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Schizophrenia chloramycin compounds and their uses

A green glomycin, compound technology, applied in the field of natural product medicine, to achieve significant anti-Alzheimer's effect

Active Publication Date: 2017-05-17
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The drugs currently on the market for the treatment of Alzheimer's disease are mainly acetylcholinesterase inhibitors and N-methyl-D-aspartate receptor antagonists (NMDA), which can improve the dementia of patients to a certain extent Symptoms, but can not fundamentally prevent the deterioration of the disease, reverse the disease, so the development of anti-Alzheimer's drugs has attracted the attention of the world, and many related biological activity screening and evaluation systems have been established

Method used

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  • Schizophrenia chloramycin compounds and their uses
  • Schizophrenia chloramycin compounds and their uses
  • Schizophrenia chloramycin compounds and their uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Mass fermentation of Arthrosporum fungus 65-12-7-1 and its sample pretreatment method

[0022] (1) Polyarthrospora fungus 65-12-7-1 was inoculated in PDB medium after being activated on PDA slant, at 25°C at 200r.min -1 Shake culture for 5 days to prepare seed solution, then inoculate 165 Erlenmeyer flasks (500mL) with PDB medium according to 5% inoculum size, at 25°C at 200r.min -1 Under the shaking culture for 12 days, the fermentation broth was obtained. The PDB medium is composed of the following components in weight to volume ratio: potatoes 200g / L, glucose 20g / L, and purified water 1L.

[0023] (2) The fermented product was added to ethyl acetate for soaking and extraction twice, and the extract was concentrated to dryness under reduced pressure to obtain a crude extract (11.5 g).

Embodiment 2

[0024] The preparation of embodiment 2 formula (II)-formula (V) compound

[0025] The crude extract was passed through a silica gel column and eluted with cyclohexane and methanol to obtain cyclohexane part C (3.8g) and methanol part M (5.6g); then methanol part M was subjected to medium and low pressure ODS column chromatography, followed by The methanol-water gradient elution with the volume ratio of 30:70, 50:50, 70:30, 90:10 and 100:0 obtained 5 fractions (M1, M2, M3, M4, M5); : 50 water-methanol elution obtained sub-fraction M2 (1.8g) through medium and low pressure liquid phase ODS column chromatography, using volume ratios successively as 30: 70, 35: 65, 40: 60, 45: 55, 50: 50 , 55:45, 100:0 methanol-water gradient elution to obtain 11 sub-fractions of M2a, M2b, M2c, M2d, M2e, M2f, M2g, M2h, M2i, M2j and M2k. Subfraction M2a (105 mg) obtained by eluting with methanol-water in a volume ratio of 35:65 was prepared by reverse-phase semi-preparative HPLC using acetonitrile...

Embodiment 3

[0033] Example 3 compound improves the learning and memory activity test method of senile dementia Drosophila

[0034] (1) Cultivation of Alzheimer's Drosophila

[0035] w 1118 (isoCJ1) was used as the control group of the experiment, the background Drosophila, abbreviated as "2U". Successful transfer into pathogenic Aβ 42 The Drosophila protein is (UAS-Aβ 42 ; abbreviated as "H29.3"). This strain of Drosophila was crossed with Drosophila expressing the Gal4 promoter in the whole brain to obtain elav-GAL4 c155 (P35) and Aβ 42 Drosophila strains.

[0036] (2) Administration of Alzheimer's Drosophila

[0037] Three groups were set up in the experiment: healthy fruit flies without drug control, diseased fruit flies without drug control and diseased fruit flies with administration.

[0038] The parents of all tested fruit flies were reared and bred in a fly house with a constant temperature of 24° C. and a constant humidity of 42% RH (Relative humidity). On the first day ...

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Abstract

The invention belongs to the field of natural product medicines, and in particular relates to a split-ring knobbed spore viridin type compound and an application thereof. The split-ring knobbed spore viridin type compound has a structure shown in a formula (I). The invention further provides the application of the chemical compound in the formula (I) in preparing medicines for preventing or treating neurodegenerative diseases. The split-ring knobbed spore viridin type compound is shown in the specification.

Description

technical field [0001] The invention belongs to the field of natural product medicaments, and in particular relates to sectiocyclines green gliomycin compounds and applications thereof. Background technique [0002] Alzheimer's disease is a kind of central nervous system degenerative disease syndrome caused by brain diseases, characterized by progressive cognitive dysfunction and memory impairment, which manifests as intelligence (including memory, learning ability, direction recognition ability, language ability, etc.) ability, comprehension, and judgment). Alzheimer's disease (Alzheimer's disease, AD), vascular dementia (VA), Lewy body dementia (Dementia with Lewy bodies, DLB) and frontotemporal dementia (Frontotemporal dementia, FTD) are generally common )Wait. Among all dementia patients, Alzheimer's disease patients account for 50-70%, which is the most common type of senile dementia. [0003] The drugs currently on the market for the treatment of Alzheimer's disease...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/77A61K31/343A61P25/28A61P25/16A61P25/14
CPCC07D307/77
Inventor 高昊陈国栋姚新生郭良栋胡丹于洋赵琴冯晓琳李小霞王高乾
Owner JINAN UNIVERSITY