The <i>N</i>-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish <i>Tg(fli1: EGFP)</i> Model
One of the most important therapies of malignant neoplasms, which are the second cause of death worldwide, is focused on the inhibition of pathological angiogenesis within the tumor. Therefore, the searching for the efficacious and relatively inexpensive small-molecule inhibitors of this process is...
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MDPI AG
2022-10-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/15/11/1308 |
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| author | Monika Gawrońska-Grzywacz Iwona Piątkowska-Chmiel Łukasz Popiołek Mariola Herbet Jarosław Dudka |
| author_facet | Monika Gawrońska-Grzywacz Iwona Piątkowska-Chmiel Łukasz Popiołek Mariola Herbet Jarosław Dudka |
| author_sort | Monika Gawrońska-Grzywacz |
| collection | DOAJ |
| description | One of the most important therapies of malignant neoplasms, which are the second cause of death worldwide, is focused on the inhibition of pathological angiogenesis within the tumor. Therefore, the searching for the efficacious and relatively inexpensive small-molecule inhibitors of this process is essential. In this research, the anti-angiogenic potential of <i>N</i>-substituted-4-methylbenzenesulphonyl hydrazone, possessing antiproliferative activity against cancer cells, was tested. For this purpose, an intersegmental vessel (ISV) angiogenesis assay was performed using 6 hpf (hours post fertilization), 12 hpf and 24 hpf embryos of zebrafish transgenic strain, <i>Tg(fli1: EGFP)</i>. They were incubated with different concentrations of tested molecule and after 24 h the development of intersegmental vessels of the trunk was analysed. In turn, the acute toxicity study in the zebrafish model was mainly conducted on strain AB, using the OECD-approved and recommended fish embryo acute toxicity test (FET) procedure. The results showed the moderate toxicity of <i>N</i>-[(3-chloro-4-methoxyphenyl)methylidene]-4-methylbenzenesulphonohydrazide in above-mentioned model with the LC<sub>50</sub> value calculated at 23.04 mg/L. Moreover, newly synthesized molecule demonstrated the anti-angiogenic potential proved in <i>Tg(fli1: EGFP)</i> zebrafish model, which may be promising for the therapy of neoplastic tumors as well as other diseases related to pathological angiogenesis, such as age-related macular degeneration and diabetic retinopathy. |
| first_indexed | 2024-03-09T18:45:19Z |
| format | Article |
| id | doaj.art-b2d9421e688a48d2b1b65696846cbf9e |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-09T18:45:19Z |
| publishDate | 2022-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-b2d9421e688a48d2b1b65696846cbf9e2023-11-24T06:17:50ZengMDPI AGPharmaceuticals1424-82472022-10-011511130810.3390/ph15111308The <i>N</i>-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish <i>Tg(fli1: EGFP)</i> ModelMonika Gawrońska-Grzywacz0Iwona Piątkowska-Chmiel1Łukasz Popiołek2Mariola Herbet3Jarosław Dudka4Department of Toxicology, Faculty of Pharmacy, Medical University of Lublin, 8B Jaczewskiego Street, 20-090 Lublin, PolandDepartment of Toxicology, Faculty of Pharmacy, Medical University of Lublin, 8B Jaczewskiego Street, 20-090 Lublin, PolandDepartment of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki Street, 20-093 Lublin, PolandDepartment of Toxicology, Faculty of Pharmacy, Medical University of Lublin, 8B Jaczewskiego Street, 20-090 Lublin, PolandDepartment of Toxicology, Faculty of Pharmacy, Medical University of Lublin, 8B Jaczewskiego Street, 20-090 Lublin, PolandOne of the most important therapies of malignant neoplasms, which are the second cause of death worldwide, is focused on the inhibition of pathological angiogenesis within the tumor. Therefore, the searching for the efficacious and relatively inexpensive small-molecule inhibitors of this process is essential. In this research, the anti-angiogenic potential of <i>N</i>-substituted-4-methylbenzenesulphonyl hydrazone, possessing antiproliferative activity against cancer cells, was tested. For this purpose, an intersegmental vessel (ISV) angiogenesis assay was performed using 6 hpf (hours post fertilization), 12 hpf and 24 hpf embryos of zebrafish transgenic strain, <i>Tg(fli1: EGFP)</i>. They were incubated with different concentrations of tested molecule and after 24 h the development of intersegmental vessels of the trunk was analysed. In turn, the acute toxicity study in the zebrafish model was mainly conducted on strain AB, using the OECD-approved and recommended fish embryo acute toxicity test (FET) procedure. The results showed the moderate toxicity of <i>N</i>-[(3-chloro-4-methoxyphenyl)methylidene]-4-methylbenzenesulphonohydrazide in above-mentioned model with the LC<sub>50</sub> value calculated at 23.04 mg/L. Moreover, newly synthesized molecule demonstrated the anti-angiogenic potential proved in <i>Tg(fli1: EGFP)</i> zebrafish model, which may be promising for the therapy of neoplastic tumors as well as other diseases related to pathological angiogenesis, such as age-related macular degeneration and diabetic retinopathy.https://www.mdpi.com/1424-8247/15/11/1308angiogenesiszebrafish<i>Tg(fli1: EGFP)</i>sulphonyl hydrazoneFET |
| spellingShingle | Monika Gawrońska-Grzywacz Iwona Piątkowska-Chmiel Łukasz Popiołek Mariola Herbet Jarosław Dudka The <i>N</i>-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish <i>Tg(fli1: EGFP)</i> Model Pharmaceuticals angiogenesis zebrafish <i>Tg(fli1: EGFP)</i> sulphonyl hydrazone FET |
| title | The <i>N</i>-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish <i>Tg(fli1: EGFP)</i> Model |
| title_full | The <i>N</i>-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish <i>Tg(fli1: EGFP)</i> Model |
| title_fullStr | The <i>N</i>-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish <i>Tg(fli1: EGFP)</i> Model |
| title_full_unstemmed | The <i>N</i>-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish <i>Tg(fli1: EGFP)</i> Model |
| title_short | The <i>N</i>-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish <i>Tg(fli1: EGFP)</i> Model |
| title_sort | i n i substituted 4 methylbenzenesulphonyl hydrazone inhibits angiogenesis in zebrafish i tg fli1 egfp i model |
| topic | angiogenesis zebrafish <i>Tg(fli1: EGFP)</i> sulphonyl hydrazone FET |
| url | https://www.mdpi.com/1424-8247/15/11/1308 |
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