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Application of toremifene citrate in preparation of medicines for inhibiting tumor cell metastasis and diffusion

A technology of toremifene citrate and tumor cells, which is applied in the direction of antineoplastic drugs, drug combinations, pharmaceutical formulations, etc., can solve problems such as the undiscovered pharmacological effects of toremifene citrate, and achieve the reduction of research and development cycle, The effect of reducing the amount of death

Inactive Publication Date: 2015-06-03
NANJING ZHONG HONG HUA FEI INFORMATION TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Other pharmacological effects of toremifene citrate have not been found in the existing published literature

Method used

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  • Application of toremifene citrate in preparation of medicines for inhibiting tumor cell metastasis and diffusion
  • Application of toremifene citrate in preparation of medicines for inhibiting tumor cell metastasis and diffusion
  • Application of toremifene citrate in preparation of medicines for inhibiting tumor cell metastasis and diffusion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Application of toremifene citrate in the preparation of drugs for inhibiting the metastasis and spread of colon cancer cells. The specific experimental plan is as follows:

[0026] 1. Experimental materials

[0027] Colon cancer cells (HT29) were used in the experimental phase of the present invention, and nocodazole (experimental concentration: 10uM) was used as the positive control. The negative control group received no treatment.

[0028] The experiment used toremifene citrate compound C 32 h 36 ClNO 8 , CAS NO. is 89778-27-8, the concentrations are 100uM, 80uM, 60uM, 40uM, 20uM, 10uM.

[0029] 2. Experimental method

[0030] For colon cancer cells cultured for 24 hours (cell density: 10 5 ) for drug stimulation for 2 hours:

[0031] (1) Centrifuge the colon cancer cells in a better state in the culture dish, and add an appropriate amount of culture medium to make a cell suspension;

[0032] (2) Take the cell suspension and count according to 10...

Embodiment 2

[0040] Example 2: Transwell cell migration assay was used to determine the effect of toremifene citrate on the migration ability of colon cancer cells.

[0041] Will 1×10 5 The HT29 cells were inoculated in Transwell chambers with a 12.0 μm membrane at the bottom, and continued to be cultured. After the cells adhered to the wall, DMEM complete medium with different concentrations of toremifene citrate was added to the upper chamber. In order to maintain the osmotic pressure, 0.05%-0.2% BSA was added, and the lower chamber was added with DMEM complete medium containing 15% FBS. Continue to cultivate for 24h. The unmigrated cells on the upper surface of the membrane were carefully wiped off with a cotton swab, and the cells that migrated to the lower surface of the membrane were fixed with 2% PFA at 37oC for 10 minutes and then stained with Giemsa. Ten visual fields were randomly selected under a high-power microscope to count the migrated cells.

[0042] Cell migration rate ...

Embodiment 3

[0045] Example 3: Damage repair experiment to detect the effect of toremifene citrate on the migration ability of tumor cells.

[0046] Take HT29 cells in the logarithmic growth phase, and add 1×10 cells to each well of a 24-well plate 5After the cells grow into a monolayer, draw a "one"-shaped scratch, wash with PBS, add different concentrations of toremifene citrate in the control group and the experimental group, and take pictures. After 22 hours of culture, take pictures again at the same part to measure the migration distance . The experiment was repeated 3 times, and the cell migration rate=[(0h average value of the experimental group-22h average value of the experimental group) / (0h average value of the blank control group-22h average value of the blank control group)]×100%.

[0047] Toremifene citrate inhibited the migration of LTEP and A549 cells at different concentrations (10-80 μg / ml) for 22 hours, and the results showed that toremifene citrate had a dose-dependen...

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Abstract

The invention discloses an application of toremifene citrate in preparation of medicines for inhibiting tumor cell metastasis and diffusion. The metastasis ability of tumor cells is inhibited by the medicines prepared from the toremifene citrate, wherein the toremifene citrate is a low-toxicity medicine, and can play a relatively large blocking role in a tumor metastasis process; and meanwhile, treatment is carried out by virtue of other related tumor medicines, so that the mortality amount of normal cells can be greatly reduced; most of the existing tumor medicines are cytotoxic medicines; and a large number of normal cells die when the tumor cells are killed.

Description

technical field [0001] The invention relates to a new application of toremifene citrate in the field of pharmacy, in particular to the application of toremifene citrate in the preparation of drugs for inhibiting tumor cell metastasis and diffusion. Background technique [0002] Toremifene citrate is a tamoxifen derivative. It can combine with estrogen receptors to produce estrogen-like effects, anti-hormone effects or both effects, which mainly depends on the length of treatment, animal species, sex and target organs. [0003] Toremifene citrate tablets are indicated for postmenopausal women with estrogen receptor positive or unknown metastatic breast cancer. [0004] Toremifene citrate competes with estrogen to bind to estrogen receptors in breast cancer cells, preventing estrogen-induced DNA synthesis and proliferation of cancer cells. High-dose toremifene citrate was used in some experimental tumors, showing that toremifene citrate has non-estrogen-dependent antitumor e...

Claims

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Application Information

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IPC IPC(8): A61K31/138A61P35/04
Inventor 滕文臣
Owner NANJING ZHONG HONG HUA FEI INFORMATION TECH CO LTD
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