Partial characterization and anticoagulant activity of sulfated galactan from the green seaweed Halimeda opuntia.

The number of deaths associated with cardiovascular diseases (CVD) increases every year, leading to an intense search for new compounds that may be employed as anticoagulants. One of the classes of bioprospected molecules comprises sulfated polysaccharides (SP) from seaweed, as heparin displays many adverse effects associated with its use. The present study aimed to characterize and evaluate the anticoagulant potential of SP extracted from the green algae Halimeda opuntia. Four PS-rich fractions, F23, F44, F60 and F75, were obtained by proteolytic digestion in papain followed by ethanol precipitation. The presence of SP was confirmed by agarose gel electrophoresis, revealing different populations in each fraction. The F44 fraction is noteworthy compared to the other fractions, presenting a 5% yield compared to the initial algae weight and anticoagulant activity revealed by the activated partial thromboplastin time (APTT) assay (intrinsic/common coagulation pathway). Surprisingly, F44 purification (SP peak P1F44) resulted in prothrombin time (PT) activity (extrinsic coagulation pathway) at a 160 µg/mL, in addition to enhanced APTT activity. The P1F44 anticoagulant activity mechanism was shown to be dependent on two coagulations factors, IIa and Xa, more potent via IIa. Future assessments will be performed to assess this fraction in the medical clinic.

Insights on chemical-biological correlations learned from investigations on the sulfated galactan from the marine alga Bothryocladia occidentalis.

Marine organisms have been proven to be a valuable source of bioactive compounds. Among them, we highlight the sulfated galactans (SGs) from seaweeds, which besides being massively exploited as industrial thickening and gelling agents (agarans and carrageenans), have also shown promising pharmacological properties. Investigations on the non-agaran/-carrageenan SG from the red algae Bothryocladia occidentalis (SGBo) have demonstrated clear correlations between physical-chemical features and biological activities. SGBo is composed of 2,3-disulfated (~33%) or 2-sulfated (33%) α-D-galactose linked to non- or 2-sulfated ß-D-galactose repetitive disaccharide units. The notable serpin-dependent/-independent anticoagulant activity of SGBo (~130 international units [IU]/mg) is higher than those of other SGs containing less 2,3-disulfated α-D-galactose units and their low-molecular-weight derivatives, and thus is directly correlated to its high molecular mass (>200 kDa) and sulfation pattern. Although SGBo has antithrombotic efficacy equivalent to heparin and decreased bleeding potential at low-doses, high-doses substantially increase thrombus formation in animal models. Such an odd dose-dependent dual antithrombotic/prothrombotic activity has been attributed to the ability of SGBo to activate factor XII. In addition to anticoagulant properties, SGBo also exerts antimalarial, antileishmanial and antiophidic activities, and, therefore, has a remarkable potential for the research and development of novel drugs.