A kind of spirosterine alkaloid glycoside alkaloid and its preparation method and use

A technology for spiro steroid alkane and alkaloid, which is applied in the field of glycoside alkaloid preparation, can solve the problems of incomplete confirmation of component efficacy and mutual influence, complex components, etc., and achieves the effect of exact function and single component.

Inactive Publication Date: 2019-02-26
XIYUAN HOSPITAL OF CHINA ACAD OF CHINESE MEDICAL SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The technical problem to be solved by the present invention is the defect that the components of the traditional Chinese medicinal plant extracts are complex, and the efficacy and mutual influence of all components cannot be fully confirmed, thereby providing a single-component compound spirostanoid alkane-type glycoside alkaloid , and further provide its preparation method and its use in the preparation of drugs for the treatment of non-small cell lung cancer

Method used

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  • A kind of spirosterine alkaloid glycoside alkaloid and its preparation method and use
  • A kind of spirosterine alkaloid glycoside alkaloid and its preparation method and use
  • A kind of spirosterine alkaloid glycoside alkaloid and its preparation method and use

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Embodiment 1

[0064] (3β,5α,22α,25R)-spirosterine alkane-3-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranosyl- The preparation method of (1→4)-β-D-galactopyranoside comprises the following steps:

[0065] (1) Take 10Kg dried whole grass of Baiying, add 80L of 70% ethanol aqueous solution by volume, extract by reflux for 3 times, extract 2h each time, filter, and combine the filtrates; the above filtrate is concentrated to a relative density of 1.05 at 50°C. The extract, add 10 times the quality of the extract to disperse in distilled water, filter, take the filtrate and add it to a D151 macroporous adsorption resin column, and sequentially use 3 times the column volume of distilled water and 3 times the column volume of the 95% ethanol aqueous solution to elute , discard the eluent, and then use 4 times the column volume to elute with an ethanol aqueous solution containing a volume fraction of 6‰ hydrochloric acid. The volume concentration of ethanol in the hydrochloric acid ethanol aqueous so...

Embodiment 2

[0076] (3β,5α,22α,25R)-spirosterine alkane-3-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranosyl- The preparation method of (1→4)-β-D-galactopyranoside comprises the following steps:

[0077] (1) Refined total alkaloids of Baiying: take 10Kg of dried whole plant of Baiying, add 60L of 70% ethanol aqueous solution by volume, extract by reflux for 4 times, extract for 2 hours each time, filter, and combine the filtrates; the above filtrate is concentrated to 50 ℃ The extract with a relative density of 1.05 was added with distilled water of 8 times the mass of the extract to disperse, filtered, and the filtrate was added to a D151 macroporous adsorption resin column, and the volume concentration of 2 times the column volume of distilled water and 4 times the column volume was 95%. Elution with ethanol aqueous solution, discarding the eluent, and then eluting with an ethanol aqueous solution containing 6‰ hydrochloric acid with a volume concentration of 6‰, the volume concentration of e...

Embodiment 3

[0083] (3β,5α,22α,25R)-spirosterine alkane-3-O-β-D-glucopyranosyl-(1→2)-O-β-D-glucopyranosyl- The preparation method of (1→4)-β-D-galactopyranoside comprises the following steps:

[0084] (1) Refining total alkaloids of Baiying: take 10Kg dried whole plant of Baiying, add 100L of 70% ethanol aqueous solution by volume, extract twice by reflux, extract for 2 hours each time, filter, and combine the filtrates; the above filtrate is concentrated to a temperature of 50°C The extract with a relative density of 1.05 was added with distilled water of 12 times the mass of the extract to disperse it, filtered, and the filtrate was taken and added to a D151 macroporous adsorption resin column, and the volume concentration of 4 times the column volume of distilled water and 2 times the column volume was 95%. Elution with ethanol aqueous solution, discard the eluent, and then use 5 times the column volume to elute with an ethanol aqueous solution containing a volume fraction of 6‰ hydroch...

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Abstract

The invention provides a spirosolane glycoalkaloid(3beta,5alpha,22alpha,25R)-spirosolane-3-O-beta-D-glucopyranosyl-(1 to 2)-O-beta-D-glucopyranosyl-(1 to 4)-beta-D-galactopyranoside, and a preparation method and a use thereof. The spirosolane glycoalkaloid has an inhibition effect on human lung gland cancer cell A549, human maxicell lung cancer cell H460 and human lung squamous cancer cell SK-MES-1, the 50% inhibiting concentration of the A549 cell is 19.22 [mu]g / ml, the 50% inhibiting concentration of the H460 cell is 80.03 [mu]g / ml, and the 50% inhibiting concentration of the SK-MES-1 cell is 54.20 [mu]g / ml. The (3beta,5alpha,22alpha,25R)-spirosolane-3-O-beta-D-glucopyranosyl-(1 to 2)-O-beta-D-glucopyranosyl-(1 to 4)-beta-D-galactopyranoside prepared in the invention, and a preparation thereof, can be used for treating non-small cell lung cancers.

Description

technical field [0001] The invention belongs to the technical field of preparation methods and medicinal uses of glycoalkaloids, and particularly relates to a spirosteroid alkaloid glycoside alkaloids and a preparation method and uses thereof. Background technique [0002] Glycoalkaloids are mainly distributed in the plants of Solanaceae and Liliaceae, and are composed of hydrophobic aglycones and hydrophilic oligosaccharide chains. Three, the oligosaccharide chain is composed of 3 to 4 monosaccharides and is a steroidal saponin. The main purpose of plant synthesis of glycoalkaloids is to defend against the invasion of microorganisms, animals and insects. Therefore, glycoalkaloids have certain toxicity. It can enhance the immunity of the body, resist pathogenic microorganisms and other physiological activities, and has potential medicinal value. Plants of Solanaceae and Liliaceae exist widely in nature, such as Baiying, potato and tomato, which have strong economic value. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00A61K31/706A61P35/00
CPCC07J71/0005
Inventor 王建农韩林
Owner XIYUAN HOSPITAL OF CHINA ACAD OF CHINESE MEDICAL SCI
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