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Compound, muscarine M receptor antagonist, composition and application

A receptor antagonist and compound technology, which is applied in the discovery and application field of the action mechanism of the active ingredients of natural medicines, to achieve the effect of broadening the scope of clinical applications

Inactive Publication Date: 2017-09-05
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

However, because atropine has effects on glands, smooth muscle, and nervous system, it has multiple side effects while treating diseases. In contrast, the discovery of M receptor antagonists with different structures, especially new compounds themselves, may have fewer side effects

Method used

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  • Compound, muscarine M receptor antagonist, composition and application
  • Compound, muscarine M receptor antagonist, composition and application
  • Compound, muscarine M receptor antagonist, composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Purification and Preparation of Alkaloid Compounds in Anisodamine Tangut

[0037] 1. Experimental instruments and reagents

[0038] Tangut Anisopolamine medicinal material was collected in Qinghai by the Northwest Plateau Botanical Institute, and was identified by Teacher Mei Lijuan. Column XCharge C18 (4.6×250mm, 7μm, Huapu Company), XCharge C18 (100×280mm, 7μm, Huapu Company), XCharge SCX (100×316mm, 7μm, Huapu Company), XCharge C18 (20×250mm , 7 μm, Huapu Company), anhydrous sodium sulfate, sodium dihydrogen phosphate dihydrate were purchased from Sinopharm Group, ethanolamine, phosphoric acid, and formic acid were purchased from Bailingwei, and preparative chromatography grade acetonitrile was purchased from Anhui Shilian.

[0039] 2. Purification and preparation of compounds

[0040] 50kg of Anisodina tanguta medicinal material was extracted with ethanol, divided into two batches of 25kg each, soaked in 80L of ethanol, heated to reflux for 2 hours, and ...

Embodiment 2

[0041] The DMR signal characteristic of embodiment 2 muscarinic M receptor antagonist on Epic platform

[0042] 1. Method

[0043] 1.1 Cell culture

[0044] HT29 human colon cancer cells were obtained from the Cell Bank of the Type Culture Collection Committee of the Chinese Academy of Sciences (Shanghai, China). HT29 cells were treated with McCoy’s 5A medium (GIBCO, product number 12800017, containing D-Glucose 4500.0mg / L, adding NaHCO 3 2.2g / L), at 37°C, with a volume content of 5% CO 2 (air) incubator.

[0045] 1.2 Cell Viability Experimental Method of Muscarinic M Receptor Antagonists

[0046] HT29 cells were treated with 2×10 4 Individuals / well density seeded to In a 384-well biosensor microplate, placed at 37°C, with a volume content of 5% CO 2 (air) incubator for 22 h, washed with HBSS buffer once before detection, then added 30 μL of HBSS buffer to each well, placed in The system was equilibrated and incubated for 1h. After balancing first in Establish a 2...

Embodiment 3B

[0051] Example 3 BDCS Antagonistic Activity to Muscarinic M Receptors

[0052] The dose-effect relationship of BDCS, a compound with strong M receptor antagonistic activity in activity screening, was further investigated by using label-free cell target pharmacology technology. First, 10 μL of the compound to be tested was added to the inoculated HT29 cells In the 384-well biosensor microplate (same as embodiment 2), in The system was monitored for 60 minutes, and then 10 μL of acetylcholine (16 μM) was added to continue monitoring for 60 minutes. The DMR signal induced by the compound is plotted with the action time, such as image 3 a (The compound concentration is diluted stepwise from 100 μM to 24.4nM, the corresponding DMR signal curves are arranged from top to bottom, and the signal changes little); the DMR response signal caused by the second step of adding acetylcholine is plotted with the action time, the result Such as image 3 b (The compound concentration was ...

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Abstract

The invention discloses a discovery and application of an acting target of hydroxyl cinnamamide compound separated from solanaceae plants, and particularly relates to a discovery of an acting target of hydroxyl cinnamamide compound N1, N8-bis (dihydrocaffeoyl) spermidine (BDCS for short) and application thereof in spasmolysis drug. Unmarked cell target pharmacology technology finds that the compound has high muscarine M receptor antagonistic activity, dose-effect relationship researches show that dose is dependently antagonistic to DMR response signals caused by acetylcholine and BDCS is a muscarine M receptor antagonist. BDCS and one or more than two of pharmaceutically-acceptable salts of BDCS are used as active ingredients of the muscarine M receptor antagonist. Current researches show that muscarine M receptor is related to diseases like spasm, analgesia, sedation and schizophrenia, so that an efficient novel ligand with the acting target being clear can be provided for related diseases.

Description

technical field [0001] The invention belongs to the field of discovery and application of the action mechanism of active ingredients of natural medicines, and specifically relates to the antispasmodic action mechanism and application of an antispasmodic active ingredient. Background technique [0002] Anisodus tanguticus Anisodus tanguticus is a plant of the genus Anisodora in the family Solanaceae. It is a unique plant in China. It is called "Tangchuan Nabao" in Tibetan. Distributed in Gansu, Tibet, Yunnan, Qinghai and other places in mainland China, it grows in areas with an altitude of 2,800 meters to 4,200 meters. It usually grows on hillsides and grassy slopes. It has not been introduced and cultivated artificially. As a traditional Tibetan medicine, Tibetan medicine uses Anisopolamine tanguta and its seeds as medicine, which has anesthetic and analgesic effects [1]. There are few reports on the chemical constituents of Anisodamine Tangut, most of which are tropine alk...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C235/34A61K31/165A61P25/20A61P25/00A61P25/18A61P25/24A61P25/16A61P39/02A61P21/02
CPCC07C235/34
Inventor 梁鑫淼杜娜娜刘艳芳张秀莉
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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