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1.
抗菌肽的抗菌机制及其临床应用   总被引:4,自引:0,他引:4       下载免费PDF全文
抗菌肽是广泛存在于生物体内的一种小分子肽, 具有广谱性、高效性、稳定性等特点, 其本身不易产生耐药性。不仅具有杀菌作用, 还能抑杀真菌、寄生虫、病毒以及肿瘤细胞且对正常细胞毒性较小。新颖抗生素发现的缺乏, 导致了大量耐药菌株的出现, 抗菌肽有可能成为一种新的抗生素替代品。本文介绍了抗菌肽的结构特点、生物活性, 并重点阐述了其抗菌机制及最新临床应用进展。  相似文献   

2.
抗菌肽是一类小分子肽,具有广谱的抗菌活性。以往对抗菌肽抗菌机制的研究主要集中在细菌细胞膜的作用上,包含桶板模型、毯式模型,环形孔模型和凝聚模型。近年来相继发现某些抗菌肽可以作用于细菌细胞内部,与核酸物质结合,阻断DNA复制、RNA合成;影响蛋白质合成;抑制隔膜、细胞壁合成,阻碍细胞分裂;抑制胞内酶的活性。本文从胞内机制和胞外机制两个角度对抗菌肽的抗菌机制进行综述,以期阐明各类抗菌肽的作用机制,为进一步研究菌株耐药性、杀菌效果及其杀菌机制提供科学根据。  相似文献   

3.
汪庆  张瑞芬  王亚楠  朱宝利  曾斌 《微生物学报》2022,62(11):4353-4366
抗菌肽是一类广泛存在于生物体内的小分子肽,参与构成生物体先天免疫,可以有效抵抗病原微生物的入侵。抗菌肽具有广谱抗菌活性,且不易产生耐药性等特点,在治疗感染性疾病方面具有独特的优势,有望成为理想的抗感染药物。然而,由于部分抗菌肽尚存在稳定性差、毒性高等问题,限制了抗菌肽的广泛应用。由于人工智能算法能有效合成具有高稳定性、低毒性的抗菌肽,在探索天然抗菌肽中展现了巨大的潜力,因此本文简述了抗菌肽的抗菌机制、结构改造以及利用机器学习和深度学习等人工智能算法进行新型抗菌肽研发的优化策略,以期为抗菌肽结构优化及研发提供新思路。  相似文献   

4.
抗菌肽的作用机制、生物活性及应用研究进展   总被引:1,自引:0,他引:1  
抗菌肽广泛存在于生物界,是辅助生物机体抵抗外来病原体入侵的重要防御分子。抗菌肽不仅能抑制、杀灭多种细菌,而且具有抗真菌、抗寄生虫、抗病毒、抗肿瘤和免疫调节等生物学活性。抗菌肽的作用机制与传统抗生素不同,不仅具有广谱抗微生物作用,而且不易诱导机体产生耐药性,因此,在治疗临床耐药菌株方面具有极大的开发潜力。  相似文献   

5.
抗菌肽结构与功能关系及分子改造研究进展   总被引:3,自引:0,他引:3  
抗菌肽是生物体产生的一种具有抗菌活性的多肽小分子,具有广谱、特异性的抗菌、抗病毒、抗肿瘤等作用。研究表明抗菌肽的正电荷含量、疏水性和肽链结构对抗菌肽的活性至关重要的。围绕以上三个方面对抗菌肽进行分子设计和改造,以期更加有效地提高抗菌肽的抗菌活性,获得到更加高效、低毒的抗菌肽产品。该文主要通过抗菌肽结构与功能的关系,介绍抗菌肽分子设计的研究进展。  相似文献   

6.
抗菌肽作用机制的研究进展   总被引:1,自引:0,他引:1  
抗菌肽是一类来源于多种生物、能有效杀灭病原体的小分子多肽,具有活性谱广、作用强且迅速、不易产生耐药等众多优点.作为新一代抗感染候选药物,抗菌肽的作用机制还未完全清楚,但目前有两种观点已得到公认,即胞膜渗透作用破坏胞膜结构完整性和作用于胞内不同靶点干扰细菌生长及代谢平衡.本文主要就抗菌肽理化性质、二级结构、作用机制以及后两者间的关系做一总结,以便更好的理解抗菌肽的构效关系,为合理设计抗菌肽提供理论基础.  相似文献   

