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

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dc.contributor.authorNader, Helena Bonciani [UNIFESP]
dc.contributor.authorLopes, Carla Cristina [UNIFESP]
dc.contributor.authorRocha, Hugo Alexandre de Oliveira [UNIFESP]
dc.contributor.authorSantos, Elizeu Antunes dos [UNIFESP]
dc.contributor.authorDietrich, Carl Peter [UNIFESP]
dc.contributor.institutionUniversidade Federal de São Paulo (UNIFESP)
dc.date.accessioned2016-01-24T12:34:14Z
dc.date.available2016-01-24T12:34:14Z
dc.date.issued2004-01-01
dc.description.abstractThe 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.en
dc.description.affiliationUniversidade Federal de São Paulo, Escola Paulista Med, Dept Bioquim, BR-04044020 São Paulo, Brazil
dc.description.affiliationUnifespUniversidade Federal de São Paulo, Escola Paulista Med, Dept Bioquim, BR-04044020 São Paulo, Brazil
dc.description.sourceWeb of Science
dc.format.extent951-966
dc.identifierhttps://dx.doi.org/10.2174/1381612043452758
dc.identifier.citationCurrent Pharmaceutical Design. Hilversum: Bentham Science Publ Ltd, v. 10, n. 9, p. 951-966, 2004.
dc.identifier.doi10.2174/1381612043452758
dc.identifier.issn1381-6128
dc.identifier.urihttps://repositorio.unifesp.br/handle/11600/27579
dc.identifier.wosWOS:000220273900003
dc.language.isoeng
dc.publisherBentham Science Publ Ltd
dc.relation.ispartofCurrent Pharmaceutical Design
dc.rightsAcesso restrito
dc.subjectHeparinsen
dc.subjectOccurrence and structural variabilityen
dc.subjectHeparinen
dc.subjectAnticloting and hemorrhagic activityen
dc.subjectAntithrombotic activity and mechanism of actionen
dc.subjectLMW-heparins and heparinoidsen
dc.subjectAntithrombotic activityen
dc.subjectAntithrombotic agents and vascular endothelial cellsen
dc.subjectAntithrombotic heparan sulfate and fucans.en
dc.titleHeparins and heparinoids: Occurrence, structure and mechanism of antithrombotic and hemorrhagic activitiesen
dc.typeResenha
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