A purified oligosaccharide compound having antithrombotic activity or a mixture of a homologous compound thereof and a pharmaceutically acceptable salt thereof, a preparation method for the mixture, a pharmaceutical composition containing the mixture, and uses thereof serving as an intrinsic factor X-enzyme (Xase) inhibitor in the preparation of drugs for preventing and/or treating thrombotic diseases.
A preparation method of a sea cucumber polysaccharide, comprising the following steps: (1) taking dry sea cucumbers, pulverizing the dry sea cucumbers into coarse particles, adding water to conduct enzymatic hydrolysis, performing centrifugation and taking a supernatant, and concentrating the supernatant to 1/5 of an original volume under a reduced pressure, and then performing centrifugation again (under the same centrifugation conditions as above) and taking a supernatant; subjecting the supernatant to three times of salting out and alcohol precipitation, then washing the precipitation twice with absolute ethanol, and evaporating the ethanol to obtain a crude sea cucumber polysaccharide; (2) dissolving the crude sea cucumber polysaccharide in pure water, loading the solution into an anion chromatography column (OH -), eluting the anion chromatography column with pure water and NaCl solutions with gradient concentrations, and collecting an NaCl eluent; and (3) subjecting the NaCl eluent to ultrafiltration for desalination, and concentrating the ultrafiltered retentate under a reduced pressure and freeze-drying the concentrate, to give the sea cucumber polysaccharide. The sea cucumber polysaccharide can be used to prepare anti-hyperlipidemia, anti-oxidation, anti-coagulation, anti-tumor, immunity-enhancing drugs and the like or healthcare products, has the effect of preventing thrombosis, and has a good auxiliary preventive effect for the elderly and people with high thrombosis risks.
Provided is an active polypeptide, the sequence being VAPEEHPVLL. The polypeptide has anticoagulation and antiplatelet aggregation effects, and exhibits significant activity in the anticoagulation (APTT, PT and TT) and inhibition of ADP-induced platelet aggregation activity and other aspects.
Disclosed is a volumetric method for determining the content of a low-molecular-weight fucosylated glycosaminoglycan. A reference sample and a test sample are separately subjected to cation exchange treatment, and an alkaline titrant is added for titration. The volume of the titrant collectively consumed by sulfate and carboxylate is recorded. The content of fucosylated glycosaminoglycan in the low-molecular-weight fucosylated glycosaminoglycan test sample is obtained by means of comparison and calculation. The operation is simple, economical and efficient, such that the method is suitable for large-scale process production.
G01N 31/18 - Burettes specially adapted for titration
G01N 27/06 - Investigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating impedance by investigating resistance of a liquid
5.
METHOD FOR PURIFYING LOW-MOLECULAR WEIGHT FUCOSYLATED GLYCOSAMINOGLYCAN BY MEANS OF TANGENTIAL FLOW ULTRAFILTRATION
Provided is a method for purifying low-molecular weight fucosylated glycosaminoglycan by means of tangential flow ultrafiltration. The method comprises the following steps: (1) dissolving a crude product in a certain proportion of water, and filtering same to obtain a mother solution; (2) installing a 30 kd membrane bag ultrafiltration system, and carrying out ultrafiltration on the mother solution, and then collecting the ultrafiltrate; (3) carrying out ultrafiltration by using a 3 kd membrane bag ultrafiltration system to remove small molecule organic and inorganic matter, and sampling trapped fluid; (4) carrying out ultrafiltration by using a 10 kd membrane ultrafiltration system, and collecting a percolate; and (5) finally, carrying out concentration by using the 3 kd membrane ultrafiltration system. The method provided by the invention has the advantages of a high efficiency, rapidness, mild conditions and a high repeatability, and provides a stable ultrafiltration process with a consistent product quality between batches for industrial production.
A purified oligosaccharide compound having antithrombotic activity or a mixture of a homologous compound thereof and a pharmaceutically acceptable salt thereof, a preparation method for the mixture, a pharmaceutical composition containing the mixture, and uses thereof serving as an intrinsic factor X-enzyme (Xase) inhibitor in the preparation of drugs for preventing and/or treating thrombotic diseases.
A purified oligosaccharide compound having antithrombotic activity or a mixture of a homologous compound thereof and a pharmaceutically acceptable salt thereof, a preparation method for the mixture, a pharmaceutical composition containing the mixture, and uses thereof serving as an endogenous factor X-enzyme (Xase) inhibitor in the preparation of drugs for preventing and/or treating thrombotic diseases.
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
8.
Extract for preventing of treating thrombotic diseases
An extract for preventing or treating thrombotic diseases, particularly, an extract of at least one of leeches and earthworms having a molecular weight of no more than 5,800 daltons is provided, wherein the extract includes 15% to 38% amino acid, 40% to 60% saccharide and 0.3% to 1% hypoxanthine. Processes for preparation, pharmaceutical compositions and uses thereof are also provided. Compared to conventional arts, the extract has safety greatly improved and drug actions maintained and even improved.
A low-molecular-weight fucosylated glycosaminoglycan (aTFG) containing 2, 5-anhydrated talose, alditol, sugar amine or N-substituted sugar amine monosaccharide component thereof, preparation method thereof, pharmaceutical composition containing the aTFG, and use thereof for preventing and/or treating thrombus diseases; the aTFG has powerful anticoagulant activity acting on an endogenous coagulation factor X enzyme, and inhibiting thrombogenesis, and therefore can be used for drugs for preventing and/or treating cardiovascular and cerebrovascular diseases.
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
10.
LOW-MOLECULAR-WEIGHT GLYCOSAMINOGLYCAN DERIVATIVE, PHARMACEUTICAL COMPOSITION THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF
Provided are a low molecular weight fucosylated glycosaminoglycan derivative (derivate of Low molecular weight Fucosylated Glycosaminoglycan, dLFG) having anticoagulant activity, a preparation method therefor, a pharmaceutical composition comprising the dLFG or a pharmaceutically acceptable salt thereof, and the use of the dLFG and pharmaceutical composition thereof in preparing medicine for treating thrombotic diseases.
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