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Monomer components having selective butyrylcholinesterase inhibitory effect in Bletilla striata (Thunb)Reichb.f. and application thereof

A way, the technology of medicinal salt, applied in the field of medicine

Active Publication Date: 2018-06-22
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Recently, we have extracted and separated several phenanthrene and dihydrophenanthrene compounds with strong selective butyrylcholinesterase inhibitory effect from Radix Bletifera. see the report

Method used

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  • Monomer components having selective butyrylcholinesterase inhibitory effect in Bletilla striata (Thunb)Reichb.f. and application thereof
  • Monomer components having selective butyrylcholinesterase inhibitory effect in Bletilla striata (Thunb)Reichb.f. and application thereof
  • Monomer components having selective butyrylcholinesterase inhibitory effect in Bletilla striata (Thunb)Reichb.f. and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: the method for the extraction, separation, purification of all compounds of the present invention:

[0031] 1.1 Plant source and identification:

[0032] In July 2015, it was purchased at the Hehuachi Medicinal Materials Market in Chengdu. It was identified as Baiji by Mr. Liu Wenbin, School of Chemical Engineering, Sichuan University. Bletilla striata(Thunb) The tuber of Reichb. f.

[0033] 1.2 Extraction and separation of Baiji medicinal materials and structural identification of compounds

[0034] (1) Take 2 kg of Baiji medicinal material, crush it into a coarse powder, and heat extract it with 95% ethanol at 50 °C. The amount of ethanol is 5 times the weight of the medicinal material. The extraction time is 24 h each time, and the extraction times are 5 times.

[0035] (2) Filter the extract and combine the filtrates. Concentrate under reduced pressure below 45 ℃ to form an extract.

[0036] (3) Use a small amount of distilled water to suspend the ...

Embodiment 2

[0069] Embodiment 2: In vitro inhibitory activity detection of compound 1-12 to cholinesterase

[0070] 12 phenanthrene and dihydrophenanthrene compounds used for activity detection are shown in Table I:

[0071] Table 1 Compounds isolated from EtOAc parts of Bletilla striat

[0072]

[0073]

[0074] According to the literature and optimized screening model for acetyl and butyrylcholinesterase inhibitors, the cholinesterase inhibitory activity of compounds 1-12 was tested, and all 12 compounds showed strong butyrylcholinesterase inhibitory activity . Its activity data are shown in Table II:

[0075] Table 2 The cholinesterase inhibitory activity of 12 compounds isolated from Bletilla striata in vitro.

[0076]

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Abstract

The invention belongs to the field of medicine science and technology, and particularly relates to monomer compounds having selective butyrylcholinesterase inhibitory activity obtained by performing separation from orchidaceae Bletilla striata (Thunb)Reichb.f. and medicial salt thereof, and a pharmaceutical composition containing the compounds. The 12 compounds disclosed by the invention have selective inhibitory effects on butyrylcholinesterase to different extents, and IC50 values of five of the 12 compounds are smaller than 10 micrometers, so that a powerful butyrylcholinesterase inhibitoryeffect is shown, and a unique advantage of the compounds in treatment of senile dementia diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the extraction and separation of natural product active ingredients and its application. The present invention relates to a variety of phenanthrene and dihydrophenanthrene compounds with strong selective butyrylcholinesterase inhibitory activity and their pharmaceutically acceptable salts, as well as pharmaceuticals containing these compounds, which are isolated from Orchidaceae Radix. pharmaceutical composition. They can be expected to be used in the prevention and treatment of learning and memory impairment and senile dementia. Background technique [0002] Alzheimer's disease (AD) occurs in old age and pre-senile age, and is a progressive neurodegenerative disease characterized by behavioral impairment and progressive cognitive impairment. Since there is no effective method to cure and control the progress of the disease, AD has become an important disease that threatens th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C43/23C07C43/295C07C41/34A61P25/28
CPCC07C43/23C07C43/295
Inventor 李延芳康允尧朱超
Owner SICHUAN UNIV
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