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Titolo:
Anticoagulant sulfated polysaccharides: Part I. Synthesis and structure-activity relationships of new pullulan sulfates
Autore:
Alban, S; Schauerte, A; Franz, G;
Indirizzi:
Univ Regensburg, Inst Pharm, D-93040 Regensburg, Germany Univ Regensburg Regensburg Germany D-93040 , D-93040 Regensburg, Germany
Titolo Testata:
CARBOHYDRATE POLYMERS
fascicolo: 3, volume: 47, anno: 2002,
pagine: 267 - 276
SICI:
0144-8617(20020215)47:3<267:ASPPIS>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
MOLECULAR-WEIGHT; HEPARIN; CHROMATOGRAPHY; DERIVATIVES; DEPENDENCE; DEXTRAN; FUCANS; ACID;
Keywords:
sulfated polysaccharides; pullulan sulfates; partial synthesis; anticoagulant activity; structure-activity relationships;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Agriculture,Biology & Environmental Sciences
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
46
Recensione:
Indirizzi per estratti:
Indirizzo: Alban, S Univ Regensburg, Inst Pharm, Univ Str 31, D-93040 Regensburg, Germany Univ Regensburg Univ Str 31 Regensburg Germany D-93040 , Germany
Citazione:
S. Alban et al., "Anticoagulant sulfated polysaccharides: Part I. Synthesis and structure-activity relationships of new pullulan sulfates", CARBOHY POL, 47(3), 2002, pp. 267-276

Abstract

In order to develop new anticoagulants as potential heparin alternatives, two pullulans with different molecular weight (MW) were used as starting polymers for the partial synthesis of a structurally new class of sulfated polysaccharides. Sulfation of these linear alpha- 1,4-/1,6-glucans was carried out by a method with a SO3-pyridine complex in DMF, which had been optimized for the modification of beta -1,3-glucans. Modifications of this methods resulted in pullulan sulfates with degrees of sulfation (DS) ranging from0.17 to 1.99 and MW between 15 and 250 kDa. More than 50% of the sulfate groups were bound to the secondary C atoms in positions 2, 3 and 4 of the glucose monomers. The anticoagulant activity of the obtained pullulan sulfates was determined in the coagulation assays prothrombin time (PT), activatedpartial thromboplastin time (APTT), Heptest((R)) and thrombin time (TT). They represent potent anticoagulants reaching the efficacy of heparin. Theiractivity not only improves with increasing DS and MW, but also: with increasing part of sulfate groups in positions 2, 3 and 4. In addition, their action profile changes in dependence on their individual structure as reflected by the ratio of the TT- to the APTT-activity. The pullulan sulfates specifically interfere with different stages of the coagulation cascade, and these interactions have different requirements on the chemical structure. (C)2002 Elsevier Science Ltd. All fights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 12:16:06