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Pharmacokinetic, Antiproliferative and Apoptotic Effects of Phenolic Acids in Human Colon Adenocarcinoma Cells Using In Vitro and In Silico Approaches

Laboratory of Functional Foods, Food and Nutrition Program, UNIRIO, Rio de Janeiro 22290-240, Brazil
Laboratory of Bioinformatics and Computational Biology, Program Postgraduate in Molecular and Cellular Biology, UNIRIO, Rio de Janeiro 22290-240, Brazil
Nutrition Program, Laboratory of Functional Foods, UFRJ, Rio de Janeiro 22290-240, Brazil
Department of Food Science, Food and Nutrition Program, Federal University of Rio de Janeiro State, Rio de Janeiro. Av. Pasteur, 296-Urca, Rio de Janeiro-RJ 22290-240, Brazil
Author to whom correspondence should be addressed.
Academic Editor: Francesca Giampieri
Molecules 2018, 23(10), 2569;
Received: 31 August 2018 / Revised: 11 September 2018 / Accepted: 13 September 2018 / Published: 8 October 2018
(This article belongs to the Special Issue Nutraceuticals and Their Medicinal Importance)
Colon cancer is the second most common cause of cancer deaths in the USA and Europe. Despite aggressive therapies, many tumors are resistant to current treatment protocols and epidemiological data suggest that diet is a major factor in the etiology of colon cancer. This study aimed to evaluate the antioxidant activity and the influence of 3,4-dihydroxyphenylacetic (3,4-DHPAA), p-coumaric (p-CoA), vanillic (VA) and ferulic (FA) acids on cell viability, cell cycle progression, and rate of apoptosis in human colon adenocarcinoma cells (HT-29). The results showed that all compounds tested reduce cell viability in human colon cancer cells. 3,4-DHPAA promoted the highest effect antiproliferative with an increase in the percentage of cells in G0/G1 phase, accompanied by a reduction of cells in G2/M phase. Cell cycle analysis of VA and FA showed a decrease in the proportion of cells in G0/G1 phase (10.0 µM and 100.0 µM). p-CoA and FA acids increased the percentage of apoptotic cells and non-apoptotic cells. 3,4-DHPAA seems to be the substance with the greatest potential for in vivo studies, opening thus a series of perspectives on the use of these compounds in the prevention and treatment of colon cancer. View Full-Text
Keywords: phenolic acid; colon cancer; cell cytotoxicity phenolic acid; colon cancer; cell cytotoxicity
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Rosa, L.D.S.; Jordão, N.A.; Da Costa Pereira Soares, N.; DeMesquita, J.F.; Monteiro, M.; Teodoro, A.J. Pharmacokinetic, Antiproliferative and Apoptotic Effects of Phenolic Acids in Human Colon Adenocarcinoma Cells Using In Vitro and In Silico Approaches. Molecules 2018, 23, 2569.

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