Ion-pair compound of chelerythrine from Chinese medicine extracts, preparation and application thereof

A technology of chelerythrine and compounds, which is applied in the direction of drug combination, application, carboxylate preparation, etc., can solve the problems of increasing the difficulty of compounding chelerythrine drugs, increasing production costs, increasing the difficulty of reaction, and achieving Conducive to long-term storage and in vivo use, increase stability, and enhance the effect of drug efficacy

Inactive Publication Date: 2010-07-14
曾建国
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in this method, two macromolecular groups with similar physical and chemical properties and the same pharmacological effects must be selected for compounding. After entering the body, the two molecules dissociate respectively to exert their medicinal effects. For the present invention, it means that one must be selected The compound of cataerythrine has similar physical and chemical properties and the same pharmacological effect as a traditional Chinese medicine extract, which not only increases the production cost, but also increases the difficulty of the reaction. To determine the primary and secondary / proportional relationship of two medicinal ingredients, and to prove whether the two medicinal active ingredients can produce a synergistic effect by relying on numerous clinical experiments, this undoubtedly increases the development of chelerythrine compound drugs. difficulty

Method used

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  • Ion-pair compound of chelerythrine from Chinese medicine extracts, preparation and application thereof
  • Ion-pair compound of chelerythrine from Chinese medicine extracts, preparation and application thereof
  • Ion-pair compound of chelerythrine from Chinese medicine extracts, preparation and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Example 1: The preparation method of the ion-pair compound generated by chelerythrine hydrochloride and shikimic acid sodium salt

[0047] Dissolve 10.0 g of chelerythrine hydrochloride (provided by the Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) in 1000 mL of water, and heat to above 90°C until all chelerythrine hydrochloride is dissolved to make celandine Red alkali hydrochloride aqueous solution (A); Dissolve 1.0 g of shikimic acid sodium salt in 200 mL of water to prepare shikimic acid sodium salt aqueous solution (B);

[0048] Slowly add (B) to (A) at above 90°C, stir continuously at 90°C, react for 30 minutes, cool to room temperature, filter, wash the precipitate fully with pure water, and dry the precipitate in vacuum at 60°C to obtain light yellow crystals, conduct 1 H-NMR, 13 The compound obtained by C-NMR and MS analysis is the ion-pair compound of chelerythrine shikimate.

Embodiment 2

[0049] Example 2: The preparation method of the ion-pair compound generated by chelerythrine and carnosic acid

[0050] Dissolve 10.0 g of chelerythrine (provided by Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) in 2000 mL of acetone, and stir to dissolve. Then directly add 10.0 g of carnosic acid, stir at normal temperature for 45 min, concentrate, dry to obtain a solid, then refine with ethyl acetate to obtain a light yellow crystal, carry out 1 H-NMR, 13 The compound obtained by C-NMR and MS analysis is the ion-pair compound of chelerythrine carnosic acid.

Embodiment 3

[0051] Embodiment 3: The preparation method of the ion-pair compound generated by chelerythrine hydrochloride and sodium rosmarinate

[0052] Take 4.5 g of chelerythrine hydrochloride (provided by the Hunan Province Traditional Chinese Medicine Extraction Engineering Research Center) and dissolve it in 1 L of water, then add 4.0 g of sodium rosmarinate, stir at 80 ° C for 30 min, cool, filter, wash, After drying, it was further refined with methanol to obtain light yellow crystals. by carrying out 1 H-NMR, 13 The compound obtained by C-NMR and MS analysis is an ion pair compound of chelerythrine and rosmarinic acid.

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Abstract

The invention relates to an ion-pair compound of chelerythrine from Chinese medicine extracts, a preparation method and application thereof. Organic acids of the invention mainly comprise chlorogenic acid, gallic acid, shikimic acid, oleanolic acid, ursolic acid, benzoic acid, salicylic acid, tartaric acid, lactic acid, sorbic acid, fumaric acid, malic acid, citric acid, maleic acid, glycyrrhizic acid, glycyrrhetinic acid, carnosic acid, P-hydroxycinnamic acid, rosmarinic acid, succinic acid, ferulic acid, protocatechuic acid, cinnamic acid, caffeic acid, chicoric acid or cortex pseudolaricis acetic acid. The ion-pair compound prepared from the chelerythrine and the organic acids has the antibacterial biological activity. The invention relates to the application of the ion-pair compound of the chelerythrine to medicine, animal remedy or daily use cosmetics.

Description

technical field [0001] The present invention relates to an ion-pair drug and preparation method of chelerythrine from a traditional Chinese medicine extract, and the pharmaceutical use of the drug in antibacterial aspects, especially in human medicine, former medicine and daily chemical products, especially relates to the medicine containing The ion-pair compound formed by chelerythrine and organic acid is used in the preparation of veterinary medicine or daily chemical products, especially the application of veterinary medicine and pharmaceutical feed additive in the direction of animal antibacterial. Background technique [0002] In recent years, due to the abuse of antibiotics by humans, the resistance of bacteria to various antibiotics has been showing a rapid upward trend. China is one of the countries with the most serious abuse of antibiotics in the world, and the resulting problem of bacterial resistance is particularly prominent. The resistance of some bacteria iso...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/056C07C62/32C07C61/39C07C69/732C07C63/08C07C65/10C07C65/03C07C51/41A61K31/4741A61K31/216A61K31/192A61K31/19A61K31/60A61P29/00A61P31/04A61P31/10A61P31/12A61K8/49A61Q1/00A61Q19/10A61Q11/00A61Q13/00A61Q15/00A61Q19/00A61Q5/00A23K1/14
Inventor 曾建国谈满良贺晓华杜方麓
Owner 曾建国
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