Application of Kukoamine in preparing anti-tumor drugs

A technology of dicortex B and anti-tumor drugs, applied in the field of biomedicine, can solve the problems of low price, weak immunogenicity, and no small molecule inhibitors of traditional Chinese medicine PD-L1

Active Publication Date: 2019-11-22
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compared with monoclonal antibodies, small-molecule PD-L1 inhibitors have the advantages of strong penetration in tumors, weak immunogenicity, low price, and can be taken orally. At present, no PD-L1 small-molecule inhibitors can be used clinically Experiments, and there are no reports of traditional Chinese medicine PD-L1 small molecule inhibitors
There is no relevant report on the use of cortex B in the preparation of antitumor drugs

Method used

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  • Application of Kukoamine in preparing anti-tumor drugs
  • Application of Kukoamine in preparing anti-tumor drugs
  • Application of Kukoamine in preparing anti-tumor drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0026] This example is a tablet that inhibits the combination of PD-1 / PD-L1 of the present invention. In terms of weight percentage, the tablet includes the following ingredients:

[0027] 10% Dicocortis B, 0.8% talcum powder, 0.02% light liquid paraffin, and starch make up to 100%.

[0028] The preparation method of the above-mentioned tablet: the lyophilized powder of Digupi extract (containing 50 g of Digustin), 4 g of talcum powder, 0.1 g of light liquid paraffin, and the starch is supplemented to a total mass of 500 g to make a soft material, and baked at low temperature. Dry granulate, sieve, and compress 2000 tablets, each containing 25 mg of cortex B, to obtain the above tablet.

Embodiment 2

[0030] This example is a capsule that inhibits the combination of PD-1 / PD-L1 according to the present invention. In terms of weight percentage, the capsule includes the following ingredients:

[0031] 95% Dicosin, 4% Corn Starch, 1% Mannitol

[0032] The preparation method of the above-mentioned capsules: 285g of dicortex B, 3g of mannitol, 12g of cornstarch, fully mixed and packed into 1000 capsules, each capsule containing 285mg of dicortex B, can make the above-mentioned capsules .

Embodiment 3

[0034] This example is an injection that inhibits the combination of PD-1 / PD-L1 of the present invention. In terms of weight / volume percentage, the injection includes the following ingredients:

[0035] 50% Dicosin, 20% Propylene Glycol, and Water for Injection make up to 100%

[0036] The preparation method of the above-mentioned injection: 500ml of Cortex Digusticum extract (containing 10g of Dicortex B), dissolves 10g of Dicortex B in 200ml of propylene glycol, adds water for injection to 1000ml, filters, bottling and sterilizing, Each bottle of 100ml can prepare the above-mentioned injection for intravenous infusion.

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Abstract

The invention relates to application of Kukoamine in preparing anti-tumor drugs, in particular to application of Kukoamine in preparing a PD-1/PD-L1 axis inhibitor, and belongs to the field of biologic medicine. The inhibitor is used for inhibiting combination of PD-1/PD-L1, and the effective ingredient of the inhibitor is Kukoamine. The traditional Chinese medicine micromolecule Kukoamin is adopted as the PD-1/PD-L1 axis inhibitor for the first time, combination of PD-1/PD-L1 is inhibited, recognition and killing for tumor cells of immune cells, particularly T cells are brought into play, then, the anti-tumor effect is achieved, and the new drug selection is supplied to tumor prevention and/or treatment.

Description

technical field [0001] The present invention relates to the application of diocetin in the preparation of antitumor drugs, in particular to the application of diocetin in the preparation of PD-1 / PD-L1 axis inhibitors, and belongs to the field of biomedicine. Background technique [0002] Malignant tumors are the leading cause of death among Chinese residents. Although surgery, chemotherapy, radiotherapy and targeted therapy have made important contributions to prolonging the life span and improving the quality of life of cancer patients, the response rate of these treatments is low, the accompanying side effects are still significant, and the therapeutic effect is still low. There is a lot of room for improvement. In the microenvironment of tumor lesions, PD-L1 on the surface of tumor cells can bind to PD-1 on the surface of immune cells to inactivate immune cells, thereby helping tumor cells escape immune surveillance. PD-1 / PD-L1 axis inhibitors can reactivate the recogni...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G16C20/50G16B25/20
CPCG16C20/50G16B25/20
Inventor 张韧伍志学郑丹娜尹衡伍海涛
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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