Application of parthenolide as platelet-activating factor (PAF) antagonist

A technology of parthenolide and activating factor, applied in antiviral agents, medical preparations containing active ingredients, applications, etc.

Inactive Publication Date: 2012-07-18
韩颖
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] At present, there is no chemically synthesized platelet activating factor antagonist on the market, but some chemical entities have entered clinical research and preclinical research, such as Lexipafant, which is mainly developed for the treatment of acute pancreatitis. Response and anti-asthma as the main therapeutic goals of Israpafant, etc.

Method used

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  • Application of parthenolide as platelet-activating factor (PAF) antagonist
  • Application of parthenolide as platelet-activating factor (PAF) antagonist
  • Application of parthenolide as platelet-activating factor (PAF) antagonist

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0017] Experimental example 1. Parthenolide PAF antagonistic activity experiment:

[0018] 1. Experimental animals:

[0019] Male Japanese white rabbits weighing 2.0 to 2.2 kg.

[0020] 2. Drugs and reagents:

[0021] Test drug: parthenolide, homemade, chromatographic purity 98.33%.

[0022] Control drug: Ginkgolide, a product of Shanghai Ronghe Pharmaceutical Technology Development Co., Ltd., with a declared content of 97.81%.

[0023] Inducer: Rabbit Platelet Activating Factor (PAF), a product of Sigma

[0024] 3. Experimental method:

[0025] Preparation of platelet rich plasma (PRP) and platelet poor plasma (PPP): blood was collected from the common carotid artery of awake rabbits and anticoagulated with 3.8% sodium citrate 9:1 (v:v) Collected in a plastic centrifuge tube, centrifuged at 900 rpm for 8 minutes, the upper layer was taken as PRP, and the remaining blood was centrifuged at 3000 rpm for 5 minutes, and the upper layer was taken as PPP. The number of platelets in PRP was con...

experiment example 2

[0032] Experimental example 2: Experimental study on the acute toxicity of parthenolide

[0033] The purpose of the experiment: to observe the acute toxicity and death of mice within one week after the test substance parthenolide was administered once by gavage, and calculate the median lethal dose (LD) of parthenolide according to the number of deaths. 50 )

[0034] 1. Test substance:

[0035] Parthenolide

[0036] 2. Preparation method:

[0037] Accurately weigh 3750mg of parthenolide, add a little Tween-80 to a mortar, grind it, slowly add distilled water to the top 30ml, and then dilute to 100mg / ml, 80mg / ml, 64mg / ml, 51.2mg in the same ratio of 0.8 / ml, five concentration emulsions are stored in the refrigerator for later use.

[0038] 3. Experimental animals:

[0039] Source: KM mice, provided by the Animal Room of Jiangsu Cancer Institute

[0040] Weight: 20±2g

[0041] Gender: each group is half male and half male

[0042] Number of animals: 10 animals per group, calculate LD 50 .

[...

Embodiment 1

[0060] Weigh 20g parthenolide and grind it through a 100-mesh sieve, add 100g starch, 20g lactose, 15g sodium carboxymethyl cellulose, 10g microcrystalline cellulose, 10g magnesium stearate, and pass the 100-mesh sieve. Mix uniformly by increasing method, granulate with proper amount of 10% starch slurry, press to make 1000 tablets or fill into 1000 capsules to make tablets or capsules. Clinically used in the treatment, adjuvant treatment and prevention of thrombosis, atherosclerosis, ischemic cardiovascular disease, cerebral ischemia, asthma, liver fibrosis and cirrhosis, nerve damage, gastrointestinal ulcer and necrosis, psoriasis, etc. . The effective rate of clinical treatment can reach over 85%.

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Abstract

The invention discloses application of parthenolide as a platelet-activating factor (PAF) inhibitor. The parthenolide can be used as a safe PAF antagonist to be applied to treatment, auxiliary treatment and prevention of diseases such as thrombus, atherosclerosis, ischemic cardio-vascular disease, cerebral ischemia, acute pancreatitis, endotoxic shock, asthma, hepatic fibrosis and hepatocirrhosis, injury of nerve, gastrointestinal ulcer and necrosis, psoriasis, systemic lupus erythematosus and acquired immune deficiency syndrome related to platelet-activating factor.

Description

Technical field [0001] The invention relates to a new application of parthenolide, a natural compound, in the field of medical technology, especially its new application as a platelet activating factor (PAF) antagonist. Background technique [0002] Parthenolide is a sesquiterpene lactone compound of natural origin, and its structural formula is as follows: [0003] [0004] Chemical name: Oxireno[9,10]cyclodeca[1,2-b]furan-9(1aH)-one,2,3,6,7,7a,8,10a,10b-octahydro-1a,5-Dimethyl- 8-methylene-,[1aR-(1aR*,4E,7aS*,10aS*.10bR*)]- [0005] Molecular formula: C 15 H 20 O 3 [0006] Molecular weight: 248.32 [0007] Parthenolide was first isolated from the Asteraceae plant parthenolide, so it was named parthenolide. Later, it was found to exist in many plants of the Compositae and Magnoliaceae, such as Anthemis melampodina, Tanacetumargenteum (Lam.) Willd.subsp.flabellifolium (Boiss.et.Heldr.) Grieson, and dense chrysanthemum. Artemisia T.densumsubsp.amani Heywood, Magnolia Magnolia denuda...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P7/02A61P9/10A61P1/18A61P1/16A61P1/04A61P17/06A61P31/18A61P37/02A61P31/04A61P11/06A23L1/30
Inventor 韩颖
Owner 韩颖
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