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Application of Piperlongumine compounds for resisting platelet aggregation

An anti-platelet aggregation and Piperamide technology, which is applied in the field of Piperamide compounds in the field of anti-platelet aggregation, can solve the problems of increased risk of patients, and achieve the effect of preventing and treating cardiovascular and cerebrovascular diseases and inhibiting platelet aggregation

Inactive Publication Date: 2012-04-25
合肥华纳生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But these drugs also have the same phenomenon similar to AR to varying degrees
On the other hand, the combination of two antiplatelet drugs will greatly increase the risk of severe bleeding in patients, so the combination of other antiplatelet drugs or alternative drugs is not an ideal method

Method used

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  • Application of Piperlongumine compounds for resisting platelet aggregation
  • Application of Piperlongumine compounds for resisting platelet aggregation
  • Application of Piperlongumine compounds for resisting platelet aggregation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Experimental materials: Aspirin used in the experiment was purchased from Alfa Aesar, 3,4,5,-trimethoxycinnamic acid was purchased from Acros, 5,6-dihydro-2(1)-pyridone and 1,2,3,4- Tetrahydropyridine is synthesized according to literature (Jerchel, Ber., 1943,76B, 413; J.Org.Chem.1961,26,718; J.Org.Chem.1964,29,2472), isobutylamine, DCC (di Cyclohexylcarbodiimide) and commonly used solvents were purchased from Beijing Chemical Reagent Company, and the solvents were all analytically pure. Unless otherwise specified, the solvents were used directly. Dichloromethane drying method: calcium hydride reevaporation to dryness.

[0031] Piperamide and its derivatives PL, P-1, P-2, and P-3 are all self-prepared (the specific structural formula is as follows):

[0032]

[0033] Preparation of Piperamides

[0034] Synthesis of Piperamide (PL): 3,4,5,-trimethoxycinnamic acid (0.714g, 3mmol) was dissolved in 25ml of dry dichloromethane, 5,6-dihydro-2(1)-pyridine was added Keto...

Embodiment 2

[0039] Experimental animals: Grade 2 male rats were provided by the Animal Center of Peking University, and EDTA, HEPES, KCl, DMSO, and bovine serum albumin required for the experiment were purchased from Huamei Bioengineering Co., Ltd. (Wuhan, China).

[0040] Experimental instruments: Coulter particle counter (MS3 type, Coulter company, the United States), platelet aggregation analyzer (470-vs, Chrono-log company, the United States)

[0041] Experimental method: blood was collected from the pinna of male rats, and 1 / 10 volume of 0.1% EDTA solution was added to prevent blood coagulation. And centrifuge the blood sample with a 230g force centrifuge for 10 minutes to obtain platelet rich plasma (PRP); then centrifuge the platelet rich blood sample with a 800g force centrifuge for 15 minutes, and the platelets will be deposited on the wall of the centrifuge tube and bottom, collect platelets, and wash twice with HEPES buffer solution (137mM NaCl, 2.7mM KCl, 1mM MgCl2, 5.6mM gluc...

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Abstract

The invention relates to application of Piperlongumine compounds for resisting platelet aggregation, in particular to application of the Piperlongumine compounds which are used for preparing medicines and health care products for controlling thrombus or cardiovascular and cerebrovascular diseases. Experimental results indicate that the Piperlongumine compounds have remarkable effects on the platelet aggregation initiated by collagen, arachidonic acid and platelet activating factors, and the inhibition efficiency of the Piperlongumine compounds is superior to aspirin and also in a linear relationship with the compound concentration; thereby indicating that the Piperlongumine compounds have very wide prospects as a category of medicines or health care products for resisting the thrombus or controlling the cardiovascular and cerebrovascular diseases.

Description

technical field [0001] The present invention relates to a new application of traditional Chinese medicine components, in particular to the application of Piperamide compounds in anti-platelet aggregation. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the most serious diseases threatening human health in the world today, and its morbidity and mortality have surpassed tumors and ranked first in the world. According to the data released by the Ministry of Health of China in 2005, among the total mortality rate of the Chinese population, the mortality rate of cardiovascular and cerebrovascular diseases ranks first. The mortality rate of cerebrovascular diseases in urban residents is 21.2%, and the mortality rate of heart disease is 17.9%. The mortality rate of heart disease is 21.2%, and the mortality rate of heart disease is 11.8%. About 2.6 million people die of cardiovascular disease every year. [0003] Atherosclerosis, plaque rupture,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4412A61K31/44A61K31/165A61P7/02A61P9/00A23L1/29A23L33/00
Inventor 高源余明辉
Owner 合肥华纳生物医药科技有限公司
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