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Application of Quzhazhigan in preparation of preparations for preventing and treating cardiac-cerebral ischemia diseases, and preparation method thereof

A technique for cardiovascular and cerebrovascular diseases and tristilbene, which is applied to the application of tristilbene in the preparation of preparations for preventing and treating cardio-cerebral ischemia and the field of preparation thereof, can solve the problems of reduced water solubility of compounds and the like, and achieves a simple and convenient process. Effect

Active Publication Date: 2010-07-28
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The substitution of the methoxy group on the benzene ring in the structure greatly reduces the water solubility of the compound

Method used

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  • Application of Quzhazhigan in preparation of preparations for preventing and treating cardiac-cerebral ischemia diseases, and preparation method thereof
  • Application of Quzhazhigan in preparation of preparations for preventing and treating cardiac-cerebral ischemia diseases, and preparation method thereof
  • Application of Quzhazhigan in preparation of preparations for preventing and treating cardiac-cerebral ischemia diseases, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1: Qualitative identification and quantitative detection of tristilbene in Lhasa rhubarb raw materials and tristilbene extract

[0058] (1) Sample source

[0059] Wild Lhasa Rhubarb Rhizome: purchased from Lhasa, Tibet, removed impurities, washed, cut into slices or blocks, and dried in the sun. Batch number: 20080913

[0060] Planting rhizomes of Rhubarb in Lhasa: Harvested in Shangri-La County, Yunnan, removed impurities, washed, cut into slices or blocks, and dried in the sun. Batch number: 20080915

[0061] Reference substance: Tristilbene, self-made, purity 99%, batch number: 080602.

[0062] (2) Sample and standard solution preparation

[0063] Reference substance solution preparation: Accurately weigh an appropriate amount of tristilbeside reference substance vacuum-dried with phosphorus pentoxide, make 1mg / ml reference substance stock solution with methanol, dilute 27% methanol-3% acetic acid solution to 25g / ml as Standard solution.

[0064] Preparat...

Embodiment 2

[0075] Example 2: Preparation of Tristilbene Extract

[0076] (1) Material: Rhizome of Rhubarb Lhasa: Purchased in Lhasa, Tibet, remove impurities, wash, cut into slices or blocks, and dry in the sun. Batch number: 20080913

[0077] Resin: D101 macroporous adsorption resin, product of Tianjin Haiguang Chemical Co., Ltd., pretreated according to the manufacturer's instructions.

[0078] (2) Preparation

[0079] i) Pretreatment of Lhasa rhubarb and determination of tristilbene content:

[0080] The collected Lhasa rhubarb plants are removed from the mud and dried, and the underground rhizomes and aboveground stems and leaves are separated, and the pulverizers are used to pulverize them into coarse powder.

[0081] Take 100 g of underground rhizomes and aboveground cauline and leaf powders, soak and reflux extraction with 95% ethanol, 120 minutes / time, and perform HPLC detection by sampling at intervals, until the extracts basically do not contain tristilbene, and combine the ...

Embodiment 3

[0105] Example 3: Preparation of pure tristilbeside from Lhasa rhubarb extract and tristilbene extract

[0106] (1) Material: Rhizome of Rhubarb Lhasa: Purchased in Lhasa, Tibet, remove impurities, wash, cut into slices or blocks, and dry in the sun. Batch number: 20080913.

[0107] (2) Preparation of Rhubarb Lhasa Extract: Take 100 g of rhizome powder of Rhubarb Lhasa dry, use 95% ethanol as extraction solvent to reflux extract 3 times (2.4L / 1.8L / 1.2L), 120min / time, combine extracts, concentrate, vacuum Dried, Laksa rhubarb extract.

[0108](3) Purification: 2 g of Rhubarb Lhasa extract was mixed with 40 g of 200-mesh silica gel, and purified by silica gel column chromatography. Adopt chloroform / methanol (V / V, 8 / 1) as eluting solvent, divide and collect different fractions, thin-layer chromatography (TLC) monitors, merge the fractions that contain tristilbene, reclaim solvent under reduced pressure, 15 % ethanol recrystallization and vacuum drying to obtain pure trizaperon...

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Abstract

The invention relates to application of Quzhazhigan serving as polyhydroxy stilbene glycoside compounds in preparation of preparations for preventing and treating ischemic cardio-cerebrovascular diseases, and a preparation method thereof. The Quzhazhigan is compounds (E)-1-(3,5-dihydroxy phenyl)-2(3-hydroxyl-4-O-beta-D-pyran glucose phenyl)ethane, and has a chemical structural formula. Test results show that the Quzhazhigan can significantly reduce injury caused by ischemia reperfusion after cardio-cerebral infarction and has wide application in the preparation of preparations for preventing and treating cardiac-cerebral ischemia diseases. The Quzhazhigan can be extracted from roots and / or rhizome of Rheum lhasaense and prepared in pure alcohol / water systems, thereby having the advantagesof simple convenient property, environment-friendly property and strong practicability.

Description

technical field [0001] The invention relates to the use of the plant active ingredient tristilbene in the preparation of preparations for preventing and treating heart and brain ischemia and a preparation method of tristilbene and tristilbene extract. The stilbene glycoside is the compound (E)-1-(3,5-dihydroxyphenyl)-2-(3-hydroxyl-4-O--D-glucopyranose phenyl)ethylene, and its preparation method It is extracted from the root and / or rhizome of Rhubarb Lhasa and prepared through purification steps. Background technique [0002] Tristilbene is the compound (E)-1-(3,5-dihydroxyphenyl)-2-(3-hydroxy-4-O-β-D-glucopyranose phenyl)ethylene, or 3 , 5,3′,4′-Tetrahydroxystilbene-3′-O-β-glucoside, also known as Quzha in Tibetan medicinal materials because of its plant source Lhasa Rhubarb rhizome (Edited by Luo Dashang. Xinxiu Jingzhu Materia Medica, Sichuan Science and Technology Press, 2004), so the compound is called tristilbeside. Stilbenes are a class of stilbene ( figure 1 ) as ...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/08A61K31/7034A61P9/10A23L1/29A23L33/00
Inventor 胡琳何金星胡群代家红胡茂
Owner KPC PHARM INC
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