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Biscogniauxia phthalide compound, composition, preparation method, and use thereof

A technology of phthalides and compounds, applied in the field of natural product medicine, can solve problems such as less drug reports

Active Publication Date: 2020-01-17
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few reports on drugs derived from natural products on the market

Method used

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  • Biscogniauxia phthalide compound, composition, preparation method, and use thereof
  • Biscogniauxia phthalide compound, composition, preparation method, and use thereof
  • Biscogniauxia phthalide compound, composition, preparation method, and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Mass fermentation of fungus 69-8-7-1 of the genus Charcoa and its sample pretreatment method:

[0056] (1) The fungus 69-8-7-1 of the genus Anthracum was inoculated on the PDB medium after being activated on the PDA slant, at 25°C at 200r.min -1 Shake culture for 5 days to prepare seed solution, and then inoculate the seed solution into 20 bottles of Erlenmeyer flasks containing rice culture medium according to the inoculum amount of 5 mL / bottle, and culture at 25°C for 48 days to obtain a fermented product. Described rice culture medium is made up of following components: rice 70g / bottle, pure water 105L / bottle.

[0057] (2) The fermented product was added to ethyl acetate and soaked and extracted 3 times, and the extract was concentrated to dryness under reduced pressure to obtain a crude extract (30.5g).

Embodiment 2

[0059] Preparation of charcoal phthalide A and charcoal phthalide B:

[0060] The crude extract was passed through a silica gel column and eluted with cyclohexane and methanol to obtain a cyclohexane part c (9.6g) and a methanol part w (16.5g); then the methanol part w was subjected to medium and low pressure ODS column chromatography, followed by Four fractions (w1, w2, w3, w4) were obtained by methanol-water gradient elution with volume ratios of 20:80, 50:50, 70:30 and 100:0; The obtained sub-fraction w2 (2.4g) was subjected to medium and low pressure liquid phase ODS column chromatography, followed by volume ratios of 10:90, 15:85, 20:80, 25:75, 30:70, 35:65, 40: 60, 45:55, 50:50, 100:0 methanol-water gradient elution to get w2-1, w2-2, w2-3, w2-4, w2-5, w2-6, w2-7, w2- 8 and w2-9 have a total of 9 sub-fractions. Subfraction w2-9 (871.4 mg) was subjected to reverse phase HPLC preparation (Phenomenex Gemini C8 column) and eluted using acetonitrile-water-formic acid (35:65...

Embodiment 3

[0073] Test method for acetylcholinesterase activity of compound

[0074] (1) Experimental principle

[0075] AChE catalyzes the hydrolysis of the substrate thioacetylcholine iodide to produce acetic acid and thiocholine iodide. Thiocholine iodide reacts with 5,5-thio-bis-2-nitrobenzoic acid (5,5-dithio-bis-2-nitrobenzoic acid, DTNB) to generate a yellow anion 5-thio-2- Nitrobenzoic acid, the latter has maximum absorption at 405nm, measuring its maximum production per unit time can reflect the activity of AChE.

[0076] (2) Preparation of experimental solutions and reagents

[0077] Weigh 2.622g NaH respectively 2 PO 4 ·H 2 O and 21.714 g Na 2 HPO 4 ·7H 2 O, mix them and add water to 1000mL, adjust the pH to 7.40 with HCl, and then configure it into 1 mol / L phosphate buffer (PB). Weigh 27.4mg of DTNB, dissolve it in 100mL of LPB to prepare DTNB with a concentration of 0.7mM, keep away from light, and store at below 4°C. Dissolve 8.7mg of thioacetylcholine iodide (ATC...

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Abstract

The invention discloses a Biscogniauxia phthalide compound or a pharmaceutically acceptable salt thereof, and discloses a preparation method thereof and a composition containing the Biscogniauxia phthalide compound or the pharmaceutically acceptable salt thereof. The invention also discloses an application of the Biscogniauxia phthalide compound or the pharmaceutically acceptable salt thereof, andthe composition thereof for preparing a medicine for preventing and / or treating senile dementia. The Biscogniauxia phthalide compound is a microbial derived compound, has the activity against seniledementia, and can be used as a medicine for preventing or treating neurodegenerative diseases.

Description

technical field [0001] The invention belongs to the field of natural product medicines, and in particular relates to a microbial-sourced charcoal phthalide compound, a composition, a preparation method and an application thereof. Background technique [0002] Alzheimer's disease is a degenerative disease syndrome of the central nervous system caused by brain diseases and characterized by progressive cognitive dysfunction and memory impairment. ability, comprehension, and judgment). Common senile dementias include Alzheimer's disease (AD), Vascular dementia (VA), Dementia with Lewy bodies (DLB) and Frontotemporal dementia (FTD). )Wait. Among all dementia patients, Alzheimer's disease patients account for 50-70%, which is the most common type of senile dementia. [0003] The medicines that have been listed for the treatment of Alzheimer's disease are mainly based on acetylcholinesterase inhibitors and N-methyl-D-aspartate receptor antagonists (NMDA) at present. The etiolog...

Claims

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Application Information

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IPC IPC(8): C07D407/04A61K31/365A61P25/28C12P17/16C12R1/645
CPCC07D407/04A61P25/28C12P17/162
Inventor 陈国栋赵欢胡丹王传喜代萍刘妍颖高昊姚新生
Owner JINAN UNIVERSITY
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