The aim of this article is to introduce the topic of newly designed peptides as well as their biological activity. We designed nine encoded peptides composed of six amino acids. All these peptides were synthesized with C-terminal amidation. To investigate the importance of increased hydrophobicity at the amino end of the peptides, all of them were subsequently synthesized with palmitic or lithocholic acid at the N-terminus. Antimicrobial activity was tested on Gram-positive and Gram-negative bacteria and fungi. Cytotoxicity was measured on HepG2 and HEK 293 T cell cultures. Peptides bearing a hydrophobic group exhibited the best antimicrobial activity. Lipopeptides with palmitic or lithocholic acid (PAL or LCA peptides) at the N-terminus and with C-terminal amidation were highly active against Gram-positive bacteria, especially against strains of Staphylococcus aureus and Candida tropicalis. The LCA peptide SHP 1.3 with the sequence LCA-LVKRAG-NH2, had high efficiency on HepG2 human liver hepatocellular carcinoma cells (97%).
- MeSH
- antibakteriální látky * farmakologie MeSH
- gramnegativní bakterie MeSH
- grampozitivní bakterie MeSH
- HEK293 buňky MeSH
- kyselina lithocholová MeSH
- lidé MeSH
- lipopeptidy * farmakologie MeSH
- mikrobiální testy citlivosti MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
BACKGROUND: The aim of this work was to compare water and organic extracts, infusions and tinctures from flowers and leaves of Calendula officinalis in terms of their biological activity and composition. The purpose of work was investigation whether the leaves and stems are really the waste or they contain interesting substances which could be utilized. Antimicrobial, antifungal, antioxidant and anti-inflammatory activities were studied. Then, the ability to inhibit collagenase was studied as well. Cytotoxicity was tested for all the samples on mammalian cell lines. METHODS: To determine the composition of extracts, infusions and tinctures phytochemical analysis (the set of colour reactions for the detection of groups of biologically active compounds) was carried out and showed that samples from flowers and leaves contain the same groups of biologically active substances (proteins and amino acids, reducing sugars, flavonoids, saponins, phenolics, terpenoids, steroids, glycosides). The antimicrobial activity of tested samples was proved, where the most sensitive bacterium was Micrococcus luteus and the most sensitive yeast was Geotrichum candidum. RESULTS: The study of anti-collagenase activity has shown that the enzymatic reaction of collagenase was affected by all tested samples and their effect was concentration dependent. Cytotoxicity of water and methanol extracts at cell lines HEK 293T and HepG2 was observed. CONCLUSION: Cells HepG2 were more sensitive than cells HEK 293T. Using cell line RAW 264.7, antiinflammatory activity of all samples was observed. Tincture of leaves was the most effective.
- MeSH
- antiflogistika izolace a purifikace toxicita MeSH
- antiinfekční látky izolace a purifikace toxicita MeSH
- antioxidancia izolace a purifikace toxicita MeSH
- buněčné linie MeSH
- buňky Hep G2 MeSH
- HEK293 buňky MeSH
- květy chemie MeSH
- lidé MeSH
- listy rostlin chemie MeSH
- měsíček chemie MeSH
- rostlinné extrakty izolace a purifikace toxicita MeSH
- viabilita buněk účinky léků MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
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
- aminokyselinové motivy MeSH
- antiinfekční látky chemie farmakologie MeSH
- biologické toxiny chemie farmakologie MeSH
- buňky Hep G2 MeSH
- dipeptidy chemie farmakologie MeSH
- houby účinky léků MeSH
- lidé MeSH
- mikrobiální testy citlivosti MeSH
- proliferace buněk účinky léků MeSH
- Staphylococcus aureus účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem 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.
- Klíčová slova
- cyklické antimikrobiální peptidy, peptidová antibiotika, hostitelská obrana, terapeutický potenciál,
- MeSH
- antibakteriální látky farmakologie terapeutické užití MeSH
- antiinfekční látky farmakologie izolace a purifikace MeSH
- bacitracin terapeutické užití MeSH
- cyklické peptidy farmakologie imunologie MeSH
- daptomycin terapeutické užití MeSH
- farmaceutický průmysl MeSH
- gramicidin terapeutické užití MeSH
- imunitní systém MeSH
- klinické zkoušky jako téma MeSH
- kolistin terapeutické užití MeSH
- lidé MeSH
- nisin terapeutické užití MeSH
- polymyxiny terapeutické užití MeSH
- Check Tag
- lidé MeSH
