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Application of compound as or in preparation of cannabinoid receptor agonist or antagonists

A technology of cannabinoid receptors and agonists, applied in the direction of anti-toxic agents, anti-inflammatory agents, drug combinations, etc., can solve the problems of unreported activity and function

Pending Publication Date: 2020-10-20
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

[0005] At present, the activity and function of the four natural compounds in Ganoderma lucidum found in the present invention on cannabinoid type I and cannabinoid type II receptors have not yet been reported

Method used

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  • Application of compound as or in preparation of cannabinoid receptor agonist or antagonists
  • Application of compound as or in preparation of cannabinoid receptor agonist or antagonists
  • Application of compound as or in preparation of cannabinoid receptor agonist or antagonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Example 1: Construction of Cannabinoid Type I Receptor and Cannabinoid Type II Receptor Screening Models

[0051] Materials: Agonist probe CP55,940 was purchased from Sigma-Aldrich, WIN55,212-2 was purchased from AbsinBioscience Inc.; antagonist probes SR141716A and SR144528 were purchased from Tocris Biosciences. Our laboratory stably transfected cannabinoid type I receptor and cannabinoid type II receptor in CHO (Chinese Hamster Ovary, Chinese hamster ovary cells) to obtain CHO-CB1 and CHO-CB2 cell lines [references for transfection process] Holmen, S.L., Vanbrocklin, M.W., Eversole, R.R., Stapleton, S.R., Ginsberg, L.C., 1995. Efficient Lipid-Mediated Transfection of DNA into Primary Rat Hepatocytes. In Vitro CellDev-An 31(5), 347-351.]. The detection platform is the third generation of Corning Imager, the detection signal is the wavelength shift caused by dynamic mass redistribution (Dynamic Mass Redistribution, DMR) of cells.

[0052] The transfected cells CHO-C...

Embodiment 2

[0064] Example 2: Preliminary Screening of Natural Compounds from Five Plants and Five Fungi on Cannabinoid Receptor Type I Receptor and Cannabinoid Type II Receptor Models

[0065] Materials: 82 natural compounds from five plants and five fungi were provided by Kunming Institute of Botany, Chinese Academy of Sciences. The five plants are safflower seed oil cake (Carthamus tinctorius L), Qingyang ginseng (Cynanchumotophyllum Schneid.), coffee (Coffee Arabica), green thorn fruit (Prinsepia utilis Royle), Maca (Lepidium meyenii, maca); five fungi Ganoderma hainanense, Ganoderma capense, Ganoderma cochlear, Ganoderma resinaceum and Ganoderma applanatum. Natural compound structures see Figure 3-5 [Isolation, purification and characterization of natural compounds related information references:

[0066]Dong, J.R., Peng, X.R., Li, L., Lu, S.Y., Zhou, L., Qiu, M.H., 2018. C21 steroidalglycosides with cytotoxic activities from Cynanchum otophyllum. Bioorganic & medicinal chemistry ...

Embodiment 3

[0093] Example 3: Characterization of Function and Activity of Active Compounds at Cannabinoid Type I and Cannabinoid Type II Receptors

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Abstract

The invention relates to discovery and application of a cannabinoid receptor new agonist and three new antagonists. The agonist is Kfb77, and the antagonists are Kfb28, Kfb68 and Kga1. In-vitro cell experiments show that the compound Kfb77 has an excitation effect on a cannabinoid type I receptor (CB1), the compound Kga1 has an antagonism effect on CB1, the compound Kfb28 has an antagonism effecton a cannabinoid type II receptor (CB2), and the compound Kfb68 has an antagonism effect on CB1 and CB2. Accordingly, the new natural agonist and antagonists for the CB1 and the CB2 provided by the invention provide candidate compounds for research and development of drugs for treating neurodegenerative diseases such as psychotic diseases, obesity / metabolic disorder related diseases, immune systemregulation and multiple sclerosis.

Description

technical field [0001] The present invention relates to the discovery and application of targeting active molecules in fungi and plants, in particular to the discovery and application of a new cannabinoid receptor agonist and three new antagonists in Zizhi and Bamboo Ganoderma lucidum. The new natural agonist of the cannabinoid receptor is Kfb77, and the new natural antagonists are Kfb28, Kfb68 and Kga1. The application includes treating one or more of diseases such as neurasthenia, insomnia and amnesia, cardiovascular and cerebrovascular diseases (such as hypertension, hyperlipidemia), inflammation, oxidative aging, obesity / metabolic disorder and the like. Background technique [0002] As two important receptors in the endocannabinoid system, cannabinoid type I and type II receptors (cannabinoid receptors, CB1 and CB2) belong to the class A rhodopsin-like family of G protein-coupled receptors and are widely distributed in A variety of tissues mediate a variety of physiolog...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61K31/352A61P25/20A61P29/00A61P25/14A61P9/12A61P3/06A61P39/06A61P3/04A61P3/00
CPCA61K31/575A61K31/352A61P25/20A61P29/00A61P25/14A61P9/12A61P3/06A61P39/06A61P3/04A61P3/00
Inventor 梁鑫淼周晗彭惺蓉侯滔张秀莉邱明华
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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