Preparation technique of lysine rhein and use thereof in tumour therapy

A technology of rhein and lysine, which is applied in the direction of antineoplastic drugs, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems that have not been seen before, and achieve the advantages of mass production, high purity, and simple process Effect

Inactive Publication Date: 2008-09-03
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] The new compound of lysine rhein (rhein lysate) involved in t

Method used

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  • Preparation technique of lysine rhein and use thereof in tumour therapy
  • Preparation technique of lysine rhein and use thereof in tumour therapy
  • Preparation technique of lysine rhein and use thereof in tumour therapy

Examples

Experimental program
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Effect test

Embodiment 1

[0055] Embodiment 1> : Preparation of lysine rhein 1

[0056] 20mg of rhein (purchased from Nanjing Qingze Pharmaceutical Technology Development Co., Ltd.) was added to the 50ml eggplant-shaped bottle, and a stirring bar and 5ml of double-distilled water were added to the eggplant-shaped bottle, stirred on a magnetic stirrer for 5 minutes, and then Weigh 30mg of lysine (purchased from Beijing Kehaijunzhou Biotechnology Center), slowly add it into the eggplant-shaped bottle in batches, observe the dissolution of rhein while adding, control the addition time within 30 minutes, and add 30mg of lysine Finally, all the rhein in the reaction solution was dissolved, stirred for 4 hours, and the temperature was controlled at 32°C. After the solution reacted for 4 hours, put the eggplant-shaped bottle in an ice bath, slowly add acetone to the reaction solution, about 6 drops / minute, and observe the change of the reaction solution while adding it dropwise. It was observed that purple ...

Embodiment 2

[0057] Embodiment two >: Preparation of lysine rhein 2

[0058] Add 20mg of rhein to a 50ml eggplant-shaped bottle, and add a stirring bar and 5ml of double-distilled water to the eggplant-shaped bottle, stir on a magnetic stirrer for 5 minutes, then weigh 30mg of lysine, and slowly add to the In the eggplant-shaped bottle, observe the dissolution of rhein while adding. The addition time is controlled at 40 minutes. After adding 30 mg of lysine, all the rhein in the reaction solution is dissolved, stirred overnight, and the temperature is controlled at 32°C. After 24 hours of reaction, slowly add acetone to the reaction solution, about 6 drops / minute, observe the change of the reaction solution while adding dropwise, and observe that the solution appears purple crystals. At this time, 16ml of acetone was added, and the addition time was 30 minutes, Continue to slowly add acetone to the reaction solution, and the purple crystals gradually increase. After adding 20ml of acetone...

Embodiment 3

[0059] Embodiment Three >: Preparation of lysine rhein 3

[0060] Add 20mg of rhein to a 50ml eggplant-shaped bottle, and add a stirring bar and 5ml of double-distilled water to the eggplant-shaped bottle, stir on a magnetic stirrer for 5 minutes, then weigh 30mg of lysine, and slowly add to the In the eggplant-shaped bottle, observe the dissolution of rhein while adding. The addition time is controlled at 30 minutes. After adding 30 mg of lysine, all the rhein in the reaction solution is dissolved, stirred overnight, and the temperature is controlled at 30°C. After reacting for 24 hours, slowly add absolute ethanol to the reaction solution, about 6 drops / minute, observe the change of the reaction solution while adding dropwise, and observe that the solution appears purple crystals. At this time, add absolute ethanol to 17.6ml, add After 30 minutes, continue to slowly add absolute ethanol to the reaction solution, and the purple crystals gradually increase. After adding 22ml ...

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Abstract

The invention relates to lysine rheinic acid, a method for making same, and the application in treatment of tumor. The method is characterized in that the carboxyl of rheinic acid in the solution and the amino of lysine to form a salt structure to enhance the degree of solubility of rheinic acid in the solution; propanone or absolute alcohol is used to make lysine rheinic acid be separated out in a crystallization form, and the stable lysine rheinic acid crystallization is obtained by separating, purifying and drying; lysine rheinic acid has a appreciable inhibitory action for proliferation and growth of tumour cell, proved by vitro and vivo experiments. The lysine rheinic acid will become an ideal candidate drug for treating tumor.

Description

Technical field: [0001] The invention relates to rhein lysate, a stable salt formed by rhein and lysine, its preparation process and application in the medical field. Background technique: [0002] Rhein (4.5-dihydroxyanthraquinone, referred to as RH) belongs to the monoanthracene nucleus 1,8-dihydroxyanthraquinone derivative, and is an active ingredient isolated and purified from many traditional Chinese medicines such as rhubarb, Polygonum multiflorum, and Polygonum cuspidatum. Rhein contains two hydroxyl groups and one carboxyl group, has strong polarity, and has electrochemical redox properties. The pharmacological effects of rhein mainly include: anti-tumor, anti-inflammatory, antibacterial and mediation of renal function. [0003] 1. Anti-tumor effect [0004] It has been reported in the literature that rhein is beneficial to melanoma, breast cancer, glioma, Ehrlich ascites carcinoma, P 388 Leukemia is inhibited. By changing the function of cells and cytoskeleton m...

Claims

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Application Information

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IPC IPC(8): C07C229/26C07C66/02A61K31/205A61P35/00
Inventor 林雅军甄永苏刘秀均吴淑英许先栋
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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