Labdane diterpenoid compounds, arborvitae seed extract, preparation method thereof and application thereof

A kind of technology of diterpenoids and compounds, applied in the field of helichanoid diterpenoids

Active Publication Date: 2012-10-24
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are few reports on the use of the extract of Boziren in neurodegenerative diseases

Method used

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  • Labdane diterpenoid compounds, arborvitae seed extract, preparation method thereof and application thereof
  • Labdane diterpenoid compounds, arborvitae seed extract, preparation method thereof and application thereof
  • Labdane diterpenoid compounds, arborvitae seed extract, preparation method thereof and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Embodiment 1: Preparation of Cypress Kernel Extract

[0045] Get the cypress kernels, mash them, and remove the cypress kernel oil by supercritical carbon dioxide extraction. Add 95% ethanol to the medicinal residues for extraction, add 10 times the volume of 95% ethanol each time, heat and reflux for extraction, recover the solvent from the extract to obtain an extract, and the relative density is above 1.20; dissolve the extract in water, extract 3 times with ethyl acetate, After the ethyl acetate extract, the solvent is recovered to obtain the terpenoid extract of Semen japonicus. The diterpenoid monomer compound of Baiziren is separated and obtained by column chromatography.

Embodiment 2

[0046] Example 2: Cypress seed extract and terpenoid anti-PD model cell experiment

[0047] Get the cypress kernel extract and cypress kernel diterpenoids in the above embodiment 1 to carry out the experiment

[0048] PC12 cells (rat adrenal pheochromocytoma cell line), which have many similar characteristics with dopaminergic neurons, were cultured in DMEM medium (containing 5% horse serum, 5% fetal bovine serum, 100U / mL penicillin, 100g / mL streptomycin), placed at 37°C, saturated humidity, containing 5% CO 2 cultured in an incubator. Change the medium every 2-3 days, and subculture when the cells grow to 70-80% full. Select the cells with good growth condition in the logarithmic growth phase and divide them into 1~5×10 5 were inoculated into 96-well culture plates, 100 μl per well. After incubating at 37°C for 24 hours, after the cells adhered to the wall, the model group was added with MPP + Medium, the experimental group was added containing MPP + and different conc...

Embodiment 3

[0054] Example 3: Anti-nematode AD model experiment of cypress kernel extract and cypress kernel diterpenoids

[0055] Get the cypress kernel extract and the cypress kernel diterpenoid compound in the above embodiment 1 to carry out the experiment.

[0056] The Caenorhaditis elegans transgenic strain CL4176 (temperature-induced expression of Aβ protein) was synchronized and cultured at 15°C until the L1 phase, and then added to the coated OP50 culture dish mixed with different concentrations of extraction drugs Among them, there are about 25 strips in each dish, and there are three plates in each group. After culturing at 15°C for 12 hours, the temperature was changed to 26°C for culturing. Count the paralysis of nematodes after 36 hours of warming, and count every 3 hours until all the nematodes are paralyzed. The results are shown in the table below, both the extract of Cypress Seed and the diterpenoids of Cypress Seed can significantly delay the paralysis of CL4176 nemato...

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Abstract

The invention provides a plurality of labdane diterpenoid compounds and derivatives thereof, which can be used for preparing pharmaceutical composition for preventing or treating neurodegenerative diseases. The invention also provides an arborvitae seed extract, the arborvitae seed extract contains one or more labdane diterpenoid compounds and the derivatives, and can be used for preparing pharmaceutical composition for preventing or treating neurodegenerative diseases.

Description

technical field [0001] The present invention relates to a helianthene-type diterpenoid compound, Semen boitae extract, a preparation method and application thereof. Background technique [0002] Neurodegenerative diseases (Neuro degenerative diseases, NDD) are a class of chronic, progressive neurological diseases, mainly including Alzheimer's disease (Alzheimer's disease, AD), Parkinson's disease (Pakinson's disease, PD), Huntington's disease (Huntington's disease) , HD), amyotrophic lateral sclerosis (Amyotuophic laterals clerosis, ALS) and so on. These diseases have complex pathophysiological processes, with different lesion sites and etiologies, but neurodegeneration is their common denominator. Patients with neurodegenerative diseases often have symptoms such as memory loss, cognitive difficulties, dementia, movement balance disorders, and loss of motor ability. The quality of life of patients is seriously reduced. economic and psychological stress. As the global popu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/60C07D307/58C07D307/28C07D307/20C07C61/35C07C62/32C07C62/36C07C62/38C07C51/42A61K31/365A61K31/341A61K31/19A61K31/194A61K36/14A61P25/28A61P25/16A61P25/14A61P25/00
CPCY02P20/54
Inventor 苏薇薇王永刚梁凤银王宁裴中刘海滨
Owner SUN YAT SEN UNIV
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