In hemolymph of insect species, compounds with remarkable properties for pharmaceutical industry are present. At the first line, there were found compounds of low molecular mass, less than 1 kDa. One of such compounds, β-alanyl-tyrosine (252 Da), was isolated from larval hemolymph of some species of holometabolous insects (e.g. Neobellieria bullata). Its paralytic activity and antimicrobial properties were described until now. In this study, we present the effect of elongation of β-alanyl-tyrosine by repeating of this motive on the biological and physical properties of prepared analogues. For assessment of antimicrobial properties of these new compounds strains of Gram-positive, Gram-negative bacteria and fungi were used, we also followed the haemolytic activity and toxic effect on human cell culture HepG2. On the base of ECD spectroscopy measurement, subsequent molecular modelling and known secondary structure of original β-alanyl-tyrosine dipeptide, the secondary structures of repeating sequences of β-AY were specified. The repeating structures of β-alanyl-tyrosine show increase in antimicrobial activity; for Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, minimal inhibitory concentration was decreased from 30 to 15 mM for 2xβ-AY, 0.4 mM for 4xβ-AY and 0.25 mM for 6xβ-AY.
- MeSH
- Amino Acid Motifs MeSH
- Anti-Infective Agents chemistry pharmacology MeSH
- Toxins, Biological chemistry pharmacology MeSH
- Hep G2 Cells MeSH
- Dipeptides chemistry pharmacology MeSH
- Fungi drug effects MeSH
- Humans MeSH
- Microbial Sensitivity Tests MeSH
- Cell Proliferation drug effects MeSH
- Staphylococcus aureus drug effects MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
Antimikrobiální peptidy jsou látky běžně se vyskytující v přírodě, které slouží organismům jako obrana proti patogenům. Od 80. let minulého století, kdy byl izolován a charakterizován první krátký peptid s antimikrobiálními účinky cecropin, byly podrobně zkoumány a navrženy jako vhodní kandidáti v dalším boji proti infekčním chorobám způsobeným hlavně rezistentními kmeny bakterií, jako je například methicilin rezistentní bakterie Staphylococcus aureus . Do současnosti bylo identifikováno více jak 1600 antimikrobiálních peptidů. Některé z nich jsou již využívány v průmyslu i jako účinná léčiva. Tento článek se zabývá jen jednou z mnoha skupin antimikrobiálních peptidů, cyklickými peptidy, které vykazují vysokou aktivitu proti bakteriím a jsou již komerčně využívány nebo se o jejich využití uvažuje a procházejí klinickými testy.
Antimicrobial peptides are substances commonly occurring in nature, they serve as defense agents against pathogens. Since the 80s of the last century, when the first short peptide with antimicrobial effect, cecropin, was isolated and characterized, they were invest igated and proposed as suitable candidates to further fight against infectious diseases mainly caused by resistant strains of bacteria such as methicillin-resistant Staphylococcus aureus . Until now more than 1600 antimicrobial peptides were identified. Some of them are already used in industry and as an effective drug. This article is engaged in only one of many groups of antimicrobial peptides, cyclic peptides, which showed high activity against bacteria and are already commercially available or their use is contemplated and they are undergoing clinical trials.
- Keywords
- cyklické antimikrobiální peptidy, peptidová antibiotika, hostitelská obrana, terapeutický potenciál,
- MeSH
- Anti-Bacterial Agents pharmacology therapeutic use MeSH
- Anti-Infective Agents pharmacology isolation & purification MeSH
- Bacitracin therapeutic use MeSH
- Peptides, Cyclic pharmacology immunology MeSH
- Daptomycin therapeutic use MeSH
- Drug Industry MeSH
- Gramicidin therapeutic use MeSH
- Immune System MeSH
- Clinical Trials as Topic MeSH
- Colistin therapeutic use MeSH
- Humans MeSH
- Nisin therapeutic use MeSH
- Polymyxins therapeutic use MeSH
- Check Tag
- Humans MeSH
