Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 22, Issue 14, Pages -Publisher
MDPI
DOI: 10.3390/ijms22147604
Keywords
Fucus vesiculosus; phlorotannins; antitumor; gastric cancer; colorectal cancer; cell cycle arrest; apoptosis; UHPLC; flow cytometry
Funding
- Operational Programme for Competitiveness and Internationalization POCI, within the European Regional Development Fund (FEDER) [PTDC/BAA-AGR/31015/2017]
- Science and Technology Foundation (FCT)
- Fundação para a Ciência e a Tecnologia [PTDC/BAA-AGR/31015/2017] Funding Source: FCT
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This study found that phlorotannin samples from Fucus vesiculosus exhibit specific cytotoxicity against gastrointestinal tumor cell lines without affecting normal cell viability. Among the tested fractions, F5 showed the highest activity against colorectal and gastric cancer cells, inducing cell death via apoptosis and necrosis. UHPLC-MS analysis identified compounds such as eckstolonol and fucofurodiphlorethol as potentially responsible for the observed cytotoxic effects.
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 Fucus vesiculosus-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 F. vesiculosus 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 F. vesiculosus 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 F. vesiculosus phlorotannin-rich extracts.
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