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Preparation method for hederagenin and salts thereof

A technology of helexin and total saponins, which is applied in the field of medicine, can solve the problems of poor water solubility of helexin, reduced dosage, serious environmental pollution, etc., to avoid the use of toxic reagents, improve the purity and yield, and prepare The effect of simple process

Active Publication Date: 2012-09-12
SHANGHAI FAMASI MEDICAL BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The process is complex in operation, high in cost, and the solvent used is highly toxic, causing serious environmental pollution, and the yield is low, so it is not suitable for large-scale industrial production, and hedera saponin has poor water solubility and low bioavailability. After salt formation, the water solubility is better, the bioavailability, and the dosage can be reduced

Method used

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  • Preparation method for hederagenin and salts thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Take 1kg of Dipsacus medicinal material, use 5L of 50% ethanol solution, reflux and extract 2 times, 1 hour each time, combine the extracts, filter, concentrate the filtrate under reduced pressure, add water to adjust the volume of the filtrate so that the solid content is about 50mg / ml, and let stand for 8 After hours, filter to remove the precipitate to obtain the supernatant; the supernatant is adsorbed to saturation by D101 macroporous adsorption resin, first use 3 times the column volume of 0.1% NaOH aqueous solution to remove impurities, and then rinse with water to the effluent pH value It is neutral, and finally eluted with a 50% ethanol solution of 3 times the column volume. The eluent is concentrated under reduced pressure to obtain Diptera total saponins; dissolve with water to make Diptera total saponins concentration 10mg / ml, add 1% NaOH, 50% Hydrolyze at ℃ for 2 hours, adjust the pH of the hydrolyzate to 2~4, let it cool, filter, and dissolve the filter resi...

Embodiment 2

[0037] Take 1kg of Dipsacus medicinal materials, use 10L 60% ethanol solution, reflux and extract twice, 1.5 hours each time, combine the extracts, filter, concentrate the filtrate under reduced pressure, add water to adjust the volume of the filtrate so that the solid content is about 100mg / ml, and let it stand for 8 After hours, filter to remove the precipitate to obtain the supernatant; the supernatant is adsorbed to saturation by D101 macroporous adsorption resin, first use 6 column volume of 0.5% NaOH aqueous solution to remove impurities, and then rinse with water to the effluent pH value It is neutral, and finally eluted with 60% ethanol solution of 6 times the column volume. The eluent is concentrated under reduced pressure to obtain the total saponins of Dipsacus; Dissolve with water to make the concentration of total saponins of Dipsacus 25mg / ml, add 5% NaOH, 80 Hydrolyze at ℃ for 4 hours, adjust the pH of the hydrolyzed solution to 2~4, let it cool, filter, and dissol...

Embodiment 3

[0039] Take 1kg of Dipsacus medicinal material, use 15L 80% ethanol solution, reflux and extract 2 times, 2 hours each time, combine the extracts, filter, concentrate the filtrate under reduced pressure, add water to adjust the volume of the filtrate so that the solid content is about 250mg / ml, and let it stand for 8 After hours, filter to remove the precipitate to obtain the supernatant; the supernatant is adsorbed to saturation by D101 macroporous adsorption resin, first use 9 times the column volume of 10% NaOH aqueous solution to remove impurities, and then rinse with water to the effluent pH value It is neutral, and finally eluted with a 90% ethanol solution of 9 times the column volume. The eluate is concentrated under reduced pressure to obtain the total saponins of Dipsacus; Dissolve with water to make the concentration of total saponins of Dipsacus 100mg / ml, add 10% NaOH, 100 Hydrolyze at ℃ for 4 hours, adjust the pH of the hydrolyzate to 2~4, leave to cool, filter, and...

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Abstract

The invention discloses a preparation method for hederagenin and the salts thereof, comprising the following steps of: extracting Dipsacus asperoides via ethanol, recovering a solvent from the extracted solution at a reduced pressure, purifying via macroporous adsorption resin or extracting and purifying via n-butyl alcohol to obtain Dipsacus asperoides total saponin, performing alkaline hydrolysis and acid hydrolysis on the Dipsacus asperoides total saponin, and then crystallizing or refining via the macroporous adsorption resin to obtain high-purity hederagenin, and reacting the hederagenin with alkali to prepare the salts of the hederagenin finally. According to the invention, the raw materials are abundant in the source and low in price; the whole preparation process is free from the use of toxic reagents, safe and low-toxicity; the preparation process is simple, high in separation and purification efficiency, greatly improved in the purity and productivity of the products, suitable for industrialized production, easy to popularize and apply, and remarkable in pharmacologic action; and a new medicine source is provided for treatment and research on hyperlipidemia.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of helexin and a salt thereof. Background technique [0002] Dipsacus is the dried root of Dipsacus asperoides C.Y. Cheng et T.M. Ai (or Dipsacus asper Wall), a plant of Dipsacaceae. It is listed as the top grade in "Shen Nong's Herbal Classic". [0003] Modern studies have shown that Dipsacus mainly contains triterpenoid saponins, alkaloids, volatile oil and other components. Pharmacological experiments have reported that the total saponins of Dipsacus and its aglycones have pharmacological activities such as promoting bone healing, anti-tumor, anti-aging, lowering blood fat, anti-depression, and lowering blood sugar. So far, 39 kinds of triterpenoid saponins have been isolated from Dipsacus chuanxiong, 37 of which are oleane-type, and 33 of which are hedera saponins, which are linked to hydroxyl groups at the C-23 position. [0004] At prese...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/56A61P3/06
Inventor 周清黄娟叶治营马仁强
Owner SHANGHAI FAMASI MEDICAL BIOTECH
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