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Application of alisol A 24-acetate in preparation of medicaments for preventing and treating arterial diseases

A technology of alisol and acetate, applied in the directions of drug combination, cardiovascular system diseases, pharmaceutical formulations, etc., to achieve the effect of low toxicity

Active Publication Date: 2014-06-11
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no published literature that alisitol A 24-acetate has the effect of anti-atherosclerosis and inhibition of vascular intimal hyperplasia

Method used

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  • Application of alisol A 24-acetate in preparation of medicaments for preventing and treating arterial diseases
  • Application of alisol A 24-acetate in preparation of medicaments for preventing and treating arterial diseases
  • Application of alisol A 24-acetate in preparation of medicaments for preventing and treating arterial diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Extraction of medicinal materials:

[0020] Method 1: Take 1 kg of dried tubers of Alisma orientalis (Sam.) Juzep., a plant of the family Alismaceae, make decoction pieces, and reflux extract with 7500ml of ethyl acetate twice, each time for 0.5 hours. The extracts were combined, and the solvent was recovered under reduced pressure to obtain 40 g of dark brown extract.

[0021] Method 2: Take 3 kilograms of dry tubers of Alisma orientalis (Sam.) Juzep., crushed into coarse particles, leak with 75% ethanol, combine the seepage, recover the solvent under reduced pressure, and obtain dark brown infusion Cream 110g.

[0022] Method 3: Take 2 kg of dry tubers of Alisma orientalis (Sam.) Juzep., crush them into coarse particles, and place them in CO 2 In supercritical extractor, extraction condition: CO 2 The pressure is 24-35MPa, the extraction temperature is 41-55°C, the extraction time is 1.5h, and 65g of dark brown extract is obtained.

[0023] Method 4: Take 1 kg of ...

Embodiment 2

[0025] Preparation of Alisitol A 24-acetate:

[0026] Take by weighing 10 g of the extract of Example 1, put it on D101 type macroporous adsorption resin, after eluting 10 column volumes with 20% ethanol, use 70% ethanol to elute 5 column volumes instead, collect 70% ethanol eluate, reduce The solvent was recovered under pressure to obtain 2 g of yellow oil; 2 g of yellow oil was dissolved in 65% methanol, and the target compound was separated by preparative HPLC. The separation conditions are: C18 column, mobile phase is 65% methanol, flow rate is 50ml / min, detection wavelength is 208nm. This gave 100 mg of alisol A 24-acetate with a purity of 95% by weight.

[0027] High resolution mass spectrum: m / z: 555.36561, C 32 h 52 o 6 Na + [M+Na], its molecular formula is C 32 h 52 o 6 .

[0028] C 13 NMR(δ):223.76、172.845、139.75、136.463、81.127、74.064、70.006、58.442、49.831、49.794、48.291、41.946、41.361、38.340、35.534、35.194、34.801、32.129、31.788、30.367、30.019、29.582、27.390 , 2...

Embodiment 3

[0030] Weigh 10 g of alisitol A 24-acetate in Example 2, add 8 g of starch, 2 g of microcrystalline cellulose, and 0.2 g of magnesium stearate, mix well, and adopt methods known in the art to make tablets and capsules doses or granules.

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PUM

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Abstract

The invention discloses an application of alisol A 24-acetate in preparation of medicaments for preventing and treating arterial diseases. Animal tests prove that the alisol A 24-acetate has a significant treatment effect against an arteriosclerosis model of an ApoE- / - mouse which is fed with a high-fat diet and combined with carotid artery injury surgery. The medicament disclosed by the invention has relatively low toxicity and is suitable for long-term use. The invention provides the medicament for treating arteriosclerosis, which has the advantages of exact curative effect, definite ingredients and controllable quality, and can meet the needs of clinical applications, by applying the modern medicine theory.

Description

technical field [0001] The invention relates to a new application of alisol A 24-acetate in medicine. Background technique [0002] Cardiovascular disease has become the number one killer threatening human health. According to the report of the World Health Organization in 2004, one out of every three deaths is caused by cardiovascular disease. Atherosclerosis is the main cause of cardiovascular events such as cerebral infarction and myocardial infarction. the main reason. [0003] Preventing the occurrence of atherosclerosis and promoting the regression of arterial plaques are the fundamental measures to reduce the incidence and mortality of cardiovascular and cerebrovascular diseases. At present, drugs for the treatment of atherosclerosis, such as atorvastatin, have been published clinical research results show that atorvastatin is the only anti-atherosclerotic drug that has been proven to reduce cardiovascular events better than vascular double eyelid surgery, Its inhib...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P9/10
Inventor 侯惠民程志红
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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