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Application of ainsliaidimer A in preparing nucleolus transcription factor inhibitor medicament

A technology of dimerizing rabbit ears and transcription factors, which is applied in the field of medicine, can solve the problem of lack of chemical components in big-headed rabbit ears, and achieve the effect of great clinical application value

Inactive Publication Date: 2012-01-18
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But little research has been done on the chemical constituents of Ainsliaea macrocephala

Method used

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  • Application of ainsliaidimer A in preparing nucleolus transcription factor inhibitor medicament
  • Application of ainsliaidimer A in preparing nucleolus transcription factor inhibitor medicament
  • Application of ainsliaidimer A in preparing nucleolus transcription factor inhibitor medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Preparation of compound dimeric terpene A

[0019] Ainsliaea macrocephala (Ainsliaea macrocephala) whole herb 5kg, reflux extraction 2 times with 80% ethanol 50L each time, 2 hours each time, the extract was concentrated under reduced pressure into liquid extract, diluted with water, extracted with 5L of petroleum ether, and then Extract with 5 L of ethyl acetate to obtain 320 g of the ethyl acetate fraction; mix the above ethyl acetate fraction with 300 g of silica gel to mix the sample, apply silica gel column chromatography, and use a chloroform-methanol system gradient with a volume ratio of 20:0 to 4:1 Elution, thin-layer chromatography detection, collect the fraction containing dimeric terpene A, then go through Sephadex column chromatography, elute with chloroform-methanol with a volume ratio of 1:1, and finally pass through C18 Reverse-phase column chromatography, eluting with methanol-water with a volume ratio of 4:6 to 6:4, and detection by thin-laye...

Embodiment 2

[0021] Example 2 Gel Retardation Electrophoresis Analysis (EMSA) Detects the Activity of NF-κB

[0022] Experiment set up control group and medicine group, control group does not add any medicine, medicine group adds 0.75ug / ml (concentration of dimeric rabbit auricine A drug) dimeric rabbit auricine A (add 0.5ml of medicine to 1× 10 7 HL-60 cells), under aseptic conditions, the cells of each group were put into culture flasks containing RPMI1640 medium containing 15% calf serum, and cultured in an incubator containing 5% carbon dioxide for 3, 6, and 12 days respectively. And 24h, collect each group of HL-60 cells. Each group is about 1×10 7 The cells were washed three times with PBS (phosphate buffered saline), and the nuclear protein was extracted using the NE-PER Nuclear and Cytoplasmic Extraction Reagents Kit (Cell Nucleus and Cell Protein Extraction Kit, Pierce Company, Cat. No.: 78833), and operated according to the instructions. The Lightshift EMSA Kit (Pierce Company...

Embodiment 3

[0023] Example 3 Detection of NF-κB in Cells by Immunoluminescence

[0024] Collect the control group and HL-60 cells treated with 0.75ug / ml dimeric auricine A for 3, 6, 12 and 24 hours respectively, and wash with PBS (as in Example 2). Add 10% buffered formalin fixative, fix for 15 minutes, and use NF-κB activation-nuclear translocation detection kit (beytotime company) (cy3-labeled secondary antibody) to detect changes in the distribution of NF-Kbp65 in cells. According to the instructions, the primary antibody was kept at 4°C for two nights, observed under a fluorescence microscope, and the site of p65 showed red fluorescence. Results The treatment of dimeric rabbit auris terpene A greatly decreased the amount of NF-κB p65 in the nucleus, and the amount of NF-κB p65 in the cytoplasm also decreased.

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Abstract

The invention provides an application of a compound ainsliaidimer A in preparing a nucleolus transcription factor inhibitor medicament. The inventor carries out experiments of detecting activity of NF (nuclear factor)-kappa B by adopting EMSA (electrophoretic mobility shift assay), detecting differences of NF-kappa B in cells by immunochemical luminescent assay, detecting expression of the NF-kappa in ainsliaidimer A acting HL-60 cells by a Western blot method, detecting expression of apoptosis related protein in lymphoma cell CA46 cell after action of the ainsliaidimer A by the Western blot method, detecting influence of the ainsliaidimer A on HL-60 cell secretion VEGF (vascular endothelial growth factor) and the like. Results prove that the ainsliaidimer A has a good inhibition effect to the activity of the NF-kappa B abnormally activated by tumor cells, so that, the compound ainsliaidimer A serving as an active component can be used for preparing a nucleolus transcription factor inhibitor medicament. The medicament can be used as novel application for treating leukemia, autoimmune diseases, renal diseases, heart cerebrovascular diseases, various inflammations, neurodegenerative disorders and eye disorders of animals and humans caused by abnormally activation of the NF-kappa B factor, thereby providing a new method for treating the diseases and disorders, and having higher clinical application value.

Description

technical field [0001] The present invention relates to medicines, in particular to the application of the big headed rabbit ear wind extract in pharmacy, especially to the application of the compound dimeric rabbit ear wind A in the preparation of nuclear transcription factor inhibitor drugs. Background technique [0002] NF-κB cell nuclear transcription factor is a nuclear protein factor that can specifically bind to the enhancer κB sequence (GGGACTTTCC) of the immunoglobulin κ chain gene, which was first discovered in the nuclear extract of B cells, so it is called NF-κB. κB. After this factor specifically combines with the κ sequence, it promotes the expression of the κ light chain gene. But then more and more evidence showed that this factor can turn on the transcription of many genes. Regulate the expression of many proteins including cytokines and inflammatory mediators, thus participating in the regulation of physiological and pathological responses of cells. [0...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P35/02A61P37/00A61P13/12A61P9/00A61P25/28A61P27/02
Inventor 张卫东苏娟单磊柳润辉李慧梁沈云亨徐希科刘慧
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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