Drug for inhibiting brain tumor and application thereof

A brain tumor and drug technology, applied in the field of medicine, can solve problems such as depression of users, limited application of temozolomide, and limited use, and achieve the effect of promoting tumor cell death, inhibiting proliferation and dryness, and reducing toxic and side effects

Active Publication Date: 2020-11-13
LVCHAN BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Temozolomide (TMZ) is a first-line clinical chemotherapy drug for the treatment of glioma, but due to the emergence of drug resistance, its clinical use is limited, an...

Method used

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  • Drug for inhibiting brain tumor and application thereof
  • Drug for inhibiting brain tumor and application thereof
  • Drug for inhibiting brain tumor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] A drug for inhibiting brain tumors, which is a TRPV4 agonist. The TRPV4 agonist can promote the influx of calcium ions in the TRPV4 signaling channel, thereby promoting the induction of autophagy in brain tumor cells and achieving a stronger anti-brain tumor effect. The dosage of the TRPV4 agonist is: the concentration is 0.01 μM-30 μM, such as 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM, 15 μM, 20 μM, 25 μM, 30 μM, etc.

[0070] In order to prove that TRPV4 agonists can inhibit brain tumors, the inventors performed bioinformatics analysis on TRPV4 gene in normal brain tissue and glioma tissue. Download the GSE50161 data set from the gene expression database of the NCBI website, download the glioma-related database in TCGA from the UCSC gene expression database, and compare the glioma tissue microarray data in each data set. The data have passed quality control and homogenization , the downloaded data was analyzed by using GraphpadPrism7 software to analyze the...

Embodiment 2

[0073] On the basis of Example 1, the TRPV4 agonist is cannabidiol, and the concentration of the cannabidiol is 0.01 μM-30 μM, such as 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM, 15μM, 20μM, 25μM, 30μM, etc.

[0074] We performed mechanistic studies on the role of cannabidiol in glioma, a typical representative of brain tumors, such as Figure 12-Figure 15 As shown, the effect of cannabidiol on glioma cell lines U251, U87, LN18, U118MG, and A172 cells was detected by MTT method, and the results showed that the inhibitory concentration of cannabidiol on glioma cell lines was IC 50 The range was 20-30 μM, and the effect of cannabidiol on primary glial cells was much lower than that of other tumor cell lines, indicating that the effect on normal cells was relatively small. In addition, the effect of cannabidiol on the clonal proliferation ability of glioma was evaluated by 3D clonal formation experiments. The results showed that cannabidiol can significantly inhibit the...

Embodiment 3

[0084] A drug for inhibiting brain tumors, which includes a TRPV4 agonist and a tumor suppressor with anti-tumor activity. The concentration ratio of the TRPV4 agonist and the tumor suppressor is (that is, the case where the two concentration units are the same in the same solution): (10-30): (10-500). The mechanism of action of the TRPV4 agonist is combined with the inhibitory mechanism of the tumor inhibitor, and the combination of the two achieves the anti-tumor effect of increasing efficiency and reducing toxic and side effects.

[0085] In this embodiment, any one or more TRPV4 agonists can be used in conjunction with any one or more tumor suppressors.

[0086] Preferably, the tumor suppressor comprises temozolomide. The temozolomide may be used in combination with at least one TRPV4 agonist.

[0087] Preferably, the TRPV4 agonist includes cannabidiol. The TRPV4 agonist cannabidiol can be used in combination with at least one tumor suppressor.

[0088] Optimally, if t...

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Abstract

The invention provides a drug for inhibiting brain tumor and application thereof. The drug for inhibiting the brain tumor comprises at least one TRPV4 agonist capable of promoting calcium ion internalflow of a TRPV4 signal channel. The drug has a good treatment effect on brain tumors and related diseases thereof, and has a good application prospect in treatment of brain tumors and related diseases thereof. The drug is applied to medicines for treating brain tumors and related diseases thereof, can reduce toxic and side effects generated in the clinical treatment process of the brain tumors and the related diseases thereof and improve the treatment effect of the brain tumors and the related diseases thereof.

Description

technical field [0001] The application relates to the technical field of medicine, in particular to a drug for inhibiting brain tumors and its application. Background technique [0002] Brain tumors refer to new organisms that grow in the cranial cavity, also known as intracranial tumors and brain cancers, which can originate from the brain, meninges, nerves, blood vessels, and brain appendages, or form by metastasizing and invading the brain from other tissues or organs of the body , Most of them can produce headache, intracranial hypertension and focal symptoms, including brain tumors and brain metastases. Here, glioma is taken as an example. [0003] Glioma is one of the most common malignant brain tumors. Benign gliomas grow slowly and have a long course of disease. The average time from the onset of symptoms to seeing a doctor is two years. The malignant tumors grow rapidly and the course of the disease is short. Most of them are within 3 months from the onset of sympt...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61K31/4188A61K45/06A61K31/045A61P35/00A61P35/04A61P25/00A61P25/08
CPCA61K31/05A61K31/4188A61K45/06A61K31/045A61P35/00A61P35/04A61P25/00A61P25/08A61K2300/00
Inventor 黄腾飞
Owner LVCHAN BIOTECHNOLOGY CO LTD
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