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Amide alkaloid for treating depression and application thereof

A technology of amides and alkaloids, which is applied in the field of medicine, can solve the problems of no compound antidepressant effect, insufficient effective rate, difficulty in obtaining curative effect, etc., achieve good antidepressant activity, reduce immobility time, and have wide application prospects

Pending Publication Date: 2022-03-11
中国人民解放军联勤保障部队第九0四医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since depression has a multi-factor, multi-link, and multi-target pathogenesis, the above-mentioned western medicine with a single action mechanism is not only difficult to obtain satisfactory curative effect, but also has serious side effects.
For example, SSRIs, which are widely used in clinical practice, have unsatisfactory clinical curative effect, and the effective rate is less than 50%. Two-thirds of patients need to change drugs several times to achieve better therapeutic effect (Trivedi MH, Rush AJ, Wisniewski SR, et al. Evaluation of Outcomes With Citalopram for DepressionUsing Measurement-Based Care in STAR*D: Implications for Clinical Practice. American Journal of Psychiatry, 2006, 163(1): 28-40.), and slow onset, large adverse reactions, easy to relapse and Expensive (Cipriani A, Zhou X, Del GC, et al. Comparative efficacy and tolerance of antidepressants for major depressive disorder in children and adolescents: a network meta-analysis. Lancet, 2016, 388(10047): 881-890.)
The research group of this application has studied the antidepressant effect and chemical composition of False Betel in the early stage, and found that False Knot has antidepressant effect for the first time, and preliminarily studied the antidepressant mechanism of False Knot, and found that its antidepressant effect is related to HPA axis, BDNF, CREB and In relation to ERK, the chemical constituents of Pseudomonas chinensis were studied, and a new compound piperlotine M was isolated: But there is no relevant report about the compound piperlotine N of the present application and its antidepressant effect

Method used

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  • Amide alkaloid for treating depression and application thereof
  • Amide alkaloid for treating depression and application thereof
  • Amide alkaloid for treating depression and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The preparation of embodiment 1 piperlotine N

[0024]False betel medicinal materials are dried, pulverized and sieved (40 mesh). Heat and reflux extraction with 12 times the volume of 80% ethanol for 3 times, each time for 1.5h, collect the extract and dry it under reduced pressure to obtain the extract of False Konjac. Take betel extract, make a suspension with water, and then carry out liquid-liquid extraction with an equal volume of petroleum ether, and extract 5 times. The extract was collected, concentrated and dried to obtain the petroleum ether part of the extract of Pseudomonas chinensis. Take a sample of the petroleum ether extraction part of Konjac, use 100-200 mesh silica gel (1:1-1.5) to mix the sample, and then separate it by column chromatography silica gel (200-300 mesh), and use petroleum ether-ethyl acetate system as the eluent. The ratio is 20:1, 10:1, 5:1, 2:1, 1:1, and gradient elution is performed. Seven fractions (Frs. 1-7) were combined after ...

Embodiment 2

[0028] Example 2: The protective effect of piperlotine N on PC12 cell injury induced by corticosterone

[0029] The CCK-8 method was used to detect the protective effect of the isolated compound on PC12 cell damage induced by high concentration of CORT, so as to detect the antidepressant activity of piperlotine N. Dilute PC12 cells in logarithmic growth phase to 2×10 5 cells / mL, seeded in a 96-well plate, 100 μL per well, placed in 37 °C 5% CO 2 Cultured in an incubator for 24 hours to allow the cells to fully adhere to the wall. Afterwards, different treatments were carried out according to the groups: for the control group, DMEM medium containing 10% fetal bovine serum was added without other treatment; for the CORT injury model group, DMEM medium containing 5×10 CORT was added -4 mol / L complete medium; administration group, dilute the compound stock solution with 1% fetal bovine serum medium to the corresponding concentration and then add, add 5×10 -4 The complete medium...

Embodiment 3

[0033] Example 3: Effect of piperlotine N on immobility time of mice in forced swimming test

[0034] A mouse model of forced swimming test (FST) was established to evaluate the antidepressant activity of piperlotine N. 50 male ICR mice were weighed and recorded, and the mice were randomly divided into 5 groups according to body weight, 10 in each group. The groups were: blank control group (administered with the same volume of distilled water); positive drug group (20 mg / kg of fluoxetine); low, medium and high doses of piperlotine N groups (administered with 10, 20, and 40 mg / kg of piperlotine N, respectively). Continuous intragastric administration for 7 days, after 1 hour of administration on the 7th day, put the mice into a transparent container with a height of 30 cm, a diameter of 15 cm and water (the water depth is 12 cm, to ensure that the mice cannot touch the bottom of the container, and the water temperature is 24-26 ° C). In a cylindrical container, let it swim in...

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Abstract

The invention relates to amide alkaloid for treating depression and application of the amide alkaloid. A compound is separated from a petroleum ether extraction part of a piper sarmentosum alcohol extract by means of silica gel column chromatography and the like, a novel compound amide alkaloid is obtained through identification, and the structure of the compound is shown as a formula I. It is further found through cell and animal experiments that the compound has a remarkable protection effect on corticosterone-induced PC12 cell injury, and the compound can be used for preparing a medicine for treating corticosterone-induced PC12 cell injury. Meanwhile, the effect of reducing mouse immobility time in a mouse forced swimming test is achieved, the obvious anti-depression curative effect is achieved, and the compound is expected to serve as an active component to be used for preparing the medicine for treating depression.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an amide alkaloid with antidepressant activity and its application in the preparation of medicines for treating depression. Background technique [0002] Depression (major depressive disorder, MDD) is a serious mood disorder, characterized by depression, anhedonia, anxiety, despair, insomnia, slow response, etc., and is one of the most common mental illnesses. Its sickness rate increases year by year, and it is reported that the worldwide sickness rate of depression is about 20%. According to statistics, as of 2015, about 322 million people worldwide suffer from depression (accounting for 4.4% of the world's total population), causing a serious burden on patients and society. According to the prediction of the World Health Organization, depression will become the world's first disease burden by 2030 (Mata DA, Ramos MA, Bansal N, et al. Prevalence of Depression and Depressive Sy...

Claims

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Application Information

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IPC IPC(8): C07D207/36A61K31/4015A61P25/24
CPCC07D207/36A61P25/24C07B2200/07
Inventor 瞿发林李清陈颖秦路平韩婷董文燊
Owner 中国人民解放军联勤保障部队第九0四医院
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