CN110151740B - Application of bibenzyl compound in preparation of medicine for promoting gastrointestinal peristalsis - Google Patents
Application of bibenzyl compound in preparation of medicine for promoting gastrointestinal peristalsis Download PDFInfo
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- CN110151740B CN110151740B CN201910615487.7A CN201910615487A CN110151740B CN 110151740 B CN110151740 B CN 110151740B CN 201910615487 A CN201910615487 A CN 201910615487A CN 110151740 B CN110151740 B CN 110151740B
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- bibenzyl
- gastrointestinal peristalsis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/075—Ethers or acetals
- A61K31/085—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon
- A61K31/09—Ethers or acetals having an ether linkage to aromatic ring nuclear carbon having two or more such linkages
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
Abstract
The scheme discloses a new application of bibenzyl compounds, and particularly relates to an application of bibenzyl compounds in preparation of medicaments for promoting gastrointestinal peristalsis. The invention carries out in-vivo animal experiments on 4,3 '-dihydroxy-3, 5' -dimethoxy bibenzyl, mainly based on the gastrointestinal peristalsis activity promotion experiments of a zebra fish model, finds that the bibenzyl can act on a cholinergic nervous system and excite an M receptor, thereby enhancing the excitability of gastrointestinal smooth muscle, improving the gastrointestinal peristalsis amplitude and frequency, effectively promoting the gastrointestinal peristalsis and being beneficial to the evacuation of intestines and stomach, and thus the application of bibenzyl compounds in the aspects of promoting the gastrointestinal peristalsis, invigorating stomach and helping digestion and M receptor agonist medicines is increased.
Description
Technical Field
The invention relates to a new application of bibenzyl compounds, in particular to an application of bibenzyl compounds in preparing medicaments for promoting gastrointestinal peristalsis.
Background
The current medicinal research on bibenzyl compounds finds that the bibenzyl compounds have antitumor activity, such as: a bibenzyl compound with application number of 201610719859.7, a preparation method thereof and application thereof in preparing antitumor drugs are published on 2 months and 1 days in 2017; bibenzyl compounds with application number 201610722925.6, a preparation method thereof, application in preparing antitumor drugs and the like are published on 25.1.2017, but researches on promoting gastrointestinal motility are not carried out until now.
Disclosure of Invention
The invention aims to provide the application of bibenzyl compounds in preparing medicaments for promoting gastrointestinal peristalsis, and has an application prospect in developing medicaments for promoting gastrointestinal peristalsis and/or invigorating stomach and helping digestion.
The bibenzyl compound in the scheme is applied to preparation of a medicine for promoting gastrointestinal peristalsis, and the bibenzyl compound or a pharmaceutically acceptable carrier thereof is applied to preparation of a medicine for promoting gastrointestinal peristalsis.
Further, the bibenzyl compound or a pharmaceutically acceptable carrier thereof is applied to preparation of M receptor agonist.
Further, the bibenzyl compound is 4,3 '-dihydroxy-3, 5' -dimethoxy bibenzyl.
The structural formula of the 4,3 '-dihydroxy-3, 5' -dimethoxy bibenzyl is as follows:
further, the bibenzyl compound is 3, 3' -dihydroxy-5-methoxyl bibenzyl.
The structural formula of the 3, 3' -dihydroxy-5-methoxyl bibenzyl is as follows:
further, the bibenzyl compound is 3,3 '-dihydroxy-4, 5' -dimethoxy bibenzyl.
The structural formula of the 3,3 '-dihydroxy-4, 5' -dimethoxy bibenzyl is as follows:
the invention adopts three compounds of 4,3 ' -dihydroxy-3, 5 ' -dimethoxy bibenzyl, 3 ' -dihydroxy-5-methoxy bibenzyl and 3,3 ' -dihydroxy-4, 5 ' -dimethoxy bibenzyl in bibenzyl compounds, respectively carries out in-vivo animal experiments, mainly based on the gastrointestinal peristalsis activity promotion experiment of a zebra fish model, finds that the bibenzyl compounds can act on a cholinergic nervous system and excite an M receptor, thereby enhancing the excitability of gastrointestinal smooth muscle, improving the peristalsis amplitude and frequency of the gastrointestinal, effectively promoting the gastrointestinal peristalsis and being beneficial to the emptying of the gastrointestinal, and therefore, the application of the bibenzyl compounds in the aspects of promoting the gastrointestinal peristalsis, strengthening the stomach and promoting digestion and M receptor agonist medicines is increased.
