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Novel compound ethyl brevicate with pharmaceutical activity

A technology of ethyl asaranoate and breviscapine, applied in the fields of organic active ingredients, organic chemistry, drug combination, etc., can solve the problems of difficult to meet the needs of clinical medicine, poor uniformity of curative effect, difficult quality control, etc.

Active Publication Date: 2012-01-04
YUNNAN BIOVALLEY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of them are mixtures of multiple compounds. Although these drugs have therapeutic effects, the multiple components will inevitably cause the following problems: poor uniformity of curative effect, difficult quality control, and difficult to control side effects (injections are especially obvious)
The only effective drug for a single compound is breviscapine preparations, which is difficult to meet the complex clinical medical needs

Method used

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  • Novel compound ethyl brevicate with pharmaceutical activity
  • Novel compound ethyl brevicate with pharmaceutical activity
  • Novel compound ethyl brevicate with pharmaceutical activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1: Extraction and preparation process of breviscapine ethyl caprylate

[0055] Take 10kg of the whole herb of Erigeron breviscapine, crush it, extract three times with 70% acetone aqueous solution, combine the three extracts, and concentrate under reduced pressure. The concentrated solution was subjected to polyamide resin chromatography, first eluted with water, then eluted with 60% ethanol, and concentrated under reduced pressure after collecting the 60% ethanol eluate, and this part was repeatedly chromatographed on silica gel to prepare scutellarin Ester (Ethyl brevicate) 50g.

Embodiment 2

[0056] Embodiment 2: Extraction and preparation process of breviscapine ethyl caprylate

[0057] Take 10kg of the whole herb of Erigeron breviscapine, crush it, extract three times with 70% ethanol aqueous solution, combine the three extracts, and concentrate under reduced pressure. The concentrated solution was chromatographed on polyamide resin, eluted with water first, and then eluted with 80% ethanol. After collecting the 80% ethanol eluate, it was concentrated under reduced pressure. This part was used for reversed-phase (Rp-18) column Analysis and separation prepared to obtain ethyl brevicate (Ethyl brevicate) 60g.

Embodiment 3

[0058] Embodiment 3: Extraction and preparation process of ethyl scutellaria caprylic acid

[0059] Take 10kg of the whole herb of Erigeron breviscapine, crush it, extract it three times with aqueous solution, combine the three extracts, and concentrate under reduced pressure. The concentrated solution was chromatographed on polyamide resin, firstly eluted with water, then eluted with 50% ethanol, and concentrated under reduced pressure after collecting the 50% ethanol eluate, this part was separated by Sephadex LH-20 40 g of ethyl brevicate (Ethyl brevicate) was prepared by repeated purification.

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Abstract

The invention relates to a novel compound of a structure formula (I). The compound can be extracted and separated from a dried whole plant of Erigeron breviscapus (Vant.) Hand.-Mazz. The compound has anti-inflammatory response, anti-platelet aggregation, anti-thrombotic and vasodilator effects, and can be used for preparing a medicament for treating cardiovascular and cerebrovascular diseases. The structure formula (I) is shown below.

Description

technical field [0001] The present invention relates to a novel compound with anti-inflammatory reaction, anti-platelet aggregation, anti-thrombosis and vasodilator effects, and a pharmaceutical composition for treating cardiovascular and cerebrovascular diseases containing the compound as an active ingredient. Specifically, it is a new compound Ethyl brevicate extracted from Erigeron breviscapus, its preparation method and its application in pharmacy. Background technique [0002] So far, the incidence of cardiovascular and cerebrovascular diseases represented by coronary heart disease and cerebral apoplexy (stroke) remains high, and its case fatality rate ranks first in the death rate of various human diseases. Finding new and effective drugs for the treatment of cardiovascular and cerebrovascular diseases is a difficult and hot spot that the pharmaceutical and clinical medicine circles are very concerned about. [0003] Erigeron breviscapus, also known as breviscapus, is...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/08A61K31/357A61P9/00
Inventor 杜江林艳和林炎海
Owner YUNNAN BIOVALLEY PHARMA CO LTD
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