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Alkaloid compound with function of inhibiting PD-1/PD-L1 interaction and application

A PD-L1, PD-1 technology, applied in the field of medicine, can solve the problems of poor tissue and swelling permeability, poor oral bioavailability, poor stability, etc.

Active Publication Date: 2022-07-01
DONGZHIMEN HOSPITAL OF BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, antibody drugs have inherent limitations, including poor tissue and tumor penetration, depletion of Fc effector functions of immune cells, and their own immunogenicity.
There are also problems such as high cost, poor stability, poor oral bioavailability, and only 20%-30% effective rate of the first-line total population of a single drug, etc., which are difficult to solve in the short term

Method used

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  • Alkaloid compound with function of inhibiting PD-1/PD-L1 interaction and application
  • Alkaloid compound with function of inhibiting PD-1/PD-L1 interaction and application
  • Alkaloid compound with function of inhibiting PD-1/PD-L1 interaction and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation of Corydalis Corydalis extract includes the following steps:

[0033] (1) After soaking 50 kg of tubers of the traditional Chinese medicine Corydalis yanhusuo W.T. Wang in 10 L of an aqueous solution of acetic acid with a concentration of 6% by volume for 24 hours, they were dried at 40°C.

[0034] The medicinal materials soaked in acetic acid aqueous solution and dried were pulverized, soaked in water for 30 minutes, and then extracted by ultrasonic for 3 times, each time with 50 L of water for 1 hour, and the extracts were combined and concentrated under reduced pressure to obtain the extract.

[0035] The extract was subjected to macroporous adsorption resin (HPD-100) column chromatography, and eluted in turn with water and 50% ethanol aqueous solution (aqueous ethanol and methanol aqueous solution are both volume concentrations, the same below), wherein 50% ethanol aqueous solution The eluate was concentrated under reduced pressure to obtain 270 g of...

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PUM

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Abstract

The invention discloses an alkaloid compound with a function of inhibiting PD-1 / PD-L1 interaction and application of the alkaloid compound. The alkaloid compound is shown as a formula (I) or a formula (II). The alkaloid compound shown as the formula (I) or the formula (II) can be obtained through plant extraction. Experiments prove that the alkaloid compound as shown in the formula (I) or the formula (II) has the activity of remarkably inhibiting PD-1 / PD-L1 interaction at the concentration of 9.1-24.0 mu M, which prompts that the alkaloid compound as shown in the formula (I) or the formula (II) can be used as an inhibitor for PD-1 / PD-L1 interaction and is used for treating PD-1 / PD-L1 mediated related diseases.

Description

technical field [0001] The present invention belongs to the technical field of medicine, and in particular, the present invention relates to an alkaloid compound with the function of inhibiting the interaction of PD-1 / PD-L1 and use thereof. Background technique [0002] Immunity is a physiological function of the human body. The human body can maintain human health by rejecting invading bacteria, viruses, and damaged cells, senescent cells and tumor cells produced by itself through the immune system. Immune checkpoint molecules are a series of molecules that produce costimulatory or inhibitory signals in immune responses. Immune checkpoint proteins that have been found so far include programmed cell death receptor 1 (PD-1), programmed cell death Receptor-ligand 1 (PD-L1), cytotoxic T lymphocyte-associated antigen 4 (CTLA-4), lymphocyte activation gene 3 (LAG3), etc. Tumor cells can weaken the immune response through abnormal regulation of immune checkpoint molecular signals...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/22A61K31/4748A61P35/00A61P37/06A61P31/04A61P31/10A61P31/12
CPCC07D491/22A61P35/00A61P37/06A61P31/04A61P31/10A61P31/12
Inventor 林生商洪才田贵华夏桂阳夏欢
Owner DONGZHIMEN HOSPITAL OF BEIJING UNIV OF CHINESE MEDICINE
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