Drawings
FIG. 1 is a fluorescent image of 4,3 '-dihydroxy-3, 5' -dimethoxy bibenzyl for promoting gastrointestinal evacuation in accordance with the present invention;
FIG. 2 is a fluorescent image of 3, 3' -dihydroxy-5-methoxybenzyl for facilitating gastrointestinal evacuation in accordance with the present invention;
FIG. 3 is a fluorescent image of 3,3 '-dihydroxy-4, 5' -dimethoxy bibenzyl for promoting gastrointestinal evacuation.
Detailed Description
The following is further detailed by the specific embodiments:
the following three specific bibenzyl compounds are proved to be applicable to preparation of medicines for promoting gastrointestinal peristalsis through a zebra fish intestinal and gastric emptying promotion experiment.
Example 1: 4,3 '-dihydroxy-3, 5' -dimethoxy bibenzyl is used for promoting the intestinal and gastric emptying of zebra fish.
The structural formula of the 4,3 '-dihydroxy-3, 5' -dimethoxy bibenzyl is as follows:
1. laboratory apparatus and main reagent
Zebra fish breeding system (Beijing Aisheng science and technology development Co., Ltd.); MGC-100 type constant temperature incubator (Shanghai-Hengscientific instruments Co., Ltd.); M165-FC type fluorescence microscopy imaging system (Leica, Germany); sodium carboxymethylcellulose (CMC-Na, batch No. M0202A, Dalian Meiren Biotech Co., Ltd.); nile Red (Nile red, batch No. D1219A, Dalian Meiren Biotech Co., Ltd.); atropine.
2. Feeding conditions
Wild AB line zebrafish fertilized for 120 hours were used in this experiment. The breeding conditions are a Beijing Aisheng zebra fish breeding system, the full-closed circulation is adopted, the water temperature is 28 ℃, the room temperature is 26 ℃, the pH value is 7.2-7.5, and the conductivity is 500-550 mu s-cm-1The irradiation conditions were alternated with 14h of light and 10h of dark. Selecting zebra fish with good growth state, breeding according to the male-female ratio of 1: 1, separating male and female parts by using a partition plate, removing the partition plate in the next morning, collecting zebra fish embryos after 2h, and incubating in a constant-temperature incubator at 28 ℃.
3. Dyeing and dosing treatment
1 control group and 3 dosing groups were designed, respectively:
solvent blank control group;
1 μ M test drug administration group;
2 μ M test drug administration group;
6 μ M test drug administration group.
The drug to be tested is 4,3 '-dihydroxy-3, 5' -dimethoxy bibenzyl solution; the unit μ M is the concentration unit micromolar.
Each group is provided with 5 repeated groups, and each repeated group randomly places the zebra fish embryos which are normally developed after fertilization for 120 hours into a 24-well plate with 15 tails per well.
The embryo culture solution in the 24-well plate of each replicate was aspirated, 1mL of 10. mu.g/L Nile Red culture solution was immediately added, and the mixture was incubated in a constant temperature incubator for 16h in the absence of light. Absorbing the incubation liquid, washing 3 times by using the culture liquid, respectively feeding 1mL of 4,3 '-dihydroxy-3, 5' -dimethoxy bibenzyl solution with corresponding concentration to the administration group, feeding 1mL of dimethyl sulfoxide culture liquid with volume fraction of 0.1% to the solvent blank control group, putting the solution into a constant temperature incubator, incubating for 6h, taking out, fixing the solution on a glass slide with a groove by using 1% of CMC-Na, enabling the eyes and the body nodes to coincide, and taking a fluorescence image of the gastrointestinal tract of the zebra fish under a fluorescence microscope, wherein the darker the fluorescence indicates that the peristalsis is faster, the quicker the gastrointestinal emptying is, and as shown in figure 1, the emptying speed is ranked as 6 mu M > 2 mu M > 1 mu M > 0 mu M.
Example 2: 3, 3' -dihydroxy-5-methoxyl bibenzyl is used for promoting the intestinal and gastric emptying of zebra fish.
The structural formula of the 3, 3' -dihydroxy-5-methoxyl bibenzyl is as follows:
the difference from example 1 is that: 1 control group and 3 dosing groups were designed, respectively:
solvent blank control group;
2 μ M test drug administration group;
8 μ M test drug administration group;
24 μ M test drug administration group.
