GABAA receptor conjugate for relieving and treating alcoholism and discomfort after drinking, composition and application of GABAA receptor conjugate and composition

An alcohol poisoning and conjugate technology, applied in the fields of dietary supplements and biomedicine, can solve the problems of unproven mechanisms and pathways of hangover and unverified effective active ingredients, so as to relieve and treat the discomfort symptoms after alcohol poisoning, Wide range of screening, efficacy in the treatment of alcoholism

Active Publication Date: 2021-12-28
HANGZHOU NUOSHEN TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although Scutellaria baicalensis is added to some anti-alcoholic prescriptions in the field of traditional Chinese medicine, Scutellaria baicalensis is used in combination with traditional Chinese medicine ingredients such as Bupleurum in the form of medicinal materials to prevent and treat alcoholism. The effective active ingredients in its extract have not been verified, and its molecular level solution Alcohol mechanisms and pathways have not been demonstrated

Method used

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  • GABAA receptor conjugate for relieving and treating alcoholism and discomfort after drinking, composition and application of GABAA receptor conjugate and composition
  • GABAA receptor conjugate for relieving and treating alcoholism and discomfort after drinking, composition and application of GABAA receptor conjugate and composition
  • GABAA receptor conjugate for relieving and treating alcoholism and discomfort after drinking, composition and application of GABAA receptor conjugate and composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Molecular docking and molecular dynamics screening of baicalin as an anti-alcohol component.

[0043] According to the above-mentioned method flow, through molecular docking and molecular dynamics simulation calculation, screen out baicalin can be in GABA A Antagonize ethanol on the receptor and the effect is better than DHM, the specific steps are as follows:

[0044] GABA expressed by α1 β2 δ2, α4 β2 δ2 and α6 β2 δ2 subunits was obtained from the PDB library A Receptor structure file. The structure of baicalin obtained through the preliminary screening of the stability test is CID 64982. Based on the calculation of binding energy after docking by CDOCKER, baicalin expresses GABA with α1 β2 δ2 subunit A The binding energy of the benzodiazepine binding domain of the receptor after docking is -65.63kcal / mol, which is a negative value, and the absolute value is higher than the binding energy of ethanol and DHM docking at the same site (respectively -12.49kcal / mol and -...

Embodiment 2

[0046] Baicalin blocks acute ethanol intoxication with results such as figure 2 shown.

[0047] The control group was pretreated with 20 g / kg saline by intraperitoneal injection 30 minutes before ethanol injection and then injected with 3 g / kg ethanol, which finally induced 67±5 minutes of LORR. Intervention with 2 mg / kg baicalin 30 minutes before ethanol injection reduced the ethanol-induced LORR to 12±3 LORR. Treatment with 2 mg / kg baicalin 30 minutes after ethanol injection reduced the ethanol-induced LORR to 42±4 (the control group LORR for this experiment was 71±4). Co-administration of 3 g / kg ethanol and 2 mg / kg baicalin reduced the duration of ethanol-induced LORR to 22±4 minutes (the LORR of the control group in this experiment was 68±3). Baicalin alone did not induce LORR. These results suggest that baicalin can antagonize acute alcoholism when administered before, during or after ethanol administration.

Embodiment 3

[0049] Molecular docking and molecular dynamics screening of isorhamnetin as antialcoholic component and isorhamnetin blocking acute ethanol intoxication.

[0050] Molecular docking and molecular dynamics simulations show that isorhamnetin and α1β2δ2 subunit express GABA A The binding energy of the benzodiazepine binding domain of the receptor after docking is -43.86kcal / mol, which is a negative value, and the absolute value is higher than the binding energy of ethanol and DHM docking at the same site (respectively -12.49 kcal / mol and - 41.84kcal / mol) large; isorhamnetin and α4 β2 δ2 subunit express GABA A The binding energy of the benzodiazepine binding domain of the receptor after docking is -44.15kcal / mol, which is a negative value, and the absolute value is higher than the binding energy of ethanol and DHM docking at the same site (respectively -11.95kcal / mol and -11.95kcal / mol and - 42.07kcal / mol) large; isorhamnetin and α6 β2 δ2 subunit express GABA A The binding energ...

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Abstract

The invention discloses an application of a GABAA receptor conjugate in preparation of health care products and medicines for relieving and treating alcoholism and discomfort after drinking, the GABAA receptor conjugate is a natural substance except DHM, and meets the following requirements: when molecular docking software is used for molecular docking and molecular dynamics calculation, after the GABAA receptor conjugate is bound with benzodiazepine binding domains of GABAA receptors expressed by subunits alpha 1 beta delta, alpha 4 beta delta and alpha 6 beta delta, the binding energy value is negative, and the absolute value of the binding energy value is not less than the absolute value of the binding energy of DHM and the same ligand and is greater than the absolute value of the binding energy of ethanol and the same ligand. The invention further discloses a composition for relieving and treating alcoholism and discomfort after drinking. The composition comprises the GABAA receptor conjugate and at least one of a liver-protecting natural substance, a gastrointestinal tract-protecting natural substance and a natural substance for inhibiting harmful alcohol metabolites in an immune system.

Description

technical field [0001] The invention relates to the technical field of dietary supplements and biomedicine, in particular to a method of antagonizing ethanol to GABA at the binding site of benzodiazepine (BZD) A Receptor active natural nutrients to eliminate alcohol intoxication and alleviate alcohol malaise. Background technique [0002] Alcoholism refers to the physiological effects and negative behaviors caused by the consumption of alcohol, which endangers the health of many people. Mild alcoholism is commonly known as drunkenness. Symptoms include mild behavioral disturbances and gastrointestinal discomfort. Higher alcohol doses may cause confusion in speech and thinking, difficulty walking and vomiting. Excessive alcohol may cause breathing difficulties, coma and even die. Excessive drinking will also increase the probability of crime and cause social unrest. [0003] Dihydromyricetin (DHM) is mostly extracted from a woody vine of the genus Vitis vinifera. It is an ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/7048A61K31/352A61K36/48A61K36/9066A61K31/357A61K36/488A61K31/185A61K31/198A61K31/19A61P25/32A61P1/16A61P39/00G16C10/00G16C20/30G16C20/50G16C20/10
CPCA61K45/06A61K31/7048A61K31/352A61K36/48A61K36/9066A61K31/357A61K36/488A61K31/185A61K31/198A61K31/19A61P25/32A61P1/16A61P39/00G16C10/00G16C20/30G16C20/50G16C20/10A61K2300/00Y02A50/30
Inventor 李骏黄易寒汤小苏
Owner HANGZHOU NUOSHEN TECH CO LTD
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