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Application of catechin in preparing medicines for treating central nervous system disease

A technology of central nervous system and catechins, applied in nervous system diseases, drug combinations, pharmaceutical formulations, etc., can solve problems such as depression without its treatment or prevention

Inactive Publication Date: 2018-12-04
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the prior art has no report on the application of catechin (1) and its pharmaceutical composition as a melatonin receptor agonist, and the treatment or prevention of central nervous system diseases related to melatonin receptors, nor its application. Reports of treatment or prevention of depression

Method used

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  • Application of catechin in preparing medicines for treating central nervous system disease
  • Application of catechin in preparing medicines for treating central nervous system disease
  • Application of catechin in preparing medicines for treating central nervous system disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Preparation of compound 1:

[0025] Take the dried hooked stems or leaves of Uncaria rhynchophylla, crush them, and extract twice with 90% ethanol under reflux, each time for 3 hours, combine the ethanol extracts, recover the ethanol under reduced pressure to obtain the extract, and dissolve the extract with 80% ethanol Adsorbed on silica gel, placed at room temperature to evaporate the solvent, crushed and sieved, and subjected to silica gel column chromatography, sequentially eluted with chloroform and 9:1 chloroform-methanol gradient, and the 9:1 chloroform-methanol eluted part continued to pass through the silica gel column Chromatography, with petroleum ether-acetone 1:1 isocratic elution, to obtain 4 components A-D, component B was prepared by MCICHP-20P gel column medium pressure, 20:80 to 80:20 acetonitrile-water gradient elution , to obtain 5 fractions C-1 ~ C-5, C-2 through Rp-C 18 The column was prepared by HPLC, eluted isocratically with acetonitrile-water ...

Embodiment 2

[0038] Compound 1 on melatonin receptor MT 1 and MT 2 Agonistic activity of the receptor.

[0039] 1 Materials and methods

[0040] 1.1 Materials:

[0041] melatonin receptor MT 1 and MT 2 The cell lines used for agonistic activity screening correspond to human kidney epithelial cells HEK293-MT 1 and HEK293-MT 2 ; Cell culture medium (Dulbecco's Modified Eagle Medium, DMEM) containing 10% fetal bovine serum; No-wash calcium flow kit.

[0042] 1.2 Instrument: CO 2 Constant temperature incubator Thermo Forma 3310 (USA); Inverted biological microscope XD-101 (Nanjing); Flexstation 3Benchtop Multi-Mode Microplate Reader (Molecular Devices, Sunnyvale, California, USA).

[0043] 1.3 Experimental process

[0044] Coat the 96-well black-walled transparent-bottom cell culture plate with the substrate BD Matrigel, put it in a constant temperature incubator at 37°C for 1 hour, absorb the supernatant, and dilute it with 4×10 4 Density per well, the corresponding HEK293 cells wer...

Embodiment 3

[0050] Effects of compound 1 on behavioral animal models related to depression

[0051] 1 Materials and methods

[0052] 1.1 Materials: Fluoxetine hydrochloride (Sarn Chemical Technology Co., Ltd., Shanghai, China); agomelatine (Sarn Chemical Technology Co., Ltd., Shanghai, China). Sodium carboxymethylcellulose 800-1200 (Sinopharm Group, Shanghai, China). Kunming mice 18-20 g (Beijing Huafukang Biotechnology Co., Ltd., Beijing, China), license number: SCXK (Beijing) 2014-0004.

[0053] 1.2 Method: The mice were divided into random groups, 10 in each group, and measured after 5 consecutive days of administration. Spontaneous activities mice were put into the bottom center of a black dark box with a length, width and height of 24x24x40cm, and the ANY-maze automatic collection system (Anymaze, Stoelting Co., Wooddale, USA) was used to record for 6 minutes, and the time was 5 minutes and 30 seconds after analysis. The number of crossings and the total distance traveled by the m...

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Abstract

The invention provides an application of catechin (1) shown as a structural formula (I) or pharmaceutical thereof and a pharmaceutical composition thereof in preparing a melatonin receptor agonist, anapplication thereof in preparing medicines for preventing or treating central nervous system disease related to melatonin receptor, and an application in preparing medicines for preventing or treating depression.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to catechin (1) or its pharmaceutically acceptable salts and pharmaceutical compositions thereof, which are used as melatonin receptor agonists, and are used in the preparation of treatment or prevention of central nervous system diseases related to melatonin receptors application in medicines. Background technique [0002] Melatonin (N-acetyl-5-methoxytryptamine, Melatonin) is an amine hormone mainly produced by the pineal gland in the human body. It was first isolated from bovine pineal tissue by Lerner et al. in 1958. The production of melatonin is mainly through the conversion of L-tryptophan into 5-hydroxytryptamine in pineal cells, and then generates N-acetyl 5-hydroxytryptamine under the action of N-acetyltransferase (AA-NAT), and finally in 5-hydroxytryptamine. Melatonin is produced by the enzyme oxindoleoxymethyltransferase (HIOMT). Melatonin receptors are...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/353A61P25/00A61P25/24
CPCA61K31/353A61K36/74A61P25/00A61P25/24
Inventor 陈纪军耿长安杨通华黄晓燕马云保张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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