A kind of carbon skin phthalide compound, composition, preparation method and use thereof

A technology of compounds and phthalides, applied in the field of natural product drugs, can solve the problem of less drug reports

Active Publication Date: 2022-07-22
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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  • A kind of carbon skin phthalide compound, composition, preparation method and use thereof
  • A kind of carbon skin phthalide compound, composition, preparation method and use thereof
  • A kind of carbon skin phthalide compound, composition, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0056] (1) The fungus 69-8-7-1 of the genus Charcoal was inoculated into the PDB medium after being activated by the PDA slant, and was incubated at 25°C for 200 r.min. -1 The seed liquid was prepared by shaking culture for 5 days, and then the seed liquid was inoculated into 20 flasks containing rice culture medium according to the inoculation amount of 5 mL / bottle, and the culture was statically cultured at 25° C. for 48 days to obtain a fermented product. Described rice culture medium is made up of following components: rice 70g / bottle, purified water 105L / bottle.

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

Embodiment 2

[0059] Preparation of carbon skin phthalide A and carbon skin phthalide B:

[0060] The crude extract was passed through a silica gel column and eluted with cyclohexane and methanol to obtain a cyclohexane fraction c (9.6 g) and a methanol fraction w (16.5 g); then the methanol fraction w was subjected to medium and low pressure ODS column chromatography, followed by 4 fractions (w1, w2, w3, w4) were obtained by gradient elution of methanol-water with volume ratios of 20:80, 50:50, 70:30 and 100:0; and methanol-water washing with a volume ratio of 70:30 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 to give w2-1,w2-2,w2-3,w2-4,w2-5,w2-6,w2-7,w2- 8 and w2-9 make a total of 9 subfractions. Subfraction w2-9 (871.4 mg) was prepared by reverse-phase HPLC (Phenomenex Gemini C8 column), elute...

Embodiment 3

[0073] Test method for acetylcholinesterase activity of compounds

[0074] (1) Experimental principle

[0075] AChE catalyzes the hydrolysis of the substrate thioacetylcholine iodide to 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 the yellow anion 5-thio-2- Nitrobenzoic acid, which has the maximum absorption at 405nm, can reflect the activity of AChE by measuring its maximum generation amount in unit time.

[0076] (2) Preparation of solutions and reagents for experiments

[0077] Weigh 2.622g NaH 2 PO 4 ·H 2 O and 21.714g Na 2 HPO 4 ·7H 2 O, mix them and add water to 1000mL, adjust the pH to 7.40 with HCl, and then prepare 1 mol / L phosphate buffer (PB). Weigh 27.4 mg of DTNB, dissolve it in 100 mL of PB, and prepare DTNB with a concentration of 0.7 mM, protect from light, and store at below 4°C. 8.7 mg of thioacetylcholine iodide (ATCh) was dissolved in 10 m...

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Abstract

The invention discloses a carbon skin phthalide compound or a pharmaceutically acceptable salt thereof, and discloses a preparation method thereof and a composition containing the above carbon skin phthalide compound or a pharmaceutically acceptable salt thereof; the present invention Also disclosed is the application of the above-mentioned carbon skin phthalide compounds or their pharmaceutically acceptable salts and their compositions for preparing medicines for preventing and / or treating senile dementia. The carbon skin phthalide compound of the present invention is a compound derived from microorganisms, has anti-senile dementia activity, 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 medicine, and specifically relates to a microbial-derived carbon skin phthalide compound, composition, preparation method and application thereof. Background technique [0002] Alzheimer's disease is a degenerative disease syndrome of the central nervous system characterized by progressive cognitive impairment and memory impairment caused by brain diseases, which manifests as intelligence (including memory, learning ability, direction recognition ability, language 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 accounts for 50-70% and is the most common type of senile dementia. [0003] The drugs currently on the market for the treatment of Alzheimer's disease are mainly acetylcholinesterase inhibitors ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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