Pharmaceutical Sciences and Health Technologies 2.
Dr. Unger, Dénes
E5UJLD
Institute of Pharmacodinamics and Biopharmacy
06702780064
denesunger2002@gmail.com
New protoapigenone derivative as antiproliferative agent
Dénes Unger1
1: Institute of Pharmacodinamics and Biopharmacy
Szóbeli
Pharmaceutical Sciences and Health Technologies 2.
English
Pharmaceutical Sciences and Health Technologies
Introduction: Cancer treatment is one of the most highlighted fields in drug development. Besides synthetic molecules, nature-inspired semisynthetic agents are also used during the design of new anticancer drugs. According to our previous findings, semisynthetic phenolic derivatives, such as our newly synthesized protoapigenone derivative, may have a significant antiproliferative effect. Based on the literature, we also know that compounds with similar chemical structures may affect mitochondrial membranes.
Aims: Our goal was to determine the mechanism of the anticancer effect of our compound on a cervical cancer cell line.
Methods: The antiproliferative effect of the compound was determined, and its IC50 value was calculated via standard MTT assay on the HeLa cell line. To confirm the change of the mitochondrial membrane potential, we performed flow cytometry analysis using JC-10 dye. We separated cells undergoing different types of cell death (early, late apoptotic, and necrotic) based on cell membrane changes using flow cytometry and Annexin V–propidium iodide (PI) staining. Furthermore, we examined the morphological changes of the cells via fluorescence microscopy after HoPI double-staining (using the mixture of blue Hoescht 33258 and red PI dyes).
Results: Our test compound’s IC50 value was 0.47 µM after 72 hours. The test compound significantly elevated the ratio of the JC-10 green fluorophore form while lowering the ratio of the red form, indicating a damaged mitochondrial membrane potential. Changes in the ratio of early- and late-apoptotic cells were observed during Annexin V-PI staining. Morphological study confirmed that characteristic changes in pre-apoptotic and apoptotic cells can be detected following treatment with our compound.
Conclusion: Based on our current findings, we have proved that our new protoapigenone derivative is a potent antiproliferative agent. It is able to cause apoptosis in cervical cancer cells via mitochondrial function changes, which are at the center of this apoptosis induction. As a result of these intracellular changes, cells undergo significant morphological changes as well.
University of Szeged
Dr Noémi Bózsity-Faragó, Dr Prof István Zupkó
I do not give consent to the publication of my abstract on the website of the congress.
in doctoral studies before complex exam (PhD)
Szabad
elfogadva
szóbeli
nem rendelkezett róla
9792
10:00
10:10