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Application of anti-depression compound on preparation of anti-depression drugs and anti-depression health-care foods

A health food, antidepressant technology, applied in the field of medicine, can solve the problems of slow onset (it takes weeks or even months, resistance to treatment, slow onset (it takes weeks or even months to slow down the effect), etc.

Active Publication Date: 2015-10-28
ZHEJIANG ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Depression is a high-incidence mental disorder. The current clinical traditional antidepressants mainly target monoamine neurotransmitters in the brain of patients with depression. Although they are effective and safe, their main defects are: slow onset ( It takes weeks or even months to effectively relieve symptoms), treatment resistance (refractory depression), and relapse, therefore, there is an urgent clinical need to develop fast-acting antidepressants for refractory depression
However, the current clinical traditional antidepressants are mainly aimed at monoamine neurotransmitters in the brains of patients with depression. Although they are effective and safe, their main defect is their slow onset (it takes weeks or even months to significantly relieve symptoms) , treatment resistance (treatment-resistant depression, treatment-resistant depression), will relapse, so there is an urgent clinical need to develop quick-acting antidepressant drugs for treatment-resistant depression [Mathew SJ, Manji HK, Charney DS.Novel drugs and therapeutic targets for severe mood. Neuropsychopharmacology 2008:1-13.2. Cryan JF, O Leary OF. A glutamate pathway to faster-acting antidepressants? Science 2010;329:913.]

Method used

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  • Application of anti-depression compound on preparation of anti-depression drugs and anti-depression health-care foods
  • Application of anti-depression compound on preparation of anti-depression drugs and anti-depression health-care foods
  • Application of anti-depression compound on preparation of anti-depression drugs and anti-depression health-care foods

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Preparation and structure identification of sarcoclindin

[0034] Taishan Radix Polygoni Multiflori 5kg is pulverized, and ethanol aqueous solution (water-containing volume percentage is 5%) percolates, obtains ethanol extract, and ethanol extract is extracted with ethyl acetate, and ethyl acetate extract is dissolved in 0.2N sulfuric acid methanol solution (being sulfuric acid solution). Form a sulfuric acid methanol solution in methanol, wherein the concentration of sulfuric acid in the sulfuric acid methanol solution is 0.2mol / L) Hydrolyze at 70°C for 5 hours, neutralize with sodium bicarbonate, concentrate, extract the concentrate with ethyl acetate, the extract is the total aglycone. 180 g of total aglycones were subjected to silica gel column chromatography, and gradient elution was performed with a dichloromethane-methanol system (dichloromethane to methanol volume ratio 100:0→40:60) to obtain Fr1-Fr8. Fr8 15g was subjected to repeated column chromatog...

Embodiment 2

[0036] Example 2: Preparation and structure identification of deacetylradixin

[0037] Taishan Baishouwu 5kg is pulverized, percolated with ethanol aqueous solution (water content is 5%), the ethanol extract is extracted with ethyl acetate, and the ethyl acetate extract is hydrolyzed with 0.2N sulfuric acid methanol at 70°C for 5 hours, and dissolved in sodium bicarbonate And, concentrated, the concentrate was extracted with ethyl acetate, and the extract was the total aglycone. 180 g of total aglycones were subjected to silica gel column chromatography, and gradient elution was performed with a dichloromethane-methanol system (100:0→40:60) to obtain Fr1-Fr8. 15g of Fr8 was subjected to repeated column chromatography on Rp-18, eluted with methanol-water system (53%→60%), detected by TLC, the same fractions were combined, and recrystallized from methanol to obtain 675 mg of deacetylradixaglycone.

[0038] Deacetylradixaglycone, C 21 h 32 o 6 , Colorless needles (methanol). ...

Embodiment 3

[0039] Example 3: Preparation and structure identification of diglucarinin

[0040] Taishan Baishouwu 5kg is pulverized, percolated with ethanol aqueous solution (water content is 5%), the ethanol extract is extracted with ethyl acetate, and the ethyl acetate extract is hydrolyzed with 0.2N sulfuric acid methanol at 70°C for 5 hours, and dissolved in sodium bicarbonate And, concentrated, the concentrate was extracted with ethyl acetate, and the extract was the total aglycone. 180 g of total aglycones were subjected to silica gel column chromatography, and gradient elution was performed with a dichloromethane-methanol system (100:0→40:60) to obtain Fr1-Fr8. Rp-18 on 10 g of Fr6 was subjected to repeated column chromatography, eluted with methanol-water system (53%→60%), detected by TLC, and the same fractions were combined and recrystallized from methanol to obtain 1.6 g of diglucarinin.

[0041] Radixanthin, C 23 h 34 o 7 , Colorless needles (methanol). IR(KBr): 3510, 169...

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Abstract

The invention discloses an application of an anti-depression compound on the preparation of anti-depression drugs and anti-depression health-care foods. The structure of the anti-depression compound is shown in the formula I. The anti-depression compound serves as the only active ingredient or one of active ingredients of the anti-depression health-care foods. The anti-depression compound is a liquid preparation or a solid preparation or a spray preparation or an aerosol preparation or the like. According to the application of the anti-depression compound on the preparation of the anti-depression drugs and the anti-depression health-care foods, the chemical structure of the anti-depression compound is different from that of any known anti-depression drug, the anti-depression compound has prominent anti-depression activity, obvious toxic and side effects do not occur, marketizing large-scale utilization and popularization are facilitated, and wide application prospects are achieved. (Please see the formula I in the specification.).

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of an antidepressant compound in the preparation of antidepressant medicine and antidepressant health food. Background technique [0002] Depression is a high-incidence mental disorder. The current clinical traditional antidepressants mainly target monoamine neurotransmitters in the brain of patients with depression. Although they are effective and safe, their main defects are: slow onset ( It takes weeks or even months to effectively relieve symptoms), treatment resistance (refractory depression), and relapse. Therefore, there is an urgent need to develop antidepressants that are quick-acting and targeted at treatment-resistant depression. [0003] According to the pathogenesis of depression around neuroplasticity, neurogenesis, hypothalamic-pituitary-adrenal (HPA) axis and other subsequent adaptive changes in the nervous system, the current targets of antidepre...

Claims

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Application Information

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IPC IPC(8): A61K31/569A61P25/24A23L1/29
CPCC07J1/00C07J31/006C07J43/003A61K9/0019A61K9/0095A61K31/569A61K31/58A61K36/24A61K36/27A61K45/06A61P25/24A61K9/0056A61K9/08A61K9/14A61K9/20A61K9/48
Inventor 叶益萍李晓誉杨叶伟赵铮蓉陈峰阳徐世芳黄文海
Owner ZHEJIANG ACAD OF MEDICAL SCI
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