Research advances in the antimicrobial activity of natural product-antimicrobial peptide (AMP) mimic conjugates

IF 4.7 2区医学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY

Bioorganic Chemistry Pub Date : 2026-06-05 Epub Date: 2026-02-08 DOI:10.1016/j.bioorg.2026.109618

Ayue Kang , Yue Tian , Yan Wang , Xinhui Li , Shengnan Xu , Ruige Yang , Longhua Yang , Yong Guo

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Abstract

The global crisis of antimicrobial resistance (AMR) has become a leading cause of death worldwide. With the traditional antibiotic pipeline increasingly depleted and the evolution of drug-resistant bacteria outpacing the development of new therapeutics—Particularly against challenges like methicillin-resistant Staphylococcus aureus (MRSA)—The development of novel antimicrobials is urgently needed. Antimicrobial peptides (AMPs), key effector molecules of innate immunity, are considered promising candidates owing to their membrane-targeting mechanisms and low potential for inducing resistance. However, their clinical translation has been hampered by poor druggability, including issues of cytotoxicity and hemolytic activity. Meanwhile, natural products represent a valuable source of privileged scaffolds with inherent antimicrobial activity or biocompatibility. The combination of natural products with AMP mimics offers a highly promising strategy for combating drug-resistant bacterial infections. This review summarizes recent advances in natural product-AMP mimic conjugates, discusses the development of their antibacterial activity and structure-activity relationships (SARs), and elucidates the mechanisms of action of some representative conjugates. Overall, this review provides new insights and strategic approaches for the rational development of antimicrobials based on natural products and AMPs

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天然产物-抗菌肽（AMP）模拟物偶联物抗菌活性研究进展

抗菌素耐药性（AMR）的全球危机已成为全世界死亡的主要原因。随着传统抗生素渠道日益枯竭，耐药细菌的进化速度超过了新疗法的发展，特别是针对耐甲氧西林金黄色葡萄球菌（MRSA）等挑战，迫切需要开发新型抗菌剂。抗菌肽（AMPs）是先天免疫的关键效应分子，由于其膜靶向机制和低诱导抗性的潜力而被认为是有前途的候选者。然而，它们的临床转化一直受到不良药物性的阻碍，包括细胞毒性和溶血活性的问题。同时，天然产物代表了具有固有抗菌活性或生物相容性的特殊支架的宝贵来源。天然产物与AMP模拟物的结合为对抗耐药细菌感染提供了一种非常有前途的策略。本文综述了天然产物- amp模拟物缀合物的研究进展，讨论了其抗菌活性和构效关系的研究进展，并对一些具有代表性的缀合物的作用机制进行了阐述。综上所述，本文为基于天然产物和抗菌肽的抗菌药物的合理开发提供了新的见解和策略途径

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来源期刊

Bioorganic Chemistry 生物-生化与分子生物学

CiteScore

9.70

自引率

3.90%

发文量

679

审稿时长

31 days

期刊介绍： Bioorganic Chemistry publishes research that addresses biological questions at the molecular level, using organic chemistry and principles of physical organic chemistry. The scope of the journal covers a range of topics at the organic chemistry-biology interface, including: enzyme catalysis, biotransformation and enzyme inhibition; nucleic acids chemistry; medicinal chemistry; natural product chemistry, natural product synthesis and natural product biosynthesis; antimicrobial agents; lipid and peptide chemistry; biophysical chemistry; biological probes; bio-orthogonal chemistry and biomimetic chemistry. For manuscripts dealing with synthetic bioactive compounds, the Journal requires that the molecular target of the compounds described must be known, and must be demonstrated experimentally in the manuscript. For studies involving natural products, if the molecular target is unknown, some data beyond simple cell-based toxicity studies to provide insight into the mechanism of action is required. Studies supported by molecular docking are welcome, but must be supported by experimental data. The Journal does not consider manuscripts that are purely theoretical or computational in nature. The Journal publishes regular articles, short communications and reviews. Reviews are normally invited by Editors or Editorial Board members. Authors of unsolicited reviews should first contact an Editor or Editorial Board member to determine whether the proposed article is within the scope of the Journal.