Applications of H1 histamine receptor antagonist in preparation of drugs for treating glioma

A kind of glioma, histamine receptor technology, applied in the field of biomedicine

Inactive Publication Date: 2021-09-14
THE FIRST AFFILIATED HOSPITAL OF WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, in the prior art, there is no report about the application of H1 hi

Method used

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  • Applications of H1 histamine receptor antagonist in preparation of drugs for treating glioma
  • Applications of H1 histamine receptor antagonist in preparation of drugs for treating glioma
  • Applications of H1 histamine receptor antagonist in preparation of drugs for treating glioma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Cell experiment

[0042] During the experiment, human glioma cell lines U87 and U251 were cultured with DMEM+10% fetal bovine serum, and the cells were seeded in 96-well plates at 5000 cells / well, and cultured in a 37°C incubator containing 5% carbon dioxide. . A series of H1 histamine receptor antagonists of different concentrations were added every other day, and the cell viability was detected by MTT method after drug incubation for 3 days. The experimental results are shown in Table 1.

[0043] Table 1

[0044] drug U87 IC 50 (μM)

U25 IC 50 (μM)

Terfenadine 4.12 2.89 Desloratadine 29.66 36.42 Hydroxyzine Hydrochloride 91.49 123.23 Chloropyramide hydrochloride 85.62 122.14 Chlorpheniramine maleate 255.72 321.98

[0045] Conclusion: Compared with other H1 histamine receptor antagonists, terfenadine can significantly inhibit the growth of tumor cells, and the dose-effect relationship of terfenadin...

Embodiment 2

[0048] Embodiment 2 in vivo animal experiments

[0049] Culture and in vivo planting of U87 glioma cells in BALB / C-nu nude mice:

[0050] Rat U87 glioma cells were cultured in high-glucose DMEM containing 10% fetal bovine serum at 37°C with 5% CO 2 subcultured in an incubator. The cells in the logarithmic growth phase were taken, washed with PBS and digested with 0.25% trypsin, the cells were collected with PBS to make a cell suspension, and the cell concentration was adjusted to 1,000,000 / μl before planting into the brain of nude mice.

[0051] Establishment of orthotopic glioma model in nude mice: U87 cells with luciferase were implanted in the subdural 3mm position 1mm in front of the sagittal suture on the right side of the rat, 2mm right of the midline. Ten nude mice of SPF grade BALB / C-nu, each weighing 25 g, were used, all male, purchased from Shrek Experimental Animal Center. Nude mice were anesthetized with isoflurane gas and fixed on a stereotaxic apparatus (model...

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Abstract

The invention discloses applications of an H1 histamine receptor antagonist in preparation of drugs for treating glioma. The H1 histamine receptor antagonist is terfenadine, a terfenadine metabolite, desloratadine, hydroxyzine dihydrochloride, chloropyramine hydrochloride or chlorpheniramine maleate. Compared with a conventional anti-glioma drug, a mechanism of acting on a brand-new drug target and killing tumor cells is completely different from that of the previous drugs, drug tolerance and drug resistance are not generated at present. A drug acting target is different from that of the previous drugs. Therefore, bright prospects are expected to bring treatment for glioma. Particularly, the selective H1 histamine receptor antagonist terfenadine can significantly inhibit proliferation and migration of glioma cells, and can effectively kill glioma cells at a low concentration. Thus, the compound terfenadine can be used for preparing drugs for treating glioma, improving prognosis and survival rate of patients with glioma, and relieving social burden.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to the application of an H1 histamine receptor antagonist in the preparation of drugs for treating neuroglioma. Background technique [0002] Glioma is a tumor that begins to grow from the glial cells of the brain or spine, accounting for 30% of all brain and central nervous system tumors and 80% of all malignant tumors. Mainly divided into astrocytoma, glioblastoma, oligodendroglioma, medulloblastoma, ependymoma and other types. The WHO divides it into Ⅰ-Ⅳ grades, in which the prognosis of high-grade glioma is extremely poor (1 year), even after complete surgical resection, it will always recur, while low-grade glioma can survive for a long time (5 -10 years). Symptoms of gliomas depend on where they grow and can cause headaches, vomiting, seizures, and cranial nerve dysfunction. [0003] The treatment of brain glioma is mainly based on surgical resection, combined with comp...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/445A61P35/00
CPCA61K45/00A61K31/445A61P35/00
Inventor 杨建静诸葛启钏王堪凯
Owner THE FIRST AFFILIATED HOSPITAL OF WENZHOU MEDICAL UNIV
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