抗菌肽protegrin的开发现状与作用机制研究

目的针对抗菌肽protegrin的开发现状、作用机制及研究方法等方面的文献进行了检索及总结,希望有助于同行在现有工作的基础上开发新型的抗菌肽。方法对国内外最新发表的抗菌肽protegrin的相关研究结果进行分析、整理和综合。结果抗菌肽protegrin是目前国际上研究比较深入的抗菌肽之一,而国内还没有相关的开发报道。结论抗菌肽protegrin是一种非常有应用价值和开发前途的新型抗菌物质。     

两栖类皮肤抗菌肽的分离纯化与抗菌活性检测技术

两栖类皮肤抗菌肽由于具有广谱、高效的抗菌活性,且不引起微生物耐药性等特点,已成为目前开发新型抗菌药物的理想材料。文章概述了两栖类抗菌肽的主要特点及其分离纯化和抗菌活性检测的主要方法,并对这些技术的原理、方法及其近年来在抗菌肽研究中的进展进行了介绍。同时本文还比较了各种方法的优缺点,对当前研究中所存在的一些问题进行了初步的探讨,以期为两栖类抗菌肽的应用提供理论依据。     

天然抗生素—抗菌肽

目的概述抗菌肽的分类、结构特征、生物活性、作用机制,指出抗菌肽研究的存在问题及应用前景。方法查阅中、英文相关文献20篇,对蟾饲五谷虫抗菌肽进行详细的概括总结。结果通过对抗菌肽的了解,了解到抗菌肽的种类,理化性质,结构特点以及家蝇抗菌肽的作用特点。结论抗菌肽的性质明确,作用机制完善,适合未来抗生素的开发利用。     

从专利角度分析微生物源抗菌肽研发现状及研发思路

目的了解微生物源抗菌肽类药物研发领域现状,为该领域内企业的研发方向提供思路建议。方法基于专利视角,对全球数据库进行专利申请趋势分析,专利竞争格局分析,专利技术主题分析。结果总体来讲国外对于抗菌肽的研究集中于抗菌肽制品及应用,国内则较为重视抗菌肽的制备技术。国外技术的发展趋于成熟,处于稳定期,创新主体对中国市场十分重视。结论建议企业在此领域研发具有独特性质的复合抗菌肽,开发高纯度抗菌肽并实现规模生产,同时注重抗菌肽的检测方法的开发,并在研发过程中合理利用现有技术。     

深度学习在抗菌肽药物研究中的应用进展

抗菌肽(AMP)作为未来最有希望解决病原微生物耐药性的新型抗菌药物之一，其研发备受关注。抗菌肽一般较短，组成多样，迄今人们已发现数千条天然抗菌肽，并建立了多个公开的抗菌肽数据库，为新型抗菌肽的研发和设计奠定了基础。另一方面，深度学习和人工智能作为信息处理的有力工具，已被大量应用于医学影像信息处理、疾病诊断、药物设计等领域，在抗菌肽的设计和研发上也受到广泛关注。在抗菌肽的信息描述方面，人们使用了伪氨基酸残基组成、位置特异性评分矩阵、独热码等多种特征向量；在深度学习方法上，研究人员应用了循环神经网络、卷积神经网络、对抗生成网络等多种算法，开发了ACEP、CLaSS等抗菌肽活性预测和序列生成模型。这些模型有望加速新型抗菌肽的发现，为应对耐药菌感染，尤其是临床上难以治疗的耐药性革兰阴性菌感染，提供新的手段。     

抗菌肽开发与应用的研究进展

抗菌肽是一类普遍存在于生物体内的阳离子两亲性多肽,是机体免疫防御的重要组成部分,具有抗菌谱广、作用强且迅速、不易产生耐药等众多优点.随着多药耐药菌临床感染的日趋加重,抗菌肽引起了人们的广泛关注,成为一类极具开发潜力的新型抗感染制剂.但生产成本高、毒副作用大和体内药动学资料匮乏严重制约了抗菌肽的开发和应用.针对上述瓶颈,国内外进行了大量的研究,已取得显著的成果.本文主要针对抗菌肽的作用特点、作用机制、研究现状,及其在医药领域中的应用前景和存在问题进行综述.     

