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Novel compound separated from immature exocarp of Juglans mandshurica Maxim, and preparation and use thereof

A compound, Qinglong's technology, is applied in the preparation of anti-tumor drugs. The field of preparation of this compound can solve the problems of lagging, stagnation, and lack of anti-tumor effects in the development of Bei Qinglongyi's medicinal resources, and achieve excellent anti-cancer activity. Effect

Inactive Publication Date: 2012-07-04
HEILONGJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the basic research on its pharmacodynamic substances has not been carried out in depth, and the literature reports mostly stay on the pharmacological effects of its crude extract and lack the antitumor effect of its active ingredients (Ji Yubin, Ma Hongtu, Yang Bo, Ji Chenfeng. Bei Qinglongyi Research on the anti-tumor effect of different extraction parts. Chinese Herbal Medicine, 2004, 35(10): 1145-1147), which led to a serious lag in the development of Beiqinglongyi, a medicinal resource

Method used

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  • Novel compound separated from immature exocarp of Juglans mandshurica Maxim, and preparation and use thereof
  • Novel compound separated from immature exocarp of Juglans mandshurica Maxim, and preparation and use thereof
  • Novel compound separated from immature exocarp of Juglans mandshurica Maxim, and preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] A new anti-tumor compound isolated from Beiqinglongyi, named Qinglongyisu A, the structural formula of the compound is:

[0024]

[0025] The preparation of a new anti-tumor compound in Beiqinglongyi is to take fresh Beiqinglongyi and soak it in ethanol for extraction, concentrate the extract, add water to the concentrated solution, and take the supernatant after centrifugation, and the supernatant is absorbed through the macropores Resin, the adsorption resin is eluted with ethanol, the eluate is evaporated to dryness and dissolved in methanol, filtered and injected into dextran gel, the methanol eluate is collected, the silica gel thin layer is qualitative, and the same components are combined to obtain the compound. 98%.

[0026] The preparation of a new anti-tumor compound in Beiqinglongyi, the fresh Beiqinglongyi soaked in ethanol for extraction, and the extract is concentrated, is to soak the fresh Beiqinglongyi in 75% ethanol for one week and extract three tim...

Embodiment 2

[0033] Compound Preparation

[0034] Material source Beiqinglongyi is the immature fruit of Juglans Mandshurica MAXIM., which was collected in Wuchang County, Heilongjiang Province in mid-July.

[0035] Extraction and separation Soak fresh Beiqinglongyi with 75% ethanol for one week, extract three times in total, combine the extracts, concentrate under reduced pressure, and concentrate to a concentrated solution with a relative density of 1.10-1.14 (50°C), add 10 times the amount of water to the concentrated solution Disperse, centrifuge, take the supernatant, inject it into the treated Diaion HP-20 macroporous adsorption resin (the ratio of the concentrated solution to the resin is 1:50), flow rate 10ml / min, wash with 3 times the volume of the column bed respectively , wash with 30% ethanol of 5 times the volume of the column bed, collect the 30% ethanol eluate, evaporate the eluate to dryness under reduced pressure to obtain a residue, dissolve the residue with a small amoun...

Embodiment 3

[0046] An application of the above compound in the field of anticancer.

[0047] Inhibits human HL-60 leukemia cells, human Kato-III gastric cancer cells and human A 549 Activity experiment of lung cancer cells:

[0048] cell culture

[0049] Human HL-60 leukemia cells, human Kato-III gastric cancer cells and human A 549 Lung cancer cells were cultured in RPMI 1640 medium supplemented with 10% FBS, L-glutamine, 100 U / ml penicillin and 100 μg / ml streptomycin. Take the cell count in the logarithmic growth phase, with 3×10 4 Inoculated in 96-well plate with 180 μl per well at 37°C, 5% CO 2 cultured in an incubator for 24 hours.

[0050] Cytotoxicity assay

[0051] Drugs of different concentrations (1-100 μM) were treated with EtOH-H 2 O (1:9) was dissolved to 20 μl as the solvent, and 20 μl of EtOH-H was added to the blank group 2 O (1:9) solution, the cells continued to be cultured for 72 hours, and then the MTT method was used for determination, that is, the cultured ce...

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Abstract

The invention relates to a novel compound separated form north Juglans regia and a preparation method and application thereof. The preparation method adopts a method for combining alcohol extraction, chromatographic separation and purification and cytoactive assay to separate the novel compound, which is not reported before and has anti-tumor function, from the north Juglans regia, and adopts mass spectrum and high-resolution nuclear magnetic resonance technique to determine the structure of the compound. The structural formula of the novel compound is the right formula (I). The novel compound is applied in the field of medicine.

Description

Technical field: [0001] The present invention relates to a new compound, which is a new substance extracted and separated from the traditional Chinese medicine Beiqinglongyi, and has antitumor activity; the present invention also relates to a preparation method of the compound; application in medicine. Background technique: [0002] Cancer is a serious disease that threatens human life. Therefore, research on anticancer drugs has always been a hot spot in the world. Compared with chemical drugs, traditional Chinese medicine anti-tumor is unique in improving immunity and reducing mutagenic toxicity. Therefore, it is necessary to find anti-tumor traditional Chinese medicine with definite curative effect from the motherland's treasure house of medicine, clarify the material basis of its efficacy, and then develop a high-efficiency and low-toxicity drug. The new drug has become the focus of many years of research in the field of traditional Chinese medicine. [0003] Beiqinglo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C62/38C07C51/42A61K31/192A61K36/52A61P35/00
Inventor 刘丽娟李巍
Owner HEILONGJIANG UNIV
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