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Preparation method of 18-alpha glycyrrhetinic acid

A technology of glycyrrhetinic acid and glycyrrhizic acid, applied in the field of bioengineering, can solve life-threatening problems and limit the clinical application of chronic liver disease

Active Publication Date: 2022-03-25
山东凤凰生物科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Unfortunately, the active pharmaceutical ingredient of glycyrrhizic acid (pentacyclic triterpene glycosides), the main liver-protecting active substance in various preparations of licorice, is 18-β glycyrrhetinic acid (glycon), although it has significant and stable However, if it is used for a long time, it will cause side effects such as high blood pressure, hypokalemia, sodium and water retention (collectively referred to as the biological activity of adrenocorticotropic hormone [ACTH]), and even lead to serious conditions such as heart failure, which is life-threatening. Thus limiting its clinical application in chronic liver disease

Method used

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  • Preparation method of 18-alpha glycyrrhetinic acid
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  • Preparation method of 18-alpha glycyrrhetinic acid

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Embodiment

[0035] A preparation method of 18-alpha glycyrrhetinic acid, the specific steps are as follows:

[0036] Step 1: Take 2kg of disc-shaped licorice decoction pieces, and carry out graded ultrafine pulverization, that is, first use a universal pulverizer to pulverize the licorice decoction pieces into fine particles with a particle size of about 20 mesh, and then use a vacuum ultrafine pulverizer to perform ultrafine grinding. Pulverize, cross 200 mesh sieves, obtain the licorice superfine powder of particle size below 200 mesh, add this powder to compound enzyme liquid (compound enzyme liquid preparation: cellulase 10g: ligninase 10g: pectinase 5g, dissolve in 8L of deionized water), pour it into a 100L reaction kettle, stir well, soak for 4 hours, then add 16L of water, decoct at 100°C for 2 hours, cool down and filter to remove slag, collect licorice extract rich in glycyrrhizic acid Liquid about 60L, concentrated into about 20L of licorice concentrated solution of one-third o...

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Abstract

The invention discloses a preparation method of 18-alpha glycyrrhetinic acid, which comprises the following steps: by taking licorice decoction pieces as a raw material, firstly carrying out enzymolysis treatment by using a compound enzyme, then decocting and concentrating to obtain a licorice concentrated solution rich in glycyrrhizic acid, and then carrying out enzymolysis under the catalytic action of a culture product of a bacillus subtilis subsp. Natto strain of a high-yield glucuronidase enzyme system to obtain the 18-alpha glycyrrhetinic acid. Continuously converting glycyrrhizic acid in the liquorice concentrated solution into 18-beta glycyrrhetinic acid to obtain a reaction solution; a culture product of a rhizopus oryzae strain of a high-yield glycyrrhetinic acid isomerase enzyme system is compounded with catalase to prepare a rhizopus oryzae mycelium-catalase co-immobilized cell catalyst, under the catalytic action of the rhizopus oryzae mycelium-catalase co-immobilized cell catalyst, the reaction liquid reacts to generate a crude product of 18-alpha glycyrrhetinic acid, and the crude product is purified to obtain the 18-alpha glycyrrhetinic acid. On the premise that the liver protection curative effect of the glycyrrhetinic acid is reserved, the side effects of 18-beta glycyrrhetinic acid caused by long-term application are removed, so that the 18-beta glycyrrhetinic acid can be safely and effectively applied to clinical treatment of various liver diseases, and the safety of clinical medication is greatly improved.

Description

technical field [0001] The invention belongs to the technical field of bioengineering, and relates to a preparation method of 18-alpha glycyrrhetinic acid. Background technique [0002] Glycyrrhiza licorice is a kind of food and medicine dual-purpose plant. It is widely used in food, feed, cosmetics and daily chemicals as flavoring agent, thickener, auxiliary agent, additive, preservative, antioxidant, etc., but its The most important use is in the field of medicine. [0003] There is a saying in Chinese medicine that there are "ten directions and nine herbs", that is, most of the compound prescriptions of Chinese medicine are inseparable from licorice, and it is known as the "national guy" of Chinese medicine; the main chemical component of licorice, glycyrrhizic acid and its active component, glycyrrhetinic acid, It is widely used in Chinese patent medicine and modern Chinese medicine. It is particularly pointed out that among the traditional Chinese medicine compounds a...

Claims

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Application Information

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IPC IPC(8): C07J63/00C12P33/06C12R1/125C12R1/845
CPCC07J63/008C12P33/06
Inventor 吴力克王静张维庄金丽李凤娟
Owner 山东凤凰生物科技股份有限公司
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