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Use of ursolic acid as colon tumor resistant medicament

A technology of colon tumors and ursolic acid, applied in the direction of antineoplastic drugs, drug combinations, medical preparations containing active ingredients, etc., to achieve the effect of inhibiting tumor angiogenesis, inhibiting proliferation, and good curative effect

Inactive Publication Date: 2011-03-30
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Before the publication of the present invention, there has not been any patent publication or report on the ursolic acid mentioned in this patent application through the EGFR / MAPK signaling pathway to play an anti-colon cancer tumor effect and related reports on the synergistic effect with oxaliplatin

Method used

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  • Use of ursolic acid as colon tumor resistant medicament
  • Use of ursolic acid as colon tumor resistant medicament
  • Use of ursolic acid as colon tumor resistant medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Inhibitory effect of ursolic acid on the proliferation of colon cancer cells

[0032] (1) Aseptically inoculate human colon cancer cells HT-29, SW620, SW480, LoVo, and RKO in a 96-well cell culture plate with 0.1ml containing 1×10 6 Cell complete cell culture medium 1640 or L-15 medium.

[0033] (2) Add 0.1ml of complete cell culture medium containing different concentrations (10μM, 20μM, 30μM, 40μM, 60μM, 80μM) of ursolic acid to each well, mix with the cells, and put the cells in a 37°C cell culture incubator ( containing 5% CO2) for 48 hours.

[0034] (3) The cell culture was terminated, and the viability of the cultured cells was measured by the MTT method.

[0035] (4) The results showed that there is an obvious dose-effect relationship in cell proliferation inhibition, and the cell line with K-RAS gene mutation has a better proliferation inhibition effect. (See figure 1 , figure 2 )

Embodiment 2

[0037] Effect of ursolic acid on promoting apoptosis of human colon cancer cells

[0038] (1) Aseptically inoculate human intestinal cancer cells SW620, SW480, LoVo, RKO in a 6-well cell culture plate, and inoculate 2ml containing 1×10 6 Cell complete cell culture medium L-15.

[0039] (2) Different concentrations of ursolic acid (15 μM, 30 μM, 60 μM for SW620 cells) were added to each well, and after mixing with the cells, the cells were placed in a 37°C cell incubator (containing 5% CO2) for 48 hours.

[0040] (3) The cell culture was terminated, and the cells were collected and sent for flow cytometry detection. The results indicated that the rate of apoptosis after the treatment of ursolic acid was related to the cell type. (See image 3 , Figure 4 ).

[0041] (4) At the same time, the cells treated with ursolic acid were collected for immunoblotting detection, and it was observed that the increase in the expression of caspase protein and the decrease in the expressio...

Embodiment 3

[0043] Inhibitory effect of ursolic acid on EGFR / MAPK signaling pathway in human intestinal cancer cells

[0044] (1) Aseptically inoculate human intestinal cancer cell SW620 in a 6-well cell culture plate, and inoculate 2ml containing 1×10 6 Cell complete cell culture medium L-15.

[0045] (2) Add different concentrations of ursolic acid (15 μM, 30 μM, 60 μM) to each well, mix well with the cells, put the cells in a 37°C cell incubator (containing 5% CO2) for 48 hours, collect the cells and extract the protein.

[0046] (3) Use real-time PCR and immunoblotting to observe the changes in phosphorylation levels of EGFR / MAPK signaling pathway proteins.

[0047] (4) It was found that after the above concentration of ursolic acid treatment, the gene level and protein phosphorylation level of EGFR / MAPK signaling pathway decreased significantly, and there was a dose-dependent relationship, among which the decrease of ERK1 / 2 gene and protein phosphorylation level was the key target....

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Abstract

The invention relates to use of ursolic acid as a colon tumor resistant medicament. The ursolic acid has the effects of inhibiting colon cancer / tumor cell proliferation and inducing apoptosis. In naked mouse in vivo experiments, the ursolic acid can effectively inhibit the proliferation of colon cancer transplanted tumor and inhibit the generation of tumor blood vessels, and has no obvious toxic or side effect on mice. The ursolic acid has the effect of inhibiting EGFR / MAPK signal channel phosphorylation of colon cancer cells, and the key target of the ursolic acid is to inhibit ERK1 / 2 protein phosphorylation. The ursolic acid which is synergetic with oxaliplatin serving as a clinical first-line chemotherapy medicament of the colon cancer has better curative effect. The ursolic acid has better proliferation inhibiting effect on the colon cancer cells of K-RAS gene mutation. The use of the ursolic acid as the colon tumor resistant medicament provides a new thought for treating the colon tumor.

Description

technical field [0001] The invention relates to the application of ursolic acid, especially as an anti-colon tumor drug. Background technique [0002] Colon cancer is one of the most common malignant tumors in the world, and its incidence is increasing year by year with the improvement of living standards in our country. The treatment of colon cancer currently adopts a comprehensive treatment including surgery, radiotherapy, chemotherapy, targeted therapy, biological and immunotherapy, etc., but no matter which method is used, the overall cure rate of colon cancer is still hovering at 50%. %, the long-term survival rate and quality of life are still not ideal. [0003] The EGFR / MAPK signaling pathway has been proved to be closely related to the proliferation, differentiation and angiogenesis of colon cancer. Cetuximab, a monoclonal antibody that treats colon cancer by blocking the EGFR signaling pathway, has been widely used clinically and has made great progress, but cetu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P35/00
Inventor 单建贞张苏展
Owner ZHEJIANG UNIV
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