7.
抗菌肽研究进展   总被引:19,自引:0,他引:19  
杨博  王永华 《生命科学》2002,14(3):144-145
抗菌肽是广泛存在于自然界生物中的一种具有抗菌、抗病毒和抗肿瘤活性的多态,由于抗菌肽具有普通抗生素所不具有的一系列优点,抗菌肽的研究已经成了现代学术和应用研究的一个热点。作者综述了抗菌肽的抗菌机制和应用研究等方面的内容。  相似文献   

8.
抗菌肽及其临床应用前景   总被引:4,自引:0,他引:4  
传统抗生素的广泛运用导致了耐药菌株的大量增加,迫切要求新型抗生素的出现。抗菌肽是广泛存在于生物体内的小分子多肽,是天然免疫系统的重要组成部分。它不仅具有广谱杀菌作用,甚至能够抑杀真菌、寄生虫、含包膜病毒以及肿瘤细胞。抗菌肽通过与致病菌胞膜的结合形成跨膜离子通道,导致了细胞内外的离子交换最终引起细胞死亡。由于它作用迅速,选择性强,而且很少有耐药性的发生,很有可能成为新一代的抗菌药物。本文简述了抗菌肽的结构特点,抗菌作用机制,生物学功能和临床应用方面的最新进展以及进一步就抗菌肽作为新型抗生素所面临的问题进行了探讨。  相似文献   

9.
抗菌肽是一类具有生物活性的小分子多肽,具有多种杀菌和抗肿瘤的活性,本文将从抗菌肽的结构、理化性质、生物活性、作用机制等方面简要概述抗菌肽的研究现状,为抗菌肽的后续开发提供一些参考。  相似文献   

10.
抗菌肽抑菌机制研究进展   总被引:3,自引:0,他引:3  
抗菌肽是由各种无脊椎动物、植物和哺乳动物的组织、细胞产生的丰富且分子多样性的一类物质。它们的氨基酸组成、两亲性、阳离子电荷和它们的大小使它们能够粘附或插入到细胞膜中形成孔洞,也就形成所谓的"木桶式"、"地毯式"和"环孔式"的机制。主要介绍几种不同的诱导细菌孔洞形成、细胞死亡的模型及耐药机制。  相似文献   

11.
抗菌肽及其工业应用前景   总被引:1,自引:0,他引:1  
抗菌肽是生物体内经诱导产生的一种对抗外源性致病菌作用的防御性小分子多肽,广泛存在于动植物和微生物体内。其分子量一般在4000Da左右,带正电荷,由30~40个氨基酸组成。抗菌肽一般都具有耐热性,100℃温度下活性最长可保持30min以上。抗菌肽具广谱抗菌活性,通过破坏细胞膜等作用,可以抑制革兰氏阴性菌、革兰氏阳性菌、真菌,有些抗菌肽还具有抗原虫、病毒及抗癌功能。抗菌肽在工业应用中展示出了广阔的前景。  相似文献   

12.
    
Cationic antimicrobial peptides have attracted increasing attention as a novel class of antibiotics to treat infectious diseases caused by pathogenic bacteria. However, susceptibility to protease is a shortcoming in their development. Cyclization is one approach to increase the proteolytic resistance of peptides. Therefore, to improve the proteolytic resistance of Polybia‐MPI, we have synthesized the MPI cyclic analogs C‐MPI‐1 (i‐to‐i+4) and C‐MPI‐2 (i‐to‐i+6) by copper(I)‐catalyzed azide–alkyne cycloaddition. Compared with MPI, C‐MPI‐1 displayed sustained antimicrobial activity and had enhanced anti‐trypsin resistance, while C‐MPI‐2 displayed no antimicrobial activity. The relationship between peptide structure and bioactivity was further investigated by probing the secondary structure of the peptides by circular dichroism. This showed that C‐MPI‐1 adopted an α‐helical structure in aqueous solution and, interestingly, had increased α‐helical conformation in 30 mM sodium dodecyl sulfate and 50% trifluoroethyl alcohol compared with MPI. C‐MPI‐2 that was not α‐helical in structure, suggesting that the propensity for α‐helix conformation may play an important role in cyclic peptide design. In addition, scanning electron microscopy, propidium iodide uptake, and membrane permeabilization assays indicated that MPI and the optimized analog C‐MPI‐1 had membrane‐active action modes, indicating that the peptides would not be susceptible to conventional resistance mechanisms. Our study provides additional insight into the influence of intramolecular cyclization at various positions on peptide structure and biological activity. In conclusion, the design and synthesis of cyclic analogs via click chemistry offer a new strategy for the development of stable antimicrobial agents. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd.  相似文献   

13.
    
