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Fatty acid compounds and preparation method and application thereof

A technology for fatty acids and compounds, applied in the field of fatty acid compounds and their preparation, can solve problems such as inability to exert normal functions, and achieve the effects of enhancing activity inhibition and promoting apoptosis

Inactive Publication Date: 2013-10-09
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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  • Fatty acid compounds and preparation method and application thereof
  • Fatty acid compounds and preparation method and application thereof
  • Fatty acid compounds and preparation method and application thereof

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 30 L / time;

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

[0043] 4) The lower layer was extracted twice with ethyl acetate, the upper layer extracts were combined three times, and vacuum-dried to obtain 48.3 g 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 in ch...

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 purified protein

[0072] PBS Bμffer: 137mM NaCl, 2.7mM KCl, 10mM NaCl 2 HPO 4 , 2mM KH 2 PO 4 100mg / ml ampicillin

[0073] Protease Inhibitor and Phosphatase Inhibitor Stock Solutions:

[0074]

[0075]

[0076] IPTG stock solution (0.8M)

[0077] Buffer W: 25mM Tris-HCl pH7.5, 150mM NaCl, 10mM β-mercaptoethanol, 1mM EDTA

[0078] Buffer W1: 25mM Tris-HCl pH7.5...

Embodiment 314

[0196] Embodiment 314Z, the preparation of 17Z-eicosadienoic acid tablet

[0197] 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-eicosadienoic acid.

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Abstract

The invention relates to fatty acid compounds and provides the fatty acid compounds and a preparation method and application thereof. The preparation method comprises the following steps of: boiling and refluxing angelica dahurica by using ethanol, filtering, and collecting filtrate to obtain angelica dahurica extracting solution; extracting the obtained angelica dahurica extracting solution, andperforming vacuum drying on solution obtained through extraction to obtain a crude angelica dahurica extract; and performing silica gel column chromatography on the crude angelica dahurica extract, and performing reversed phase silica gel column chromatography to obtain a compound 1, a compound 2 and a compound 3 respectively. The fatty acid compounds can be prepared into specific inhibitors for inhibiting protein tyrosine phosphatase-Src homology domain-containing protein tyrosine phosphatase 2 (PTP-SHP2), and achieve the effects of resisting cancer as well as preventing and treating PTP-SHP2-related human diseases by inhibiting PTP. The fatty acid compounds are widely applied to the preparation of medicines for preventing and treating cancer.

Description

technical field [0001] The invention relates to fatty acid compounds, in particular to fatty acid compounds and their preparation method and application. 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 (such as protein tyrosine kinase) in the cell signal transduction pathway related to the differentiation and proliferation of tumor cells 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 and antibody targeted drugs, have become an important direction in the research and development of anticancer drugs today (1, Zhang Shige. Progress and clinical e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C57/03C07C51/42A61K31/201A61P35/00
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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