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Application of fatty acid compounds in the preparation of drugs for the prevention and treatment of liver cancer

A fatty acid treatment technology for liver cancer, applied in drug combinations, digestive system, anti-tumor drugs, etc., can solve problems such as inability to perform normal functions, and achieve the effect of enhancing activity inhibition and promoting apoptosis

Inactive Publication Date: 2014-10-29
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When apoptosis is initiated, 116kD PARP is in Asp 216 -Gly 217 It is cut into two fragments of 31kD and 85kD by caspase-3, so that the two zinc finger structures in PARP that bind to DNA are separated from the catalytic region at the carboxyl end, and cannot perform normal functions

Method used

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  • Application of fatty acid compounds in the preparation of drugs for the prevention and treatment of liver cancer
  • Application of fatty acid compounds in the preparation of drugs for the prevention and treatment of liver cancer
  • Application of fatty acid compounds in the preparation of drugs for the prevention and treatment of liver cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] The preparation of embodiment 1 fatty acid compound

[0039] 1. Prepare the alcoholic extract of Angelica dahurica

[0040] 1) Weigh 3kg of dried Angelica dahurica root, add 30L of 60% ethanol, stir, boil and reflux for 2 hours in the extraction tank, filter, and collect the filtrate;

[0041] 2) The filter residue was boiled and refluxed with 60% ethanol to extract twice, filtered, and the filtrate was collected. The dosage of 60% ethanol was 30L / time;

[0042] 3) Merge the filtrates for 3 times, extract with ethyl acetate, the amount of extractant is 30L each time, and collect the upper layer extract;

[0043] 4) The lower layer was extracted twice with ethyl acetate, and the upper layer extracts were combined for three times, and vacuum-dried to obtain 48.3g of the alcoholic extract of Angelica dahurica (coded as: AD).

[0044] 2. Silica gel column chromatography and ODS column chromatography to prepare monomeric compounds

[0045] 1) Soak 200-300 mesh silica gel ...

Embodiment 2

[0058] Embodiment 2 fatty acid compound pharmacodynamics experiment

[0059] 1. Experimental materials and reagents

[0060] (1) Experimental cell: human liver cancer cell HepG2

[0061] (2) Strains

[0062] pGEX4T1-PTP-SHP2 E. coli BL21

[0063] pGEX4T1-VHR E. coli BL21

[0064] pGEX4T1-HEPTP E. coli BL21

[0065] (3) Medicinal material Hangzhou Angelica dahurica produced in Zhejiang

[0066] (4) Main reagents

[0067]

[0068] (5) culture medium

[0069] LB liquid medium:

[0070] 1% (g / ml) Tryptone, 0.5% (g / ml) Yeast Extract, 1% (g / ml) NaCl

[0071] (6) Buffers and reagents required for GST protein purification

[0072] PBS Bμffer: 137mM NaCl, 2.7mM KCl, 10mM NaCl 2 HPO 4 ,2mM KH 2 PO 4

[0073] 100mg / ml ampicillin

[0074] Protease Inhibitor and Phosphatase Inhibitor Stock Solutions:

[0075]

[0076]

[0077] IPTG stock solution (0.8M)

[0078] Buffer W: 25mM Tris-HCl pH7.5, 150mM NaCl, 10mM β-mercaptoethanol, 1mM EDTA

[0079] Buffer W1: 25mM ...

Embodiment 314

[0197] Embodiment 314Z, the preparation of 17Z-eicosadienoic acid tablet

[0198] Get 14Z, 17Z-eicosadienoic acid 1g, microcrystalline cellulose 27g and magnesium stearate 2g and mix, and the mixture is pressed into a tablet with a diameter of 6mm and a weight of 300mg with a single-punch tablet machine. The tablet contains 10mg of 14Z, 17Z-21-eicosadienoic acid.

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Abstract

The invention relates to fatty acid compounds, and provides an application of a fatty acid compound in preparation of medicines for preventing and treating the liver cancer. Angelica is boiled by ethanol, flows back and then is filtered, and a filtrate is collected, so that an angelica extract is obtained; the obtained angelica extract is extracted, an obtained solution after the extraction is subjected to vacuum drying, and a crude angelica extract is obtained; and the crude angelica extract is subjected to column chromatography on silica gel and column chromatography on reverse phase silica gel, so that a compound 1, a compound 2 and a compound 3 are obtained respectively. The fatty acid compound can be prepared into a specific inhibitor of PTP-SHP2; through inhibiting PTP (protein tyrosine phosphatase), the anticancer function and the function of preventing and treating human diseases relevant to PTP-SHP are played; and the fatty acid compound can be widely applied to preparation of medicines for preventing and treating cancers.

Description

technical field [0001] The invention relates to fatty acid compounds, in particular to the application of fatty acid compounds in the preparation of drugs for preventing and treating liver cancer. Background technique [0002] In recent years, with the rapid development of pharmaceutical and life science research, various basic processes such as signal transduction, apoptosis, angiogenesis and the interaction between cells and extracellular matrix in malignant tumor cells are gradually being elucidated. Using some key enzymes in cell signal transduction pathways related to tumor cell differentiation and proliferation (such as protein tyrosine kinase) as drug screening targets, discover new drugs with high efficiency, low toxicity and strong specificity that selectively act on specific targets. Antineoplastic drugs, namely molecular targeted drugs (molecular targeted drugs) and antibody targeted drugs (antibody targeted drugs), have become an important direction of anticancer...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/201A61P35/00A61P1/16
Inventor 陈海峰吕忠显陈全成刘东萍崔传文孔桂萍李阳
Owner XIAMEN UNIV
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