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Application of arctiin in preparation of antidepressant drug, and antidepressant drug

An antidepressant and arctiin technology, applied in the field of medicine, can solve the problems of high price, significant antidepressant effect, and large side effects of antidepressant drugs, and achieve the effect of reducing costs and prices

Inactive Publication Date: 2018-08-17
YANBIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problem of large side effects and high price of antidepressant drugs in the prior art, the present invention provides an application of arctiin in the preparation of antidepressant drugs. The antidepressant effect of arctiin is remarkable and the toxicity is low. Inexpensive and not easy to relapse

Method used

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  • Application of arctiin in preparation of antidepressant drug, and antidepressant drug
  • Application of arctiin in preparation of antidepressant drug, and antidepressant drug
  • Application of arctiin in preparation of antidepressant drug, and antidepressant drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Study on the effect of arctiin and arctigenin on mice with chronic unpredictable depression

[0039] 1. Materials and Reagents

[0040] 1.1 Experimental animals

[0041] 60 SPF grade C57BL / 6 mice, male, weighing (20±2) g, (purchased from Liaoning Changsheng Biotechnology Co., Ltd., license number: SCXKliao 2015-001).

[0042] 1.2 Experimental drugs

[0043] Arctiin (Nanjing Chunqiu Biological Engineering Co., Ltd., batch number: 20362-31-6, determined by HPLC, purity ≥ 98%);

[0044] Arctigenin (Nanjing Chunqiu Bioengineering Co., Ltd., batch number: 7770-78-7, determined by HPLC, purity ≥ 98%);

[0045] Positive control drug: Sertraline Hydrochloride Tablets (Zhejiang Jingxin Pharmaceutical Co., Ltd., 50mg / tablet, batch number: A1602262);

[0046] 5-HT (5-hydroxytryptamine), DA (dopamine), TNF-α (tumor necrosis factor-α), IL-1β (interleukin 1β) kit (Shanghai Enzyme Biotechnology Co., Ltd.);

[0047] NO (nitric oxide) kit (Japan Wako Pure Chemical Industr...

Embodiment 2

[0096] Example 2 Cytotoxicity Experiment

[0097] Raw264.7 cells in the logarithmic growth phase were treated with 2.5.×10 4 The density of cells / well was uniformly planted in a sterile 96-well plate, overnight (12h), when the cells grew to 60%, the cells were treated with different concentrations of arctiin and arctigenin, and the incubator (37 ° C, 5% CO 2 ) for 36 h, add 10 μL of MTT solution (5 mg / mL) to each well, incubate for 3.5 h, suck out the medium, add 150 μL dimethyl sulfoxide (DMSO) to each well, and shake for 5 min. Absorbance was measured with a microplate reader at a wavelength of 570 nm. Calculate the half-inhibitory concentration (IC) of arctiin and its aglycon 50 ).

[0098] Table 5 IC of arctiin and aglycon on Raw264.7 cells 50 Impact

[0099]

[0100] It can be seen from the data in Table 5 that the median inhibitory concentration of arctiin on mice is significantly higher than that of arctigenin, which indicates that arctiin is less toxic than arc...

Embodiment 3

[0101] The preparation of embodiment 3 arctiin sublingual lozenges

[0102] Raw materials and their dosage: arctiin 5g, mannitol 30g, lactose 40g, carboxymethylcellulose sodium 2g and magnesium stearate 1g.

[0103] Preparation process: dry all raw materials, crush and sieve through a 100-mesh sieve for pretreatment, mix arctiin with mannitol, lactose and sodium carboxymethyl cellulose, add an appropriate amount of 70% ethanol to make a soft material, pass through a 14-mesh sieve to prepare into granules, air-dried at 55°C for 2 hours, turned once every 0.5h, granulated with 16-mesh and 100-mesh sieves, added magnesium stearate and mixed evenly, and pressed the mixture into tablets in a tablet machine, namely Get arctiin sublingual tablet.

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Abstract

The invention relates to the field of medicines, and provides an application of arctiin in preparation of an antidepressant drug. As an effective component, the arctiin monomer can achieve effective antidepressant effect. The arctiin can also be used in combination with other antidepressant drugs. The invention also provides the antidepressant drug including arctiin and medicinal excipients. Researches show that the toxicity of the arctiin is far less than that of arctigenin. Moreover, pharmacological experiments show that the arctiin and the arctigenin both have significant antidepressant effects, and moreover, the arctiin and the arctigenin have no significant difference in the antidepressant effect at the same dose. Therefore, the antidepressant drug prepared with the arctiin as the effective component has lower toxicity and remarkable antidepressant effect. Meanwhile, the price of raw material of the arctiin is significantly lower than that of arctigenin, and the cost and price ofthe antidepressant drug can be effectively reduced. Therefore, the antidepressant drug with low toxicity, low cost and significant effect is obtained.

Description

technical field [0001] The invention relates to the field of medicines, in particular to an application of arctiin in preparing antidepressant medicines and an antidepressant medicine containing arctiin. Background technique [0002] Depression is a common chronic mental disorder, characterized by persistent depression, often accompanied by anxiety, physical discomfort and sleep disturbance (Xu P, Wang KZ, Lu C, et a1.Antidepressant-like effects and cognitive enhancement of the total phenols extract of Hemerocallis citrina Baroni in chronic unpredictable mild stress rats and its related mechanism[J].Journal of Ethnopharmacology,2016,194:819-826), at least 10% of depressed patients will develop bipolar disorder Phenomena, manifested as manic episode behavior, some patients showed obvious motor agitation and anxiety behavior, and severe patients even had psychotic symptoms such as hallucinations (Yue Lili, Bai Guangze. Research status of depression and anxiety disorders[J] . ...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P25/24
CPCA61K31/7048A61P25/24
Inventor 朴莲荀徐翔陆莹姜彤郭建鹏金学军南极星
Owner YANBIAN UNIV
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