Heparins and heparinoids: Occurrence, structure and mechanism of antithrombotic and hemorrhagic activities
Nader, Helena Bonciani [UNIFESP]
Lopes, Carla C.
Rocha, Hugo Alexande de Oliveira [UNIFESP]
Santos, Elizeu Antunes dos [UNIFESP]
Dietrich, Carl Peter [UNIFESP]
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The correlation between structure, anticloting, antithrombotic and hemorrhagic activities of heparin, heparan sulfate, low molecular weight heparins and heparin-like compounds from various sources that are in used in clinical practice or under development is briefly reviewed. Heparin-like molecules composed exclusively of iduronic acid 2-O-sulfate residues have weak anticloting activities, whereas molecules that contain both iduronic acid 2-O sulfate, iduronic acid and small amounts or glucuronic acid, such as heparin, or mixed amounts of glucuronic and iduronic acids (mollusk heparins) possess high anticloting and anti-Xa activities. These results also suggest that a proper combination of these elements might produce a strong antithrombotic agent. Heparin isolated from shrimp mimics the pharmacological activities of low molecular weight heparins. A heparan sulfate derived from bovine pancreas and a sulfated fucan from brown algae have a potent antithrombotic activity in arterial and venous thrombosis model in vivo with a negligible activity upon the serine-proteases of the coagulation cascade in vitro. These and other results led to the hypothesis that antithrombotic activity of heparin and other antithrombotic agents is due at least in part by their action on endothelial cells stimulating the synthesis of an antithrombotic heparan sulfate. All the antithrombotic agents derived from heparin and other heparinoids have hemorrhagic activity. Exceptions to this are a heparan sulfate from bovine pancreas and a sulfated fucan derived from brown algae, which have no hemorrhagic activity but have high antithrombotic activities in vivo. Once the structure of these compounds are totally defined it will be possible to design an ideal antithrombotic.
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LACK of CORRELATION BETWEEN INVITRO and INVIVO ANTITHROMBOTIC ACTIVITY of HEPARIN FRACTIONS and RELATED-COMPOUNDS - HEPARAN-SULFATE AS AN ANTITHROMBOTIC AGENT INVIVO Bianchini, P.; Osima, B.; Parma, B.; Nader, H. B.; Dietrich, C. P. (Elsevier B.V., 1985-12-01)
A sulfated polysaccharide, fucans, isolated from brown algae Sargassum vulgare with anticoagulant, antithrombotic, antioxidant and anti-inflammatory effects Guerra Dore, Celina Maria P.; Faustino Alves, Monique Gabriela das C.; Pofirio Will, Luiza Sheyla E.; Costa, Thiago G.; Sabry, Diego A. [UNIFESP]; Souza Rego, Leonardo Augusto R. de; Accardo, Camila de Melo [UNIFESP]; Rocha, Hugo Alexandre O. .; Filgueira, Luciana Guimaraes A.; Leite, Edda Lisboa (Elsevier B.V., 2013-01-02)Fucan (SV1) sulfated polysaccharides from the brown algae Sargassum vulgare were extracted, fractionated in acetone and examined with respect to chemical composition, anticoagulant, anti-inflammatory, antithrombotic effects ...
Structural and hemostatic activities of a sulfated galactofucan from the brown alga Spatoglossum schroederi - An ideal antithrombotic agent? Rocha, Hugo Alexandre Oliveira [UNIFESP]; Moraes, Fabio A. [UNIFESP]; Trindade, Edvaldo da Silva [UNIFESP]; Franco, CRC; Torquato, Ricardo José Soares [UNIFESP]; Veiga, Silvio Sanches [UNIFESP]; Valente, A. P.; Mourao, PAS; Leite, E. L.; Nader, Helena Bonciani [UNIFESP]; Dietrich, Carl Peter [UNIFESP] (Amer Soc Biochemistry Molecular Biology Inc, 2005-12-16)The brown alga Spatoglossum schroederi contains three fractions of sulfated polysaccharides. One of them was purified by acetone fractionation, ion exchange, and molecular sieving chromatography. It has a molecular size ...