GPR35 receptor agonist and application thereof

A receptor agonist and carrier technology, applied in anti-inflammatory agents, non-central analgesics, digestive system, etc., to achieve the effect of broadening the scope of clinical application

Inactive Publication Date: 2016-11-23
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there is no report about the effect of hydroxyrubidin on the GPR35 receptor in the anthraquinone compounds of Rubiaceae

Method used

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  • GPR35 receptor agonist and application thereof
  • GPR35 receptor agonist and application thereof
  • GPR35 receptor agonist and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: The discovery that the anthraquinone compound hydroxyrubidin acts on the GPR35 receptor

[0024] HT-29 cells were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences; Mintanin was purchased from Sigma; ML145 was purchased from Tocris. The detection platform is the third generation of Corning Imager, the detected signal is the wavelength shift caused by cell dynamic mass reset (DMR).

[0025] HT-29 cells in the logarithmic growth phase were inoculated into In a 384-well biosensor microplate, the volume of cell suspension inoculated in each well is 40 μL, and the number of cells inoculated in each well is 3.2×10 4 , and then place the 384-well plate in a cell culture incubator (5% CO 2 , 37° C.) for 22-24 hours, when the cell confluence reached about 95%, the experiment was carried out.

[0026]First, monitor the DMR response signal caused by 10 μM hydroxylibidin and 1 μM fenbuterol on HT-29 cells in real time, respectively, and then ...

Embodiment 2

[0028] Example 2: Verification that the anthraquinone compound hydroxyrubidin acts on the GPR35 receptor

[0029] We verified the agonist activity of hydroxyrubidin on the GPR35 receptor by desensitization assay and antagonism assay.

[0030] Desensitization analysis: add hydroxylizarin (maximum working concentration 100 rubirin, 2-fold dilution, 14 concentration gradients) into the HT-29 cells that have been inoculated 384-well biosensor microplates, in Monitor on the system for 1h, then add fentanil (working concentration 1μM) to continue to monitor for 1h, plot the DMR response of 1μM fentanil with the logarithmic dose of hydroxyrubizin, as shown in figure 2 a. It can be seen from the figure that the treatment with hydroxyrubizin alone caused a dose-dependent DMR response signal, and continued to add a fixed concentration of fentanil to the treatment, and the sensitivity of the GPR35 receptor to the agonist fentanil decreased, showing desensitization The phenomenon, a...

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PUM

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Abstract

The invention relates to a GPR35 receptor agonist and an application thereof as a medicine, and particularly, discloses discovery that an anthraquinone compound from a rubiaceous plant acts on a target site being a GPR35 receptor. The GPR35 receptor agonist herein employs hydroxyl-alizarin and / or one or more than two pharmaceutically acceptable salts of the hydroxyl-alizarin as active components. An in-vitro cell experiment proves that the hydroxyl-alizarin is an agonist of the GPR35 receptor. At present, the study proves that the GPR35 receptor is related to the diseases, comprising asthma, cardiac failure, hypertension, inflammation, coronary heart disease, metabolic syndrome, pain, cancer and the like, and as a result, a new high-effective ligand is provided for the related diseases with definite target sites.

Description

technical field [0001] The invention belongs to the field of GPR35 receptor agonists, and relates to the discovery of the action target of Rubiaceae anthraquinone compounds, in particular the discovery of the action target of hydroxylizarin in the anthraquinone compounds. The anthraquinone compound is hydroxylizarin and its pharmaceutically acceptable salt-forming compound; the target is the GPR35 receptor; the application is for the treatment of asthma, heart failure, hypertension, inflammation, coronary heart disease Prevention and treatment of diseases such as metabolic syndrome and pain. Background technique [0002] The dry roots and rhizomes of Rubia cordifolia L. contain a large amount of anthraquinone compounds (Anthraquinone compounds), which have various types and complex structures, and have the functions of promoting blood flow, stopping bleeding, clearing tendons and activating collaterals, relieving cough and expectorant, etc. , and exhibit a variety of pharma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P9/00A61P37/02A61P29/00A61P1/16A61P11/06A61P9/04A61P9/12A61P9/10A61P3/00
Inventor 梁鑫淼侯滔张秀莉史丽颖王纪霞魏来何牮
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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