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Application of polyguluronic acid propyl sulfate in preparation of anticoagulant medicine

The technology of propyl guluronic acid and polyguluronic acid is applied in the application field of poly propyl guluronic acid sulfate in the preparation of anticoagulant drugs, and can solve the problem of strong side effects of anticoagulant drugs. , easy pollution and other problems, to achieve significant anticoagulant effect, less toxic and side effects, and enhance the effect of the fibrinolytic system

Active Publication Date: 2020-09-04
MARINE BIOMEDICAL RES INST OF QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aiming at the disadvantages of strong side effects and easy pollution of anticoagulant drugs in the prior art, the present invention provides the application of polyguluronate propyl sulfate in the preparation of anticoagulant drugs. The present invention proves that polygulose Propyl erythoxylate sulfate has a strong anticoagulant effect and has the technical prospect of being developed into an anticoagulant drug

Method used

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  • Application of polyguluronic acid propyl sulfate in preparation of anticoagulant medicine
  • Application of polyguluronic acid propyl sulfate in preparation of anticoagulant medicine
  • Application of polyguluronic acid propyl sulfate in preparation of anticoagulant medicine

Examples

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Embodiment 1

[0023] Embodiment 1: the preparation of polyguluronic acid propyl ester sulfate

[0024] The invention uses polyguluronic acid (Mw=12.83kDa, purity 80.0%) as a starting material, and prepares polyguluronic acid propyl sulfate through propyl esterification and sulfate esterification.

[0025] The preparation method of the polyguluronic acid propyl ester sulfate is as follows: weigh 10.00 g of polyguluronic acid, add 5.00 mL of ethanol-water mixed solution, stir evenly, and swell overnight. After adding 40.00mL of 1,2-propylene oxide (density 0.83g / mL) into the reaction flask, stir and add 0.08g NaOH, add 10.00g of polyguluronic acid swollen overnight, and reflux at 36°C Reaction 8h. After the reaction, the precipitate was washed three times with 85% ethanol solution, and the obtained sandy precipitate was vacuum-dried overnight to obtain polypropyl guluronate.

[0026] In an ice bath, slowly drop 16.00 mL of chlorosulfonic acid (density 1.77 g / mL) into 70.79 mL of anhydrous f...

Embodiment 2

[0033] Example 2: Effect of polyguluronic acid propyl sulfate on mouse coagulation time (CT) and bleeding time (BT)

[0034] Forty male Kunming mice of 18-22 g were randomly divided into blank group, heparin group, PSS group and PGGS group, with 10 mice in each group. Adaptive feeding for 7 days. All were administered by intraperitoneal injection, and the administration volume was 0.1mL / 10g. The blank group was given the same amount of normal saline, the heparin group was given a dose of 15 mg / kg, and the doses of the PSS group and the PGGS group were both 28 mg / kg. kg. After 30 minutes of administration, a capillary glass tube was inserted into the venous plexus of the mouse's inner canthus to take blood, and the time from blood collection to the appearance of coagulation filaments was recorded as the index of testing coagulation time (CT); Transect, and start timing to record the time from the natural outflow of blood to the natural cessation of blood, which is the indicat...

Embodiment 3

[0039] Example 3: Effect of polyguluronic acid propyl ester sulfate on platelet aggregation

[0040] The effect of polyguluronic acid propyl sulfate on platelet aggregation was evaluated by ADP-induced platelet aggregation in mouse plasma.

[0041] Get 84 male Kunming mice of 22-26g, be randomly divided into blank group, clopidogrel group, heparin group, PGGS administration group (different dosage, low dose 10mg / kg, middle dose 50mg / kg, high dose 100mg / kg) 12 in each group. Adaptive feeding for 3 days. The clopidogrel group was administered by intragastric administration, and the rest were administered by intraperitoneal injection, with an administration volume of 0.1 mL / 10 g, for 7 consecutive days. 30 minutes after the last administration, the eyeballs were picked to take blood, and immediately mixed with sodium citrate at a ratio of 1:9, and then centrifuged at 3000rpm for 10 minutes to prepare plasma. ADP was used as an inducer to measure the platelet aggregation rate. T...

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Abstract

The invention provides application of propyl polyguluronate sulfate in the preparation of anticoagulants. The molecular skeleton of the propyl polyguluronate sulfate is linear glycosidic polymer formed by connecting L-guluronic acid through alpha-(1,4) glucosidic bond having the following structural formula shown in the scpecification, wherein R is CH2CH (OH)CH3 or CH2CH (OSO3-)CH3 or metal cation, R ' is H or SO<3><->, n is not more than 100. As prove by experiments, that propyl polyguluronate sulfate can be use for the treatment of hypercoagulable diseases such as thrombosis, and has low bleeding risk, and is mainly characterized in that the blood coagulation time in mice is remarkably prolon, the aggregation of platelets is inhibited, and the activity of the fibrinolysis system is improved, but the bleeding time is not prolonged significantly. The propyl polyguluronate sulfate is used for the treatment of hypercoagulable diseases such as thrombus. A series of experiments prove thatthe propyl polyguluronate sulfate can be developed into an anticoagulant drug and has a broad development and application prospect.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to the application of polyguluronic acid propyl sulfate in the preparation of anticoagulant medicines. Background technique [0002] The formation of local blood clots is the main cause of myocardial infarction and stroke and other arterial diseases and venous embolism diseases and the death of patients. It has the characteristics of high morbidity, disability and mortality, and seriously threatens human life. healthy. Anticoagulant drugs can prolong the blood coagulation process by affecting certain coagulation factors in the coagulation process, so as to prevent and treat diseases such as vascular embolism or thrombosis, and play an important role in preventing the occurrence and development of stroke and other thrombotic diseases. [0003] Currently the most widely used anticoagulant drugs are heparin and low molecular weight heparin extracted from the small intestinal mucos...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/737A61P7/02C08B37/00
CPCA61K31/737C08B37/0084
Inventor 管华诗李春霞辛萌何小溪李全才于广利赵峡
Owner MARINE BIOMEDICAL RES INST OF QINGDAO CO LTD
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