Process for producing desulfated polysaccharide, and desulfated heparin
AssigneeSeikagaku Corporation
InventorsSaburo Hara, Keiichi Yoshida, Masayuki Ishihara
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Abstract
This invention relates to a process for producing a desulfated polysaccharide, which comprises reacting a sulfated polysaccharide having a saccharide in which a primary hydroxyl group is sulfated, as a constituent sugar, with a silylating agent represented by the following formula (I) 1 wherein R1s are the same or different and each represent a hydrogen atom or a halogen atom, R2 represents a lower alkyl group, and R3s are the same or different and each represent a lower alkyl group, an aryl group or a halogen atom, and a desulfated heparin obtained by this production process.
Claims14
A process for producing a desulfated polysaccharide, which comprises reacting a sulfated polysaccharide having a saccharide in which a primary hydroxyl group is sulfated, as a constituent sugar, with a silylating agent represented by the following formula (I)
- 3
- wherein R1s are the same or different and each represent a hydrogen atom or a halogen atom, R2 represents a lower alkyl group, and R3s are the same or different and each represent a lower alkyl group, an aryl group or a halogen atom,
- to selectively desulfate a sulfate group bonded to the primary hydroxyl group.
A selectively desulfated heparin which comprises having the following characteristics:
- (1) in an unsaturated disaccharide composition measured by using enzymatic digestion and high performance liquid chromatography, the ΔDiHS-tri(U,6,N)S content is 10 to 40%, and the ΔDiHS-di(U,N)S content is 30 to 60%,
- (2) the content of a disaccharide containing an N-substituted sulfate group is 75 to 95%,
- (3) the weight average molecular weight is 4,000 to 30,000 dalton,
- (4) the anti-thrombin activity is 20 U/mg to-150 U/mg, and
- (5) the effect of accelerating the activity of a basic fibroblast growth factor to cellular proliferation is maintained to be 80% or more of that of heparin which is not desulfated.
Dependencies are inferred from the claim text.