Drug with neuroprotective effect and application of drug

A technology of nerve protection and medicine, which is applied in the field of medicine to achieve good curative effect, increase concentration and obvious curative effect

Active Publication Date: 2020-10-27
MUDANJIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The mechanism and use of these compounds in the treatment of nervous tension and other diseases have not been reported yet

Method used

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  • Drug with neuroprotective effect and application of drug
  • Drug with neuroprotective effect and application of drug
  • Drug with neuroprotective effect and application of drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 Preparation of theaflavin-3'-gallate and granules thereof

[0029] The formula (I) compound of the present invention, its name is theaflavin-3'-gallate:

[0030]

[0031] Molecular weight: 704.630; CAS number: 28543-07-9; source: Chengdu Purifa Technology Development Co., Ltd.\Chengdu Zhibiao Pure Biotechnology Co., Ltd., purity ≥ 98%;

[0032] Preparation of theaflavin-3'-gallate granules

[0033] Prescription: Theaflavin-3'-gallate 300g

[0034] Excipients: β-cyclodextrin, γ-cyclodextrin, microcrystalline cellulose, low-substituted hydroxypropyl cellulose, povidone K30 and water. The dosage of β-cyclodextrin is 0.6 times of the weight of theaflavin-3'-gallate, the dosage of γ-cyclodextrin is 0.4 times of that of theaflavin-3'-gallate, and the dosage of microcrystalline cellulose is 0.6 times of that of tea 1 times the weight of flavin-3'-gallate, the amount of low-substituted hydroxypropyl cellulose is 0.17 times the weight of theaflavin-3'-gallate,...

Embodiment 2

[0039] The toxicology experiment of embodiment 2 formula (I) compound

[0040] 1. Acute toxicity test

[0041] (1) Oral administration

[0042]Kunming mice were used, weighing 20g±2g, half male and half male. Theaflavin-3'-gallate granules were made into 20% aqueous suspension, administered orally to fasting mice 3 times a day, 0.3mL each time, with a total amount of 180mg / kg, and observed continuously for 7 days , no death or side effects were seen;

[0043] (2) Injection administration

[0044] Kunming mice were used, weighing 20g±2g, half male and half male. Theaflavin-3'-gallate was formulated into 2% injection. Injection administration, each 0.4mL. The measured LD50(ip)=25.76+6.35g / kg, LD50(iv)=18.55+4.68g / kg.

[0045] 2. Long-term toxicity test

[0046] SD rats with a body weight of 200±20 g, half male and half male, 180 in total. Oral administration respectively. Theaflavin-3'-gallate was formulated into 20% aqueous suspension, and the doses were 1mg / kg, 5mg / k...

Embodiment 3

[0049] Example 3 Observed the main pharmacological effects of theaflavin-3'-gallate through animal experiments

[0050] 1. The effects of theaflavin-3'-gallate granules of this embodiment on the autonomous activities of animals

[0051] 1. Animal grouping: 30 Kunming mice, weighing 20-22g, half male and half male;

[0052] 2. Preparation of the test product: Mix 30 g of the granules obtained in this embodiment and 100 ml of water evenly to obtain a suspension, place it in an ordinary refrigerator for refrigerated storage (4° C.), take it out and place it at room temperature 1 hour before the test administration. That is, the granule test product is obtained;

[0053] 3, animal grouping, by random principle, 30 mice are divided into 3 groups at random, i.e. blank control group, contrast group (clomipramine) and test group (the granule tested product that this embodiment obtains), each Group 10.

[0054] 4. Animal administration route and dosage: Administration method: animal...

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Abstract

The invention provides a drug with a neuroprotective effect and application of the drug. The drug is theaflavin-3'-gallate, and a structure of the drug is shown as a formula (I). A compound of the formula (I) has obvious effects on depressive neurosis, the antidepressant effect of theaflavin-3'-gallate is mainly realized by increasing the content of 5-HT and DA in brain and increasing the concentration of synaptic cleft neurotransmitter, and theaflavin-3'-gallate has obvious relieving and therapeutic effects on nervous tension symptoms. The theaflavin-3'-gallate further has a good curative effect on cardiac neurosis.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a medicine with neuroprotective effect and application thereof, and more specifically relates to a theaflavin-3'-gallate or a pharmaceutical derivative thereof and application thereof. Background technique [0002] Gallic acid is also known as "gallic acid" and "gallic acid". The scientific name is "3,4,5-trihydroxybenzoic acid". Molecular formula C 7 h 6 o 5 . Widely present in plants such as Rhubarb palmatum, Eucalyptus eucalyptus, and dogwood, it is a polyphenolic compound that exists in nature and has a wide range of applications in the fields of food, biology, medicine, and chemical industry. Theaflavin-3'-gallate is a main monomer of theaflavins in black tea, and it is also one of the main indicators of the color and flavor of black tea soup. The existing literature shows that theaflavins have various pharmacological and health functions, such as lowering ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61P25/00A61P25/24
CPCA61K31/353A61P25/00A61P25/24
Inventor 冯莹刘颖于成龙任春娜杨雪琦郭玲
Owner MUDANJIANG MEDICAL UNIV
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