Application of epilupinine and derivative thereof in preparation of medicine for treating depression

A technology of lupine and derivatives, which is applied in the field of medicine, can solve the problems of high social burden risk and suicide risk, and the prevention or treatment of depression that has not been seen before, so as to reduce immobility time and ensure reliability Effect

Active Publication Date: 2022-06-24
BEIJING ANDING HOSPITAL CAPITAL MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patients with such treatment-resistant depression have a higher risk of social burden and suicide risk
So far

Method used

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  • Application of epilupinine and derivative thereof in preparation of medicine for treating depression
  • Application of epilupinine and derivative thereof in preparation of medicine for treating depression
  • Application of epilupinine and derivative thereof in preparation of medicine for treating depression

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] 10 kg of Lupin (Lupinus micranthus) seeds were crushed and extracted with 95% ethanol under reflux for 3 times, 50 liters each time, and the extraction time was 2 hours each time. The extract was concentrated under reduced pressure to obtain 2.5 kg of extract. The ethanol extract was suspended in 6 liters of distilled water, adjusted to pH 1-3 of the aqueous solution with a 2mol / L dilute hydrochloric acid solution, and extracted 3 times with chloroform, 6 liters each time; the acid aqueous solution was adjusted to pH with a 2mol / L NaOH solution l0-11, extract 3 times with chloroform, each 6 liters. Chloroform was recovered to obtain 80.0 g of total alkaloids. The total alkaloids were crudely fractionated by silica gel column chromatography and eluted with a gradient of chloroform-methanol system (10:0-0:10) to obtain 6 fractions (Frs.A-F). Among them, Fr.B (9.6g) was separated and purified by silica gel column chromatography and Sephadex LH-20 to obtain 2g of compound ...

Embodiment 2

[0054] Take 150 g of epilupinine and appropriate amount of auxiliary materials, sieve, mix well, put into capsules, and make 1000 epilupinine capsules. The content of epilupinine was obtained according to quantitative analysis, which was used as the basis for the dosage.

Embodiment 3

[0056] 150 g of epilupinine was diluted with water and modified with stevioside to prepare a 10% liquid medicine, and the oral liquid of epilupinine was prepared. The content of epilupinine was obtained according to quantitative analysis, which was used as the basis for the dosage.

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Abstract

The invention provides application of epilupinine (1-EPILLUPININE) and a derivative of the epilupinine (1-EPILLUPININE) in preparation of a medicine for treating depression. The application dosage is 0.01-30 mg of epilupinine or the derivative thereof per kilogram of body weight, and the anti-depression effect can be achieved within 60 minutes after administration. After the medicine is administrated for 5 days, the obvious anti-depression effect is generated in the low dosage and the high dosage. Research results show that in a mammal mouse tail suspension experiment, the epilupinine or the derivative thereof has a rapid anti-depression effect, and is more effective than a conventional anti-depression drug imipramine. According to the method, a forced swimming experiment and a mouse tail suspension experiment are adopted as drug screening experiments, and meanwhile, an Open field test is carried out, so that the autonomous activity of a mouse is detected, and interference of central excitants is avoided. The anti-depression drug has the advantages of being remarkable in anti-depression effect, quick in effect taking, small in dosage, small in side effect and the like, and is expected to become a new anti-depression drug which is quick, efficient and novel in mechanism.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the application of epilupinine (1-EPILUPININE) and derivatives thereof in the preparation of drugs for treating depression and the prepared antidepressant drugs. Background technique [0002] Major depressive disorder (MDD) is a severe, recurrent and disabling mental illness that affects approximately 300 million people worldwide. The incidence of depression in China is 4.2%, and there are about 56 million people with depression. Depression is the second leading cause of life lost (years) due to disability and has become a major public health problem that needs to be addressed urgently. Depression can be seen clinically as low mood, emotional depression, low self-esteem and depression, and even pessimism and world-weariness, and there may be suicide attempts or behaviors. The current clinical first-line antidepressants mainly include selective serotonin reuptake inhibitors, sero...

Claims

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Application Information

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IPC IPC(8): A61K31/4375A61K36/48A61K45/06A61P25/24
CPCA61K31/4375A61K36/48A61K45/06A61P25/24A61K2300/00
Inventor 杜静吉腾飞阚伟京王刚
Owner BEIJING ANDING HOSPITAL CAPITAL MEDICAL UNIV
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