Application of 13-hydroxy-8,9-dehydroshizukanolide in preparing medicine for anti-platelet aggregation

An anti-platelet aggregation, caryophyllol technology, applied in the field of biomedicine, to achieve excellent anti-platelet aggregation effect

Inactive Publication Date: 2021-02-23
南京盖斯夫医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] 13-Hydroxy-8,9-dehydrocaryophyllol is a known natural compound that has been shown to have analgesic properties (Antinoception caused by the extract of Hedyosmum brasiliense and its active principle, the sesquiterpene lactone 13-hydroxy-8,9 -dehydroshizukanolide.Planta Med.1999) and antidepressant (Evaluation of behavioral and pharmacological effects of Hedyosmum brasiliense and isolated sesquiterpenelactones in rodents.J Ethnopharmacol.2010) activity, other activities are still under study

Method used

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  • Application of 13-hydroxy-8,9-dehydroshizukanolide in preparing medicine for anti-platelet aggregation
  • Application of 13-hydroxy-8,9-dehydroshizukanolide in preparing medicine for anti-platelet aggregation
  • Application of 13-hydroxy-8,9-dehydroshizukanolide in preparing medicine for anti-platelet aggregation

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Experimental program
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Effect test

Embodiment 1

[0017] 1. Experimental materials

[0018] The chemical structure of 13-hydroxy-8,9-dehydrocaryophyllol is as follows figure 1 As shown, the purity is 98.5%.

[0019] The body weight of New Zealand male rabbits is (2±0.2) kg, and they are ready for use after one week of adaptive feeding.

[0020] 2. Experimental method

[0021] The in vitro anti-platelet aggregation activity assay method is the Born turbidimetric method, with aspirin as a positive control drug, the specific operation method reference (Tang Quan et al., 13-hydroxy-8,9-dehydrocaryophyllol design, synthesis and anti-platelet aggregation research , 2020):

[0022] Locally anesthetize the rabbit with 1% procaine hydrochloride, intubate the carotid artery to take blood, put it into 3.8% sodium citrate solution (the volume ratio of the blood taken to the sodium citrate solution is 9:1), Centrifuge at 1000r / min for 15min to obtain platelet-rich plasma (PRP). Dissolve 13-hydroxy-8,9-dehydrocaryophyllol and aspirin ...

Embodiment 2

[0030] An anti-platelet aggregation tablet, capsule or injection, the active ingredient is 13-hydroxy-8,9-dehydrocaryophyllol in different contents, and the excipients are commonly used excipients for tablets or capsules or injections.

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Abstract

The invention discloses application of 13-hydroxy-8,9-dehydroshizukanolide in preparing a medicine for anti-platelet aggregation. Experiments find that 13-hydroxy-8,9-dehydroshizukanolide with different concentrations has an obvious inhibition effect on platelet aggregation, and IC50 values of 13-hydroxy-8,9-dehydroshizukanolide are superior to the IC50 values of aspirin with ADP (2.6 mM vs. 11.8mM) and AA (0.42 mM vs. 4.1 mM) as inducers, respectively. Therefore, the 13-hydroxy-8,9-dehydroshizukanolide has relatively excellent anti-platelet aggregation activity, and has an application prospect of being developed into anti-platelet aggregation medicines.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to the medical use of 13-hydroxy-8,9-dehydrocaryophyllol, in particular to the use of 13-hydroxy-8,9-dehydrocaryophyllol for preparing anti-platelet aggregation medicines. Background technique [0002] Cardiovascular and cerebrovascular diseases refer to ischemic or hemorrhagic diseases in the heart, brain and systemic tissues caused by hyperlipidemia, hypertension, blood viscosity, atherosclerosis, etc., which pose a serious threat to human health. In recent years, with the aggravation of aging and the acceleration of the pace of life in our country, the incidence of cardiovascular and cerebrovascular diseases has increased year by year, and it has become the number one killer of residents' death. Molecular biology studies have shown that the onset of most cardiovascular and cerebrovascular diseases is related to arteriovenous thrombosis, and platelet aggregation is one of the main factors ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P7/02
CPCA61K31/365A61P7/02
Inventor 郭守山郭守河
Owner 南京盖斯夫医药科技有限公司
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