universidad Autónoma de Puebla (FCQ-BUAP), Ciudad Universitaria, Puebla, México.

出版信息

J Membr Biol. 2024 Aug;257(3-4):165-205. doi: 10.1007/s00232-024-00315-2. Epub 2024 Jul 11.

Abstract

Scorpion venoms have proven to be excellent sources of antimicrobial agents. However, although many of them have been functionally characterized, they remain underutilized as pharmacological agents, despite their evident therapeutic potential. In this review, we discuss the physicochemical properties of short scorpion venom antimicrobial peptides (ssAMPs). Being generally short (13-25 aa) and amidated, their proven antimicrobial activity is generally explained by parameters such as their net charge, the hydrophobic moment, or the degree of helicity. However, for a complete understanding of their biological activities, also considering the properties of the target membranes is of great relevance. Here, with an extensive analysis of the physicochemical, structural, and thermodynamic parameters associated with these biomolecules, we propose a theoretical framework for the rational design of new antimicrobial drugs. Through a comparison of these physicochemical properties with the bioactivity of ssAMPs in pathogenic bacteria such as Staphylococcus aureus or Acinetobacter baumannii, it is evident that in addition to the net charge, the hydrophobic moment, electrostatic energy, or intrinsic flexibility are determining parameters to understand their performance. Although the correlation between these parameters is very complex, the consensus of our analysis suggests that there is a delicate balance between them and that modifying one affects the rest. Understanding the contribution of lipid composition to their bioactivities is also underestimated, which suggests that for each peptide, there is a physiological context to consider for the rational design of new drugs.

摘要

蝎毒液已被证明是极好的抗菌药物来源。然而,尽管其中许多毒液已经具有功能特征,但它们作为药理学药物仍未得到充分利用,尽管它们具有明显的治疗潜力。在这篇综述中,我们讨论了短蝎毒液抗菌肽(ssAMPs)的物理化学性质。ssAMPs 通常较短(13-25 个氨基酸)且酰胺化,其已被证明的抗菌活性通常可以通过净电荷、疏水力矩或螺旋度等参数来解释。然而,为了全面了解它们的生物学活性,考虑目标膜的特性也非常重要。在这里,我们通过对与这些生物分子相关的物理化学、结构和热力学参数进行广泛分析,提出了一个用于合理设计新型抗菌药物的理论框架。通过比较这些物理化学性质与 ssAMPs 在致病菌(如金黄色葡萄球菌或鲍曼不动杆菌)中的生物活性,显然,除了净电荷、疏水力矩、静电能或固有柔韧性之外,这些参数都是决定其性能的重要因素。尽管这些参数之间的相关性非常复杂,但我们分析的共识表明,它们之间存在微妙的平衡,并且改变其中一个会影响其他参数。对脂质组成对其生物活性的贡献的理解也被低估了,这表明对于每种肽,都需要考虑生理环境来合理设计新药。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e9e0/11289363/0c61563ddba1/232_2024_315_Fig1_HTML.jpg

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