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In Silico Analysis, Anticonvulsant Activity, and Toxicity Evaluation of Schisandrin B in Zebrafish Larvae and Mice
The aim of this study is to evaluate the anticonvulsant potential of schisandrin B, a main ingredient of Schisandra chinensis extracts. Schisandrin B showed anticonvulsant activity in the zebrafish larva pentylenetetrazole acute seizure assay but did not alter seizure thresholds in the intravenous p...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10455331/ https://www.ncbi.nlm.nih.gov/pubmed/37629132 http://dx.doi.org/10.3390/ijms241612949 |
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author | Nieoczym, Dorota Banono, Nancy Saana Stępnik, Katarzyna Kaczor, Agnieszka A. Szybkowski, Przemysław Esguerra, Camila Vicencio Kukula-Koch, Wirginia Gawel, Kinga |
author_facet | Nieoczym, Dorota Banono, Nancy Saana Stępnik, Katarzyna Kaczor, Agnieszka A. Szybkowski, Przemysław Esguerra, Camila Vicencio Kukula-Koch, Wirginia Gawel, Kinga |
author_sort | Nieoczym, Dorota |
collection | PubMed |
description | The aim of this study is to evaluate the anticonvulsant potential of schisandrin B, a main ingredient of Schisandra chinensis extracts. Schisandrin B showed anticonvulsant activity in the zebrafish larva pentylenetetrazole acute seizure assay but did not alter seizure thresholds in the intravenous pentylenetetrazole test in mice. Schisandrin B crosses the blood–brain barrier, which we confirmed in our in silico and in vivo analyses; however, the low level of its unbound fraction in the mouse brain tissue may explain the observed lack of anticonvulsant activity. Molecular docking revealed that the anticonvulsant activity of the compound in larval zebrafish might have been due to its binding to a benzodiazepine site within the GABA(A) receptor and/or the inhibition of the glutamate NMDA receptor. Although schisandrin B showed a beneficial anticonvulsant effect, toxicological studies revealed that it caused serious developmental impairment in zebrafish larvae, underscoring its teratogenic properties. Further detailed studies are needed to precisely identify the properties, pharmacological effects, and safety of schisandrin B. |
format | Online Article Text |
id | pubmed-10455331 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-104553312023-08-26 In Silico Analysis, Anticonvulsant Activity, and Toxicity Evaluation of Schisandrin B in Zebrafish Larvae and Mice Nieoczym, Dorota Banono, Nancy Saana Stępnik, Katarzyna Kaczor, Agnieszka A. Szybkowski, Przemysław Esguerra, Camila Vicencio Kukula-Koch, Wirginia Gawel, Kinga Int J Mol Sci Article The aim of this study is to evaluate the anticonvulsant potential of schisandrin B, a main ingredient of Schisandra chinensis extracts. Schisandrin B showed anticonvulsant activity in the zebrafish larva pentylenetetrazole acute seizure assay but did not alter seizure thresholds in the intravenous pentylenetetrazole test in mice. Schisandrin B crosses the blood–brain barrier, which we confirmed in our in silico and in vivo analyses; however, the low level of its unbound fraction in the mouse brain tissue may explain the observed lack of anticonvulsant activity. Molecular docking revealed that the anticonvulsant activity of the compound in larval zebrafish might have been due to its binding to a benzodiazepine site within the GABA(A) receptor and/or the inhibition of the glutamate NMDA receptor. Although schisandrin B showed a beneficial anticonvulsant effect, toxicological studies revealed that it caused serious developmental impairment in zebrafish larvae, underscoring its teratogenic properties. Further detailed studies are needed to precisely identify the properties, pharmacological effects, and safety of schisandrin B. MDPI 2023-08-18 /pmc/articles/PMC10455331/ /pubmed/37629132 http://dx.doi.org/10.3390/ijms241612949 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Nieoczym, Dorota Banono, Nancy Saana Stępnik, Katarzyna Kaczor, Agnieszka A. Szybkowski, Przemysław Esguerra, Camila Vicencio Kukula-Koch, Wirginia Gawel, Kinga In Silico Analysis, Anticonvulsant Activity, and Toxicity Evaluation of Schisandrin B in Zebrafish Larvae and Mice |
title | In Silico Analysis, Anticonvulsant Activity, and Toxicity Evaluation of Schisandrin B in Zebrafish Larvae and Mice |
title_full | In Silico Analysis, Anticonvulsant Activity, and Toxicity Evaluation of Schisandrin B in Zebrafish Larvae and Mice |
title_fullStr | In Silico Analysis, Anticonvulsant Activity, and Toxicity Evaluation of Schisandrin B in Zebrafish Larvae and Mice |
title_full_unstemmed | In Silico Analysis, Anticonvulsant Activity, and Toxicity Evaluation of Schisandrin B in Zebrafish Larvae and Mice |
title_short | In Silico Analysis, Anticonvulsant Activity, and Toxicity Evaluation of Schisandrin B in Zebrafish Larvae and Mice |
title_sort | in silico analysis, anticonvulsant activity, and toxicity evaluation of schisandrin b in zebrafish larvae and mice |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10455331/ https://www.ncbi.nlm.nih.gov/pubmed/37629132 http://dx.doi.org/10.3390/ijms241612949 |
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