Heparins and heparinoids: Occurrence, structure and mechanism of antithrombotic and hemorrhagic activities

Heparins and heparinoids: Occurrence, structure and mechanism of antithrombotic and hemorrhagic activities

Autor Nader, Helena Bonciani Autor UNIFESP Google Scholar
Lopes, Carla C. Google Scholar
Rocha, Hugo Alexande de Oliveira Autor UNIFESP Google Scholar
Santos, Elizeu Antunes dos Autor UNIFESP Google Scholar
Dietrich, Carl Peter Autor UNIFESP Google Scholar
Instituição Universidade Federal de São Paulo (UNIFESP)
Resumo 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.
Assunto heparins
occurrence and structural variability
anticloting and hemorrhagic activity
antithrombotic activity and mechanism of action
LMW-heparins and heparinoids
antithrombotic activity
antithrombotic agents and vascular endothelial cells
antithrombotic heparan sulfate and fucans.
Idioma Inglês
Data 2004-01-01
Publicado em Current Pharmaceutical Design. Hilversum: Bentham Science Publ Ltd, v. 10, n. 9, p. 951-966, 2004.
ISSN 1381-6128 (Sherpa/Romeo, fator de impacto)
Editor Bentham Science Publ Ltd
Extensão 951-966
Fonte http://dx.doi.org/10.2174/1381612043452758
Direito de acesso Acesso restrito
Tipo Resenha
Web of Science WOS:000220273900003
URI http://repositorio.unifesp.br/handle/11600/27579

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