Flavonoid compounds existing in millettia pachycarpa and capable of inhibiting AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) and application of flavonoid compounds

A technology of flavonoids and compounds, applied in the field of medicine, can solve problems such as the application of anti-senile dementia has not yet been reported

Inactive Publication Date: 2017-06-30
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

And some of the isoflavones have good anti-estrogen-like effects, cytotoxicity and activity of inducing tumor cell apoptosis, but the cholinesterase inhibitory activity of the plant and the isolated compound and its role in anti-senile dementia Apps in have not been reported yet

Method used

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  • Flavonoid compounds existing in millettia pachycarpa and capable of inhibiting AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) and application of flavonoid compounds

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Experimental program
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Embodiment 1

[0027] Embodiment 1: the method for the extraction, separation, purification of 3 compounds of the present invention:

[0028] (1) Take 4.5kg of the seeds of Spathiphyllum sagittata, crush them and place them in a heat reflux device, immerse the medicinal materials in 95% ethanol, heat and reflux with an electric heating mantle for extraction, 3 hours each time, and extract 3 times.

[0029] (2) Concentrating the ethanol extract in vacuo, recovering ethanol, and obtaining an ethanol concentrate.

[0030] (3) Dilute the ethanol concentrate with an appropriate amount of water, and extract the resulting suspension with petroleum ether. The extraction adopts the principle of a small amount and multiple times. For the first time, half the volume of petroleum ether in the aqueous solution is used for extraction, and then the amount of petroleum ether is gradually reduced until the color of the petroleum ether layer is very light. The emulsified layer during the extraction process is...

Embodiment 2

[0045] Embodiment 2 compound is to the in vitro inhibitory activity of cholinesterase

[0046] According to the literature and the optimized screening model for cholinesterase inhibitors, the activity of the compounds isolated from Fructus Palismanthus was tested, and it was found that the compounds had high inhibitory activity, and their activities are shown in Table 1.

[0047] Table 1 Compounds inhibit AChE and BChE activities in vitro

[0048] Compound number IC 50 for AChE ( mu M)

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Abstract

The invention belongs to the technical field of medicine and particularly relates to flavonoid compounds separated from millettia pachycarpa as a leguminous plant and having AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) inhibiting activity, pharmaceutical salts of the flavonoid compounds and pharmaceutical composition containing the compounds. The three flavonoid compounds have a remarkable inhibiting effect on AChE and BuChE and show unique advantages in preventing and treating learning and memory disorder and senile dementia diseases.

Description

technical field [0001] The invention relates to the technical field of medicine. Specifically, the present invention relates to 3 kinds of flavonoid compounds with strong acetyl and butyrylcholinesterase inhibitory activity isolated from the leguminous plant Thuja japonica and pharmaceutically acceptable salts thereof, as well as the pharmaceutical composition. It 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) is a progressive neurodegenerative disorder, clinically manifested as deteriorating cognitive and memory functions, progressive decline in daily life ability, and various neuropsychiatric symptoms and behavioral disorders . The disease is mostly a primary disease of the brain, with a slow onset, progressive course, and a family history. It is the most common disease that causes dementia in the elderly. The most prominent neuropathohistological f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/58C07D493/04A61K31/352A61P25/28A23L33/105
Inventor 李延芳屠言贝
Owner SICHUAN UNIV
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