Synthesis and antimicrobial evaluation of two peptide LyeTx I derivatives modified with the chelating agent HYNIC for radiolabeling with technetium-99m
| Autor: | Leonardo Lima Fuscaldi, Natália Gabriela Silva Pinheiro, Jarbas M. Resende, Valbert Nascimento Cardoso, Raquel Silva Araújo, Daniel Moreira dos Santos, Simone Odília Antunes Fernandes, Maria Elena de Lima, André Luís Branco de Barros |
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| Jazyk: | angličtina |
| Předmět: |
HYNIC
lcsh:Arctic medicine. Tropical medicine MALDI-ToF-MS RP-HPLC lcsh:RC955-962 Reducing agent HYNIC EDDA Tricine Antimicrobial peptides Context (language use) Peptide 010403 inorganic & nuclear chemistry Toxicology 01 natural sciences MALDI-ToF-MS 03 medical and health sciences chemistry.chemical_compound Septic and aseptic inflammation 0302 clinical medicine lcsh:RA1190-1270 lcsh:Zoology EDDA Chelation lcsh:QL1-991 lcsh:Toxicology. Poisons chemistry.chemical_classification Tricine Chromatography LyeTx I derivatives Research Technetium-99m Química Antimicrobial Imaging agent 0104 chemical sciences Infectious Diseases chemistry Antimicrobial peptides LyeTx I derivatives 030220 oncology & carcinogenesis RP-HPLC Immunology Differential diagnosis Animal Science and Zoology Parasitology |
| Zdroj: | Repositório Institucional da UFMG Universidade Federal de Minas Gerais (UFMG) instacron:UFMG Journal of Venomous Animals and Toxins including Tropical Diseases, Volume: 22, Article number: 16, Published: 20 MAY 2016 Journal of Venomous Animals and Toxins including Tropical Diseases v.22 2016 The Journal of venomous animals and toxins including tropical diseases Universidade Estadual Paulista (UNESP) instacron:UNESP The Journal of Venomous Animals and Toxins Including Tropical Diseases Journal of Venomous Animals and Toxins including Tropical Diseases, Vol 22, Iss 0 (2016) |
| ISSN: | 1678-9199 |
| DOI: | 10.1186/s40409-016-0070-y |
| Popis: | Current diagnostic methods and imaging techniques are not able to differentiate septic and aseptic inflammation. Thus, reliable methods are sought to provide this distinction and scintigraphic imaging is an interesting option, since it is based on physiological changes. In this context, radiolabeled antimicrobial peptides have been investigated as they accumulate in infectious sites instead of aseptic inflammation. The peptide LyeTx I, from the venom of Lycosa erythrognatha, has potent antimicrobial activity. Therefore, this study aimed to synthesize LyeTx I derivatives with the chelating compound HYNIC, to evaluate their antimicrobial activity and to radiolabel them with 99mTc. Two LyeTx I derivatives, HYNIC-LyeTx I (N-terminal modification) and LyeTx I-K-HYNIC (C-terminal modification), were synthesized by Fmoc strategy and purified by RP-HPLC. The purified products were assessed by RP-HPLC and MALDI-ToF-MS analysis. Microbiological assays were performed against S. aureus (ATCC® 6538) and E. coli (ATCC® 10536) in liquid medium to calculate the MIC. The radiolabeling procedure of LyeTx I-K-HYNIC with 99mTc was performed in the presence of co-ligands (tricine and EDDA) and reducing agent (SnCl2 . 2H2O), and standardized taking into account the amount of peptide, reducing agent, pH and heating. Radiochemical purity analysis was performed by thin-layer chromatography on silica gel strips and the radiolabeled compound was assessed by RP-HPLC and radioactivity measurement of the collected fractions. Data were analyzed by ANOVA, followed by Tukey test (p-values |
| Databáze: | OpenAIRE |
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