The drug to be tested is 3, 3' -dihydroxy-5-methoxyl bibenzyl solution.
The fluorescence map for promoting gastrointestinal emptying is shown in fig. 2: the emptying rates were ranked as 24. mu.M > 8. mu.M > 2. mu.M > 0. mu.M.
Example 3: 3,3 '-dihydroxy-4, 5' -dimethoxy bibenzyl is used for promoting the intestinal and gastric emptying of zebra fish.
The structural formula of the 3,3 '-dihydroxy-4, 5' -dimethoxy bibenzyl is as follows:
the difference from example 1 is that: 1 control group and 3 dosing groups were designed, respectively:
solvent blank control group;
4 μ M test drug administration group;
a 12 μ M test drug administration group;
36 μ M test drug administration group.
The drug to be tested is 3,3 '-dihydroxy-4, 5' -dimethoxy bibenzyl solution.
The fluorescence map for promoting gastrointestinal emptying is shown in fig. 3: the emptying rates were ordered 36. mu.M > 12. mu.M > 4. mu.M > 0. mu.M.
The foregoing is merely an example of the present invention and common general knowledge of known specific structures and features of the embodiments is not described herein in any greater detail. It should be noted that, for those skilled in the art, without departing from the structure of the present invention, several changes and modifications can be made, which should also be regarded as the protection scope of the present invention, and these will not affect the effect of the implementation of the present invention and the practicability of the patent. The scope of the claims of the present application shall be determined by the contents of the claims, and the description of the embodiments and the like in the specification shall be used to explain the contents of the claims.
Claims (2)
1. The application of bibenzyl compounds in preparing medicaments for promoting gastrointestinal peristalsis is characterized in that: the bibenzyl compound is one of 4,3 ' -dihydroxy-3, 5 ' -dimethoxy bibenzyl, 3 ' -dihydroxy-5-methoxy bibenzyl and 3,3 ' -dihydroxy-4, 5 ' -dimethoxy bibenzyl, and the bibenzyl compound or a pharmaceutically acceptable carrier thereof is applied to preparation of a medicament for promoting gastrointestinal motility.
2. The use of bibenzyls according to claim 1 for the preparation of a medicament for promoting gastrointestinal motility, characterized in that: the bibenzyl compound or a pharmaceutically acceptable carrier thereof is applied to the preparation of M receptor agonist.
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3960931A (en) * | 1973-03-23 | 1976-06-01 | Biorex Laboratories, Limited | 1,2-Diphenyl-ethane derivatives |
| CN102058567A (en) * | 2011-01-18 | 2011-05-18 | 广州中医药大学 | Application of 3',4-dyhydroxyl-3,5'-dimethoxybibenzyl in preparing medicaments for treating cataract |
| CN105709071A (en) * | 2014-05-05 | 2016-06-29 | 烟台民望机电技术有限公司 | Medicine for treating postnatal constipation and preparation method of medicine |
| CN109096232A (en) * | 2018-08-08 | 2018-12-28 | 遵义医学院 | A kind of dibenzyl dimer class compound and its method and application that separation is extracted from HERBA DENDROBII |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9849125B1 (en) * | 2015-11-03 | 2017-12-26 | Banner Lifie Sciences LLC | Anti-overingestion dosage forms |
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3960931A (en) * | 1973-03-23 | 1976-06-01 | Biorex Laboratories, Limited | 1,2-Diphenyl-ethane derivatives |
| CN102058567A (en) * | 2011-01-18 | 2011-05-18 | 广州中医药大学 | Application of 3',4-dyhydroxyl-3,5'-dimethoxybibenzyl in preparing medicaments for treating cataract |
| CN105709071A (en) * | 2014-05-05 | 2016-06-29 | 烟台民望机电技术有限公司 | Medicine for treating postnatal constipation and preparation method of medicine |
| CN109096232A (en) * | 2018-08-08 | 2018-12-28 | 遵义医学院 | A kind of dibenzyl dimer class compound and its method and application that separation is extracted from HERBA DENDROBII |
Non-Patent Citations (2)
| Title |
|---|
| "Influence of cinaciguat on gastrointestinal motility in apo-sGC mice";SARAH M. R. COSYNS等;《Neurogastroenterol Motil》;20141231(第26期);参见摘要 * |
| "石斛"厚肠胃"相关功效药理学研究及应用进展";颜美秋等;《中草药》;20161130;第47卷(第21期);参见摘要 * |
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