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Uses of Petasites tricholobus franch extract in medicament preparation for preventing and controlling cardiovascular and cerebrovascular diseases

A technique for cardiovascular and cerebrovascular diseases and trichomonas, applied in the field of medicine

Active Publication Date: 2008-11-05
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, there is no report about the cardio-cerebrovascular pharmacological activity of the butterbur extract and its active substances butterbur lactones.

Method used

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  • Uses of Petasites tricholobus franch extract in medicament preparation for preventing and controlling cardiovascular and cerebrovascular diseases
  • Uses of Petasites tricholobus franch extract in medicament preparation for preventing and controlling cardiovascular and cerebrovascular diseases
  • Uses of Petasites tricholobus franch extract in medicament preparation for preventing and controlling cardiovascular and cerebrovascular diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1. Preparation of Butterbur pilaris Extract

[0043] The preparation method steps of the butterbur extract of the present invention are as follows:

[0044] (1) extraction

[0045] After 10 kg of the rhizome of Butterbur pilaris is pulverized, use 50 L of 90% ethanol to percolate to obtain the extract according to the conventional method, and the extract is concentrated under reduced pressure and then centrifuged, and the supernatant is taken for subsequent use;

[0046] (2) Purification

[0047] The above supernatant was subjected to polystyrene type porous adsorption resin adsorption, rinsed with water and 50% aqueous ethanol to remove impurities, then eluted with 80L of 80% aqueous alcohol, and the eluate was collected.

[0048] (3) Concentration and drying

[0049] Concentrate the eluent under reduced pressure and dry it to obtain the extract of Butterbur pilaris.

Embodiment 2

[0050] Example 2. Preparation of Partial Butterbur Lactone Compounds Contained in the Butterbur pilaris Extract

[0051] Take 20 g of the butterbur extract prepared in Example 1, dissolve it in petroleum ether, perform silica gel column chromatography as usual, and use petroleum ether-acetone 50-5:1 chromatography to obtain Homofukinolide (7.9 mg), honeysuckle Butterburide-Ia (29mg), Butterburide-IIa (65mg), Butterburide-B (1.6g), Butterburide-IIIa (2.8g), Butterburide -IVa (2.9g), butterbur lactone-Va (50mg), butterbur lactone-D (2.6g), wherein butterbur lactone-Va is a new compound. The chemical structures of these compounds are shown in Table 1. They are butterbur lactone compounds, which were determined and analyzed by HPLC, wherein butterbur lactone-D, butterbur lactone-B, butterbur lactone-IVa and butterbur lactone The sum of the contents of the four compounds of columba lactone-IIIa accounts for more than 50% of the total extract, so the main component of the columba p...

Embodiment 3

[0052] Embodiment 3. prepare butterbur lactone compounds with butterbur trichomes

[0053] 35Kg of dry leaves of Butterbur pilaris were refluxed and extracted three times with ethanol, the amount of ethanol was 175L, 70L, 35L respectively, and the extraction time was 2 hours, 1 hour, and half an hour respectively. The extract was concentrated under reduced pressure and dissolved in water to make a suspension, which was sequentially extracted with petroleum ether and ethyl acetate to obtain petroleum ether extract and ethyl acetate extract respectively. The ethyl acetate extract was eluted with a gradient of n-hexane-ethyl acetate (8:1-1:1) by silica gel column chromatography (chromatographic silica gel 200-300 mesh, Shandong Yantai Zhifu Huangwu Silica Gel Development and Experimental Factory) According to the results of TLC monitoring, the eluents were combined into thirteen parts. The fourth fraction was subjected to silica gel column chromatography, eluting with n-hexane:e...

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Abstract

The invention relates to the field of medical technology, which discloses a new usage of a petasites tricholobus franch extract and the contained bakkenolide compound in the preparation of drugs for prevention and treatment for cardiovascular and cerebrovascular diseases. The biological activity tests show that, the petasites tricholobus franch extract and the contained bakkenolide compound can significantly reduce the encephalic necrosis percentage of the rats with local cerebral ischemia, improve the behavior score of the ischemic rats and alleviate volume of brain edema and cerebral infarction of the rats with ischemia reperfusion injury, thus prompting that the petasites tricholobus franch extract and the contained bakkenolide compound have significant protective effect on the cerebral ischemia injury. The petasites tricholobus franch extract and the contained bakkenolide compound can further significantly reduce the J-point displacement caused by ISO and the LDH level in plasma, significantly reduce the scope of myocardial ischemic myocardial infarction of the rats caused by coronary artery ligation and lower the LDH level in the plasma of the rats with the myocardial ischemia. As the petasites tricholobus franch extract and the contained bakkenolide compound have good effects on the prevention and the treatment for heart and brain ischemic diseases aspects, the petasitestricholobus franch extract and the contained bakkenolide compound can be used in the preparation of drugs for prevention and treatment for cardiovascular and cerebrovascular diseases, including coronary heart disease, cerebral ischemia, cerebral infarction (stroke), myocardial infarction and so on.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a new application of butterbur extract and butterbur lactone compounds contained therein in the preparation of drugs for preventing and treating cardiovascular and cerebrovascular diseases. Background technique [0002] Petasites tricholobus Franch. belongs to the genus Petasites tricholobus Franch. Its rhizomes are used in the folk for detoxification and blood stasis, and for external application to treat bruises, fractures and snakebites. In order to develop and utilize the plant, the present inventor has carried out systematic chemical composition and pharmacological research on the plant, and has used four new butterbur lactone compounds and butterbur lactone compounds in Butterbur pilaris. Applied for a patent (patent publication number: CN1844114) for the treatment of diseases that may be related to histamine and / or leukotrienes, and applied for the extract of Butterbur pila...

Claims

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Application Information

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IPC IPC(8): A61K36/28C07D307/94A61K31/365A61P9/10A61K125/00
Inventor 郭美丽张福金刘宏艳李润平
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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