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Application of glabridin in preparation of drugs to treat thrombotic diseases

A technique for thrombotic diseases and glabridin, which is applied in the field of medicine and can solve problems such as reports on the application of glabridin that have not been seen

Inactive Publication Date: 2018-11-13
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] But there is no report on the application of glabridin in the preparation of medicines for the treatment of thrombotic diseases at present

Method used

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  • Application of glabridin in preparation of drugs to treat thrombotic diseases
  • Application of glabridin in preparation of drugs to treat thrombotic diseases
  • Application of glabridin in preparation of drugs to treat thrombotic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 Glabridin inhibits activity of platelet activating factor receptor (PTAFR)

[0029] 1. Experimental materials

[0030] 1.1 Cell line: CHO-K1, a Chinese hamster ovary cell line stably transfected with PTAFR, was constructed by Jiangsu Kangyuan Pharmaceutical Co., Ltd. using liposome transfection technology.

[0031] 1.2 Main reagents: F12 medium and fetal bovine blood (FBS) were purchased from Hyclone Company; Zeocin and HBSS were purchased from Invitrogen Company; calcium flux detection kit (calcium 6 dye) was purchased from Molecular Device Company; PAF (C16), WEB2086 Purchased from tocris; HEPES purchased from Nanjing Shengxing Biotechnology Co., Ltd.; DMSO purchased from sigma company.

[0032] 1.3 Instruments: FLIPR tetra microplate reader, Molecular Devices; pipette, eppendorf; ultra-clean bench, purchased from Shanghai Jiejia Air Purification Technology Co., Ltd.; CDX-K1 inverted microscope, purchased from Olympus; countess The automatic cell counti...

Embodiment 2

[0052] Example 2 Effect of Glabridin on Platelet Activity in Thrombosis Model Rats

[0053] 1. Experimental materials

[0054] 60 clean-grade SD rats, weighing about 180-220g, half male and half male, were purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.; p-selectin, vWF, GPⅡb / Ⅲa and TXB2 kits were purchased from Shanghai Research Institute Jin Biotechnology Co., Ltd.; the rest of the reagents were of domestic analytical grade.

[0055] 2. Experimental method

[0056] 2.1 Experimental grouping and modeling

[0057] Sixty SD rats were randomly divided into 5 groups after routine feeding for one week: sham operation group, model group, glabridin low, medium and high dose groups, with 12 rats in each group. The medication group was dissolved in normal saline at 100, 200, and 400 mg / kg body mass for intragastric administration of glabridin, while the sham operation group and model group were intragastrically administered the same amount of normal sa...

Embodiment 3

[0072] Example 3 Effect of Glabridin on Rabbit Hyperlipidemia Thrombosis Model

[0073] 1. Experimental materials

[0074] 40 male healthy Japanese big-eared white rabbits, weighing 2.2-2.5kg, aged 5-6 months, were purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.

[0075] 2. Experimental method

[0076] 2.1 Hyperlipidemia model establishment and grouping

[0077] Experimental rabbits were fed with basic feed in a single cage for 3 days, and blood was collected from ear veins on an empty stomach the next morning to check serum total cholesterol (TC). On the day of blood collection, 1% cholesterol was fed to each rabbit at 100 g / kg per day. At the end of the 14th day of the experiment, blood from the ear vein was collected to check the serum TC. If the serum TC level is more than 5 times higher than before feeding cholesterol, it means that the rabbit hyperlipidemia model is successful. The above 40 hyperlipidemic rabbits were randomly divided i...

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Abstract

The invention discloses application of glabridin in preparation of drugs to treat thrombotic diseases and belongs to the technical field of medicine. Experiments show that glabridin can significantlyinhibit platelet activating factor receptors, and can significantly reduce, in vivo, p-selectin, vWF, GPIIb / IIIa and TXB2 levels in serum of a thrombosis model rat due to external application of FeCl3solution. venous injection of glabridin can significantly inhibit the rise of whole blood PAF (platelet activating factor) concentration induced by artery thrombosis and can significantly reduce IP3content in platelets and the expression of platelet IP3 receptors; it is indicated that glabridin can inhibit platelet PAF-IP3-IP3R-[Ca2+]i signal transduction pathway, and the inhibition is one of mechanisms of glabridin to inhibit platelet activating and gathering. Glabridin can inhibit thrombosis via multiple targets and multiple pathways, and is functional in and worthy of treating thromboticdiseases.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to the application of glabridin in the preparation of medicines for treating or preventing thrombotic diseases. Background technique [0002] Thromboembolic disease is a disease that seriously endangers the health of middle-aged and elderly people. It has a high incidence rate and a high disability and death rate. Thrombosis is a complex process involving multiple factors and progressive development. The abnormal coagulation of blood occurs due to the activation of platelets and coagulation factors in a flowing state. Thrombosis plays a promoting role in the occurrence and development of cardiovascular and cerebrovascular diseases, and is also one of the main causes of death and disability. Thrombosis conditions include damage to the vascular intimal membrane, changes in blood flow regime, and increased blood coagulation. Therefore, inhibiting platelet function and preventing blood ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P7/02
CPCA61K31/352
Inventor 萧伟陶晓倩苏真真王俨如丁岗王振中
Owner JIANGSU KANION PHARMA CO LTD
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