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Flavane derivatives in dragon's blood and application of pharmaceutical composition of flavane derivative

A technology of drugs and compounds, applied in the field of medicine, can solve the problems of poor curative effect, high bleeding risk and unsatisfactory curative effect of ADP receptor inhibitors

Pending Publication Date: 2021-08-27
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although the existing antithrombotic drugs have achieved certain effects in the prevention or treatment of thromboembolic diseases, they still have unsatisfactory curative effect, high bleeding risk, need for coagulation function monitoring, easy to induce anti-drug antibody production or injection administration poor compliance
Especially antiplatelet drugs, thromboxane synthesis inhibitors are less effective, ADP receptor inhibitors have a high risk of bleeding, and platelet surface glycoprotein GPIIb / IIIa inhibitors need to be administered by injection

Method used

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  • Flavane derivatives in dragon's blood and application of pharmaceutical composition of flavane derivative
  • Flavane derivatives in dragon's blood and application of pharmaceutical composition of flavane derivative
  • Flavane derivatives in dragon's blood and application of pharmaceutical composition of flavane derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Determination of the regulatory effect of compounds XJ-8 and XJ-11 on the release of ATP from rat platelets

[0030] Sprague Dawley rats were anesthetized by intraperitoneal injection of pentobarbital sodium (40 mg / kg), and blood was collected from the abdominal aorta by laparotomy into vacuum anticoagulated blood collection tubes containing sodium citrate. Centrifuge at 200g at room temperature for 10 minutes, take the upper platelet-rich plasma, then centrifuge at 1000g at room temperature for 10 minutes, and discard the supernatant. Add an equal volume of CGS buffer (containing 1.7mM citric acid, 18.3mM sodium citrate, 10mM glucose, 120mM sodium chloride, 2μN prostaglandin E1) to resuspend the platelets, centrifuge at 1000g for 10 minutes at room temperature, discard the supernatant, and repeat. Using modified bench solution (containing 137mM sodium chloride, 2.9mM potassium chloride, 0.34mM disodium hydrogen phosphate, 12mM sodium bicarbonate, 5mM 4-hydr...

Embodiment 2

[0034] Example 2: Determination of the inhibitory effect of compounds XJ-8 and XJ-11 on rat platelet aggregation

[0035]Sprague Dawley rats were anesthetized by intraperitoneal injection of pentobarbital sodium (40 mg / kg), and blood was collected from the abdominal aorta by laparotomy into vacuum anticoagulated blood collection tubes containing sodium citrate. Centrifuge at 200 g for 10 minutes at room temperature, and take the upper layer of platelet-rich plasma. Take 200 μl of plasma into a platelet aggregation assay tube, add 25 μl of XJ-8 or XJ-11 prepared by modified benchtop solution to a final concentration of 5, 10, and 20 μM, incubate at 37°C for 10 minutes, and then add 25 μl of type I collagen to a final concentration of 5 μg / ml, start the platelet aggregation assay, and the assay time is 5 minutes. In addition, part of the platelet-rich plasma was centrifuged at 1000 g at room temperature for 10 minutes, and the supernatant was discarded. Add an equal volume of...

Embodiment 3

[0039] Example 3: Determination of the Effects of XJ-8 and XJ-11 on the Bleeding Time of Mice

[0040] 64 male BALB / c mice aged 8-10 weeks were randomly divided into 8 groups, control group (Control), positive drug aspirin (Aspirin) 200mg / kg group, XJ-8 and XJ-11 20, 40, 80mg / kg dose group. After the mice were fed adaptively for 3 days, aspirin, XJ-8 and XJ-11 were prepared as suspensions with 0.5% sodium carboxymethylcellulose aqueous solution, and then the mice in each administration group were given the corresponding doses of aspirin, XJ-11 by intragastric administration. 8 or XJ-11, the control group was given an equal volume of 0.5% sodium carboxymethylcellulose aqueous solution. After 3 hours of administration, 0.5 cm of the mouse tail was excised with a scalpel blade, and then the mouse tail was placed in a 5 ml centrifuge tube filled with 4 ml of 37°C normal saline, and the bleeding time was observed and recorded.

[0041] The results showed that the bleeding time (m...

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Abstract

The invention discloses two flavane derivatives extracted and separated from dragon's blood and an application of pharmaceutical compositions thereof in preparation of drugs for preventing or treating thromboembolic diseases, and especially the flavane derivatives used for preparing medicines for preventing or treating cerebral arterial thrombosis, myocardial infarction, unstable angina pectoris, peripheral arterial thrombosis, restenosis after angioplasty or endarterectomy, deep venous thrombosis and pulmonary thrombosis.

Description

technical field [0001] The invention relates to the application of two flavan derivatives in dried blood in the preparation of medicines for preventing or treating thromboembolic diseases, and belongs to the technical field of medicine. Background technique [0002] With the aging of the population and changes in people's lifestyles and eating habits, thromboembolic diseases have increasingly become a major global health problem, and have become the number one cause of global death. Its scope mainly includes arterial thromboembolic disease and venous thromboembolic disease. Arterial thromboembolic diseases mainly include ischemic stroke, myocardial infarction, unstable angina, peripheral arterial thrombosis, and restenosis after angioplasty or endarterectomy. Venous thromboembolic diseases mainly include deep vein thrombosis and pulmonary thromboembolism. [0003] In addition to controlling the primary disease, the current methods for preventing or treating thromboembolic ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61P7/02A61P9/10A61P9/00
CPCA61K31/353A61P7/02A61P9/10A61P9/00A61K36/889
Inventor 朱枝祥李军屠鹏飞王丽丽庞道然郭冉李芸芊孙建宁王铁山王文萱
Owner BEIJING UNIV OF CHINESE MEDICINE
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