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Preparation method for hederagenin and salts thereof

A technology for helexin and total saponins, which is applied in the field of medicine, can solve the problems of poor water solubility of helexin, reduced dosage, low bioavailability and the like, avoid the use of toxic reagents, improve purity and yield, Simple preparation process

Active Publication Date: 2014-03-12
SHANGHAI FAMASI MEDICAL BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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
  • Preparation method for hederagenin and salts thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Take 1 kg of Dipsacus medicinal material, use 5L 50% ethanol solution, reflux extraction twice, each time for 1 hour, 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 it stand for 8 After more than 1 hour, filter, remove the precipitate, and obtain the supernatant; the supernatant is absorbed to saturation by D101 macroporous adsorption resin, first remove impurities with 0.1% NaOH aqueous solution of 3 times the column volume, and then wash with water until the pH value of the effluent It is neutral, and finally eluted with 50% ethanol solution of 3 times the column volume, and the eluent is concentrated under reduced pressure to obtain the total saponins of Dipsacus; Hydrolyze at ℃ for 2 hours, adjust the pH value of the hydrolyzate to 2-4, let it cool, filter, add 30% ethanol solution to dissolve the filter residue to make the concentration ...

Embodiment 2

[0037]Take 1 kg of Dipsacus medicinal material, use 10L of 60% ethanol solution, reflux extraction 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 more than 1 hour, filter and remove the precipitate to obtain the supernatant; the supernatant is adsorbed to saturation by D101 macroporous adsorption resin, first remove impurities with 0.5% NaOH aqueous solution of 6 times the column volume, and then wash with water until the pH value of the effluent It is neutral, and finally eluted with 60% ethanol solution of 6 times the column volume, and the eluent is concentrated under reduced pressure to obtain the total saponins of Dipsacus; Hydrolyze at ℃ for 4 hours, adjust the pH value of the hydrolyzate to 2-4, let it cool, filter, add 50% ethanol solution to dissolve the filter residue to make the concentrat...

Embodiment 3

[0039] Take 1 kg of Dipsacus medicinal material, use 15L of 80% ethanol solution, reflux extraction twice, each time for 2 hours, combine the extracts, filter, concentrate the filtrate under reduced pressure, add water to adjust the volume of the filtrate to contain about 250 mg / ml of solids, and let it stand for 8 After more than 1 hour, filter and remove the precipitate to obtain the supernatant; the supernatant is adsorbed to saturation by D101 macroporous adsorption resin, first remove impurities with 9 times column volume of 10% NaOH aqueous solution, and then wash with water until the pH value of the effluent It is neutral, and finally eluted with 90% ethanol solution of 9 times the column volume, and the eluent is concentrated under reduced pressure to obtain the total saponins of Dipsacus; Hydrolyze at ℃ for 4 hours, adjust the pH value of the hydrolyzate to 2-4, let it cool, filter, add 80% ethanol solution to dissolve the filter residue to make the concentration 100mg...

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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 dry root of Dipsacus asperoides C.Y.ChengetT.M.Ai (or DipsacusasperWall), a plant of the family Dipsaceae, which is listed as 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 presen...

Claims

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Application Information

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