Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives
The interaction of positively charged polymers (polycations) with a biological membrane is considered to be the cause of the frequently observed toxicity of these macromolecules. If it is possible to obtain polymers with a predominantly negative effect on bacterial and fungal cells, such systems wou...
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MDPI AG
2021-08-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/14/9/838 |
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| author | Kamil Kaminski Magdalena Skora Paweł Krzyściak Sylwia Stączek Agnieszka Zdybicka-Barabas Małgorzata Cytryńska |
| author_facet | Kamil Kaminski Magdalena Skora Paweł Krzyściak Sylwia Stączek Agnieszka Zdybicka-Barabas Małgorzata Cytryńska |
| author_sort | Kamil Kaminski |
| collection | DOAJ |
| description | The interaction of positively charged polymers (polycations) with a biological membrane is considered to be the cause of the frequently observed toxicity of these macromolecules. If it is possible to obtain polymers with a predominantly negative effect on bacterial and fungal cells, such systems would have great potential in the treatment of infectious diseases, especially now when reports indicate the growing risk of fungal co-infections in COVID-19 patients. We describe in this article cationic derivatives of natural beta-glucan polymers obtained by reacting the polysaccharide isolated from <i>Saccharomyces boulardii</i> (SB) and <i>Cetraria islandica</i> (CI) with glycidyl trimethyl ammonium chloride (GTMAC). Two synthesis strategies were applied to optimize the product yield. Fungal diseases particularly affect low-income countries, hence the emphasis on the simplicity of the synthesis of such drugs so they can be produced without outside help. The three structures obtained showed selective anti-mycotic properties (against, i.e., <i>Scopulariopsis brevicaulis</i>, <i>Aspergillus brasiliensis</i>, and <i>Fusarium solani</i>), and their toxicity established using fibroblast 3T3-L1 cell line was negligible in a wide range of concentrations. For one of the polymers (SB derivative), using in vivo model of <i>Aspergillus brasiliensis</i> infection in <i>Galleria mellonella</i> insect model, we confirmed the promising results obtained in the preliminary study. |
| first_indexed | 2024-03-10T07:19:45Z |
| format | Article |
| id | doaj.art-e1d7413969c44a88a8d51c0d98ef7bf6 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T07:19:45Z |
| publishDate | 2021-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-e1d7413969c44a88a8d51c0d98ef7bf62023-11-22T14:44:08ZengMDPI AGPharmaceuticals1424-82472021-08-0114983810.3390/ph14090838Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan DerivativesKamil Kaminski0Magdalena Skora1Paweł Krzyściak2Sylwia Stączek3Agnieszka Zdybicka-Barabas4Małgorzata Cytryńska5Faculty of Chemistry, Jagiellonian University, Gronostajowa 2 St., 30-387 Krakow, PolandDepartment of Infections Control and Mycology, Chair of Microbiology, Jagiellonian University Medical College, Czysta 18 St., 31-121 Krakow, PolandDepartment of Infections Control and Mycology, Chair of Microbiology, Jagiellonian University Medical College, Czysta 18 St., 31-121 Krakow, PolandDepartment of Immunobiology, Institute of Biological Sciences, Faculty of Biology and Biotechnology, Maria Curie-Sklodowska University, Akademicka 19 St., 20-033 Lublin, PolandDepartment of Immunobiology, Institute of Biological Sciences, Faculty of Biology and Biotechnology, Maria Curie-Sklodowska University, Akademicka 19 St., 20-033 Lublin, PolandDepartment of Immunobiology, Institute of Biological Sciences, Faculty of Biology and Biotechnology, Maria Curie-Sklodowska University, Akademicka 19 St., 20-033 Lublin, PolandThe interaction of positively charged polymers (polycations) with a biological membrane is considered to be the cause of the frequently observed toxicity of these macromolecules. If it is possible to obtain polymers with a predominantly negative effect on bacterial and fungal cells, such systems would have great potential in the treatment of infectious diseases, especially now when reports indicate the growing risk of fungal co-infections in COVID-19 patients. We describe in this article cationic derivatives of natural beta-glucan polymers obtained by reacting the polysaccharide isolated from <i>Saccharomyces boulardii</i> (SB) and <i>Cetraria islandica</i> (CI) with glycidyl trimethyl ammonium chloride (GTMAC). Two synthesis strategies were applied to optimize the product yield. Fungal diseases particularly affect low-income countries, hence the emphasis on the simplicity of the synthesis of such drugs so they can be produced without outside help. The three structures obtained showed selective anti-mycotic properties (against, i.e., <i>Scopulariopsis brevicaulis</i>, <i>Aspergillus brasiliensis</i>, and <i>Fusarium solani</i>), and their toxicity established using fibroblast 3T3-L1 cell line was negligible in a wide range of concentrations. For one of the polymers (SB derivative), using in vivo model of <i>Aspergillus brasiliensis</i> infection in <i>Galleria mellonella</i> insect model, we confirmed the promising results obtained in the preliminary study.https://www.mdpi.com/1424-8247/14/9/838antifungalbeta-glucanpolycations<i>Galleria mellonella</i> model |
| spellingShingle | Kamil Kaminski Magdalena Skora Paweł Krzyściak Sylwia Stączek Agnieszka Zdybicka-Barabas Małgorzata Cytryńska Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives Pharmaceuticals antifungal beta-glucan polycations <i>Galleria mellonella</i> model |
| title | Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives |
| title_full | Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives |
| title_fullStr | Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives |
| title_full_unstemmed | Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives |
| title_short | Synthesis and Study of Antifungal Properties of New Cationic Beta-Glucan Derivatives |
| title_sort | synthesis and study of antifungal properties of new cationic beta glucan derivatives |
| topic | antifungal beta-glucan polycations <i>Galleria mellonella</i> model |
| url | https://www.mdpi.com/1424-8247/14/9/838 |
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