A kind of cyclopentenone compound and its preparation method and application

The technology of cyclopentenone and compound is applied in the application field of preparing medicine for treating Alzheimer's disease, can solve the problems such as no medicine, and achieve the effect of strong anti-oxidation

Active Publication Date: 2020-06-16
NINGBO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are no reports on the chemical structure of this compound and its antioxidant and anti-neurotoxic activity, so there are no related drugs on the market

Method used

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  • A kind of cyclopentenone compound and its preparation method and application
  • A kind of cyclopentenone compound and its preparation method and application
  • A kind of cyclopentenone compound and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A cyclopentenone compound structural formula is shown in I,

[0030]

[0031] Formula I.

Embodiment 2

[0033] The preparation method of the cyclopentenone compound shown in I formula specifically comprises the steps:

[0034] (1) Fermentation production

[0035] Trichoderma ( Trichoderma sp.) was revived by streaking, inoculated on PDA solid medium (potato extract 8.0 g, glucose 20 g, distilled water 1 L, sea crystal 35 g, agar 20 g), and cultured in a 28°C incubator for 5 days; The colonies obtained from PDA solid medium were inoculated into 1000 mL Erlenmeyer flasks of PDB liquid medium (8.0 g of potato extract, 20 g of glucose, 1 L of distilled water, and 35 g of sea crystal). A total of 270 flasks were inoculated. , 125 rpm, shaker fermentation culture for 14 days to obtain the fermentation liquid;

[0036] (2) Obtaining the extract

[0037] Extract the fermentation broth with equal volume of ethyl acetate for 3 times, take the extract and concentrate under reduced pressure to remove the ethyl acetate to obtain the crude extract of the bacterial liquid; soak the extract...

Embodiment 3

[0047] Test for neurotoxic activity

[0048] (1) Experimental samples

[0049] Preparation of test sample solution: The test sample is the pure compound I isolated and purified in Example 2 above, and an appropriate amount of sample is accurately weighed for activity test. The indicator cells used in this experiment are SH-SY5Y nerve cells.

[0050] experimental method

[0051] 1. The antioxidant properties of compound Ⅰ were determined by DPPH free radical scavenging assay. Drugs at various concentrations were added to DPPH in methanol (0.2 mM). Add the mixture (200 μL / well) to the 96-well plate and shake at room temperature for 20 min. Absorbance was measured at 517 nm with a microplate reader. Vitamin C was used as a positive control. The DPPH radical scavenging activity was calculated using the following formula: DPPH radical scavenging activity (%)=[(absorbance of control−absorbance of sample) / absorbance of control]×100.

[0052] 2. Aβ fibrillation was analyzed by ...

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PUM

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Abstract

The invention discloses a cyclopentenone compound, a preparation method and application thereof. The cyclopentenone compound is characterized by having a structural formula shown as I. The preparation method includes the steps of: conducting fermentation culture on marine fungus Trichoderma sp. with a preservation number of 12969 to acquire a fermentation broth containing a new cyclopentenone compound, then extracting the fermentation broth with ethyl acetate to obtain a crude extract, subjecting the extract to pressure reduced silica gel column chromatography, and finally carrying out reversed phase semi-preparative high performance liquid chromatography separation and purification, thus obtaining the cyclopentenone compound. The cyclopentenone compound can be used in preparation of drugs for treatment of Alzheimer's disease, and has the advantages of strong antioxidation, anti-Abeta fibrillation, oligomerization properties and neuroprotective effect.

Description

technical field [0001] The invention relates to a cyclopentenone compound, in particular to a method for preparing the cyclopentenone compound with marine fungi and the application of the compound in the preparation of drugs for treating Alzheimer's disease. Background technique [0002] With the average life expectancy of the world's population increasing year by year, the world is gradually entering an aging society, so research on senile diseases and their drug treatment has attracted much attention. Alzheimer's disease (AD for short) is a degenerative disease of the central nervous system that occurs in old age and early old age, mainly with progressive cognitive impairment and memory impairment, accompanied by personality changes and behavior changes. Statistics show that the survival period of AD patients is expected to reach 20 years, but most cases can only survive 8 to 10 years after diagnosis, and it has become the fourth killer of human beings. [0003] Drug ther...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C49/707C12P7/26A61P25/28A61P39/06C12R1/885
CPCC07C49/707C12P7/26
Inventor 何山丁立建崔魏严小军王钦文方芳赵佳颖
Owner NINGBO UNIV
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