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Xylaric acid with neuroprotective activity as well as preparation method and application of xylaric acid

A neuroprotection and compound technology, which is applied in the fields of medicine, microorganisms and compounds, can solve the problems of limited development work, inability to determine the effective chemical components of the mechanism of action of carbonobacteria niger for regulating nerves, and the like, and achieves the effect of rich sources.

Active Publication Date: 2022-04-29
SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current research on the mechanism of action of C. nigriscens on the regulation of nerves is mainly extended from the related targets of previous research on mood disorders (for example, based on the hypothesis of monoamine transmitters, etc.), so far researchers have not been able to To determine the mechanism of action and effective chemical components of C.
The existing technology is very limited in the research on the antidepressant and neuroprotective activity of the chemical constituents of C. nigritiformis, as well as the development of related drugs

Method used

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  • Xylaric acid with neuroprotective activity as well as preparation method and application of xylaric acid
  • Xylaric acid with neuroprotective activity as well as preparation method and application of xylaric acid
  • Xylaric acid with neuroprotective activity as well as preparation method and application of xylaric acid

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Experimental program
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Effect test

Embodiment 1

[0039] The extraction method of embodiment 1 carboxylic acid:

[0040] Xylaria nigripes was collected in Ailao Mountain, Yunnan Province in 2013, and was identified by Professor Dai Yucheng of Beijing Forestry University. The Institute's Medicinal Fungi and Ethnic Medicine Research Group is also the strain reported in the document "Four new resorcinol derivatives with neuroprotective activities from Xylaria nigripes" (Lan-Qing Li, et al. Natural Product Research (2021), DOI: 10.1080 / 14786419.2021.1897591) , see line 5 of Section 3.2 of this document for details. Publicly available for purchase from the research group.

[0041] The preparation method of the above-mentioned strain (No. CGBWSHF00611) is as follows: place the fruiting body of C. nigritiformis in an inoculation box, and disinfect the surface of the mushroom body with 75% alcohol. After sterilizing with a scalpel, cut longitudinally in the middle of the mushroom stalk, cut 5 squares at the mushroom cap and the mushr...

Embodiment 2

[0057] Embodiment 2: The carboxylic acid shown in the formula I prepared in embodiment 1 is tested for the protective effect on nerve cells

[0058] 1. Experimental drugs and reagents

[0059]Cell culture medium RPMI-1640, gas-permeable cell culture flask, 96-well cell culture plate, 24-well cell culture plate, PC12 cells, fetal bovine serum, trypsin, CCK8 kit, penicillin-streptomycin double antibody solution (penicillin working concentration 100U / mL, working concentration of streptomycin is 0.1mg / L), carboxylic acid, amitriptyline, phosphate buffer saline PBS (0.03mol / L, pH=7.2), microporous filter, syringe, Hoechst Staining kit , ethanol, DMSO, 4% paraformaldehyde cell fixative, Triton X-100, 50ml centrifuge tube, 15ml centrifuge tube, EP tube, 1ml tip, 200ul tip, gloves, masks, etc.

[0060] 2. Experimental equipment

[0061] Three-gas incubator, constant temperature incubator, microplate reader, ordinary microscope, fluorescence microscope, centrifuge, high-pressure stea...

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Abstract

The invention relates to the technical field of medical microorganisms and medical compounds, and particularly discloses a compound extracted from a xylaria nigripes rice fermentation product, the compound is named as xylaric acid, the system is named as ((8R, 12R)-9-ethoxy-9-carbonyl-7-phenylpropane-8-substituted)-D-leucine, the preparation method of the compound is disclosed, and the application of the compound in pharmacy is also disclosed. The compound disclosed by the invention has relatively remarkable neuroprotective activity, can be applied to preparation of novel neuroprotective medicines, and is used for treating depression including but not limited to anxiety disorder and improving cognitive impairment and motion retardation of patients with neurodegenerative diseases. The result of the embodiment shows that the xylaric acid provided by the invention can obviously improve the survival rate of the damaged nerve cell PC12 of the model, and has a better inhibition effect on the apoptosis of the nerve cell PC12.

Description

technical field [0001] The present invention relates to the technical fields of medicine, microbes and compounds, in particular to a compound Xylarinic acid extracted from rice fermented product of Xylaria nigripes, its preparation method and its application in the field of pharmacy new use. The compound has remarkable neuroprotective activity and can be used in the preparation of new neuroprotective drugs. Background technique [0002] Natural products refer to the chemical components of animal and plant extracts or the components of animals and microorganisms or their metabolites, mainly including proteins, amino acids, polysaccharides, terpenoids, steroids, phenylpropanoids and other compounds (chemical Progress, 2002, 05, 405-407). Due to the advantages of abundant natural product resources, novel and unique structure, strong biological activity, wide range of targets, and unique mechanism of action, it is widely used in the discovery of active lead compounds and the p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/36C12P13/04C12N1/14A61P25/22A61P25/24A61P25/20C12R1/645
CPCC07C229/36C12P13/04C12N1/14A61P25/22A61P25/24A61P25/20C07B2200/07Y02A50/30
Inventor 王献刘吉开李兰清李静
Owner SOUTH CENTRAL UNIVERSITY FOR NATIONALITIES
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