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Medical application of aporphine alkaloid

A technology of alkaloids and uses, applied in the field of pharmacotherapeutics, can solve problems such as low response rate and slow onset time

Active Publication Date: 2021-06-22
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is aimed at existing clinical antidepressants such as slow onset time, low response rate, side effects (such as withdrawal effects, digestive tract symptoms, etc.) After visible xerostomia, constipation, diarrhea) and other problems, a kind of antidepressant medical application of aporphyl alkaloid is provided, and pharmacological experiments show that the aporphyl alkaloid antidepressant drug effect shown in formula III is better, and Compared with fluoxetine, it has better antidepressant effect, higher response rate and faster onset

Method used

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  • Medical application of aporphine alkaloid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1: Zebrafish in vivo pharmacological experiment of the first series of aporphi alkaloids

[0038] The open field test (OFT) was used to test the antidepressant activity of the reserpine zebrafish depression model, and fluoxetine (Flu) was selected as the positive control drug.

[0039] Instrument: Zebrafish Behavior Analyzer

[0040] Reagents: compounds Ia, Ib, Ic, Id, Ie, Ig, Ii, Ik (all known compounds); fluoxetine, reserpine (purity ≥ 99.0%), purchased from Sigma Aldrich (Shanghai) Trading Ltd.

[0041] Zebrafish: wild-type AB adult zebrafish, provided by Wuhan National Zebrafish Resource Center, and bred in the zebrafish laboratory of Nanjing Ruiying Runze Biomedical Technology Co., Ltd. The zebrafish breeding method is carried out according to The ZebrafishBook, and it is cultured in circulating water , the water quality is maintained through the circulating water system, the water temperature is kept at 28.5°C, the daily fixed light and dark time is 1...

Embodiment 2

[0044] Embodiment 2: Zebrafish in vivo pharmacological experiments of IV series of aporphi alkaloids

[0045] Reagents: Compounds IVa, IVb, IVc, IVd, IVe, IVf, IVg, IVi, IVk (all known compounds).

[0046] Zebrafish were randomly divided into 12 groups, blank control group (10), model group (10), positive control group (10, fluoxetine 1 μ M), administration group: IVa group (10, 1 μ M), Group IVb (10 strips, 1 μM), Group IVc (10 strips, 1 μM), Group IVd (10 strips, 1 μM), Group IVe (10 strips, 1 μM), Group IVf (10 strips, 1 μM), Group IVg (10 strips , 1 μM), IVi group (10 pieces, 1 μM), IVk group (10 pieces, 1 μM), and the rest are the same as in Example 1.

[0047] Result: if image 3 and Figure 4 As shown, compared with the blank control group, the total moving distance and swimming speed of the model group zebrafish were significantly reduced ( #### P**** P*** P** P* P<0.05).

Embodiment 3

[0048] Embodiment 3: the zebrafish in vivo pharmacological experiment of Ie

[0049]

[0050] Zebrafish were randomly divided into 4 groups, blank control group (10), model group (10), positive control group (10, fluoxetine 1 μM), Ie group (10, 1 μM). The animal trajectory tracking system traces the following variables of the zebrafish movement curve within 5 minutes: A total swimming distance; B average speed; C immobility time; D immobility frequency; E meandering degree; F rotation angle; G angular velocity. All the other are with embodiment 1.

[0051] Result: if Figure 5 and Image 6 As shown, compared with the blank group, the total moving distance and swimming speed of the model group zebrafish were significantly reduced ( #### P#### P**** P**** P<0.001), and all the behavioral indicators showed that compound Ie had the best effect, showing better antidepressant efficacy than fluoxetine.

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Abstract

The invention discloses an application of aporphine alkaloid shown in a formula III in preparation of an antidepressant drug. R1 and R2 are respectively and independently selected from alkoxy and methylenedioxy, R3 and R4 are respectively and independently selected from H, OH, alkoxy and methylenedioxy, but when R3 and R4 cannot be H at the same time or R1 and R2 are both selected from methoxy, R3 cannot be OH, and R4 cannot be H. Pharmacological experiments show that the aporphine alkaloid shown in the formula III has a better anti-depression drug effect, and compared with fluoxetine, the aporphine alkaloid has a better anti-depression effect, a higher response rate and a faster effect.

Description

technical field [0001] The invention belongs to the field of pharmacotherapeutics, and relates to the medical use of aporphil alkaloids, in particular to the use of aporphil alkaloids in antidepressants. Background technique [0002] Depression is a kind of mental disorder with persistent depressed mood as the main clinical symptom. sense of worth, and even suicidal ideation and behavior when severe. Sometimes there are accompanying symptoms such as decreased energy, changes in appetite, more or less sleep, anxiety, decreased concentration, restlessness, etc. The etiology and pathogenesis of depression have not yet been fully elucidated. Low content of central norepinephrine, serotonin, dopamine and other monoamine neurotransmitters and low receptor function are considered to be the cause of depression. [0003] Existing clinical antidepressants have disadvantages such as slow onset time, low response rate, and side effects (such as withdrawal effects, gastrointestinal sy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/473A61K31/4741A61P25/24
CPCA61K31/473A61K31/4741A61P25/24Y02A50/30
Inventor 孙建博陈莉万怡莉
Owner CHINA PHARM UNIV
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