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Application of flavonoid compound CH625 to preparation of drugs for resisting glioma

A technology of flavonoids and glioma, applied in the direction of antineoplastic drugs, drug combinations, active ingredients of ketones, etc., to achieve the effect of excellent quality, mature technology and wide selection range

Inactive Publication Date: 2018-05-08
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the effect of CH625 on tumors has not been reported

Method used

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  • Application of flavonoid compound CH625 to preparation of drugs for resisting glioma
  • Application of flavonoid compound CH625 to preparation of drugs for resisting glioma
  • Application of flavonoid compound CH625 to preparation of drugs for resisting glioma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] [Example 1] Effect of CH625 on mice bearing glioma

[0032] (1) Grouping and handling of animals

[0033] Rat C6 glioma cells (5×10 6 ) were inoculated subcutaneously and intracranially into Wistar rats. When the subcutaneous tumor diameter was about 0.5 cm, the tumor-bearing rats were randomly divided into control group, CH625 treatment group (intraperitoneal injection of 25 and 50 mg / kg), and sunitinib (80 mg / kg) treatment group, with 8 rats in each group. Mouse GL261 glioma cells (2×10 6 ) were inoculated subcutaneously and intracranially into C57BL / 6 mice, and when the diameter of the subcutaneous tumor was about 0.5 cm, they were grouped and treated in the same way as rats, with 10 mice in each group. The animals were sacrificed 24 hours after the last administration, the tumor weight was weighed, and the tumor inhibition rate was calculated.

[0034] (2) Experimental detection

[0035] 1. Record survival rate and detect 14, 15-EET-EA levels: observe the survi...

Embodiment 2

[0046] Based on the results and conclusions of the above experiments, it can be confirmed that CH625 is an effective drug for the treatment of glioma. [Example 2] Study on CH625 treating glioma by inhibiting CYP4X1 in BMDMs

[0047] (1) Grouping and handling of animals

[0048] Mouse bone marrow-derived mononuclear macrophages (BMDMs) were transfected with CYP4X1 lentiviral particles (Santa Cruz, CA, USA) to construct CYP4X1 overexpressed CYP4X1 high BMDMs cells.

[0049] GL261 cells (9×10 5 ) with BMDMs or CYP4X1, respectively high BMDMs (3×10 5 ) was inoculated subcutaneously in the right hind limb of C57BL / 6 mice at a ratio of 3:1. When the tumor diameter was about 0.5 cm, the tumor-bearing mice were randomly divided into control group and GH625 (i.p.25, 50 mg / kg) group, with 8 mice in each group. Mice were sacrificed 8 days after treatment, and tumors were harvested and analyzed.

[0050] (2) Experimental detection

[0051] 1. Weigh the mouse tumor and record the...

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PUM

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Abstract

The invention discloses application of a flavonoid compound CH625 to the preparation of drugs for resisting glioma, and belongs to the field of medicine. The CH625 in vivo antitumous effect is researched through experimental methods, such as immunofluorescence, Western blot and flow cytometry, on the basis of construction of a glioma model, and results show that the CH625 induces vascular normalization by inhibiting the generation of active anti-glioma vessels of CYP4X1, thereby achieving the effect of resisting glioma. The preparation method of the CH625 is very skillful, and a CH625 monomerwith high purity and excellent quality can be obtained through natural extraction or chemical synthesis, does not have toxic or side effects on human body, is rapid in efficacy, nonirritant, safe to use and good in effect.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicines, and in particular relates to a new application of a flavonoid compound CH625 in the preparation of inhibiting tumor angiogenesis so as to treat neuroglioma. Background technique [0002] Glioblastoma (GBM) is the most common primary malignant brain tumor (Wick et al., 2017). Angiogenesis plays an important role in the development of glioma (Turkowski et al., 2018). Vascular endothelial growth factor (VEGF) inhibitors are often used clinically to block glioma angiogenesis, but failed to improve overall survival (Wick et al., 2016); angiogenesis inhibitors sorafenib, sunitinib Or bevacizumab can increase the expression of PD-L1 in clinical treatment and promote an immunosuppressive microenvironment (Ramjiawan et al., 2017). The current challenge is to overcome these limitations and advance the benefits of anti-angiogenic therapy. Therefore, promoting the normalization of tumor blood ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61P35/00
CPCA61K31/12
Inventor 杨静汪辰龙黄可晴周晓阳刘筱潇邱苗刘妍灼
Owner WUHAN UNIV