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Application of carotene base compounds in the preparation of anti-breast cancer drugs

A kind of artesunate alkaloid, anti-breast cancer technology, applied in the field of medicine, to achieve the effect of mild side effects, prolong life and slow down growth

Inactive Publication Date: 2016-04-20
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There is no relevant literature report on the research of carartemisinin against breast cancer

Method used

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  • Application of carotene base compounds in the preparation of anti-breast cancer drugs
  • Application of carotene base compounds in the preparation of anti-breast cancer drugs
  • Application of carotene base compounds in the preparation of anti-breast cancer drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of Carotene Alkaline Compounds

[0025] Grind the dried Artemisia annua, extract twice with 80% and 95% ethanol under reflux, each time for two hours, concentrate the extract under reduced pressure to form an extract, dilute with water, adjust the pH to 2-3 with 2% HCl, and then Sequentially extract with petroleum ether and ethyl acetate to obtain the petroleum ether and ethyl acetate parts; then add 2% NaOH to the water layer to adjust the pH to 11, extract with chloroform to obtain the chloroform parts; the chloroform part is a silica gel column (200-300 mesh) , eluted with 6 gradients of chloroform:methanol (20:0, 20:1, 10:1, 5:1, 2:1, 0:1) to obtain a fraction of Fr.1-Fr.6, Fr. .1 fraction was subjected to repeated silica gel (200-300 mesh) column chromatography, gradient elution with cyclohexane:methanol:diethylamine (30:1:1~5:1:1), and SephadexLH-20 column chromatography After separation, two compounds were obtained, which were identified a...

Embodiment 2

[0030] Example 2: Inhibitory activity of carotene base compounds on breast cancer cell MCF-7 (purchased from Shanghai Institute of Biological Sciences, Chinese Academy of Sciences)

[0031] Dissolve 6 carrageenate base compounds in DMSO (1000×), and set the concentration gradient of the 6 carrageenate base compounds: 0, 1, 5, 10, 25, 50, 100 μM, respectively in the experimental Cell viability was detected at 0, 24, 48, and 72 hours after the start, and the DMSO content was lower than 0.1% during drug treatment.

[0032] Cell viability detection method: MTT assay, 96-well plate with a concentration of 3-5×10 4 100 μl of cell suspension per ml, placed in a 37°C, 5% CO2 incubator. After 12 hours, drugs with a gradient concentration were added, 100 μl / well, and triplicate wells were set up. 37°C, 5% CO2 for 24 hours. Add 20 μl of 5 mg / ml MTT solution to each well, stop the culture after 4 hours of action, and carefully absorb the culture solution in the well. Add 150 Ul DMSO to ...

Embodiment 3

[0037] Example 3: Inhibitory activity of hornartemisinic compounds on RhoGTPs protein

[0038] Carrageenate base compounds have obvious inhibitory effects on RhoGTPs family targets. Therefore, it is concluded that these compounds play their role by acting on RhoGTPs. Table 2 shows the inhibitory activity of these compounds on the Rac1 protein in the RhoGTPs family (purchased from Cytoskeleton).

[0039] MCF-7 cells were starved for 48 hours without FBS in MEM culture medium, and then the compounds of 0, 1, 5, 10, 25, 50, and 100 μM concentrations were used to act on the cells for 24 hours, and then treated with EGF Stimulate the cells for 2 minutes, finally extract the total protein, detect the inhibitory activity with G-LISA kit, and calculate the IC 50 , the results are shown in Table 2

[0040] The inhibitory activity (IC 50 ,μM)

[0041]

[0042] It can be seen from the above results that the six artemisinin compounds have significant inhibitory activity on the Rac...

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Abstract

The invention relates to the technical field of medicine, in particular to application of incarvillateine compounds in preparation of anti-breast cancer drugs. Two kinds of methods, namely an operative treatment method and a drug treatment method, can be used for treating breast cancer at present, however, breasts are usually needed to be excised in the operative treatment method, which does serious harm to bodies and minds of women, while the side effect of the drug treatment method is large. Incarvillateine compounds can inhibit the activity of a breast cancer cell MCF-7 and RhoGTOs family target cells, so that after the incarvillateine compounds are applied to the preparation of anti-breast cancer drugs, the growth speed of tumors can be effectively reduced, the lifetime of a patient can be prolonged and the side effect is slight.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of cartilage artemisinin compounds in the preparation of anti-breast cancer drugs. Background technique [0002] Breast cancer is one of the common malignant tumors in women. According to statistics, the incidence rate accounts for 7%-10% of all kinds of malignant tumors in the whole body. About 500,000 people die of breast cancer in the world every year, which seriously threatens the health of women. [0003] The methods for treating breast cancer include surgical treatment and drug treatment, and surgical treatment is often mastectomy, which seriously damages women's body and mind. Drug therapy is the same as other cancer treatments. Most of them are chemotherapy. Commonly used drugs include cisplatin, bleomycin, vincristine, mitomycin, fluorouracil, paclitaxel, etc. These drugs effectively prolong the life of patients Or improve the patient's quality of life....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/435A61P35/00C07D221/04
Inventor 张寿德张卫东李洪林
Owner EAST CHINA UNIV OF SCI & TECH
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