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Application of glycocholic acid in preparation of antitumor drugs

An anti-tumor drug, glycocholic acid technology, applied in the direction of anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve problems such as short history

Inactive Publication Date: 2019-04-05
DALIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The history of drug treatment of tumors in modern medical oncology is very short, less than 70 years so far, but drug treatment has achieved many major achievements in less than a century, making drug treatment an indispensable part of comprehensive tumor treatment
Its physiological function is mainly to promote the digestion and absorption of fat in the intestinal tract, but it has not been reported as a drug, especially in anti-tumor drugs

Method used

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  • Application of glycocholic acid in preparation of antitumor drugs
  • Application of glycocholic acid in preparation of antitumor drugs
  • Application of glycocholic acid in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The in vitro antitumor experiment of embodiment 1 glycocholic acid

[0029] 1. Cell lines: 4T1 (mouse breast cancer cells), MCF-7 (human breast cancer cells), NIH: OVCAR-3 (human ovarian cancer cells), RL95-2 (human endometrial cancer cells), HCC827 ( Human non-small cell lung cancer cells) (all of the above were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences)

[0030] 2. Culture medium: RPMI-1640 (Gibco product number 31800022); high glucose DMEM medium (Gibco product number 11965092)

[0031] 3. Method

[0032] 3.1 Collect the cells in the logarithmic growth phase, adjust the cell concentration to 5×10 with 1640 medium and DMEM medium respectively 4 cells / ml, add 100 μl of cell suspension into a 96-well plate.

[0033] 3.2 5% CO 2 After culturing at 37°C for 24 hours, the 4T1 mouse breast cancer cells were added with a concentration gradient of (0.1nmol / L, 0.2nmol / L, 0.4nmol / L, 0.8nmol / L, 1.6nmol / L, 3.2nmol / L, 6.4nmol / L), MCF-7, NIH:OVCA...

Embodiment 2

[0037] Embodiment 2 animal model measures glycocholic acid tumor inhibition rate

[0038] 1. Materials: 10-week-old female BABL / c mice were purchased from the SPF Experimental Animal Center of Dalian Medical University. 4T1 tumor cells were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences.

[0039] 2. Method:

[0040] 2.1 Modeling: Collect 4T1 mouse breast cancer cells in the logarithmic growth phase, adjust the cell concentration to 2×10 with PBS 6 / ml. Inject 0.1 ml of the cell suspension into the right underarm of the mouse with a sterile syringe.

[0041] 2.2 Administration: Glycocholic acid 15 mg / kg (twice / day) was administered on the second day after modeling, 0.2 mL each time, for two consecutive weeks. On the evening of the last administration, the mice were fasted, and the mice were killed by neck dislocation on the 15th day. The axillary tumor tissues of the mice were aseptically removed, weighed and pressed Calculate the tumor inhibitio...

Embodiment 3

[0043] Example 3 Real-time PCR Determination of Glycocholic Acid-specific Target RNA Expression in Tumor Cells

[0044] 1. Materials: 4T1 mouse breast cancer cells were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences.

[0045] 2. Methods: RNA was extracted from 4T1 cells after glycocholic acid intervention, and Real-time PCR was performed after reverse transcription to determine the changes in the expression of glycocholic acid-specific target RNA.

[0046] 3. Results: After the intervention of glycocholic acid, the expression of related RNA increased by 1.5 times, see Figure 5 , Image 6 . The results of the intervention of glycocholic acid on tumor cells were confirmed from the RNA level, and the mechanism of glycocholic acid inhibiting the growth of tumor cells was revealed.

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Abstract

The invention relates to application of chemical drugs in the field of medicine, in particular to application of glycocholic acid in preparation of antitumor drugs. The novel applicable field of glycocholic acid is provided herein; glycocholic acid is applicable to the preparation of antitumor drugs, mainly for breast cancer, ovarian cancer, endometrial carcinoma, lung cancer or their combinations; as an effective active ingredient to antitumor drugs, glycocholic acid has effective treatment quantity of 4T1 (mouse breast cancer cells) under 0.4-1.6 nmol / L, and MCF-7 (human breast cancer cells), NIH OVCAR-3 (human ovarian carcinoma cells), RL95-2 (human endometrial cancer cells), and HCC827 (human non-small cell lung cancer cells) under 16-128 mu mol / L. The application is helpful for the development of novel antitumor drugs.

Description

technical field [0001] The invention relates to the application of chemical drugs in the field of medicine, in particular to the application of glycocholic acid in antitumor drugs. Background technique [0002] Malignant tumors are one of the major diseases that seriously endanger human health. According to the World Health Organization (WHO) report, a total of 8.4 million people died of malignant tumors in the world in 2010, and it is estimated that the number may increase to 10 million by 2020. The number of new cases of malignant tumors in my country is about 1.8 million every year, and about 1.3 million people die of malignant tumors. Malignant tumors have become the primary cause of death in my country. [0003] The history of drug treatment of tumors in modern medical oncology is very short, less than 70 years so far, but many major achievements have been made in drug treatment in less than a century, making drug treatment an indispensable part of comprehensive tumor t...

Claims

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Application Information

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IPC IPC(8): C07J41/00A61K31/575A61P35/00
CPCA61K31/575A61P35/00C07J41/0061
Inventor 梁文波童玉春项蓉蓉江一鸣宋捷
Owner DALIAN UNIV
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