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Method for preparing PD-1/PD-L1 inhibitor from aconitum gymnandrum maxim

A technology of PD1-PDL1 and Lurui Aconitum, applied in the application field of natural products, can solve the problems of side effects, high cost, poor oral administration, etc.

Inactive Publication Date: 2020-07-07
QINGHAI UNIV FOR NATITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the inherent disadvantages of antibody therapy, such as high cost, poor oral administration, immune-related side effects, and the overall effective rate of single-drug first-line population is only 20%-30%

Method used

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  • Method for preparing PD-1/PD-L1 inhibitor from aconitum gymnandrum maxim
  • Method for preparing PD-1/PD-L1 inhibitor from aconitum gymnandrum maxim
  • Method for preparing PD-1/PD-L1 inhibitor from aconitum gymnandrum maxim

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Preparation of Crude Extract of Active Components of Aconitum Aconitum

[0046] The preparation method of the active ingredient of Lurui Aconitum that effectively blocks the combination of PD1-PDL1 is as follows:

[0047] (1) Extraction: Select the high-quality Aconitum aconitum branches, leaves and roots, wash and dry them with pure water, then crush the branches, leaves and roots, soak them in 60% ethanol for 8 hours, extract twice and filter to obtain the filtrate, and decompress Recover the solvent, add 70% ethanol to the filter residue and ultrasonically extract twice, extract 3 hours each time, concentrate under reduced pressure to obtain 70% ethanol extract; use 83% ethanol to extract once in the same way, concentrate under reduced pressure to obtain 83% ethanol extract, and combine to obtain Ethanol total extract. The total ethanol extract is completely dissolved in water at 1:3, and then extracted with ethyl acetate, the ratio of water to ethyl aceta...

Embodiment 2

[0053] Example 2 Preparation of Crude Extract of Active Components of Aconitum Aconitum

[0054] The preparation method of the active ingredient of Lurui Aconitum that effectively blocks the combination of PD1-PDL1 is as follows:

[0055] (1) Extraction: select high-quality Aconitum aconitum branches, leaves and roots, wash and dry them with pure water, then crush the branches, leaves and roots, soak them in 74% ethanol for 4 hours, extract twice and filter to obtain the filtrate, and recover the solvent under reduced pressure. Add 80% ethanol to the filter residue and ultrasonically extract twice, extract 4 hours each time, concentrate under reduced pressure to obtain 80% ethanol extract; use 85% ethanol to extract once in the same way, concentrate under reduced pressure to obtain 85% ethanol extract, combine to obtain ethanol total extract paste. The total ethanol extract is completely dissolved in water at a ratio of 1:4, and then extracted with ethyl acetate, the ratio of...

Embodiment 3

[0061] Example 3 Preparation of Crude Extract of Active Components of Aconitum Aconitum

[0062] The preparation method of the active ingredient of Lurui Aconitum that effectively blocks the combination of PD1-PDL1 is as follows:

[0063] (1) Extraction: Select high-quality Aconitum aconitum branches, leaves and roots, wash and dry them with pure water, then crush the branches, leaves and roots, soak them in 75% ethanol for 4 hours, extract twice and filter to obtain the filtrate, and decompress Recover the solvent, add 80% ethanol to the filter residue and ultrasonically extract twice, extract 2 hours each time, concentrate under reduced pressure to obtain 80% ethanol extract; use 85% ethanol to extract once in the same way, concentrate under reduced pressure to obtain 85% ethanol extract, and combine to obtain Ethanol total extract. The total ethanol extract is completely dissolved in water at a ratio of 1:4, and then extracted with ethyl acetate, the ratio of water to ethy...

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Abstract

The present invention discloses an active ingredient extracted from aconitum gymnandrum maxim as a natural plant and an extraction method of the active ingredient. More particularly the active ingredient extracted from the aconitum gymnandrum maxim can effectively block PD1-PDL1 combination to remove, inhibit, reduce or block PD1-PDL1 interaction and subsequent action; a pharmaceutical compositionof the active ingredient and a pharmaceutical carrier can effectively become a novel PD1-PDL1 inhibitor; and the PD1-PDL1 inhibitor is applied to anti-tumor related diseases, so that references are provided for clinical treatment schemes.

Description

Technical field: [0001] The present invention relates to the technical field of application of natural products, extracting active ingredients from the natural plant Aconitum aconitum, and more specifically relates to extracting active ingredients from Aconitum aconitum that can eliminate, inhibit, reduce or block the combination of PD1-PDL1 and the The active ingredient can be a pharmaceutical composition with a pharmaceutically acceptable carrier, and it can be used in related diseases. Background technique: [0002] The body's immune system can identify tumor cells, regulate tumor growth, and even eliminate tumors, and T cells play a central role in this process. The activation of T cells first requires the first signal stimulation provided by antigen-presenting cells, and also requires the second signal stimulation provided by co-stimulatory molecules. Costimulatory molecules not only provide co-stimulatory signals to enhance immunity, but also provide co-inhibitory sig...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/714A61P35/00A61P35/02A61K125/00A61K127/00A61K135/00
CPCA61K36/714A61K2236/333A61K2236/55A61P35/00A61P35/02
Inventor 王敏吴疆林鹏程姚政许地元王泽
Owner QINGHAI UNIV FOR NATITIES
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