Preparation and in vitro anticoagulant activities of alginate sulfate and its quaterized derivatives

• Published in: Carbohydrate polymers Vol. 52; no. 1; pp. 19 - 24
• Main Authors: Ronghua, Huang, Yumin, Du, Jianhong, Yang
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.04.2003; Elsevier Science
• Subjects: Alginate sulfate; Anticoagulant activity; Applied sciences; Biological and medical sciences; Blood. Blood coagulation. Reticuloendothelial system; Exact sciences and technology; Medical sciences; Natural polymers; Pharmacology. Drug treatments; Physicochemistry of polymers; Quaterization; Starch and polysaccharides; Alginate sulfate; Quaterization; Anticoagulant activity; Anticoagulant; Alginates; Experimental study; In vitro; Biological activity; Sulfatation; Polyelectrolyte; Chemical modification; Structure activity relation; Preparation; Organic sulfate; Oside polymer; Quaternary ammonium polymer
• ISSN: 0144-8617; 1879-1344
• DOI: 10.1016/S0144-8617(02)00258-8

Alginate sulfate (AS) and its ***quaterized derivatives (QAS-1, QAS-2, and QAS-3) were prepared from sodium alginate. Their structure was characterized by elemental analysis, FT-IR, 13C NMR, and gel permeation chromatography. The in vitro coagulation assay of human plasma containing the sulfates indicated that AS had considerably high anticoagulant activity especially to the intrinsic coagulation pathway. Its APTT reached 226s at 16.7μg/ml, comparing to that of heparin 125s at 10μg/ml. After quaterization the anticoagulant activities of QAS-1, QAS-2, and QAS-3 decreased as the degree of substitution of quaterization increased. The lowest one was given by QAS-3, which gave APTT as 260s at 66.7μg/ml, while AS did as 24min at the same concentration. It could be concluded that AS could be used as a novel anticoagulant drug, and its quaterized derivatives, which contained a great many of sulfate groups but low anticoagulant activity, might have potential application in other field such as anti-HIV.