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Novel application of triterpenoid acid compound as A beta fiber formation inhibitor drug

A technology of compounds and inhibitors, which is applied in the field of triterpenic acid compounds as Aβ fiber formation inhibitor drugs, to achieve the effect of improving behavioral ability, inhibiting the formation of Aβ fibers, and reducing Aβ content

Pending Publication Date: 2021-09-07
SOUTHWEST MEDICAL UNIVERISTY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, no encouraging compounds have been found from traditional Chinese medicine for the treatment of Alzheimer's disease

Method used

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  • Novel application of triterpenoid acid compound as A beta fiber formation inhibitor drug
  • Novel application of triterpenoid acid compound as A beta fiber formation inhibitor drug
  • Novel application of triterpenoid acid compound as A beta fiber formation inhibitor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Validation and screening of Aβ fibrosis inhibitors in Scutellaria baicalensis

[0084] Yu L, Wu A G, Wong K W, et al. The New Application of UHPLC-DAD-TOF / MS in Identification of Inhibitors on β-Amyloid Fibrillation From Scutellaria baicalensis[J].other,2019,10. In this journal, potential inhibitors of Aβ fibrosis in Scutellaria baicalensis were screened by pre-incubating Aβ(1-42) with Scutellaria baicalensis extract and then analyzed by UHPLC-DAD-Q / TOF-MS / MS. Compared with Scutellaria baicalensis extract alone, xanthosides and xanthosides were found to be significantly lower in the Aβ-containing culture medium, indicating that xanthosides and xanthosides are potent inhibitors of Aβ fibrosis in Scutellaria baicalensis.

[0085] Embodiment 1 uses the high-throughput screening method provided by the present invention to verify

[0086] Preparation of Scutellaria baicalensis extract

[0087] Scutellaria baicalensis was weighed and pulverized, then distilled and extra...

Embodiment 2

[0103] Preparation of Kaixinsan Extract

[0104] Weigh and crush Kaixin San (the Kaixin San contains ginseng, Polygala, Shichangpu, and Poria cocos), then distill and extract with 10 times the volume of water for 1.5 hours, repeat the extraction 4 times, combine the extracts, filter, concentrate, and then The concentrated extract was dissolved into a 400 mg / mL solution with DMSO (dimethyl sulfoxide) to obtain the Chinese herbal medicine extract to be tested.

[0105] Preparation of biotinylated Aβ(1-42) peptide

[0106] 5 mg of Aβ(1-42) peptide was dissolved in hexafluoroisopropanol (HFIP, Sigma) solution, then the HFIP solution was dispensed into new 1.5 mL test tubes and dried under nitrogen flow, then, in the test tubes Add 10 μL of DMSO (dimethyl sulfoxide) and an appropriate volume of PBS (comprising 15% DMSO and 0.02% Tween 20) to obtain a working concentration of 100 mg / mL of Aβ(1-42).

[0107] Biotin (EZ-LinkNHS-LC-LC-Biotin (Thermo Scientific, USA)) with a molar...

Embodiment 3

[0124] Separation and purification of PPAC, DTA and TA from Poria cocos

[0125] Firstly, take Poria cocos powder, soak it with ethyl acetate reagent, and then use a rotary evaporator to rotate and collect, and repeat 3 times to obtain Poria cocos extract. The ethyl acetate extract of Poria cocos was roughly separated using a silica gel chromatography column, and 100ml fractions were collected and divided into one group, and then the target compound was detected by mass spectrometry, and finally purified by ultra-fast high-performance liquid phase. Finally, three compounds were successfully isolated, including pyripolic acid C, dehydroturmoic acid, and turmolic acid.

[0126] Figure 9 The representative total ion chromatograms in show the UHPLC-DAD-Q / TOF-MS / MS analysis of PPAC, DTA, TA and Poria cocos extract. Among them, S1: Poria cocos extract; S2: PPAC; S3: DTA; S4: TA. From Figure 10 It shows that the measured accurate masses of PPAC, DTA and TA are [MH]-481.3388, ...

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Abstract

The invention relates to novel application of a triterpenoid acid compound as an A beta fiber formation inhibitor drug, and particularly relates to application of the triterpenoid acid compound in the A beta fiber formation inhibitor drug. The triterpenoid acid compound is at least one of polyporus umbellatus acid C, dehydro-geosolic acid and geosolic acid. Multiple aspects verify that the triterpenoid acid compound can remarkably inhibit formation of A beta fibers, save PC-12 cells induced by A beta (1-42), reduce the A beta content of caenorhabditis elegans AD and improve the behavior ability of caenorhabditis elegans AD. Molecular docking results show that the triterpenoid acid compound has good binding performance with A beta. The compound capable of inhibiting formation of the A beta fibers is researched, and the compound has very important social significance in developing drugs for neuroprotection.

Description

technical field [0001] The present invention relates to the technical field of Aβ fibril formation inhibitors, and relates to a new application of a triterpene acid compound as an Aβ fibril formation inhibitor, in particular to a new application of a triterpene acid compound as an Aβ fibril formation inhibitor drug. Background technique [0002] Alzheimer's disease (AD), an age-related neurodegenerative disease, has become the most common dementia, accounting for nearly 60%-80% of all cases. Epidemiological data indicate that the prevalence of Alzheimer's disease increases as the world population ages. The clinical symptoms of AD are mainly manifested as progressive memory loss, cognitive dysfunction, distraction, mood disturbance and personality changes. Currently, Alzheimer's disease remains an irreversible and incurable neurodegenerative disease. [0003] Mechanistic studies have shown that the pathology of Alzheimer's disease is closely related to the occurrence of neu...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P25/28
CPCA61K31/575A61P25/28
Inventor 吴安国秦大莲周晓刚邱文乔唐勇吴建明郭垊松朱凤丹
Owner SOUTHWEST MEDICAL UNIVERISTY
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