Phenylpropanoid-based sulfonamide promotes cyclin D1 and cyclin E down-regulation and induces cell cycle arrest at G1/S transition in estrogen positive MCF-7 cell line
| Autor: | Ana Cláudia Chagas de Paula, Marisa Ionta, Diogo Teixeira Carvalho, Helloana Azevedo-Barbosa, Thiago Belarmino de Souza, Guilherme Álvaro Ferreira-Silva, Danielle Ferreira Dias, Carolina Faria Silva |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Cyclin E Cell cycle checkpoint Population Cell Down-Regulation Antineoplastic Agents Toxicology 03 medical and health sciences 0302 clinical medicine Cyclin D1 Cell Line Tumor medicine Humans education Oncogene Proteins education.field_of_study Sulfonamides Phenylpropionates Chemistry Cell Cycle G1/S transition General Medicine Hep G2 030104 developmental biology medicine.anatomical_structure MCF-7 030220 oncology & carcinogenesis Cancer research |
| Zdroj: | Toxicology in vitro : an international journal published in association with BIBRA. 59 |
| ISSN: | 1879-3177 |
| Popis: | Cancer is one of the most critical problems of public health in the world and one of the main challenges for medicine. Different biological effects have been reported for sulfonamide-based compounds including antibacterial, antifungal, and antitumor activities. Herein, a series of phenylpropanoid-based sulfonamides (4a, 4a', 4b, 4b', 5a, 5a', 5b and 5b') were synthesized and their cytotoxic activity was evaluated against four cell lines derived from human tumours (A549 - lung, MCF-7 - breast, Hep G2 - hepatocellular carcinoma, and HT-144-melanoma). Cell viability was significantly reduced in the MCF-7 cell line when compounds 4b, 4b' and 5a were used; IC50 values were lower than those found for their precursors (eugenol and dihydroeugenol) and sulfanilamide. We observed that 4b induced cell cycle arrest at G1/S transition. This is probably due to its ability to reduce cyclin D1 and cyclin E expression. Moreover, 4b also induced apoptosis in MCF-7 cells as demonstrated by an increase in the cell population positive for annexin V in treated cultures in comparison to the control group. Taken together, the data showed that 4b is a promising antitumor agent and it should be considered for further in vivo studies. |
| Databáze: | OpenAIRE |
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