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Composition for preventing or treating neurodegenerative diseases, containing diterpene-based compound

Inactive Publication Date: 2022-01-20
KOREA RES INST OF BIOSCI & BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a diterpene that can improve the activity of Nurr1 and inhibit inflammation in neurons, making it useful for preventing or treating neurodegenerative diseases like Parkinson's disease.

Problems solved by technology

Patients with neurodegenerative diseases may experience severe degeneration in cognitive or motor abilities, and as these diseases are predominantly progressive, their quality of life and expectations for life may be significantly reduced as a result.
Most of these drugs do not provide causal treatment of Parkinson's disease, but act to control conditions, and thus need to be administered continually.
Although many medicines have been produced and commercialized for the treatment of Parkinson's disease so far, an essential therapeutic agent for completely treating Parkinson's disease has not yet been developed.

Method used

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  • Composition for preventing or treating neurodegenerative diseases, containing diterpene-based compound
  • Composition for preventing or treating neurodegenerative diseases, containing diterpene-based compound
  • Composition for preventing or treating neurodegenerative diseases, containing diterpene-based compound

Examples

Experimental program
Comparison scheme
Effect test

example 1-b

[0086]4.47 kg of the stem and root of Daphne genkwa were chopped, and then immersed in 12 L 80% ethanol for 4 hours, filtered to separate the solids and a first liquid component. The separated solid was again immersed in 12 L 80% ethanol for 4 hours, and filtered to obtain a second liquid component. The first liquid component and the second liquid component were mixed, the mixture was concentrated under reduced pressure, and the residue was lyophilized to prepare 255.1 g of extract of Daphne genkwa.

Example 2: Separation of Active Ingredient by Various Solvents from the Extract of Daphne genkwa

[0087]The extract of the flower of Daphne genkwa obtained in Example 1-a was sequentially fractionated with 2 L of distilled water and 2 L of hexane, chloroform, ethyl acetate, and butanol, respectively. The chloroform layer was concentrated under reduced pressure, and the chloroform fraction (17.6 g) was eluted with a gradient mixed solvent (100:0, 50:1, 20:1, 10:1, 5:1, 2:1, 1:1) of chlorof...

example 3

Compounds on Nurr1 Activity

[0157]As in Example 2, Nurr1 activity according to the concentration of the diterpene isolated from the extract of Daphne genkwa was confirmed through luciferase analysis.

[0158]Specifically, after synthesizing a vector in which the gene having the nucleotide sequence (5′-CTCGGAGGACAGTACTCCG-3′, SEQ ID NO:1) to which the GLA4 gene can bind is repeated 8 times to the reporter gene, luciferase, is synthesized, 3 types of plasmid DNA, including DNA containing Nurr1-LBD and DNA with β-galactosidase, were transfected into BE(2)C cells. After 6 hours, the compounds 1 to 10 separated in Example 2 were treated according to the concentrations in Table 1 below. The cells thus treated were cultured in a 5% carbon dioxide incubator at 37° C. for 20 hours, and then luciferase analysis was performed. As a control, 0.1% DMSO was used, and at this time, the activity was increased by multiple, and Amodiaquine was used as a positive control.

TABLE 1Final treatment concentrati...

example 4

n Activity on Nitric Oxide Production in a Microglia BV-2 Cell

[0161]The death of cranial nerve cells due to an inflammatory reaction in a microglia cell has been reported as one of the main causes of degenerative brain diseases such as dementia and Parkinson's disease. (Sarkar S et al., Neurotoxicology, 44, 250-262 (2014); Bower J H et al., Neurology, 67, 494-496 (2006)). Accordingly, the inhibition activity on nitric oxide production, a representative inflammatory factor, was investigated for the compounds isolated from Example 2 in a microglia. Specifically, microglia BV-2 cells were put into a 96-well plate at 5×104 cells / well, and cultured for 2 days, followed by incubation with LPS (1 mg / mL) for 24 hours with the compound isolated in Example 2 above. The culture supernatant was measured for absorbance at 540 nm using the Griess reagent to quantify nitrite to investigate the amount of nitric oxide production. Minocyline was used as a positive control.

[0162]As a result of the inv...

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Abstract

The present invention relates to a pharmaceutical composition for preventing or treating neurodegenerative diseases comprising a diterpene, or a pharmaceutically acceptable salt thereof.Specifically, the diterpene of the present invention can prevent or treat neurodegenerative diseases caused by inhibition of Nurr1 activity by activating Nurr1 and inhibiting the inflammatory response.

Description

BACKGROUNDTechnical Field[0001]The present invention relates to a pharmaceutical composition for preventing or treating neurodegenerative diseases comprising a diterpene, or a pharmaceutically acceptable salt thereof.[0002]In addition, the present invention relates to a health functional food for preventing or improving neurodegenerative diseases comprising a diterpene, or a pharmaceutically acceptable salt thereof.Background Art[0003]As various bio-regulatory functions of natural physiologically active substances separated from natural substances are known, research in fields such as development of new drugs using natural physiologically active substances and health functional food has been actively conducted. However, natural products contain a wide variety of physiologically active substances, but the physical and chemical properties of each substance are different, so even if the same natural product is extracted as a target, the kinds of bioactive substances that are separated ...

Claims

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Application Information

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IPC IPC(8): A61K31/36A61K31/232A23L33/105
CPCA61K31/36A23L33/105A61K31/232A61P25/16A61P25/28A61K31/231A61K31/216A61K36/83
Inventor KIM, WON GONHAN, BAEK SOOBYUN, JEONG SUNGUYEN, VAN MINHCHOI, HA YOUNG
Owner KOREA RES INST OF BIOSCI & BIOTECH
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