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Nodulisporium viridian E and application thereof

A technology of chlortetracycline and polysporidium, which is applied in the field of natural product medicine to achieve the effect of significant anti-senile dementia activity

Active Publication Date: 2015-06-10
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 symptoms of dementia in patients to a certain extent , but cannot fundamentally prevent the deterioration of the disease and reverse the disease, so the development of anti-Alzheimer's drugs has attracted worldwide attention, and many related biological activity screening and evaluation systems have been established

Method used

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  • Nodulisporium viridian E and application thereof
  • Nodulisporium viridian E and application thereof
  • Nodulisporium viridian E and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1 Large-scale fermentation of Arthrobacter sp. 65-12-7-1 and its sample pretreatment method

[0018] (1) Polyarterial fungus 65-12-7-1 is activated by PDA slope and inoculated into PDB medium, at 25℃ at 200r.min -1 The seed solution was prepared by shaking culture for 5 days, and then inoculated into 165 Erlenmeyer flasks (500 mL) containing PDB medium according to the inoculum amount of 5%. -1 After shaking for 12 days, the fermentation broth was obtained. The PDB medium is composed of the following components in a weight-volume ratio: potato 200g / L, glucose 20g / L, and purified water 1L.

[0019] (2) Adding ethyl acetate to the fermented product for immersion extraction twice, and concentrating the extract to dryness under reduced pressure to obtain a crude extract (11.5 g).

Embodiment 2

[0020] Example 2 Preparation of Nodularia polysporum chloromycin E

[0021] 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 the methanol part M was subjected to medium and low pressure ODS column chromatography, followed by The methanol-water gradient elution with volume ratios of 30:70, 50:50, 70:30, 90:10 and 100:0 yielded 5 fractions (M1, M2, M3, M4, M5); then the volume ratio was 50 The fraction M2 (1.8g) obtained by elution with :50 methanol-water was subjected to medium and low pressure liquid phase ODS column chromatography, followed by volume ratio 30:70, 35:65, 40:60, 45:55, 50:50, 55:45, 100:0 methanol-water gradient elution, M2a, M2b, M2c, M2d, M2e, M2f, M2g, M2h, M2i, M2j and M2k a total of 11 sub-fractions were obtained. The sub-fraction M2a (105 mg) obtained by eluting methanol-water with a volume ratio of 35:65 was prepared by reversed-phase HPLC,...

Embodiment 3

[0026] The compound of Example 3 improves the learning and memory activity of senile dementia flies

[0027] (1) Cultivation of senile dementia fruit flies

[0028] w 1118 (isoCJ1) As the control background fruit fly of the experiment, it is abbreviated as "2U". Successfully transferred to pathogenic Aβ 42 The protein of Drosophila is (UAS-Aβ 42 ; Abbreviated as "H29.3"). This strain of Drosophila was crossed with the whole brain expressing Gal4 promoter Drosophila to obtain elav-GAL4 c155 (P35) and Aβ 42 Of the fruit fly strain.

[0029] (2) Administration of Drosophila

[0030] The experiment set up three groups of healthy fruit flies drug-free control, disease fruit flies drug-free control and disease fruit flies administration.

[0031] The parents of all tested fruit flies were raised and reproduced in a house with a constant temperature of 24°C and a constant humidity of 42% RH (Relative humidity). On the first day after the emergence of the fruit flies, the control group, the ...

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Abstract

The invention belongs to the field of natural product medicines, and particularly relates to nodulisporium viridian E used as a viridian compound and application of the nodulisporium viridian E. The nodulisporium viridian E has a structure shown in a formula (I) in the specification. The invention also provides application of the compound in the general formula (I) in preparation of a medicine for preventing or treating neurodegenerative diseases.

Description

Technical field [0001] The present invention belongs to the field of natural product medicines, and specifically relates to Nodularia polysporin E and its use. Background technique [0002] Alzheimer’s disease is a central nervous system degenerative disease syndrome that is caused by brain diseases and is characterized by progressive cognitive dysfunction and memory impairment. It is manifested in intelligence (including memory, learning ability, direction recognition ability, language Ability, comprehension, and judgment). Alzheimer's disease (AD), Vascular dementia (VA), Dementia with Lewy bodies (DLB) and Frontotemporal dementia (FTD) are commonly seen in Alzheimer's disease. )Wait. Among all dementia patients, Alzheimer's disease accounts for 50 to 70%, which is the most common type of senile dementia. [0003] At present, the drugs that have been marketed for the treatment of Alzheimer's disease are mainly acetylcholinesterase inhibitors and N-methyl-D-aspartate receptor a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J71/00A61K31/58A61P25/28
CPCC07J71/0005
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