The Key Role of Sulfation and Branching on Fucoidan Antitumor Activity

Abstract

There is an urgent need for antitumor bioactive agents with minimal or no side effects over normal adjacent cells. Fucoidan is a marine-origin polymer with known antitumor activity. However, there are still some concerns about its application due to the inconsistent experimental results, specifically its toxicity over normal cells and the mechanism behind its action. Herein, three fucoidan extracts (FEs) have been tested over normal and breast cancer cell lines. From cytotoxicity results, only one of the extracts shows selective antitumor behavior (at 0.2 mg mL ), despite similarities in sulfation degree and carbohydrates composition. Although the three FEs present different molecular weights, depolymerization of selected samples discarded M as the key factor in the antitumor activity. Significant differences in sulfates position and branching are observed, presenting FE 2 the higher branching degree. Based on all these experimental data, it is believed that these last two properties are the ones that influence the cytotoxic effects of fucoidan extracts.

Fucoidan Inhibition of Osteosarcoma Cells is Species and Molecular Weight Dependent

“…Fucoidans from various different species of brown seaweed have been studied for anti-cancer applications. While most of the research revolves around more common forms of cancer, such as breast and colon cancer [6], use of fucoidan against osteosarcoma has recently been a keen area of interest [31][32][33], as even though it is a relatively less common cancer, the implications can be severe [34]. For the first time, here, we investigated the variable effects of crude fucoidan derived from two different species of brown algae, namely, F. vesiculosus (commercial source) and S. filipendula (derived from Colombian coast), and further evaluated the effect of different molecular weight fractions from 10-50 kDa (LMW), 50-100 kDa (MMW) and >100 kDa (HMW) fractions of fucoidan from S. filipendula on MG63 human osteosarcoma cells.…”

Crude Fucoidan Extracts Impair Angiogenesis in Models Relevant for Bone Regeneration and Osteosarcoma via Reduction of VEGF and SDF-1

“…The co-cultures consisted of bone marrow derived mesenchymal stem cells, respectively the osteosarcoma cell line MG63, and human blood derived endothelial cells (Outgrowth endothelial cells (OEC)) [14,15]. As demonstrated in a large number of in vitro and in vivo, studies fucoidans shows anti-viral [16,17], anti-tumor [18,19,20], anti-oxidant [21], anti-inflammatory [22] and anti-coagulant [23] properties.…”

Effect of Hydrolyzed Fucoidan from The Brown Seaweed Sargassum Binderi Sonder Towards Human Breast Cancer T47d Cell Lines

“…These factors contribute to the fact that fucoidan structure is complex (Shevchenko et al, 2015). Apart from its complex structures, fucoidan has been found to inhibit the growth of cancer cells (Oliver, Ramon, Andreia, & Tiago, 2017;Vishchuk, Ermakova, & Zvyagintseva, 2013;Usui, Asari, & Mizuno., 1980;Isnansetyo et al, 2017).…”

“…General aspects that influence the fucoidan bioactivity are monosaccharide composition, sulfate content, molecular weight, binding model/ position, and the arrangement of monosaccharide residues. The number of branching sulfate groups also appears to be the key of higher bioactivities fucoidan since it highly affects the negatively charged fucoidan that inhibit the cancer cell proliferation (Oliver, Ramon, Andreia, & Tiago, 2017). In this study, fucoidan depolymerization was carried out by acid hydrolysis method with trifluoroacetic acid (TFA) at various concentrations and incubation times.…”