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A class of compounds derived from forsythia, its preparation method and its application in the prevention and treatment of Parkinson's disease

A compound and composition technology, applied in the field of medicine, can solve the problems of Parkinson's disease of traditional Chinese medicine Forsythia suspensa and the patent documents of preparation method of monomeric forsythia compound, etc., and achieve the inhibition of neuroinflammatory response and structure of microglia. Novel, inhibitory effect on induced neurotoxicity

Active Publication Date: 2019-01-01
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research report on the use of the traditional Chinese medicine Forsythia for the treatment of Parkinson's disease, and there is no patent document on the preparation method of the Forsythia compound monomer with PC12 cell protection

Method used

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  • A class of compounds derived from forsythia, its preparation method and its application in the prevention and treatment of Parkinson's disease
  • A class of compounds derived from forsythia, its preparation method and its application in the prevention and treatment of Parkinson's disease
  • A class of compounds derived from forsythia, its preparation method and its application in the prevention and treatment of Parkinson's disease

Examples

Experimental program
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Effect test

Embodiment 1

[0038] 10kg of forsythia medicinal material was reflux extracted with 20L of 70% ethanol solvent for 3 times, each time for 2 hours, the extract was concentrated to obtain 1.4kg of extract, the density of the extract was adjusted to 1.10 with distilled water, and 2L of petroleum ether was used in turn , chloroform, ethyl acetate and n-butanol were extracted 3 times successively, and the n-butanol part reclaimed the solvent to obtain 450 g of medicinal extract, which was dispersed and dissolved in distilled water (4L), and the supernatant was passed through a D101 type macroporous adsorption resin with a filling volume of 10L. Use water, 15% ethanol, 30% ethanol, 50% ethanol, 95% ethanol gradient (20L) for elution, collect the 50% ethanol elution fraction, recover the solvent and go through Sephadex LH-20 gel column chromatography, ODS reverse phase The above compounds forsythoneoside A (30 mg), forsythoneoside B (25 mg), forsythoneoside C (15 mg), and forsythoneoside D (15 mg) ...

experiment example 1

[0051] Effects of Forsythia Compounds on Nerve Cells (PC12) Injury in Vitro

[0052] Take the PC12 cells (simulated neuron cells) that cover a single layer, discard the original culture medium, add DMEM complete culture medium with 5% FBS and 5% horse serum, and blow gently with a pipette to completely disperse the cells. 4 Cells / mL density, 100 μL per well was inoculated in 96 culture plates treated with poly-lysine (0.1 mg / mL) in advance, cultured for 24 hours and then used for experiments. The experiment was divided into blank group, model group and drug-dosed group. The blank group was given complete medium, the rotenone model group was added with a complete medium with a final concentration of 4 μM rotenone to act on the cells for 48 hours (simulated PD model), and the oxygen-glucose deprivation (OGD) group was used with a low-glucose complete medium with a final concentration of 5 mM Sodium dithionite acts on cells for 24h (simulating cerebral ischemia model), Aβ 25-35...

experiment example 2

[0062] Effects of forsythia compounds on the activation of microglial cells (BV2) induced by lipopolysaccharide (LPS) in vitro

[0063] Take the BV2 cells (simulated neuroglial cells) that cover a single layer, discard the original culture medium, add 10% FBS DMEM complete culture medium, and blow gently with a pipette to completely disperse the cells. 5 Cells / mL density, 300 μL per well was inoculated in a 24-well culture plate treated with polylysine (0.1 mg / mL) in advance, and cultured for 24 hours before use in the experiment. The experiment was divided into blank group, model group and drug-dosed group. The blank group was given complete medium, and the LPS model group was given complete medium with a final concentration of 100ng / mL LPS (simulating neuroinflammation model). In the drug-dosing group, 10 μM, 1 μM or 0.1 μM of the test compound was added while modeling. The cells were treated for 24 hours, the cell morphology was observed under a microscope, the supernatan...

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Abstract

The invention relates to a compound with a novel structure in fructus forsythia, a preparation method and application thereof in control of Parkinson's disease. Pharmacological experiments prove that the compound can effectively inhibit rotenone induced PC12 cell damage, improve lipopolysaccharide (LPS) induced microglial cell neuroinflammation reaction and reduce the release of inflammatory factors, has good anti-Parkinson's disease effect, and has an effective dose up to 0.1 micromol / L. The compound can be used for preparation of drugs for control of Parkinson's disease.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a novel compound isolated from Chinese medicine forsythia and its application in preventing and treating Parkinson's disease. Background technique [0002] Parkinson's disease (PD) is the most common neurodegenerative disease characterized by motor dysfunction. The incidence rate of people over 65 years old is 1%. There are about 1.7 million Parkinson's patients in my country. The incidence of the disease increases with the increase of age, and the aggravation of population aging makes the number of patients also show an upward trend year by year. PD is a serious threat to human health, not only brings great pain to patients, but also creates a heavy burden on families and society. At present, there is no effective treatment for the disease, and the commonly used levodopa replacement therapy can only last for about 5 years. With the progress of the disease, the efficacy of le...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/07C07H17/04C07H1/08A61K31/7048A61P25/16
Inventor 陈乃宏张培成宋修云张凡张挽青杨桠楠冯子明姜建双
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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