Derivate of low molecular weight fucosylated glycosaminoglycan and medical composition and preparation method and application thereof

A glycosaminoglycan, low molecular weight technology, applied in the field of medicine, can solve the problems of bleeding tendency bleeding, uncontrollable degree of product depolymerization, danger and the like

Active Publication Date: 2013-06-12
JIUZHITANG +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Antithrombotic drug therapy is the basic means of clinical prevention and treatment of thrombotic diseases, but antithrombotic drugs including fibrinolytic, anticoagulant, and antiplatelet drugs all have major and common defects: bleeding tendency and serious bleeding risk
The advantage of the peroxidative depolymerization method is t

Method used

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  • Derivate of low molecular weight fucosylated glycosaminoglycan and medical composition and preparation method and application thereof
  • Derivate of low molecular weight fucosylated glycosaminoglycan and medical composition and preparation method and application thereof
  • Derivate of low molecular weight fucosylated glycosaminoglycan and medical composition and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0131] [Example 1]

[0132] Preparation of low molecular weight fucosylated glycosaminoglycan derivative (dLFG) derived from Thelenota ananas:

[0133] 1.1 Material

[0134] Plum Ginseng (Thelenota ananas Jaeger), commercially available, visceral and dry body wall; benzethonium chloride, benzyl chloride, tetrabutylammonium hydroxide (TBA), N,N-dimethylformamide (DMF), hydroxide The reagents used in sodium, sodium chloride and ethanol are all commercially available analytical reagents.

[0135] 1.2 method

[0136] (1) Extraction and preparation of FGAG (FGAG from Thelenota ananas, TAG) derived from plum ginseng: Take 300 g of dried plum ginseng body wall, and refer to literature method (Kariya et al., J Biol Chem, 1990, 265(9): 5081-5085 ) TAG was prepared with a yield of about 1.5%, a purity of 98% (HPGPC, area normalization method), and a weight average molecular weight (Mw) of 65,890 Da.

[0137] (2) Preparation of TAG quaternary ammonium salt: Take 1.2g of TAG obtained in step (1) a...

Example Embodiment

[0167] [Example 2]

[0168] β-elimination and depolymerization of TAG to prepare series of molecular weight oligomeric fucosylated glycosaminoglycan derivatives (dLFG):

[0169] 2.1 Material:

[0170] The TAG derived from plum ginseng was prepared with the method described in Example 1. Other reagents are the same as in Example 1.

[0171] 2.2 Method

[0172] (1) Preparation of TAG quaternary ammonium salt: Prepare 5.02 g of TAG quaternary ammonium salt according to the method described in Example 1.

[0173] (2) Preparation of TAG benzyl esters with different degrees of benzyl esterification: the TAG quaternary ammonium salt obtained in step (1) was dissolved by adding 50 mL of DMF, adding 25 mL of benzyl chloride, and reacting under stirring at 35°C. And take a sample of about 15mL at different reaction times, respectively add 1:9 (v / v) saturated NaCl-100mL of absolute ethanol to the taken out solution, centrifuge at 3500rpm for 20min, the resulting precipitate is 50mL 1:9 (v / v) satu...

Example Embodiment

[0183] [Example 3]

[0184] Preparation of β-elimination depolymerization products of FGAG from different sea cucumbers:

[0185] 3.1 Materials

[0186] Apostichopus japonicus, Holothuria edulis, Ludwigothurea grisea, Holothuria leucospilota, and Holothuria nobilis are all commercially available dry bodies.

[0187] 3.2 Method

[0188] (1) Crush the dried body walls of imitation sea cucumber, red belly sea cucumber, Brazilian ginseng, jade-foot sea cucumber, and black-milk sea cucumber, respectively take 300g of the pulverized material, and extract the FGAG contained in it as described in the method (1) of Example 1, and weigh them respectively These are AJG, HEG, LGG, HLG and HNG.

[0189] (2) Take about 1g of AJG, HEG, LGG, HLG and HNG respectively, and prepare the β-elimination and depolymerization products dLFG according to the methods (2) to (5) described in the examples, which are called dAJG, dHEG, dLGG, HLG and dHNG. The basic steps of the depolymerization of the FGAG β elimin...

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Abstract

The invention provides a derivate of low molecular weight fucosylated glycosaminoglycan (dLFG) and a medical composition containing the dLFG or pharmaceutically acceptable salt and application of the dLFG and the medical composition for preparing medicines for treating thrombotic diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a low molecular weight fucosylated glycosaminoglycan derivative (derivate of Low molecular weight Fucosylated Glycosaminoglycan, dLFG) with anticoagulant activity, its preparation method, containing the dLFG or its pharmaceutical The pharmaceutical composition of the above acceptable salt, and the application of dLFG and its pharmaceutical composition in the preparation of drugs for the treatment of thrombotic diseases. Background technique [0002] Thromboembolic diseases, including ischemic stroke, coronary heart disease, and venous thromboembolism, are the main cause of death in humans. Antithrombotic drug therapy is the basic method for clinical prevention and treatment of thrombotic diseases, but antithrombotic drugs including fibrinolytic, anticoagulant, and antiplatelet drugs all have major and common defects: bleeding tendency and serious bleeding risk. [0003] The cla...

Claims

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Application Information

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IPC IPC(8): C08B37/00A61K31/726A61P7/02
Inventor 赵金华刘吉开吴明一高娜卢锋李姿
Owner JIUZHITANG
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