Application of maprotiline hydrochloride in preparation of medicine for inhibiting tumour cell transfer and diffusion

A technology of maprotiline hydrochloride and tumor cells, applied in the pharmaceutical field of maprotiline hydrochloride, can solve the problems of undiscovered pharmacological effects of maprotiline hydrochloride, increased blood drug concentration, unsuitable combination, etc., to reduce the death dose , R&D cycle reduction, and the effect of large blocking effect

Inactive Publication Date: 2015-04-29
NANJING WENZHI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] 5. When combined with fluoxetine, the blood concentration of both will increase, so it is not suitable to be used in combination
[0009] Other pharmacological effects of maprotiline hydrochloride have not been found in the existing open literature

Method used

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  • Application of maprotiline hydrochloride in preparation of medicine for inhibiting tumour cell transfer and diffusion
  • Application of maprotiline hydrochloride in preparation of medicine for inhibiting tumour cell transfer and diffusion
  • Application of maprotiline hydrochloride in preparation of medicine for inhibiting tumour cell transfer and diffusion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 ： Application of maprotiline hydrochloride in the preparation of drugs for inhibiting the metastasis and spread of colon cancer cells. The specific experimental plan is as follows:

[0030] 1. Experimental materials

[0031] 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.

[0032] Wherein experiment adopts maprotiline hydrochloride compound C 20 h 24 ClN, CAS NO. is 10347-81-6, 10262-69-8 (maprotiline), the concentrations are 50uM, 10uM, 5uM, 1uM, 0.5uM respectively.

[0033] 2. Experimental method

[0034] For colon cancer cells cultured for 24 hours (cell density: 10 5 ) for drug stimulation for 2 hours:

[0035] (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;

[0036] (2) ...

Embodiment 2

[0044] Example 2 ： Transwell cell migration assay was used to determine the effect of maprotiline hydrochloride on the migration ability of colon cancer cells.

[0045] 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 adhere to the wall, add DMEM complete medium with different concentrations of maprotiline hydrochloride to the upper chamber. To maintain osmotic pressure, add 0.05%-0.2% BSA, and add DMEM complete medium containing 15% FBS to the lower chamber and continue culturing 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 37°C for 10 minutes and then stained with Giemsa. Ten visual fields were randomly selected under a high-power microscope to count the migrated cells.

[0046] Cell migration rate = [the average numb...

Embodiment

[0050] Example 3 ： Damage repair assay was used to detect the effect of maprotiline hydrochloride on the migration ability of tumor cells.

[0051] Take HT29 cells in the logarithmic growth phase, and add 1×10 cells to each well of a 24-well plate 5 After the cells grow into a monolayer, draw a "one"-shaped scratch, wash with PBS, add different concentrations of maprotiline hydrochloride to 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%.

[0052] The anti-migration assay of maprotiline hydrochloride on LTEP and A549 cells at different concentrations (0.5-50 μg / ml) for 22 hours showed that maprotiline hydrochlori...

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PUM

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Abstract

The invention discloses application of maprotiline hydrochloride in preparation of a medicine for inhibiting tumour cell transfer and diffusion. According to the invention, the tumour cell transfer capability is inhibited by utilizing the medicine prepared from maprotiline hydrochloride; maprotiline hydrochloride is a low-toxicity medicine and plays a great blocking role in a tumour diffusion process; at the same time, treatment is carried out by adopting other related tumour medicines; therefore, the death amount of normal cells can be greatly reduced; but, most of existing tumour medicines are cytotoxic medicines, and lots of normal cells also die while tumour cells are killed.

Description

technical field [0001] The invention relates to a new application of maprotiline hydrochloride in the field of pharmacy, in particular to an application of maprotiline hydrochloride in the preparation of drugs for inhibiting tumor cell metastasis and diffusion. Background technique [0002] Maprotiline hydrochloride is a tetracyclic antidepressant used for various types of depressive neurosis such as intrinsic, reactive, and menopausal. The main effect is to selectively inhibit the reuptake of norepinephrine in the peripheral and central nervous system, but has no effect on the reuptake of serotonin. This product has both anti-anxiety effects, sedative, anticholinergic, and blood pressure lowering effects. Its antitumor effects have not attracted much attention. [0003] The main effects of maprotiline hydrochloride are: [0004] 1. When used in combination with antihistamines, it can enhance the anticholinergic effect. [0005] 2. Cimetidine can increase the blood conce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/137A61P35/04
CPCA61K31/137
Inventor 滕文臣
Owner NANJING WENZHI BIOTECH
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