两亲α-螺旋抗菌肽的分子设计研究现状与进展

抗菌肽以其广谱、快速、特异性作用及抗菌、抗病毒、抗肿瘤等活性,成为具有重要潜在价值的新型药物.最大限度地发挥其活性和降低毒性,是抗菌肽新药开发的首要问题.用分子设计手段改造抗菌肽已成为解决这一问题的关键.以两亲α-螺旋抗菌肽为对象,对分子设计过程中遵守阳离子性和两亲性的原则及影响活性的物理化学参数,可以采取序列修饰或全新设计的方法,以达到定向改造的目的.对分子设计在医药上的应用和发展前景进行了综述和展望.     

抗菌肽抗菌机制及与抗生素协同作用的研究进展

抗菌肽(antimicrobial peptides, AMPs)是一种新型抗生素，对多种细菌，多重耐药细菌均具有抗菌活性。然而，其副作用也是制约抗菌肽研发的主要障碍。研究者使用模式细胞膜，揭示抗菌肽与细胞膜之间的作用方式，开展抗菌肽开发和筛选研究。另外，研究者还将抗菌肽与常规抗生素联合使用，可以协同提高抗菌效果。研究初步揭示了AMPs和常规抗生素之间协同作用的机制。本综述探讨了模式细胞膜在AMPs发现筛选中的应用，及AMPs和常规抗生素之间联合用药的研发现状。     

新型抗菌药物研究进展

抗菌药物的研究开发处于相对低谷,而耐药菌感染治疗急需新型抗菌药物,由此所产生的矛盾需要企业、政府与科研部门协调解决。现阶段新型抗菌药物的研究与开发主要在三个方面进行:①通过结构修饰,继续对已有抗菌药物进行深入开发,获得新产品;②利用基础科学研究成果,寻找新的抗菌靶位,设计新的先导化合物,研究全新抗菌药物;③研究抗感染治疗的全新方法,如抗菌肽、噬菌体等。这些有望为耐药菌感染控制提供有效方法。     

新型抗菌肽PDK160在皮肤及软组织感染局部治疗中的应用

目的研究新型抗菌肽PDK160在皮肤及软组织感染局部治疗中的应用以及作用机制。方法采用体外杀菌试验、溶血性试验、耐药性试验等评价抗菌肽PDK160在小鼠体内创面感染模型和猪皮肤体外感染中的抗菌效果。结果抗菌肽PDK160在体外对革兰阳性菌和革兰阴性菌均具有广谱杀菌作用。另外,PDK160的强效杀微生物活性和广谱抗菌活性与溶血活性无关。PDK160在小鼠的创面感染和猪皮肤感染体外模型中,表现出明显的抗感染效果。在小鼠皮下或局部应用不会导致任何不良反应。结论PDK160可能是局部治疗感染的一种新的治疗方法,值得进一步的研究。     

Iseganan (IntraBiotics pharmaceuticals)

Iseganan (IB-367) is a protegrin under development by IntraBiotics, as part of a larger protegrin program, for the potential treatment of oral mucositis, a frequent side effect of anticancer therapies. The company is developing three formulations of the drug: A rinse for the potential treatment of mucositis, an aerosolized liquid for the potential treatment of respiratory infection and a gel formulation for the potential treatment of pneumonia [376325]. Iseganan kills a broad-spectrum of bacteria and fungi, including those resistant to conventional antimicrobial drugs, by attaching to and destroying the integrity of the lipid cell membrane [241594]. Until August 1999, Pharmacia & Upjohn was a codeveloper of iseganan. IntraBiotics re-acquired the global rights to iseganan in December 1999, and both companies agreed to terminate the collaboration [335766]. In May 2000, analysts at SG Cowen predicted the drug's potential market at US $100 to US $200 million [376325].     

Novel therapies based on cationic antimicrobial peptides

Cationic antimicrobial peptides serve as critical defense molecules protecting the host from invading bacteria, viruses and fungi. These antimicrobial peptides are widely distributed in nature and in vertebrates they have been localized to numerous tissues and cells. Cationic antimicrobial peptides can be expressed constitutively or under certain circumstances they can be induced in response to infection, inflammatory mediators, and cytokines. Although, their original and primary function was believed to be antimicrobial, it is now becoming clear that these antimicrobial peptides have a wide repertoire of functions with interesting ramifications on the immune system that are not solely antimicrobial. An area of active research is the determination of the mechanism(s) of action of antimicrobial peptides which have yet to be clarified. However, current consensus is that the mechanism is sufficiently different from conventional antibiotics that the development of resistance could be remote. Their broad spectrum activity, low potential to induce resistance and diverse functions make antimicrobial peptides an attractive family of compounds that have potential to be developed as therapeutics for treating certain infections.     

