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Application of quassia alkaloids serving as indoleamine-2,3-dioxygenase (IDO) inhibitor

A technology of dioxygenase and alkaloids, applied in the field of medical applications, can solve the problems such as no related reports on alkaloids

Inactive Publication Date: 2019-02-22
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] So far, there is no relevant report on the application of bitterwood alkaloids as IDO inhibitors

Method used

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  • Application of quassia alkaloids serving as indoleamine-2,3-dioxygenase (IDO) inhibitor
  • Application of quassia alkaloids serving as indoleamine-2,3-dioxygenase (IDO) inhibitor
  • Application of quassia alkaloids serving as indoleamine-2,3-dioxygenase (IDO) inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 In Vitro Activity Screening and Evaluation

[0019] The IDO biological activity detection system was established, and the IDO recombined and purified in vitro was used as the research model, and the enzyme reaction kinetic monitoring method was used to measure the inhibitory activity of the alkaloids on IDO, and the Ki and IC were calculated. 50 value and further examine the type of inhibition for active compounds. The six kinds of bitterwood alkaloid compounds studied in the experiment have different structural skeletons, and the chemical structures are as follows:

[0020]

[0021] 1. Detection of IDO inhibitory activity

[0022] Reaction conditions: Mix 100mM potassium phosphate buffer (pH 6.5), 40mM vitamins, 200μg / mL catalase, 20μM methylene blue, 300mM substrate L-tryptophan and 100mM test sample, and incubate the mixture at 37°C for 5 minutes , then add IDO enzyme to the above mixture, react at 37°C for 30 minutes, add 200 μL of 30% (w / v) trichloro...

Embodiment 2

[0034]Example 2 In vivo activity evaluation

[0035] For the in vitro screening of active compounds, tumor mice were used as research models to investigate the effect of bitterwood alkaloids on tumor growth, and the ratio of kynurenine to tryptophan in serum was detected by HPLC to reflect the change of IDO activity, and the screening obtained high efficiency and low toxicity Novel IDO inhibitor drug candidates.

[0036] 1. Study on the inhibitory effect of 1-formic acid-β-carbaline on tumor growth

[0037] Take the human lung cancer A549 cells in the logarithmic growth phase, count the cells, put them into a 50mL centrifuge tube, resuspend them in 50% PBS buffer (pH 7.4) and 50% Matrigel, and adjust the cell concentration to 8×10 7 Cells / mL, pipette the cells to disperse them evenly. Aspirate the cell suspension and inject it into the anterior right mammary fat pad of healthy female Balb / C nude mice, inoculate 150 μL (1.2×10 7 cells / mL only). Select 30 tumor-bearing mice ...

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Abstract

The invention provides application of natural quassia alkaloids or pharmacologically acceptable salts of the natural quassia alkaloids serving as an indoleamine-2,3-dioxygenase (IDO) inhibitor. The quassia alkaloids or the pharmacologically acceptable salts of the quassia alkaloids serving as the IDO inhibitor can be used for preparing drugs, food, health products, food additives or nutritional supplements for preventing and / or curing pathological feature diseases caused by the fact that tryptophan metabolic pathways are mediated by IDO over-activation, and the diseases are selected from one or more of cancers, depression, Alzheimer disease and Parkinsonism.

Description

technical field [0001] The invention belongs to the field of medical applications, and relates to the medical use of eucalyptus alkaloids or their pharmaceutically acceptable salts, in particular to the use of chorizo ​​alkaloids or their pharmaceutically acceptable salts as IDO inhibitors. Background technique [0002] Indoleamine-2,3-dioxygenase (IDO) is an intracellular enzyme containing heme, which is the rate-limiting enzyme of human extrahepatic tryptophan metabolism, and can catalyze the indole ring in the tryptophan molecule Oxidative cleavage, catabolism along the kynuric acid pathway. As an immunomodulatory enzyme, IDO is related to the occurrence of a variety of diseases closely related to tryptophan deficiency, including cancer, depression, Alzheimer's disease, Parkinson's disease, autoimmune diseases, etc. [0003] In the tumor microenvironment, IDO can be highly expressed by various cells such as tumor cells, dendritic cells (DC), macrophages (MФ), endothelial...

Claims

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Application Information

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IPC IPC(8): A61K31/437C07D471/04A61P35/00A61P25/24A61P25/28A61P25/16A61P37/06A61P27/12
CPCA61K31/437A61P25/16A61P25/24A61P25/28A61P27/12A61P35/00A61P37/06C07D471/04
Inventor 许卉李志勇王宁杨倩文李乔张杰许晓蒙
Owner YANTAI UNIV
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