Application of asterric acids compound in inhibition of activity of acetylcholin esterase

A technology of acetylcholinesterase and compounds, which is applied in the field of medicine and can solve problems not specifically related to the activity of acetylcholinesterase

Inactive Publication Date: 2018-08-07
JIANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing studies have shown that this class of compounds has significant antibacterial activity, but have not specifically addressed the acetylcholinesterase activity of this class of compounds

Method used

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  • Application of asterric acids compound in inhibition of activity of acetylcholin esterase
  • Application of asterric acids compound in inhibition of activity of acetylcholin esterase
  • Application of asterric acids compound in inhibition of activity of acetylcholin esterase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Embodiment 1: In vitro inhibitory activity test of acetylcholinesterase of compound 1

[0016] (1) Drugs and reagents

[0017] Acetylcholinesterase (AChE, Sigma Company), 50mmol / L, pH8.0 phosphate-buffered saline (PBS), 15mmol / L5,5-dithio-2-nitrobenzoic acid (dithiobis-nitrobenzoic acid, DTNB) Solution (Sigma Company) (prepared with 50mmol / L, pH 8.0PBS), 15mmol / L thioacetylcholine (Acetyl thiocholine, ATch, Sigma Company, prepared with 50mmol / L, pH 8.0PBS), 4% lauryl sulfate Sodium (SDS, Sigma Company), positive control Huperzine A (National Institute for the Control of Pharmaceutical and Biological Products), 0.75mol / L MgCl 2 Solution, methanol is analytically pure.

[0018] (2) Experimental method

[0019] Refer to the literature (Zhang Yi, Feng Yan, Li Xiaoming, et al. Research on the inhibition of acetylcholinesterase activity by seaweed components [J]. Ocean and Limnology, 2005,36(5):459-464.) to make appropriate improvements. The reference substance for the de...

Embodiment 2

[0026] Embodiment 2: In vitro inhibitory activity test of acetylcholinesterase of compound 2

[0027] (1) Drugs and reagents

[0028] Acetylcholinesterase (AChE, Sigma Company), phosphate-buffered saline (PBS) at 50mmol / L, pH8.0, 15mmol / L 5,5-dithio-2-nitrobenzoic acid (dithiobis-nitrobenzoic acid, DTNB ) solution (Sigma Company) (prepared with 50mmol / L, pH 8.0PBS), 15mmol / L thioacetylcholine (Acetyl thiocholine, ATch, Sigma Company, prepared with 50mmol / L, pH 8.0PBS), 4% dodecyl Sodium sulfate (SDS, Sigma company), positive control Huperzine A (National Institute for the Control of Pharmaceutical and Biological Products), 0.75mol / L MgCl 2 Solution, methanol is analytically pure.

[0029] (2) Experimental method

[0030] Refer to the literature (Zhang Yi, Feng Yan, Li Xiaoming, et al. Research on the inhibition of acetylcholinesterase activity by seaweed components [J]. Ocean and Limnology, 2005,36(5):459-464.) to make appropriate improvements. The reference substance for ...

Embodiment 3

[0037] Embodiment 3: In vitro inhibitory activity test of acetylcholinesterase of compound 3

[0038] (1) Drugs and reagents

[0039] Acetylcholinesterase (AChE, Sigma Company), phosphate-buffered saline (PBS) at 50mmol / L, pH8.0, 15mmol / L 5,5-dithio-2-nitrobenzoic acid (dithiobis-nitrobenzoic acid, DTNB ) solution (Sigma Company) (prepared with 50mmol / L, pH 8.0PBS), 15mmol / L thioacetylcholine (Acetyl thiocholine, ATch, Sigma Company, prepared with 50mmol / L, pH 8.0PBS), 4% dodecyl Sodium sulfate (SDS, Sigma company), positive control Huperzine A (National Institute for the Control of Pharmaceutical and Biological Products), 0.75mol / L MgCl 2 Solution, methanol is analytically pure.

[0040] (2) Experimental method

[0041] Refer to the literature (Zhang Yi, Feng Yan, Li Xiaoming, et al. Research on the inhibition of acetylcholinesterase activity by seaweed components [J]. Ocean and Limnology, 2005,36(5):459-464.) to make appropriate improvements. The reference substance for ...

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Abstract

The invention belongs to the field of biological medicines, and particularly relates to research of an asterric acids compound for inhibition of activity of acetylcholin esterase as shown in general formula (I). The invention provides application of a compound with the structure as shown in general formula (I) and as an acetylcholin esterase inhibitor.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the application of a kodinate compound in inhibiting the activity of acetylcholinesterase. Background technique [0002] Asterric acid compounds are a class of compounds with a diphenyl ether structure, widely exist in fungal metabolites, and have a wide range of pesticide and pharmaceutical activities. References: Wu Qinglai, Yang Xinling, Ling Yun. Research progress of natural product kodysacid and its analogs[J]. Journal of Pesticide Science, 2012,14(4):353-362. [0003] At present, the reports on kodiic acid and its analogues are mostly derived from the isolation, extraction and biological activity of microbial metabolites. Li Huiling et al. screened the strain 2QR1 with bactericidal activity from the endophytic fungus Euonymus japonicus, and the ethyl acetate extract of the fermentation broth had a significant effect on the mycelial growth and antibacterial activity of p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/235A61P25/28
CPCA61K31/235A61P25/28
Inventor 张志斌朱笃颜日明汪涯肖依文杨慧林江玉梅
Owner JIANGXI NORMAL UNIV
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