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Preparation method of tonkinin A and application of tonkinin A to resisting tumors

A technology of clasperrin and flash extraction, which is applied in the directions of antineoplastic drugs, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve the problem that it is not suitable for the industrial preparation of claspirin A, and the preparation amount is small. , low sample yield, etc.

Inactive Publication Date: 2014-10-01
NANJING ZELANG MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the complicated operation, small amount of preparation, and low sample yield, it is not suitable for the industrial preparation of bucklesin A

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Preparation of bucklelin A

[0021] Take the root of the buckwheat, crush it, weigh 1kg, add 5 times of 80% ethanol solution, the extraction voltage is 140V, the extraction time is 90s, carry out flash extraction, filter to obtain the extract, and the extract is passed through a filter with a molecular weight cut-off of 3000 Ultrafiltration membrane ultrafiltration and nanofiltration membrane concentration with a molecular weight cut-off of 500, the operating pressure is 0.8MPa, the membrane concentrate is concentrated and dried under reduced pressure to obtain a crude extract; high-speed countercurrent chromatography is used to separate and purify bucklein in the crude extract A, take petroleum ether-ethyl acetate-methanol-water as the two-phase solvent system with a volume ratio of 5:4:6:2, and the upper phase is filled with a high-speed countercurrent chromatographic column as the stationary phase. The mobile phase is used as the mobile phase, the flow rate is 3mL / mi...

Embodiment 2

[0023] Anti-tumor application of bucklein A

[0024] 1. Materials

[0025] Animals: Kunming mice, male and female, weighing 20±2g, provided by Nanjing University of Traditional Chinese Medicine.

[0026] Cell line: Sarcoma 180 ascites-type tumor line (S180), provided by Shanghai Institute of Materia Medica, Chinese Academy of Sciences.

[0027] 2. Method

[0028] Take 50 mice and inoculate each mouse with S 180 Tumor fluid was randomly divided into 5 groups the next day, 10 rats in each group, which were normal saline control group (NS group), positive control group, low-dose bucklein A group (1mg / kg), middle-dose group (2mg / kg ), high dose group (4mg / kg). 24 hours after inoculation, the buckletonin A administration group was intragastrically administered for 7 consecutive days, and the positive control group was intraperitoneally injected twice during the test, and administered every other day. During this period, the general activities, fur and feces of the mice were ob...

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Abstract

The invention discloses a preparation method and an application of a plant extract and in particular relates to a preparation method of tonkinin A and an application of tonkinin A to resisting tumors. The preparation method comprises the following steps: (1) grinding the roots of Uvaria tonkinensis Finet et Gagnep, carrying out flash extraction with an alcohol solution and carrying out filtration, thus obtaining an extracting liquid; (2) treating the extracting liquid with a membrane separation system and carrying out concentration and drying, thus obtaining a crude extract; (3) separating and purifying tonkinin A in the crude extract by adopting high-speed countercurrent chromatography and collecting the component tonkinin A, wherein a two-phase solvent system is petroleum ether-ethyl acetate-methanol-water; the upper phase is a stationary phase; and the lower phase is a mobile phase; and (4) carrying out vacuum concentration on the component tonkinin A, carrying out precipitation and crystallization and filtering out the crystals, thus obtaining tonkinin A. The preparation method is simple and convenient in process operation, is high in yield, is slight in pollution and is suitable for producing high-purity tonkinin A. Tonkinin A has the function of accelerating tumor resistance. Adding an intestinal absorption enhancer to an oral formula of tonkinin A is beneficial to improving the bioavailability.

Description

technical field [0001] The invention discloses a preparation method and application of a plant extract, and in particular relates to a preparation method and anti-tumor application of bucklesin A. Background technique [0002] Tonkinin A (Tonkinin A) is an acetylsarginine compound, CAS No. 182806-02-6, molecular formula C 37 h 66 o 7 , the molecular weight is 622.93, and the molecular structure formula is: [0003] [0004] Uvaria tonkinensis Finet et Gagnep. is derived from the root of Annonaceae (Annonaceae) Uvaria tonkinensis Finet et Gagnep. It has anti-tumor promoting effect and has selective cytotoxic activity on human tumor cell lines. [0005] At present, the secondary metabolites of Annonaceae plants, acetylsarginine compounds of Annonaceae, are regarded as potential resources of new anti-tumor drugs, and they are candidates for anti-tumor drugs. [0006] Through literature search, most of the existing acetylarginine active substances are extracted by using s...

Claims

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Application Information

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IPC IPC(8): C07D307/58A61K47/36A61K47/28A61K47/12A61K31/365A61P35/00
CPCC07D307/58A61K31/365A61K36/185
Inventor 刘东锋杨成东
Owner NANJING ZELANG MEDICAL TECH
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