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Use and preparation method of pinosylvi

A technology of silver pinesin and its use, which is applied in the field of use and preparation of silver pinesin, can solve problems such as undiscovered, and achieve the effect of strong nerve inhibition

Inactive Publication Date: 2019-05-17
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, so far, other more efficient and precise targets and mechanisms of silver pinesin have not been discovered, and studies have found that silver pinesin has a certain inhibitory effect on neural activity

Method used

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  • Use and preparation method of pinosylvi
  • Use and preparation method of pinosylvi
  • Use and preparation method of pinosylvi

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The invention provides a kind of preparation method of silver pinesin, the preparation reaction formula is:

[0034]

[0035] 1-(2-(3,5-dimethoxyphenyl)ethynyl)benzene 0.2mmol, 47.6mg, bis(1,5-cyclooctadiene) iridium(I) chloride dimer 0.005mmol , 4.2mg, 0.04mmol and 15.9mg of 1,2-bis(diphenylphosphine)ethane were added to a 15ml pressure-resistant tube under nitrogen protection, then EtOH 4mmol, 232mL and THF1.5mL were added, and the reaction solution was heated at 120°C Stir for 24 hours. After the reaction is complete, cool to room temperature and add 10ml of ethyl acetate to dilute.

[0036] The reaction mixture was washed 3 times with saturated brine, the organic phase was extracted with ethyl acetate, the organic phase was dried over anhydrous sodium sulfate, and the crude product was concentrated under reduced pressure and purified by column chromatography (ethyl acetate / petroleum ether=1 / 4) to obtain E- 1,2-bis(4-methoxyphenyl)vinyl)benzene, white solid 38 mg...

Embodiment 2

[0043] The present invention also provides a use of silver pinesin prepared by the preparation method described in Example 1 for the preparation of antipsychotic drugs. The following specific experimental procedures are used to verify the inhibitory effect of silver pinesin and its crystals on nerve activity.

[0044] In this experiment, the blank control group was zebrafish E3 culture medium, and the other control group was the antidepressant drug phenelzine sulfate, which was diluted with E3 culture medium (1g / ml, 0.1g / ml, 0.01g / ml). Solution E3 was diluted to prepare different concentrations of silver permethrin (1g / ml, 0.1g / ml, 0.01g / ml, note: if insoluble, add a little DMSO, not more than 0.5%). Embryos of the transgenic zebrafish line Tg(hb9:gfp) were collected and screened under a microscope to remove individuals with abnormal morphology. Add approximately 10 healthy embryos to wells of a 96-well plate containing E3 solution.

[0045] At 6hpf, remove the E3 culture med...

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PUM

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Abstract

The invention provides use and preparation method of pinosylvin. The pinosylvin is used for preparing a medicine for inhibiting nerve activity, and is also used for preparing an antipsychotic drug. Itis found through the study of the pinosylvi that the pinosylvi has a strong function of blocking the activation of a nerve signal transduction system, and further experiments prove that the pinosylvicrystal can be specifically combined with a neuron and a strong neural inhibition effect occurs.

Description

technical field [0001] The present invention relates to the application and preparation method of silver pinesin for nerve suppression, in particular to the application of silver pinesin (trans-3,5-dihydroxy stilbene) in the field of antipsychotics. Background technique [0002] Pinosylvin is a derivative of natural trans-1,2-stilbene, which appears in wood pulp of pine and eucalyptus, tea oil and herbal medicine, and is a stilbene. [0003] Due to the very similar molecular structure and properties of silver loosenine derivatives, it is very difficult to purify silver loosenine in the experiment. At present, there is no extensive pharmacological research on silver loosenine. Aldehydration, so it has a good antioxidant effect, which is supported by a large number of studies. Other derivatives of stilbene, such as resveratrol, have been extensively studied in pharmacology, and are hot spots in the research and development of various antioxidant products. Silver pine has ver...

Claims

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Application Information

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IPC IPC(8): A61K31/05A61P25/00C07C37/055C07C39/21
Inventor 龚胜男孙斐王成牛顾明星王小蓉王贵栓吴小龙杨锦飞
Owner NANTONG UNIVERSITY
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