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. (September 2019)

• Record Type: Journal Article
• Authors: Azevedo-Barbosa, Helloana; Ferreira-Silva, Guilherme Álvaro; Silva, Carolina Faria; de Souza, Thiago Belarmino; Dias, Danielle Ferreira; de Paula, Ana Claudia Chagas; Ionta, Marisa; Carvalho, Diogo Teixeira
• Is Part Of: Toxicology in vitro. Volume 59(2019)
• Page Start: 150
• Page End: 160
• Publication Date: 2019-09
• Subjects: Phenylpropanoids -- Sulfonamides -- Molecular hybridization -- Antiproliferative activity -- Breast cancer; Toxicity testing -- In vitro -- Periodicals; Toxicology -- Periodicals; 615.9
• DOI: 10.1016/j.tiv.2019.04.023
• Languages: English
• ISSNs: 0887-2333

Abstract

Abstract: 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 and5b′ ) 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 compounds4b, 4b′ and5a were used; IC50 values were lower than those found for their precursors (eugenol and dihydroeugenol) and sulfanilamide. We observed that4b 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 that4b is a promising antitumor agent and it should be considered for further in vivo studies. Highlights: Phenylpropanoid-based sulfonamide inhibits cell cycle progression of MCF-7 cells. Phenylpropanoid-based sulfonamide promotes cyclin D and E down-regulation in MCF-7 cells. Phenylpropanoid-based sulfonamide has pro-apoptotic activity on MCF-7 cells.