Related Experiment Video
Updated: Aug 22, 2025
In Vivo Imaging and Quantitation of the Host Angiogenic Response in Zebrafish Tumor Xenografts
Published on: August 14, 2019
The N-Substituted-4-Methylbenzenesulphonyl Hydrazone Inhibits Angiogenesis in Zebrafish Tg(fli1: EGFP) Model
Monika Gawrońska-Grzywacz1, Iwona Piątkowska-Chmiel1, Łukasz Popiołek2
1Department of Toxicology, Faculty of Pharmacy, Medical University of Lublin, 8B Jaczewskiego Street, 20-090 Lublin, Poland.
Abstract:
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 N-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, Tg(fli1: EGFP). 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 N-[(3-chloro-4-methoxyphenyl)methylidene]-4-methylbenzenesulphonohydrazide in above-mentioned model with the LC50 value calculated at 23.04 mg/L. Moreover, newly synthesized molecule demonstrated the anti-angiogenic potential proved in Tg(fli1: EGFP) 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.
Insights
Researchers tested a novel small molecule for anti-angiogenic properties, crucial for inhibiting tumor growth. The compound, N-substituted-4-methylbenzenesulphonyl hydrazone, showed promising anti-angiogenic potential in zebrafish embryos without significant toxicity.
Area of Science:
- Pharmacology
- Oncology
- Developmental Biology
Background:
- Malignant neoplasms are a leading cause of death globally.
- Inhibiting tumor angiogenesis is a key therapeutic strategy.
- Novel small-molecule inhibitors are needed for effective cancer treatment.
Purpose of the Study:
- To evaluate the anti-angiogenic potential of N-substituted-4-methylbenzenesulphonyl hydrazone.
- To assess the antiproliferative activity of the compound against cancer cells.
- To determine the toxicity profile of the synthesized molecule.
Main Methods:
- An intersegmental vessel (ISV) angiogenesis assay was performed using transgenic zebrafish embryos (Tg(fli1:EGFP)).
- Embryos were exposed to varying concentrations of the tested molecule.
- Acute toxicity was assessed using the OECD-approved fish embryo acute toxicity test (FET).
Main Results:
- The synthesized molecule, N-[(3-chloro-4-methoxyphenyl)methylidene]-4-methylbenzenesulphonohydrazide, demonstrated anti-angiogenic potential in zebrafish.
- Moderate toxicity was observed, with a calculated LC50 value of 23.04 mg/L.
- The compound possesses antiproliferative activity against cancer cells.
Conclusions:
- N-substituted-4-methylbenzenesulphonyl hydrazone shows promise as an anti-angiogenic agent.
- This compound could be beneficial for treating neoplastic tumors and angiogenesis-related diseases like AMD and diabetic retinopathy.