Susceptibility of human and murine Chlamydia trachomatis serovars to granulocyte‐ and epithelium‐derived antimicrobial peptides

Abstract: Four antimicrobial peptides, protegrin‐1, RTD‐1, cryptdin‐4, and indolicidin, were tested for their ability to inhibit the in vitro growth of Chlamydia trachomatis serovars E, L2, and mouse pneumonitis (MoPn). In general, protegrin‐1 was found to have the strongest anti‐chlamydial activity. Overall, of the three serovars tested, L2 was the most susceptible while MoPn was the most resistant to these peptides.     

鲎血源主要生物活性物质功能研究进展

鲎血阿米巴细胞大小颗粒中存在多种生物活性物质,在这些物质中,抗脂多糖因子,鲎素抗菌肽,鲎防御素和D因子等是鲎先天免疫系统中的重要功能物质,体外研究表明,它们对细菌、真菌、病毒等有强烈的抑制作用,而对正常细胞毒性较低,是开发肽类抗菌药的重要候选物质。本文主要介绍存在于阿米巴细胞中的鲎源抗菌物质,对其结构、功能、作用机理以及基因工程重组鲎素的研究进展进行综述,并对鲎源抗菌肽的发展趋势进行讨论。     

华芙露的抗菌实验研究

目的：观察由明矾、薄荷、硫磺和硼酸等组成的外用药剂华芙露的抗菌、抗真菌作用,急性毒性试验及皮肤刺激试验,并观察其对临床感染性皮肤病等的疗效。方法：选取青霉素菌等14种常见细菌、真菌和皮肤癣菌,分别进行明矾、薄荷的抗菌实验和华芙露的抗菌实验,结果：华芙露有很好的抗菌、抗真菌作用。     

Computer simulation of antimicrobial peptides

Naturally occurring and synthetic peptides may be a novel class of clinically useful antibiotics. A large body of experimental data on structure function relationships for such peptides is available, but the molecular mechanism of their action remains elusive in most cases. Computer simulations can give detailed insights into the interactions between peptides and lipid bilayers, at least one crucial step in the antimicrobial mechanism. Here we review recent simulations of antimicrobial peptides and discuss potential future contributions of computer simulations in understanding and ultimately designing antimicrobial peptides.     

抗菌肽研究进展

文章归纳并讨论了抗菌肽的来源及分类、作用及其分子机制、应用领域、基因表达策略和应用前景等。     

Peptides and proteins with antimicrobial activity

The increase of microbial resistance to antibiotics has led to a continuing search for newer and more effective drugs. Antimicrobial peptides are generally found in animals, plants, and microorganisms and are of great interest to medicine, pharmacology, and the food industry. These peptides are capable of inhibiting pathogenic microorganisms. They can attack parasites, while causing little or no harm to the host cells. The defensins are peptides found in granules in the polymorphonuclear neutrophils (PMNs) and are responsible for the defense of the organism. Several animal defensins, like dermaseptin, antileukoprotease, protegrin, and others, have had their activities and efficacy tested and been shown to be effective against bacteria, fungi, and protists; there are also specific defensins from invertebrates, e.g., drosomycin and heliomicin; from plants, e.g., the types A and B; and the bacteriocins, e.g., acrocin, marcescin, etc. The aim of the present work was to compile a comprehensive bibliographic review of the diverse potentially antimicrobial peptides in an effort to systematize the current knowledge on these substances as a contribution for further researches. The currently available bibliography does not give a holistic approach on this subject. The present work intends to show that the mechanism of defense represented by defensins is promising from the perspective of its application in the treatment of infectious diseases in human, animals and plants.     

连翘叶提取物抑菌作用的研究

目的探讨连翘叶提取物及连翘苷的体外抑菌作用。方法K-B纸片扩散法。结果青翘、老翘、连翘叶提取物及连翘苷均有一定的抑菌作用,并且连翘叶的抑菌作用优于老翘及青翘。结论连翘叶提取物有较好的抑菌作用。