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Nutritional composition containing GABA receptor stimulant and CB1 receptor stimulant, and preparation method and application thereof

A nutritional composition and receptor agonist technology, applied in the fields of dietary supplements and biomedicine, can solve problems such as limited GABA content and inability to exert product efficacy well

Active Publication Date: 2021-07-30
HANGZHOU NUOSHEN TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Aiming at the deficiencies in this field, the present invention provides a nutritional composition containing GABA and a CB1 receptor agonist, which can be directly taken orally, and solves the problem that the sleep-promoting and calming products mainly based on GABA in the field of health care products are taken orally. Introducing exogenous GABA, the content of GABA that penetrates the blood-brain barrier and binds to its receptors in the brain is limited, and the product efficacy cannot be well exerted

Method used

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  • Nutritional composition containing GABA receptor stimulant and CB1 receptor stimulant, and preparation method and application thereof
  • Nutritional composition containing GABA receptor stimulant and CB1 receptor stimulant, and preparation method and application thereof
  • Nutritional composition containing GABA receptor stimulant and CB1 receptor stimulant, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] According to the process of the above method, through molecular docking and molecular dynamics simulation calculations, it is screened that rutin can be used as an agonist of the CB1 receptor to form a nutrient combination with GABA, and the specific steps are as follows:

[0057] Obtain the active and inactive forms of the CB1 receptor structure files from the PDB library, respectively 5XRA.pdb and 5TGZ.pbd. The structure of rutin obtained through the preliminary screening of the stability test is CID 5280805. According to the calculation of binding energy after docking by CDOCKER, the binding energy of rutin after docking with active CB1 receptor is -48.6002kcal / mol, and the binding energy after docking with inactive CB1 receptor is -31.6176kcal / mol. The binding energies of the two forms of CB1 receptors after docking are negative, and the comparison of the two values ​​shows that rutin is more likely to bind to the active CB1 receptor. Judging from this, rutin can a...

Embodiment 2

[0059] According to the process of the above method, through molecular docking and molecular dynamics simulation calculations, EGCG can be used as an agonist of CB1 receptor to form a nutrient combination with GABA. The specific steps are as follows:

[0060] Obtain the active and inactive forms of the CB1 receptor structure files from the PDB library, respectively 5XRA.pdb and 5TGZ.pbd. The structure of EGCG obtained through the preliminary screening of the stability test is CID 65064. The binding energy after docking by CDOCKER is calculated, the binding energy of EGCG after docking with active CB1 receptor is -54.4430kcal / mol, and the binding energy after docking with inactive CB1 receptor is -43.5688kcal / mol, EGCG and two kinds of The binding energy of the formal CB1 receptor after docking is negative, and the comparison of the two values ​​shows that EGCG is more likely to bind to the active CB1 receptor. It can be judged that EGCG can act as an agonist of CB1 receptor i...

Embodiment 3

[0062] Based on the results of Example 1, GABA powder was mixed with rutin powder and fed orally to the mice in the experimental group. For the effect of GABA / rutin weight ratio on sleep duration and quality, the experimental group was further divided into five groups, one group took 100mg / kg GABA orally, and the other took 100mg / kg (m / m=100 / 5, the same below) GABA / rutin combination, a group of oral 100mg / kg (100 / 12) GABA / rutin combination, a group of oral 100mg / kg (100 / 50) GABA / rutin combination, a group of oral 100mg / kg rutin, in small A total of six groups of mice were monitored by EEG 45 minutes after dosing. Depend on Figure 4 (a) It can be seen that compared with the control group (taking no preparations), the sleep duration of the 100mg / kg GABA group was longer than that of the control group, and the 100mg / kg (100 / 5) GABA / rutin group was slightly longer than the 100mg / kg GABA group , 100mg / kg (100 / 12) GABA / rutin group was significantly more than the control group (~...

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Abstract

The invention discloses a nutritional composition containing a GABA receptor stimulant and a CB1 receptor stimulant, and a preparation method thereof. The nutritional composition comprises the GABA and the CB1 receptor stimulant in a mass ratio of 100: (3-40), and the sum of the mass of the GABA receptor stimulant and the mass of the CB1 receptor stimulant is not lower than 47% of the total mass of the nutritional composition. The preparation method comprises the following steps: uniformly mixing the components in proportion, and then filling, tabletting or filling. The invention also provides application of the nutritional composition in preparation of medicines and health-care products for relieving anxiety, relieving difficulty in falling asleep, improving sleep quality and / or treating fatigue, anxiety, hypomnesis, slow response and reduced motility caused by insomnia and mental stress, and application in oral preparations.

Description

technical field [0001] The invention relates to the technical fields of dietary supplements and biomedicine, in particular to a nutritional composition containing GABA and a CB1 receptor agonist and its preparation and application. Background technique [0002] γ-Aminobutyric acid (GABA) is a naturally occurring non-protein amino acid and is an important inhibitory neurotransmitter in the mammalian central nervous system. About 30%-50% of the central nervous system synapses use GABA as a transmitter . [0003] GABA will have a powerful calming (inhibiting) effect on the brain. When GABA acts on excitatory nerves, after binding to the receptors on the excitatory nerve synapses, the neuron endings cannot release neurotransmitters to the lower nervous system. A neuron, the signal conduction between nerves is interrupted, thereby inhibiting the overexcitation of the central nervous system, reducing anxiety, calming emotions, and promoting better sleep. GABA also has a protecti...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/197A61K31/7048A61K31/353A61K9/00A61P25/20A61P25/22A61P39/00A61P25/28A61P25/14A23L33/175A23L33/105A23L33/125
CPCA61K45/06A61K31/197A61K31/7048A61K31/353A61K9/0053A61P25/20A61P25/22A61P39/00A61P25/28A61P25/14A23L33/175A23L33/105A23L33/125A23V2002/00A61K2300/00A23V2200/322A23V2200/31A23V2250/2117A23V2250/2116A23V2250/038
Inventor 李骏黄易寒汤小苏
Owner HANGZHOU NUOSHEN TECH CO LTD
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