Antitumor Activity of Fucus vesiculosus -Derived Phlorotannins through Activation of Apoptotic Signals in Gastric and Colorectal Tumor Cell Lines

• Published in: International journal of molecular sciences Vol. 22; no. 14; p. 7604
• Main Authors: Catarino, Marcelo D, Fernandes, Iva, Oliveira, Hélder, Carrascal, Mylene, Ferreira, Rita, Silva, Artur M S, Cruz, Maria Teresa, Mateus, Nuno, Cardoso, Susana M
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 16.07.2021; MDPI
• Subjects: antitumor; Antitumor activity; Apoptosis; Apoptosis - drug effects; Bioactive compounds; Biocompatibility; Biological activity; Caco-2 Cells; Cell activation; Cell cycle; cell cycle arrest; Cell death; Cell Line, Tumor; Chromatography, High Pressure Liquid - methods; Colon; Colorectal cancer; Colorectal Neoplasms - drug therapy; Colorectal Neoplasms - metabolism; Cytotoxicity; Fibroblasts; Flow cytometry; Flow Cytometry - methods; Fucus - metabolism; Fucus vesiculosus; Gastric cancer; Gastrointestinal system; Gastrointestinal tract; Gastrointestinal Tract - drug effects; Humans; Leukemia; Marine environment; Metabolites; Necrosis; Pancreatic cancer; phlorotannins; Plant Extracts - pharmacology; Seaweed - metabolism; Seaweeds; Signal Transduction - drug effects; Stomach Neoplasms - drug therapy; Stomach Neoplasms - metabolism; Tannins - pharmacology; Tumor cell lines; Tumors; Fucus vesiculosus; colorectal cancer; gastric cancer; antitumor; apoptosis; flow cytometry; UHPLC; cell cycle arrest; phlorotannins
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms22147604

Seaweeds are one of the largest producers of biomass in the marine environment and a source of multiple bioactive metabolites with valuable health benefits. Among these, phlorotannins have been widely recognized for their promising bioactive properties. The potential antitumor capacity of -derived phlorotannins remains, however, poorly explored, especially in gastrointestinal tract-related tumors. Therefore, this work aimed to evaluate the cytotoxic properties and possible mechanisms by which crude extract (CRD), phlorotannin-rich extract (EtOAc), and further phlorotannin-purified fractions (F1-F9) trigger cell death on different tumor cell lines of the gastrointestinal tract, using flow cytometry. The results indicate that samples exert specific cytotoxicity against tumor cell lines without affecting the viability of normal cells. Moreover, it was found that, among the nine different phlorotannin fractions tested, F5 was the most active against both Caco-2 colorectal and MKN-28 gastric cancer cells, inducing death via activation of both apoptosis and necrosis. The UHPLC-MS analysis of this fraction revealed, among others, the presence of a compound tentatively identified as eckstolonol and another as fucofurodiphlorethol, which could be mainly responsible for the promising cytotoxic effects observed in this sample. Overall, the results herein reported contribute to a better understanding of the mechanisms behind the antitumor properties of phlorotannin-rich extracts.