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Application of bibenzyl compounds in the preparation of drugs for promoting gastrointestinal motility

A technology of gastrointestinal motility and compounds, applied in the direction of drug combination, digestive system, ether/acetal active ingredients, etc., can solve problems such as promoting gastrointestinal motility that have never been done before

Active Publication Date: 2022-01-25
ZUNYI MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The current medicinal research on bibenzyl compounds has found that they have anti-tumor activity, such as: Bibenzyl compounds with application number 201610719859.7, its preparation method and its use in the preparation of anti-tumor drugs were published on February 1, 2017 ; On January 25, 2017, the bibenzyl compound with the application number 201610722925.6 and its preparation method and its use in the preparation of anti-tumor drugs were announced. However, until now, there has been no research on promoting gastrointestinal motility

Method used

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  • Application of bibenzyl compounds in the preparation of drugs for promoting gastrointestinal motility
  • Application of bibenzyl compounds in the preparation of drugs for promoting gastrointestinal motility
  • Application of bibenzyl compounds in the preparation of drugs for promoting gastrointestinal motility

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Experiment of 4,3'-dihydroxy-3,5'-dimethoxybibenzyl promoting gastrointestinal emptying in zebrafish.

[0019] 4,3'-dihydroxy-3,5'-dimethoxybibenzyl structure:

[0020] 1. Experimental instruments and main reagents

[0021] Zebrafish breeding system (Beijing Aisheng Science and Technology Development Co., Ltd.); MGC-100 constant temperature incubator (Shanghai Yiheng Scientific Instrument Co., Ltd.); M165-FC type fluorescent microscope imaging system (Germany Leica); carboxymethyl Sodium cellulose (CMC-Na, batch number: M0202A, Dalian Meilun Biotechnology Co., Ltd.); Nile red (Nile red, batch number: D1219A, Dalian Meilun Biotechnology Co., Ltd.); atropine.

[0022] 2. Breeding conditions

[0023] In this experiment, wild AB line zebrafish were used 120 hours after fertilization. Breeding conditions are Beijing Aisheng Zebrafish Breeding System, fully closed circulation, water temperature 28°C, room temperature 26°C, pH 7.2-7.5, conductivity 500-550μs·cm...

Embodiment 2

[0033] Example 2: Experiment of 3,3'-dihydroxy-5-methoxybibenzyl promoting gastrointestinal emptying in zebrafish.

[0034] 3,3'-dihydroxy-5-methoxybibenzyl structural formula:

[0035] The difference with Example 1 is: design 1 control group and 3 administration groups, respectively:

[0036] Solvent blank control group;

[0037] 2μM drug administration group to be tested;

[0038] 8μM drug administration group to be tested;

[0039] 24 μM test drug administration group.

[0040] The drug to be tested is 3,3'-dihydroxy-5-methoxybibenzyl solution.

[0041] Promote gastric emptying fluorescent picture figure 2 Shown: the order of emptying speed is 24μM>8μM>2μM>0μM.

Embodiment 3

[0042] Example 3: Experiment of 3,3'-dihydroxy-4,5'-dimethoxybibenzyl promoting gastrointestinal emptying in zebrafish.

[0043] 3,3'-dihydroxy-4,5'-dimethoxybibenzyl structure:

[0044] The difference with Example 1 is: design 1 control group and 3 administration groups, respectively:

[0045] Solvent blank control group;

[0046] 4μM drug administration group to be tested;

[0047] 12μM drug administration group to be tested;

[0048] 36μM test drug administration group.

[0049] The drug to be tested is 3,3'-dihydroxy-4,5'-dimethoxybibenzyl solution.

[0050] Promote gastric emptying fluorescent picture image 3 Shown: the order of emptying speed is 36 μM>12 μM>4 μM>0 μM.

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Abstract

This scheme discloses the new use of bibenzyl compounds, specifically relates to the application of bibenzyl compounds in the preparation of drugs for promoting gastrointestinal motility. In the present invention, 4,3'-dihydroxy-3,5'-dimethoxybibenzyl was carried out in vivo animal experiments, mainly based on the gastrointestinal peristalsis activity experiment of the zebrafish model, and found that it can act on the cholinergic nervous system , stimulate M receptors, thereby enhancing the excitability of gastrointestinal smooth muscle, increasing the amplitude and frequency of gastrointestinal motility, effectively promoting gastrointestinal motility, and facilitating gastrointestinal emptying. Digestive and M-receptor agonist drugs.

Description

technical field [0001] The invention relates to a new application of bibenzyl compounds, in particular to the application of bibenzyl compounds in the preparation of drugs for promoting gastrointestinal motility. Background technique [0002] The current medicinal research on bibenzyl compounds has found that they have anti-tumor activity, such as: Bibenzyl compounds with application number 201610719859.7, its preparation method and its use in the preparation of anti-tumor drugs were published on February 1, 2017 On January 25, 2017, the bibenzyl compound with the application number 201610722925.6 and its preparation method and its use in the preparation of anti-tumor drugs were announced. However, until now, there has been no research on promoting gastrointestinal motility. Contents of the invention [0003] The present invention intends to provide the application of a bibenzyl compound in the preparation of drugs for promoting gastrointestinal motility, which has the app...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/09A61P1/00A61P1/14
CPCA61K31/09A61P1/00A61P1/14
Inventor 肖世基刘贵园张茂生李晓飞
Owner ZUNYI MEDICAL UNIVERSITY
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