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Stilbene compound separated from rheum lhasaense and application of stilbene compound in treatment of nervous system diseases

A technology of stilbene and Lhasa rhubarb, which is applied to nervous system diseases, medical preparations containing active ingredients, drug combinations, etc.

Active Publication Date: 2021-05-25
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few research reports on Rhubarb Lhasa, and only two documents reported that it contains 12 phytochemical components, all of which are stilbene components, including 6 resveratrol monomer derivatives, 4 Resveratrol dimer and 2 resveratrol trimers

Method used

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  • Stilbene compound separated from rheum lhasaense and application of stilbene compound in treatment of nervous system diseases
  • Stilbene compound separated from rheum lhasaense and application of stilbene compound in treatment of nervous system diseases
  • Stilbene compound separated from rheum lhasaense and application of stilbene compound in treatment of nervous system diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Separation and Characterization of Stilbene Compounds from Rhubarb Lhasa

[0039] 1. Extraction and separation of stilbene compounds from Lhasa rhubarb

[0040] The Lhasa rhubarb medicinal material is crushed, extracted with 95% ethanol, and concentrated under reduced pressure to obtain the extract. After extraction, it is divided into chloroform part, ethyl acetate part, n-butanol part and water part. The samples from the ethyl acetate part were loaded on the MCI packed chromatography column, and were rinsed with 30%, 50%, 70% and 100% ethanol solvents respectively, and each solvent rinsed 4-5 column volumes. Among them, compounds 1 and 2 were isolated from the 50% ethanol fraction, and compound 3 was isolated from the 70% fraction.

[0041] 2. Structural analysis of new compounds

[0042] Compound 1: brown powder, molecular ion peak m / z 595.1423 [M+Na] given by (+)HRESIMS + (calcd for 595.1428, see attached figure 1 ) to determine its molecular formula...

experiment example 1

[0052] Experimental example 1 Acetylcholinesterase (AChE) inhibitory activity screening experiment

[0053] 1. Test method

[0054] Acetylcholinesterase inhibitory activity is based on the improved Ellman method, and the inhibitory effect of compounds 1 and 2 on AChE was measured in a 96-well plate. The reagents used in the experiment include the reaction substrate ATCI, the chromogenic agent DTNB and the reaction terminator in 1% SDS buffer containing (1g SDS in PBS (ph8.0)). The assay steps are as follows: first, mix 60 μL of PBS (pH 8.0), 10 μL of 3 mM DTNB, 20 μL of the test compound and 20 μL of 0.50 U / mL AChE solution in a 96-well plate, and incubate at 37°C for 10 minutes to activate the enzyme; secondly, the 10 μL of substrate (ATCI) was added to the microplate and incubated at 37°C for 15 minutes. Third, add 80 μL of 1% SDS solution to stop the reaction. Finally, the absorbance was measured at 405 nm using a multi-functional microplate reader (Tecan Infinite M200, ...

experiment example 2

[0063] Experimental Example 2 Animal Experiment and Behavioral Experiment of Compound 1

[0064] 1 Experimental method

[0065] 1.1 Animal experiments

[0066] Animal experiments mainly study the new compound 1 (comp.1, picatanol-3'-O-β- D -[2″-(3,5-dihydroxy-4-methoxybenzoyl)]-glucopyranoside) preventive effect on cognitive impairment. 60 SPF grade C57 male mice of 8 weeks old ( Purchased from Speiford (Beijing) Biotechnology Co., Ltd.), fed in plastic cages, free access to food and water, room temperature 25 ± 2 ° C, humidity 55 ± 10%, maintaining a circadian rhythm of 12h light and 12h dark. Male mice were randomly divided into 5 groups (12 mice per group): (1) blank control group (Control, Vehicle), (2) model group (Model, Scopolamine, 1.5 mg·kg -1 ), (3) Positive drug group (DNP, Scopolamine+Donepezil, 3.0mg·kg -1 ), (4) low dose group (Compound 1, Scopolamine+comp.1, 70mg·kg -1 ), (5) high dose group (Compound 1, Scopolamine+comp.1, 350mg·kg -1 ). The mice were gi...

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Abstract

The invention discloses a stilbene compound separated from rheum lhasaense and an application of the stilbene compound in treatment of nervous system diseases. Three novel stilbene compounds are separated from rheum lhasaense, and the structural formulas of the stilbene compounds are shown as a formula I, a formula II or a formula III. The invention further discloses a method for separating the stilbene compound from rheum lhasaense. The result of in-vitro determination of the inhibitory activity of the compound on acetylcholin esterase shows that the compound has a relatively strong inhibitory effect on acetylcholin esterase. The compound shown in the formula I is further subjected to animal experiments and behavioral experiments such as NOR, MWM and PAT, cholinergic detection and oxidative stress detection to evaluate the improvement effect of the compound shown in the formula I on the cognitive impairment induced by scopolamine, and experimental results show that the compound shown in the formula I can remarkably improve the cognitive impairment induced by scopolamine of experimental animals. The stilbene compound provided by the invention can be used for preparing medicines for treating neurodegenerative diseases.

Description

technical field [0001] The present invention relates to stilbene compounds, especially the stilbene compounds isolated from Lhasa rhubarb. The present invention further relates to stilbene compounds and their use in the preparation of drugs for treating nervous system diseases, which belong to the stilbene compounds isolated from plants. Styrenic compounds and fields of use thereof. Background technique [0002] Lhasa rhubarb (Rheum lhasaense A.J.Li et P.K.Hsiao) is a plant belonging to the wave leaf group of the genus Rhubarb in the Polygonaceae family, and is endemic to my country. Its wild species are mainly distributed in Tibet, and at present, artificial cultivation has also begun in some areas of Sichuan and Yunnan. Lhasa rhubarb, as a national medicine, is often used to treat stomach diseases, and local Tibetans call it Quza. Early literature analysis found that Lhasa rhubarb does not contain the characteristic components of rhubarb plants - anthraquinone and anthro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/203C07H1/08C07D307/80A61P25/28A61P25/16A61P25/14A61P25/00A61K31/343A61K31/7034
CPCC07H15/203C07H1/08C07D307/80A61P25/28A61P25/16A61P25/14A61P25/00
Inventor 何春年刘青申洁李珮肖培根
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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