The increasing emergence of multidrug‐resistant bacteria is a huge problem to society providing significant risks to public health. This has been further escalated by a decline in the clinical translation of new antibacterial drug classes since the 1980s. In this article, we describe the synthesis, antibacterial/antibiofilm activity and in vitro toxicity of synthetic low molecular weight lipopeptides mimetics of polymyxin. C12‐KTKCKFLKKC‐NH2 and C14‐KTKCKFLKKC‐NH2 lipopeptides demonstrated activity against both planktonic and biofilm forms of Staphylococcus epidermidis, Staphylococcus aureus, MRSA, Escherichia coli, and Acinetobacter baumannii. Peptide‐outer membrane interaction was studied using lipopolysaccharide neutralization and N‐phenyl‐1‐napthylamine assays. C12‐conjugated peptide significantly neutralized lipopolysaccharide at concentrations lower than minimum inhibitory concentration values against Gram‐negative E coli, by an average of 90% and demonstrated up to double the outer membrane permeabilization ability of 10 mg/mL polymyxin B. Polymyxin‐mimetic lipopeptides have the potential to undergo further in vitro and in vivo study to enable clinical translation and help alleviate the current antimicrobial crisis.  相似文献   

14.
    
A novel antimicrobial peptide derived from ovalbumin has been discovered. First, the peptide fragment RKIKVYLPRMK (TK9.1) was identified based on computerized predictions of the secondary structure of peptides in a protein data bank. Using HeliQuest, the sequence was developed into RKIKRYLRRMI (TK9.1.3), which was synthesized using Fmoc‐solid phase peptide synthesis, and found to have strongly antimicrobial activity against Gram‐positive and Gram‐negative bacteria, and fungi but not cytotoxic to HeLa cells and hemolysis in mouse red blood cells. Although ovalbumin itself does not have an antibacterial activity, our results suggest that it may supply the organisms that consume it with antimicrobial peptides, in support of their immunodefence.  相似文献   

15.
牛乳酪蛋白源抗菌肽的研究进展   总被引:1,自引:0,他引:1  
抗菌肽是具有抗菌活性的肽类物质的总称。除了广泛存在于生物体内的内源性抗菌肽外,已从酪蛋白的酶解产物中获得了多种外源性抗菌肽。抗菌肽的抗菌机理独特,有望成为新一代抗菌剂。简要综述了牛乳酪蛋白源抗菌肽的种类、抗菌机理及其研究展望。  相似文献   

16.
    
Antimicrobial peptides (AMPs), with their extraordinary properties, such as broad-spectrum activity, rapid action and difficult development of resistance, have become promising molecules as new antibiotics. Despite their various mechanisms of action, the interaction of AMPs with the bacterial cell membrane is the key step for their mode of action. Moreover, it is generally accepted that the membrane is the primary target of most AMPs, and the interaction between AMPs and eukaryotic cell membranes (causing toxicity to host cells) limits their clinical application. Therefore, researchers are engaged in reforming or de novo designing AMPs as a ‘single-edged sword’ that contains high antimicrobial activity yet low cytotoxicity against eukaryotic cells. To improve the antimicrobial activity of AMPs, the relationship between the structure and function of AMPs has been rigorously pursued. In this review, we focus on the current knowledge of α-helical cationic antimicrobial peptides, one of the most common types of AMPs in nature.  相似文献   

17.
抗菌肽是一类由特定基因编码的小分子多肽,广泛分布于各种生物中,是生物天然免疫的重要效应分子,其对缺乏获得性免疫系统的昆虫尤为重要。蜜蜂是一种对环境极其重要的社会性模式昆虫,又有着极高的经济价值,因此蜜蜂抗菌肽有着较大的研究意义。本文对蜜蜂4种天然免疫抗菌肽(Apidaecin、Abaecin、Hymenoptaecin和Defensin)和蜂产品中的抗菌肽(Jelleines、Melittin和Apamin)研究进展进行了综述,介绍了它们的功能、作用机制及其应用,提出了蜜蜂抗菌肽未来可行的研究方向,旨在推动蜜蜂抗菌肽的研究。  相似文献   

18.
抗菌肽的研究进展   总被引:5,自引:0,他引:5  
抗菌肽是一大类具有新型抗菌机理的抗生素,本文综述了抗菌肽的分类情况,抗菌肽的作用机制,以及部分正在开发的抗菌肽品种。  相似文献   

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