Method for preparing low molecular weight heparin with high activity

A low-molecular-weight heparin, active technology, applied in the field of biomedicine, to achieve the effects of increased activity, reduced production costs, and huge industrial application value
CN101591401AInactive Publication Date: 2009-12-02JIANGNAN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
JIANGNAN UNIV
Publication Date
2009-12-02
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for preparing low molecular weight heparin with high activity, which is characterized in that the prior low molecular weight heparin with low anticoagulant activity is used as a substrate, a PAPS (3'-phosphoadenosine-5'-phosphoric acid sulfuric acid) regeneration system is adopted, and a heparin biosynthetic enzyme 3-O-sulfate-transferase is used for modifying the substrate to obtain the low molecular weight heparin with high anticoagulant activity; and the PAPS regeneration system can use extremely cheap PNPS (p-nitryl potassium phenolsulfonate) as an enzyme-modified reactive sulfate donor to further save the cost and make the industrialization possible. The method adopts the 3-O-sulfate-transferase with high enzyme activity to combine with the PAPS regeneration system, performs selective modification on the low molecular weight heparin, and increases the number of anticoagulant activity centers so as to greatly improve the anti-thrombosis activity of the heparin. The method provides a path for the enzymatic industrial production of the low molecular weight heparin with high activity.
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Description

technical field

[0001] The invention relates to a method for preparing high-activity low-volume heparin. It belongs to the field of biomedicine. Background technique

[0002] Heparin is a polysaccharide formed by hexuronic acid (L-iduronic acid, D-glucuronic acid) and D-glucosamine sulfate alternately with 1-4 glycosidic bonds, its molecular weight is between 3000-40000Da, and the average molecular weight is 15000Da; Heparin has been used as an anticoagulant and antithrombotic agent for more than 60 years. The anticoagulant activity of heparin is mainly through the binding of antithrombin (AT-III) at the pentose sugar active center containing 3-glucosamine at position 3-position, inducing its conformational change, thus showing anticoagulant activity. The anticoagulant activity of heparin includes antithrombotic activity (anti-factorXa) and anticoagulant (anti-factor IIa) activity. Anticoagulant activity is also related to the molecular weight of heparin. However, becaus...

Claims

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