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Polybenzyl derivative and its pharmaceutical composition, its preparation method and its application

A compound, Gastrodia elata technology, applied in the preparation of sugar derivatives, drug combinations, preparation of organic compounds and other directions, can solve the problems of reports, no biological activity, no reports of polybenzyl derivatives, etc.

Active Publication Date: 2021-12-10
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

[0003] There is no report about polybenzyl derivatives 1-12 in the prior art, nor is there any report about its biological activity

Method used

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  • Polybenzyl derivative and its pharmaceutical composition, its preparation method and its application
  • Polybenzyl derivative and its pharmaceutical composition, its preparation method and its application
  • Polybenzyl derivative and its pharmaceutical composition, its preparation method and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Compound 1-6 separation and purification:

[0027] Partial extraction and separation from ethyl acetate of Gastrodia elata. Fresh Gastrodia elata (45.0kg) slices were soaked in 90% ethanol for three times, filtered, the residue was soaked in 50% ethanol for three times and filtered, the residue was boiled once, all the filtrates were combined, and concentrated under reduced pressure until alcohol-free. Extract with ethyl acetate 3 times, obtain ethyl acetate extraction part (102g), water phase is through macroporous resin, water, 50% ethanol and 90% elution respectively, obtain water part (1.6kg), 50% ethanol (71g ), 90% (8g). Mix 88g of sample with 88g of silica gel, and use 880g of silica gel for wet packing. with EtOAc:CHCl 3 The system was eluted at 0:100, 5:95, 10:90, 20:80, 40:60, and MeOH, and 5 fractions were obtained. Guided by activity tracking, the active part and the inactive part were separated and purified, as shown in the table 2 is the test results o...

Embodiment 2

[0060] Compounds 1-12 on melatonin receptor MT 1 and MT 2 Agonistic activity of the receptor.

[0061] 1 Materials and methods

[0062] 1.1 Materials:

[0063] 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.

[0064] 1.2 Instrument: CO 2 Constant temperature incubator Thermo Forma 3310 (USA); Inverted biological microscope XD-101 (Nanjing); Flexstation 3 Benchtop Multi-Mode Microplate Reader (Molecular Devices, Sunnyvale, California, USA).

[0065] 1.3 Experimental process

[0066] 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 cell...

preparation Embodiment

[0076] 1. Compound 1-12 was prepared according to the method of Example 1. After dissolving with a small amount of DMSO, water for injection was added as usual, finely filtered, potted and sterilized to make an injection.

[0077] 2. Compound 1-12 was prepared according to the method of Example 1. After dissolving with a small amount of DMSO, it was dissolved in sterile water for injection, stirred to dissolve, filtered with a sterile suction filter funnel, and then sterile finely filtered. Packed in ampoules, freeze-dried at low temperature and sealed aseptically to obtain powder injection.

[0078] 3. According to the method of Example 1, the compound 1-12 was firstly prepared, and the excipient was added according to the weight ratio of the compound 1-12 to the excipient at a ratio of 9:1 to make a powder.

[0079] 4. According to the method of Example 1, the compound 1-12 was firstly prepared, and the excipient was added according to the weight ratio of the compound 1-12 t...

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Abstract

The present invention provides the polybenzyl derivative (1‑12) represented by structural formula (I) or its pharmaceutical composition, its preparation method, its application in the preparation of melatonin receptor agonist, and its preparation in the treatment or Use in drugs for the prevention of diseases of the central nervous system associated with melatonin receptors.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to derivatives (1-12) of phenolic compound polybenzyl (1-12) or pharmaceutically acceptable salts thereof and pharmaceutical compositions thereof, which are used as melatonin receptor agonists, and are used in the preparation of treatment or prevention of melatonin Drug application in the central nervous system diseases related to hormone receptors. 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 oxindo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C43/23C07C43/178C07C41/34C07C213/00C07C215/76C07C319/14C07C323/20C07H1/00C07H15/203A61K31/085A61K31/075A61K31/136A61K31/10A61K31/7034A61P25/00
Inventor 陈纪军陈思月耿长安马云保黄晓燕张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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