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Yacon diterpene acid compounds, medicine composition, preparation method and use in preparation of medicine treating diabetes mellitus

A technology of yagon diterpene acid and tribute diterpene salt, which is applied in the application field of preparation of drugs for treating diabetes, can solve the problems of no yagon extract, reports, and inability to apply anti-diabetic drugs, etc., and achieves a simple preparation method, Good inhibitory effect

Active Publication Date: 2008-07-23
珍奥集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, there is no definite report on the anti-diabetic active ingredients in yagon, and no report on the extract of yagon
Therefore, the existing yagon can only be applied to food or drink, and cannot be used in the preparation of antidiabetic drugs

Method used

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  • Yacon diterpene acid compounds, medicine composition, preparation method and use in preparation of medicine treating diabetes mellitus
  • Yacon diterpene acid compounds, medicine composition, preparation method and use in preparation of medicine treating diabetes mellitus
  • Yacon diterpene acid compounds, medicine composition, preparation method and use in preparation of medicine treating diabetes mellitus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation of Argonium Diterpene Acid A, Argonium Diterpene Acid B, Argonium Diterpene Acid C, Argonium Diterpene Acid D:

[0031] a. Take 3 kg of dry Yagong leaves, and use 10 times the amount of water or hydrous ethanol to reflux extract 3 times, each time for 2 hours, and concentrate the extract to obtain the Yagong leaf concentrated extract;

[0032] b. Add water to 2L to pass through the macroporous resin column, first elute with water until the sample outflow is reduced, then elute with 95% ethanol, collect the 95% ethanol eluate, concentrate under reduced pressure to obtain the extract;

[0033] c. Put the extract on a silica gel column, and use CHCl3-MeOH gradient elution to obtain a total of 8 parts of Fr.1-Fr.8,

[0034] d. Take Fr.1 (CHCl 3 -MeOH 10:1 elution fraction) fractions were separated by preparative HPLC with ODS as stationary phase (Kromasil ODS, 300mm×10mm, 5μm), and MeOH-H 2 O 74:26 is the mobile phase, and it is detected by a differential dete...

Embodiment 2

[0045] The preparation of triterpenic acid A sodium salt: the ethanol solution of triterpenic acid A prepared as in Example 1 and the Na of 0.1mol / L 2 CO 3 The aqueous solution is equimolarly mixed and reacted, and dried under reduced pressure to obtain the product.

Embodiment 3

[0047] Tablet: active ingredient 10mg

[0048] Lactose 187mg

[0049] Corn starch 50mg

[0050] Magnesium Stearate 3mg

[0051] Preparation method: mix the active ingredient (the product obtained in Example 1 or Example 2), lactose and starch, uniformly moisten it with water, sieve the wetted mixture and dry it, then sieve it, add magnesium stearate, and then sieve the mixture Compressed tablets, each tablet weighs 250mg, and the active ingredient content is 10mg.

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PUM

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Abstract

The invention discloses a smallanthus sonchifolius diterpenoid acid and the salt as shown in general formula (I), drug combination using the compound as active component, the preparation method and the application of the compound and the drug combination in treating diabetes. The smallanthus sonchifolius diterpenoid acid and the salt is characterized in that: smallanthus sonchifolius leaf is extracted using water or hydrous ethanol; the extractant is concentrated to get concentrated extractant for smallanthus sonchifolius leaf which is arranged onto macroporous resin column; firstly water is used for elution until outflow of sample is decreased; 95% of ethanol is used for elution; 95% of ethanol eluent is then collected and decompressed and concentrated to get extraction; the extraction is arranged onto silica column; chloroform - methanol gradient is used for elution to get 1 to 8 of fractions; the fraction 1 is taken to prepare HPLC; ODS is used as a fixed phase and MeOH-H2O 74 : 26 is used as mobile phase; refractive index detector is used for detecting; relative chromatographic peak can be collected, thereby getting needed products through the preparation.

Description

technical field [0001] The invention relates to an agonist diterpene acid compound (argonium diterpene acid and its salt), a pharmaceutical composition using the compound as an active ingredient, a preparation method and an application in the preparation of a medicine for treating diabetes. Background technique [0002] Yagong (Smallanthus sonchifolius (Poepp. & Endl.) H. Robinson, formerly known as Polymnia sonchiflia), Asteraceae (Asteraceae), tubular flower subfamily (Heliantheae) plant, originally grown in the Andes at an altitude of 880-3500m, extending from Venezuela to the northeast of Argentina. Yagon has been planted all over other continents. It was first planted on a small scale in several states of the United States, and then sold as a special vegetable in supermarkets in New Zealand. In the 1980s, Yagon was introduced from New Zealand to Japan in Asia, and then It has been introduced to Italy, Germany, France, the Czech Republic, South Korea, Brazil, Russia and ...

Claims

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Application Information

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IPC IPC(8): C07C59/42C07C51/42A61K31/19A61P3/10
Inventor 窦德强邱鹰昆康廷国项征董锋
Owner 珍奥集团股份有限公司
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