Flavonoids with an Oligopolysulfated Moiety A New Class of Anticoagulant Agents

• Tipo: Artigo em Revista Científica Internacional
• Data: 2011

Autores

Marta Correia da Silva (Autor) Outra; Emilia Sousa (Autor) FFUP; Barbara Duarte (Autor) Outra; Franklim Marques (Autor) FFUP; Felix Carvalho (Autor) FFUP; Luis M Cunha Ribeiro (Autor) Outra; Madalena M M Pinto (Autor) FFUP

Revista

Título: Journal of Medicinal Chemistry

Vol. 54 Nº 1

Páginas: 95-106

ISSN: 0022-2623

Editora: American Chemical Society

Indexação

ISI Proceedings

ISI Web of Knowledge - 48 Citações

Scopus - 51 Citações

Classificação Científica

FOS: Ciências médicas e da saúde > Medicina básica

Outras Informações

ID Authenticus: P-002-VVM

DOI: 10.1021/jm1013117

Abstract (EN): Polysulfated (oligo)flavonoids were synthesized and assayed for their in vitro and in vivo anticoagulant activities The approach was based on molecular hybridization of two classes of anticoagulants, sulfated polysaccharides and sulfated flavonoids The synthesis was optimized using microwave-assisted sulfation with triethylamine-sulfur trioxide The obtained polysulfated flavonosides were highly effective in increasing clotting times and able to completely block the clotting process, in contrast to their corresponding aglycones The thromboelastography proved that polysulfated flavonosides possess good whole blood anticoagulation activity The following structure activity relationships were found 3-O-rutinosides (10, 13) were direct inhibitors of FXa, while 7-O-rutinosides (7, 8) showed inhibition of FXa by ATIII activation Furthermore, compounds 7 and 13 were stable in plasma and active in vivo and preliminary toxicity studies would lead us to rule out acute side effects From the overall results, the polysulfated flavonosides showed the potential as new effective and safe agents for anticoagulant therapy

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 12