Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivo
Biological properties of new synthetic triindolylmethylium antibiotics of the triindolylmethane group, including compounds containing a maleimide fragment in the structure, are studied. Their high antibacterial activity in vitro, mainly against gram-positive bacteria, but also against strains with m...
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| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | Russian |
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LLC "Publishing House OKI"
2020-05-01
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| Series: | Антибиотики и Химиотерапия |
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| Online Access: | https://www.antibiotics-chemotherapy.ru/jour/article/view/104 |
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| author | E. P. Mirchink E. B. Isakova S. N. Lavrenov A. Yu. Simonov V. A. Golibrodo A. A. Panov O. P. Bychkova V. V. Tatarskiy A. S. Trenin |
| author_facet | E. P. Mirchink E. B. Isakova S. N. Lavrenov A. Yu. Simonov V. A. Golibrodo A. A. Panov O. P. Bychkova V. V. Tatarskiy A. S. Trenin |
| author_sort | E. P. Mirchink |
| collection | DOAJ |
| description | Biological properties of new synthetic triindolylmethylium antibiotics of the triindolylmethane group, including compounds containing a maleimide fragment in the structure, are studied. Their high antibacterial activity in vitro, mainly against gram-positive bacteria, but also against strains with multiple drug resistance, was shown. The compounds, that showed the least in vitro toxicity on human donor fibroblasts PF-hTERT, were subjected to further testing in animals (mice). The LD50 and LD10 values identified were 24.2 and 16.9 mg/kg, respectively, for LCTA-2701 compound and 41.8 and 34.1 mg/kg for LCTA-2841 compound. In vivo testing of chimeric compounds showed their high efficiency in the model of staphylococcal sepsis in mice and a fairly good tolerability. ED50 values were 1.09 mg/kg for LCTA-2701 compound and 18.27 mg/kg for LCTA-2841 compound, and their chemotherapeutic index was, respectively, 22.2 and 2.3. |
| format | Article |
| id | doaj-art-dda33262d19d4ba4b5b41e4778eea460 |
| institution | Matheson Library |
| issn | 0235-2990 |
| language | Russian |
| publishDate | 2020-05-01 |
| publisher | LLC "Publishing House OKI" |
| record_format | Article |
| series | Антибиотики и Химиотерапия |
| spelling | doaj-art-dda33262d19d4ba4b5b41e4778eea4602025-08-03T13:04:42ZrusLLC "Publishing House OKI"Антибиотики и Химиотерапия0235-29902020-05-016311-121217103Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivoE. P. Mirchink0E. B. Isakova1S. N. Lavrenov2A. Yu. Simonov3V. A. Golibrodo4A. A. Panov5O. P. Bychkova6V. V. Tatarskiy7A. S. Trenin8Gause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsN. N. Blokhin National Medical Research Centre of OncologyGause Institute of New AntibioticsBiological properties of new synthetic triindolylmethylium antibiotics of the triindolylmethane group, including compounds containing a maleimide fragment in the structure, are studied. Their high antibacterial activity in vitro, mainly against gram-positive bacteria, but also against strains with multiple drug resistance, was shown. The compounds, that showed the least in vitro toxicity on human donor fibroblasts PF-hTERT, were subjected to further testing in animals (mice). The LD50 and LD10 values identified were 24.2 and 16.9 mg/kg, respectively, for LCTA-2701 compound and 41.8 and 34.1 mg/kg for LCTA-2841 compound. In vivo testing of chimeric compounds showed their high efficiency in the model of staphylococcal sepsis in mice and a fairly good tolerability. ED50 values were 1.09 mg/kg for LCTA-2701 compound and 18.27 mg/kg for LCTA-2841 compound, and their chemotherapeutic index was, respectively, 22.2 and 2.3.https://www.antibiotics-chemotherapy.ru/jour/article/view/104triindolylmethanemaleimidechimeric (hybrid) antibioticsantibacterial and antifungal activity in vitro and in vivocytotoxicityin vivo toxicityefficacy in a model of staphylococcal sepsis in mice |
| spellingShingle | E. P. Mirchink E. B. Isakova S. N. Lavrenov A. Yu. Simonov V. A. Golibrodo A. A. Panov O. P. Bychkova V. V. Tatarskiy A. S. Trenin Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivo Антибиотики и Химиотерапия triindolylmethane maleimide chimeric (hybrid) antibiotics antibacterial and antifungal activity in vitro and in vivo cytotoxicity in vivo toxicity efficacy in a model of staphylococcal sepsis in mice |
| title | Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivo |
| title_full | Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivo |
| title_fullStr | Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivo |
| title_full_unstemmed | Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivo |
| title_short | Study of the Activity and Toxicity of New Antibacterial Agents Based on Triindolylmethane Derivatives in vivo |
| title_sort | study of the activity and toxicity of new antibacterial agents based on triindolylmethane derivatives in vivo |
| topic | triindolylmethane maleimide chimeric (hybrid) antibiotics antibacterial and antifungal activity in vitro and in vivo cytotoxicity in vivo toxicity efficacy in a model of staphylococcal sepsis in mice |
| url | https://www.antibiotics-chemotherapy.ru/jour/article/view/104 |
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