Sulfacted oilgosacharides having anticoagulant/antithrombotic activity

An oligosaccharide and anti-coagulation technology, which is applied in the direction of active carbohydrate ingredients, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems of low bioavailability, low-efficiency anticoagulants, and high molecular weight of heparin

Inactive Publication Date: 2004-08-11
AUSTRALIEN NAT UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Third, heparin can only be administered intravenously due to its high molecular weight, and its bioavailability is very low when injected subcutaneously (5,6)
These preparations retain the anticoagulant factor Xa and antithrombotic activity of native heparin, but they are low potency anticoagulants

Method used

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  • Sulfacted oilgosacharides having anticoagulant/antithrombotic activity
  • Sulfacted oilgosacharides having anticoagulant/antithrombotic activity
  • Sulfacted oilgosacharides having anticoagulant/antithrombotic activity

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Preparation of sulfated oligosaccharides

[0041] In this example, two sources of oligosaccharides were used for subsequent sulfation. The first raw material is an oligosaccharide derived from a natural polysaccharide compound. Its common preparation method includes enzymatic or chemical partial depolymerization of polysaccharides and fractionation of the obtained oligosaccharides according to size. Examples of polysaccharides used to produce oligosaccharides are amylose, dextran, cellulose, laminarin, pectin, chitin, chitosan, mannan, and phosphomannan produced by the yeast Pichia holstii exopolysaccharides. The second raw material is a fully synthetic oligosaccharide containing hexose, which is obtained by chemical polymerization of hexose monomers. A method of making such fully synthetic oligosaccharides is disclosed in the prior International Patent Application PCT / AU96 / 00238. Also described in the same patent application is a structure P-6-Man-α-(1→3)-Man-α-(1→...

Embodiment 2

[0043] Anti-aggregation effect of sulfated oligosaccharides

[0044] Table 1 summarizes the anticoagulant activity of 19 sulfated oligosaccharide compounds as measured by the activated partial thromboplastin time (APTT) test. Similar results were obtained from the thrombin time test. Initially, it was clear that the 11 tested sulfated oligosaccharides exhibited significantly more anticoagulant activity than heparin and tedeparin (LMW heparin). Chain length, monosaccharide composition and linkages all appear to be decisive factors. The effect of chain length is particularly pronounced on the maltose series, in which di-, tri- and tetrasaccharides are less active, while sulfate esters of maltopentaose, maltohexaose and maltoheptaose are quite effective anticoagulants (Table 1, figure 1 ). In addition, an unexpected feature of the maltose series is that the chain length increased by only one residue from maltotetraose to maltopentaose, but the anticoagulant activity was incre...

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Abstract

A method for the anticoagulant and / or antithrombotic treatment of a human or other warm-blooded animal patient in need of such treatment, comprises administration to the patient of an effective amount of at least one sulfated oligosaccharide, wherein the oligosaccharide has the general formula I: R1-(Rx)n-R2 wherein R1 and R2 and each Rx represents a monosaccharide unit, all of which may be the same or different, adjacent monosaccharide units being linked by 1}2, 1}3, 1}4 and / or 1}6 glycosidic bonds and n is an integer of from 1 to 6.

Description

field of invention [0001] The present invention relates to sulfated oligosaccharides, and in particular to the use of certain sulfated oligosaccharides as anticoagulant and / or antithrombotic agents. Background of the invention [0002] Heparin, a glycosaminoglycan produced by mammalian mast cells, has been widely used as an anticoagulant in the prevention of postoperative thrombosis and in the treatment of acute venous thrombosis over the past 50 years. The anticoagulant activity of heparin is mainly manifested in its ability to promote the inactivation of several key proteases in the coagulation cascade by the protease inhibitor antithrombin III, especially (coagulation) factor Xa and thrombin (1,2). Thrombin, on the other hand, is the terminal (transfer) enzyme that converts soluble fibrinogen to insoluble fibrin in a cascade. In fact, a specific pentameric saccharide compound in heparin has been identified that binds antithrombin III with high affinity and thereby causes...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/702A61K31/715A61K36/06A61P7/02
CPCA61K31/715A61P7/02
Inventor C·R·帕里施W·B·考登
Owner AUSTRALIEN NAT UNIV
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