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Application of alisol A 24-acetate in preparing drug for treating adiposis

A technology of acetate and alisol, which is applied in the field of alisol A 24-acetate, can solve the problems of unreported pharmacodynamic research data on weight loss, insignificant weight loss effect, and unclear basis of effective substances, etc. To achieve the effect of clear ingredients, exact curative effect and controllable quality

Inactive Publication Date: 2014-05-28
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Chinese patent 200510106261.2 discloses a drug for the treatment of obesity. This patent mainly discloses the weight loss effect of Forsythia adenocarpus, but there are problems such as unclear effective material basis and insignificant weight loss effect.
[0007] Alisol A 24-acetate (24-acetate Alisol A) is the main active ingredient in the traditional Chinese medicine Alisol. At present, there are few reports on Alisol A 24-acetate in the existing literature. Japanese scholar Imai Y in In 1970, a paper entitled Hypocholesterolemic effect of alisol A-24-monoacetate and its related compounds in rats was published on Jpn J Pharmacol (1970Jun;20(2):222-8). Reported alisol A 24-acetic acid Ester has the effect of lowering blood fat, but there is no report on the weight loss pharmacodynamics research data at the whole animal level;

Method used

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  • Application of alisol A 24-acetate in preparing drug for treating adiposis
  • Application of alisol A 24-acetate in preparing drug for treating adiposis
  • Application of alisol A 24-acetate in preparing drug for treating adiposis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Extraction of medicinal materials:

[0022] 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.

[0023] 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.

[0024] 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.

[0025] Method 4: Take 1 kg of ...

Embodiment 2

[0027] Preparation of Alisitol A 24-acetate:

[0028] 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.

[0029] 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 .

[0030] 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 , 26...

Embodiment 3

[0032] 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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Abstract

The invention discloses an application of alisol A 24-acetate in preparing a drug for treating adiposis. Proved by an animal test that the alisol A 24-acetate has remarkable therapeutic effect to an obesity model caused by feeding with a high-fat feed and can be used for preparing the drug for treating and preventing the adiposis. With the adoption of the application, a modern medicine theory is applied, and the drug for treating the adiposis with definite therapeutic effect, clear compositions and controllable quality is provided and can satisfy the needs of clinical applications. The invention firstly discloses that the alisol A 24-acetate is used for inhibiting weight and fat increase of a mouse caused by a high-fat diet, has the obvious effects of weight reduction, fat reduction and adiposity prevention and has important significance on the clinical applications.

Description

technical field [0001] The present invention relates to a new application of alisol A 24-acetate. Background technique [0002] With the improvement of people's living standards, the incidence of obesity is also increasing. [0003] Obesity is generally divided into two categories, one is obesity caused by disease, which is obesity caused by endocrine disorders caused by diseases (encephalitis, brain tumor, arthritis or chronic diseases requiring hormones). Symptomatic obesity. This type of obese patients accounts for about 5% of the total obese people. [0004] Another type of obesity is due to the intake of calories during the diet, which greatly exceeds the calories consumed by itself. And excess fat and other nutrients are accumulated in the body to form fat cells, which leads to obesity. People who belong to this type of obesity become simple obesity, accounting for more than 90% of the total number of obese people. [0005] At present, the drugs for treating obesit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P3/04
Inventor 侯惠民程志红
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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