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Evaluation of New Antimicrobial Agents Based on tris(1H-Indol-3-yl)methylium Salts: Activity, Toxicity, Suppression of Experimental Sepsis in Mice
| Content Provider | MDPI |
|---|---|
| Author | Trenin, Alexey S. Isakova, Elena B. Treshchalin, Michael I. Polozkova, Vasilisa A. Mirchink, Elena P. Panov, Alexey A. Simonov, Alexander Y. Bychkova, Olga P. Tatarskiy, Victor V. Lavrenov, Sergey N. |
| Copyright Year | 2022 |
| Description | The antimicrobial activity and toxicity of three novel synthetic antibacterial agents containing tris(1H-indol-3-yl)methylium fragment were studied in vitro and in vivo. All compounds in vitro revealed high activity (minimal inhibitory concentration (MIC) 0.13–1.0 µg/mL) against bacteria that were either sensitive or resistant to antibiotics, including multidrug-resistant clinical isolates. The derivatives combining high antimicrobial activity with relatively low cytotoxicity against human donor fibroblasts HPF-hTERT were subjected to further testing on mice. In vivo they revealed fairly good tolerance and relatively low toxicity. Acute toxicity was evaluated, and the main indicators of toxicity, including $LD_{50}$ and $LD_{10}$, were determined. A study of compounds in vivo showed their efficiency in the model of staphylococcal sepsis in mice. The efficiency of compounds may be due to the ability of indolylmethylium salts to form pores in the cytoplasmic membrane of microbial cells and thereby facilitate the penetration of molecules into the pathogen. |
| Starting Page | 118 |
| e-ISSN | 14248247 |
| DOI | 10.3390/ph15020118 |
| Journal | Pharmaceuticals |
| Issue Number | 2 |
| Volume Number | 15 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2022-01-19 |
| Access Restriction | Open |
| Subject Keyword | Pharmaceuticals Pharmacology and Pharmacy Tris(1h-indol-3-yl)methylium Turbomycin Overcoming of Drug Resistance Toxicity in Vitro and in Vivo Staphylococcal Sepsis |
| Content Type | Text |
| Resource Type | Article |
