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Naturally derived FFA4 (GPR120) receptor agonist and application thereof

A receptor agonist, solvate technology, applied in the field of medicine, to achieve the effect of expanding the scope of clinical applications

Pending Publication Date: 2020-06-23
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

[0006] At present, the naphthoquinone compounds acetylshikonin, chrysanthemum quinone and shikonin in the family Boraginaceae, and the extracts of Burgeonaceae plants containing acetylshikonin and / or chrysanthemum quinone and / or shikonin act on the GPR120 receptor has not yet been reported

Method used

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  • Naturally derived FFA4 (GPR120) receptor agonist and application thereof
  • Naturally derived FFA4 (GPR120) receptor agonist and application thereof
  • Naturally derived FFA4 (GPR120) receptor agonist and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: The discovery that the naphthoquinone compound acetylshikonin acts on the GPR120 target on the transfected cell CHO-GPR120.

[0038] The transfection process of the transfected cell CHO-GPR120: First spread the CHO-K1 cells on a 10cm culture dish, incubate at 5% CO2 and 37°C for 18-24h, then conduct GPR120 transient transfection, the plasmid and transfection reagent Lipo2000 are 8ug respectively and 24uL. After 24 hours of transient transformation, replace with F12K+10% FBS medium containing 600ug / mL zeocin, and change the medium every 2-3 days (the liquid is F12K+10%FBS medium containing 600ug / mL zeocin), and the duration is about 1 month.

[0039] Probe molecule agonist TUG891 and antagonist AH7614 were purchased from TOCRIS. The detection platform is Corning's third-generation Epic imager, and the detected signal is the wavelength shift caused by cell dynamic mass reset (DMR).

[0040] CHO-GPR120 cells in logarithmic growth phase were inoculated into 38...

Embodiment 2

[0048] Example 2: In addition to transfected cells, verification experiments on the target of acetylshikonin GPR120 were also performed on HT29 cells endogenously expressing GPR120.

[0049] HT29 cells were purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences; the probe molecular agonists and antagonists, still using TUG891 and AH7614, were purchased from TOCRIS. The detection platform is Corning's third-generation Epic imager, and the detected signal is the wavelength shift caused by cell dynamic mass reset (DMR).

[0050] Inoculate HT29 cells in the logarithmic growth phase into 384 microwell plates provided by Epic, the volume of cell suspension in each well is 40 μL, and the inoculated density is 3.2×104 cells / well, and then place the inoculated 384 plates in In a cell incubator, culture at 5% CO2 and 37° C. for 18-24 hours, and perform the experiment when the degree of cell confluence reaches above 95%.

[0051] Firstly, the DMR signals induced by 12....

Embodiment 3

[0056] Example 3: On the transfected cell CHO-GPR120, the activity of GPR120 extracted from Xinjiang soft comfrey extract extracted with 95% ethanol was found.

[0057] The transfection process of the transfected cell CHO-GPR120: First spread the CHO-K1 cells on a 10cm culture dish, incubate at 5% CO2 and 37°C for 18-24h, then conduct GPR120 transient transfection, the plasmid and transfection reagent Lipo2000 are 8ug respectively and 24uL. After 24 hours of transient transformation, replace with F12K+10% FBS medium containing 600ug / mL zeocin, and change the medium every 2-3 days (the liquid is F12K+10%FBS medium containing 600ug / mL zeocin), and the duration is about 1 month.

[0058] Probe molecular agonist TUG891 was purchased from TOCRIS. The detection platform is Corning's third-generation Epic imager, and the detected signal is the wavelength shift caused by cell dynamic mass reset (DMR).

[0059] CHO-GPR120 cells in logarithmic growth phase were inoculated into 384 mi...

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Abstract

The invention relates to an FFA4 (GPR120) receptor agonist and an application thereof. Particularly the invention relates to a discovery of an effect target from a natural plant naphthoquinone compound, wherein the target point is a G protein coupled receptor GPR120, and the GPR120 receptor agonist is acetylshikonin, lapachol, alkannin, and / or corresponding pharmaceutically acceptable salts, solvates, polymorphs and pharmaceutical compositions of acetylshikonin, lapachol and alkannin. In-vitro cell target experiments show that acetylshikonin, lapachol and alkannin are agonists of GPR120. In vitro cell experiment tests show that a boraginaceae plate extract which is subjected to cold leaching by 95% ethanol also has GPR120 agonistic activity. Studies show that GPR120 receptors are associated with non-steroidal anti-inflammatory drug-induced gastric injury, bone stuffiness, Crohn's diseases and other diseases, and therefore the agonists have potential pharmaceutical uses.

Description

technical field [0001] The invention belongs to the field of medical technology, specifically the field of GPR120 agonists, and relates to the discovery of the action target of naphthoquinone compounds in natural plants, specifically acetylshikonin, chrysanthemum quinone and shikonin in naphthoquinone compounds, and containing Discovery of targets of acetylshikonin and / or chrysanthemum quinone and / or shikonin in extracts from plants of the family Boraginaceae. The compound is acetylshikonin and / or chrysanthemum quinone and shikonin and / or their corresponding pharmaceutically acceptable salts, solvates or polymorphs and pharmaceutical compositions, and containing acetylshikonin and / or The Baginaceae plant extract of chrysanthemum quinone and / or shikonin; the target is the GPR120 receptor; the application is for non-steroidal anti-inflammatory drugs to induce gastric damage, osteoporosis and Crohn's disease, etc. Treatment and prevention. [0002] technical background [0003...

Claims

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Application Information

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IPC IPC(8): A61K31/122A61K31/222A61K36/30A61P29/00A61P1/00A61P19/10
CPCA61K31/122A61K31/222A61K36/30A61P29/00A61P1/00A61P19/10A61K2300/00
Inventor 梁鑫淼徐芳芳张秀莉侯滔周晗
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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