Ursodesoxycholic acid and use thereof

A kind of use, technology of compound, application field in preventing and treating arterial thrombosis disease

Inactive Publication Date: 2015-07-01
SHANGHAIMED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cardiovascular use of ursodeoxyc

Method used

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  • Ursodesoxycholic acid and use thereof
  • Ursodesoxycholic acid and use thereof
  • Ursodesoxycholic acid and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] Example 1. Inhibitory effect of ursodeoxycholic acid on ADP-induced human platelet aggregation

[0085] The purpose of this example is to prove that ursodeoxycholic acid can inhibit ADP-induced aggregation of human platelets.

[0086] In this example, the platelets were prepared as follows: platelets were obtained from healthy volunteers who signed informed consent, and the volunteers did not take any antiplatelet drugs such as aspirin and clopidogrel within 20 days before blood collection. Anticoagulant ACD (85mmol L -1 Sodium citrate, 71.38mmol L -1 Citric acid, and 27.78mmolL -1 glucose). Centrifuge at 300xg for 20 minutes to obtain platelet-rich plasma, take the upper layer of platelet-rich plasma and centrifuge at 900xg for 10 minutes to obtain platelets, and finally resuspend with Tyrode's buffer (138mmol L -1 Sodium chloride (NaCl), 2.7mmol L -1 Potassium chloride (KCl), 2 mmol L -1 Magnesium Chloride (MgCl 2 ), 0.42 mmol L -1 Sodium dihydrogen phosphate ...

Embodiment 2

[0091] Example 2. Inhibitory effect of ursodeoxycholic acid 150 μM on human platelet aggregation induced by other various agonists

[0092]The purpose of this example is to prove that ursodeoxycholic acid can inhibit the aggregation of human platelets induced by thrombin and collagen.

[0093] In this example, the preparation of platelets and the aggregation induction and measurement methods of platelets are the same as those in Example 1. The results are shown in Table 2. Ursodeoxycholic acid at 150 μM inhibits thrombin (Chrono-log Company, Havertown, PA) (0.1 U / mL), and collagen (Chrono-log Company, Havertown, PA) (1 μg / mL) Induced aggregation of human platelets.

[0094] Table 2: Ursodeoxycholic acid inhibits thrombin- and collagen-induced aggregation of human platelets.

[0095] Ursodeoxycholic acid concentration (μM)

Embodiment 3

[0096] Example 3. Inhibitory effect of ursodeoxycholic acid on platelet spreading.

[0097] The purpose of this example is to prove that ursodeoxycholic acid can inhibit platelet spreading.

[0098] In this embodiment, the preparation of platelets is the same as in Example 1, and the experimental process of platelet spreading is as follows:

[0099] 1) Coating of coverslips or culture plates: Coat coverslips or disposable culture plates with 20 μg / mL fibrinogen (fibrinogen, Chrono-log Company, Havertown, PA) (dissolved in PBS), 4°C Overnight, 2% bovine serum albumin blocked non-specific binding sites at 37°C for 1 hour, and washed once with PBS.

[0100] 2) Adjust the concentration of platelets in the control group or ursodeoxycholic acid treatment group to 1.8×10 with HEPES-Tyrode buffer 6 / 500 μL, inoculated on the fibrinogen-coated coverslips in a 24-well plate, 500 μL per well, and incubated at 37°C for 2 hours.

[0101] 3) Take out the above coverslip, wash once with p...

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Abstract

The invention relates to chenodeoxycholic acid and a use thereof. The invention concretely comprises uses of the compound shown in the formula (I) in preparation of drugs for resisting platelet aggregation and thrombogenesis and preventing and treating platelet abnormal activation-related diseases. The chenodeoxycholic acid has effects of resisting platelet aggregation and spreading, can be used as a novel platelet aggregation-resistant and antithrombotic drug for treating blood platelet abnormal activation-related diseases such as thrombotic diseases, hypercoagulable state viral diseases, tumors, coronary heart diseases, apoplexy, hypertension, abdominal aortic aneurysm, leukemia and disseminated intravascular coagulation (DIC).

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to the new application of Ursodeoxycholic Acid (UDCA) in anti-platelet aggregation and its application in the prevention and treatment of arterial thrombosis diseases. technical background [0002] With the improvement of living standards, stroke, coronary heart disease and other arterial thrombotic diseases have become the number one killer threatening the health of people in our country and developed countries. Therefore, it is very important to prevent and treat cardiovascular and cerebrovascular thrombotic diseases. Intravascular thrombosis caused by abnormal activation of platelets is the pathological basis of arterial thrombosis coronary heart disease and stroke. The process includes aggregation and spreading of platelets. Therefore, antiplatelet drugs that inhibit platelet activation are the main means of prevention and treatment of such diseases. Antiplatelet drugs widely...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P7/02A61P31/12A61P35/00A61P9/10A61P9/12A61P35/02
Inventor 顾建新张思周梅玲孙琳琳
Owner SHANGHAIMED
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