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Usnic acid derivatives, preparation method thereof and application thereof in preparation of anti-senile dementia drugs

A derivative, the technology of usnic acid, applied in the application field of usnic acid derivatives and its preparation, preparation and treatment of anti-senile dementia drugs, which can solve problems such as stupor and sluggishness of organisms

Active Publication Date: 2020-04-28
WUYI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when acetylcholinesterase is excessive, AchE inhibits the spontaneous discharge of dopaminergic cells in the substantia nigra, causing the organism to act sluggishly and stupor, thereby causing Alzheimer's symptoms

Method used

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  • Usnic acid derivatives, preparation method thereof and application thereof in preparation of anti-senile dementia drugs
  • Usnic acid derivatives, preparation method thereof and application thereof in preparation of anti-senile dementia drugs
  • Usnic acid derivatives, preparation method thereof and application thereof in preparation of anti-senile dementia drugs

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Embodiment 1

[0028] A method for preparing usnic acid derivatives derived from deep-sea fungi. The usnnic acid derivatives are isolated from the fermented extract of Ochroconis sp. FS449 derived from deep-sea. The deep-sea fungus Ochroconis sp.FS449 is isolated from Indian Ocean deep-sea sediments.

[0029] The deep-sea fungus Ochroconis sp. FS449 was deposited in the Guangdong Provincial Microbial Culture Collection Center (GDMCC) on October 29, 2019, with a preservation number of GDMCC: 60825 and a classification name of Ochroconis sp. The address of the preservation unit is: 5th Floor, Building 59, Compound, No. 100 Xianlie Middle Road, Guangzhou City.

[0030] The concrete preparation method of described usnic acid derivative is as follows:

[0031] 1) Seed solution culture of the deep-sea fungus Ochroconis sp.FS449: insert the deep-sea fungus Ochroconissp.FS449 into the seed medium, and cultivate it in a shaker at a rotation speed of 120rpm at 28°C for 5 days to obtain a seed culture...

Embodiment 2

[0049] Compound 1-4 inhibitory activity test experiment of acetylcholinesterase.

[0050] Use thioacetylcholine and DTNB (5,5'-dithiobis(2-nitrobenzoic acid)) as substrates to prepare thioacetylcholine standard products in PBS, prepare 1mM compound 1-4 standard solutions with DMSO, and prepare 1mM compound 1-4 standard solutions with DMSO Dilute to different concentrations of 0.1mM, 0.05mM, 0.01mM, prepare 15mM thioacetylcholine and 15mM DTNB solutions with PBS and a small amount of EDTA, respectively. 10 μL of compounds at different concentrations were added to a mixture of 0.8 μL of acetylcholinesterase (1.0 U / mL) dissolved in PBS and 10 μL of 15 mM DTNB, and incubated at 37° C. for 2 minutes. Add 10 μL of 15 mM thioacetylcholine, incubate at 37°C for 20 minutes, add 1% SDS to terminate the reaction, measure the absorbance at 410 nm with a microplate reader (Thermo Scientific, Multiskan GO), and calculate the inhibition rate. 1 mM neostigmine methosulfate (Shanghai McLean B...

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Abstract

The invention discloses usnic acid derivatives as well as a preparation method and application thereof in preparation of anti-senile dementia drugs. It is reported for the first time that the usnic acid derivatives have acetylcholin esterase inhibition activity. The structural formulas of the usnic acid derivatives (compounds 1-4) are shown as formulas 1-4. The compounds 1-4 have relatively good activity of inhibiting acetylcholin esterase; IC50s of the compounds are 51.0 + / -9.3 mu M, 50.0 + / -2.1 mu M, 50.0 + / -8.6 mu M and 75.0 + / -1.3 mu M respectively, and the compounds can be used for preparing acetylcholin esterase inhibition drug lead compounds in the later period through structural modification optimization. Therefore, the usnic acid derivatives derived from deep sea fungi have the clinical application potential of preventing and treating senile dementia.

Description

technical field [0001] The invention belongs to the technical field of natural medicines, and in particular relates to a kind of usnic acid derivatives derived from deep-sea fungi, a preparation method thereof and an application in preparation of anti-senile dementia medicines. Background technique [0002] With the improvement of people's living standards and changes in diet structure, more and more people suffer from cardiovascular diseases. With the continuous increase in the proportion of the elderly population in our country, there are more and more patients with dementia, which has caused serious inconvenience to the happy life of the elderly and the work and life of their children. Therefore, the development of new anti-senile dementia drugs is very important for improving the quality of life of the elderly and promoting the pension security work in our country. [0003] Acetylcholinesterase (AchE) is a key enzyme in biological nerve transmission. In cholinergic syna...

Claims

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Application Information

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IPC IPC(8): C07D307/91A61P25/28C12P17/04C12R1/645
CPCC07D307/91A61P25/28C12P17/04
Inventor 章卫民陈书帅李冬利刘昭明叶伟李赛妮刘洪新李浩华许丽琼
Owner WUYI UNIV
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