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Application of compound separated and extracted from burdock to serving as STAT3 inhibitor

A compound and inhibitor technology, applied in the field of medicine, can solve the problems of no reports, and achieve the effects of reduced dosage, low toxicity and side effects, and broad anti-cancer application prospects.

Inactive Publication Date: 2016-06-08
HUBEI UNIVERSITY OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The effect of arctigenin on STAT3 and whether it has therapeutic effect on triple-negative breast cancer as a combination drug have not been reported so far.

Method used

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  • Application of compound separated and extracted from burdock to serving as STAT3 inhibitor
  • Application of compound separated and extracted from burdock to serving as STAT3 inhibitor
  • Application of compound separated and extracted from burdock to serving as STAT3 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Arctigenin inhibits the activation of p-STAT3-tyr(705) in triple-negative breast cancer cells

[0040] The specific implementation method is as follows:

[0041] Four MDA-MB-231 cells treated with different concentrations of natural compound arctigenin (Atn) were obtained as follows: MDA-MB-231 and MDA-MB-468 cells were divided into four groups, one group of MDA - MB-231 (or MDA-MB-468) cells in L-15 medium containing 10% fetal bovine serum (add fetal bovine serum (Hyclone) to the volume of fetal bovine serum in L-15 medium (Gibco) Concentration is 10% culture medium obtained) in 37 ℃ for 24 hours, collect MDA-MB-231 cells, obtain the MDA-MB-231 cells that the arctigenin of 0M is processed; A group of MDA-MB-231 cells are in 4×10 -7 M medium (add arctigenin to the L-15 medium containing 10% fetal bovine serum until the concentration of arctigenin is 4×10 -7 M obtained culture medium) at 37 ℃ for 24 hours, collected MDA-MB-231 (or MDA-MB-468) cells, to obtain 4 × 10 ...

Embodiment 2

[0046] Detection Experiment of Arctigenin's Inhibition of Transcriptional Activity in Triple Negative Breast Cancer Cells by Nuclear Plasma Separation

[0047] Four kinds of MDA-MB-231 cells treated with different concentrations of natural compound arctigenin (Atn) were obtained as follows: MDA-MB-231 and MDA-MB-468 cells were divided into four groups, one group of MDA - MB-231 (or MDA-MB-468) cells in L-15 medium containing 10% fetal bovine serum (add fetal bovine serum (Hyclone) to the volume of fetal bovine serum in L-15 medium (Gibco) Concentration is 10% culture medium obtained) in 37 ℃ for 24 hours, collect MDA-MB-231 cells, obtain the MDA-MB-231 cells that the arctigenin of 0M is processed; A group of MDA-MB-231 cells are in 4×10 -7 M medium (add arctigenin to the L-15 medium containing 10% fetal bovine serum until the concentration of arctigenin is 4×10 -7 M obtained culture medium) at 37 ℃ for 24 hours, collected MDA-MB-231 (or MDA-MB-468) cells, to obtain 4 × 10 -...

Embodiment 3

[0057] Arctigenin and paclitaxel synergistically inhibit triple-negative breast cancer MDA-MB-231 and MDA-MB-468 cell detection experiment

[0058] After MDA-MB-231 and MDA-MB-468 cells were pre-attached for 24 hours, different concentrations of (OM, 4×10 -7 M, 8×10 -7 M) arctigenin (Atn) combined with paclitaxel (Tax, 0M, 3 × 10 -8 M, 4×10 -8 M) Treat MM.1S cells, add MTT detection reagent after 44 hours and incubate for another 4 hours, then measure the absorbance value at 570nm (OD570) with a microplate reader. The result is as Figure 5 and Figure 6 As shown, the treatment of arctigenin combined with paclitaxel can significantly reduce the OD570 of MDA-MB-231 and MDA-MB-468 cells, showing a significant synergistic effect. Arctigenin and paclitaxel synergistically inhibit triple-negative breast cancer MDA-MB-231 and MDA-MB-468 cells.

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Abstract

The invention belongs to the technical field of medicine, and particularly relates to an application of a compound separated and extracted from burdock to serving as an STAT3 inhibitor. The compound I can be used for a medicine composition for treating triple negative breast cancer. The compound I and docetaxel are combined into a compound preparation for treating triple negative breast cancer for use. Phosphorylation of STAT3 is remarkably inhibited through burdock aglycone in a cell and animal tumor-bearing model, and the burdock aglycone is free of obvious toxic and side effects on other normal tissues. The application has the advantages of being proper in dosage, remarkable in curative effect, clear in action target, small in toxic and side effect and the like, and has the broad anticancer application prospect in clinic. The compound preparation has the low toxic and side effects. As the toxicity of the burdock aglycone is quite low, and the burdock aglycone and the docetaxel are used as a composition, under the condition that the same anticancer curative effect is achieved, the dosage of the docetaxel can be remarkably decreased, and therefore the toxic and side effects brought by the docetaxel can be further reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the use of a compound isolated and extracted from burdock as a STAT3 inhibitor. Background technique [0002] Breast cancer is a common malignant tumor that seriously threatens women's health. About 1.400000 women in the world suffer from breast cancer every year, and 450000 die from the disease. In my country, breast cancer is increasing rapidly at a rate of 3% per year, and the age of onset is 10-15 years younger than that in Western countries. Triple-negative breast cancer (TNBC) refers to a special type of breast cancer that is negative for estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor (HER2). 15%-20% of all breast cancers. Metastasis is the main characteristic of TNBC, and it is also an important cause of patient death. Finding genes related to breast cancer metastasis and effective intervention are of great sign...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K31/337A61P35/00
CPCA61K31/337A61K31/365A61K2300/00
Inventor 刘莹李珊李健郭阳唐微汪选斌
Owner HUBEI UNIVERSITY OF MEDICINE
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