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
- Anti-Bacterial Agents * pharmacology MeSH
- Gram-Negative Bacteria MeSH
- Gram-Positive Bacteria MeSH
- HEK293 Cells MeSH
- Lithocholic Acid MeSH
- Humans MeSH
- Lipopeptides * pharmacology MeSH
- Microbial Sensitivity Tests MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article 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
- Anti-Inflammatory Agents isolation & purification toxicity MeSH
- Anti-Infective Agents isolation & purification toxicity MeSH
- Antioxidants isolation & purification toxicity MeSH
- Cell Line MeSH
- Hep G2 Cells MeSH
- HEK293 Cells MeSH
- Flowers chemistry MeSH
- Humans MeSH
- Plant Leaves chemistry MeSH
- Calendula chemistry MeSH
- Plant Extracts isolation & purification toxicity MeSH
- Cell Survival drug effects MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article 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
- 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
