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Applications of stilbene compounds for preparing medicament for preventing and treating depression

A stilbene compound and a technology for depression are applied in the field of new uses in the preparation of drugs for the prevention and treatment of depression, and can solve the problems of large side effects, difficult control of addiction, and insignificant clinical treatment effects.

Active Publication Date: 2014-01-15
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the use of helexin and its derivatives, naringin, 7-O-β-D-acetylated sugar-coumarin, emodin methyl ether, etc. in the treatment of depression drugs has also been developed in recent years, However, there are still some deficiencies in clinical treatment effects, such as insignificant clinical effects, large side effects, and difficulty in controlling addiction.

Method used

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  • Applications of stilbene compounds for preparing medicament for preventing and treating depression
  • Applications of stilbene compounds for preparing medicament for preventing and treating depression
  • Applications of stilbene compounds for preparing medicament for preventing and treating depression

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0027] Experimental Example 1: Toxicity Test

[0028] 1. Materials

[0029] 1.1 Drugs: Trizastilbene and piceatanol were prepared by Kunming Pharmaceutical Group Co., Ltd., and the purity was tested to be greater than 98.0%, and they were stored in a desiccator.

[0030] 1.2 Animals: healthy Kunming mice, both male and female, weighing 18-22g, provided by Kunming Pharmaceutical Group Co., Ltd., license number: SCXK (Dian) 2009-0001.

[0031] , Acute toxicity test in mice

[0032] Under the maximum dosage concentration and maximum dosage volume, the mice were orally administered 1:1 tristilbeside and piceatanol mixed powder 5g / kg, and observed continuously for 14 days. No death or abnormal toxic reaction was found in the experimental mice . It shows that the maximum tolerated dose of trizaperoside and piceatanol administered to mice is 5g / kg.

[0033] , Long-term toxicity test in mice

[0034] The 1:1 mixed powder of tristilbene and piceatanol was divided into three gro...

experiment example 2

[0041] Experimental Example 2: Mouse Tail Suspension Experiment

[0042] 1. Drugs: Trizabetaside and piceatanol were prepared by Kunming Pharmaceutical Group Co., Ltd., and the purity was tested to be greater than 98.0%, and they were stored in a desiccator. During the experiment, 0.9% normal saline was used to make a suspension for later use. Prozac (fluoxetine hydrochloride), Eli Lilly Suzhou Pharmaceutical Co., Ltd.

[0043] 2. Animals: healthy Kunming mice, both male and female, weighing 18-22 g, provided by Kunming Pharmaceutical Group Co., Ltd., license number: SCXK (Dian) 2009-0001.

[0044]3. Method: Healthy Kunming mice were randomly divided into 8 groups, 10 in each group, which were blank control group (normal saline); positive control group (fluoxetine hydrochloride 20.0mg / kg); Picetanol high, medium and low dose groups (30.0, 20.0, 10.0 mg / kg). Oral administration, once a day, for 7 consecutive days. Animals had free access to food and water during the exper...

experiment example 3

[0048] Experiment 3: Forced mice to swim

[0049] 1. Drugs: same as experimental example 2.

[0050] 2. Animals: Same as Experiment 2.

[0051] 3. Method: Healthy Kunming mice were randomly divided into 8 groups, 10 in each group, which were blank control group (normal saline); positive control group (fluoxetine hydrochloride 20.0mg / kg); Picetanol high, medium and low dose groups (30.0, 20.0, 10.0 mg / kg). Oral administration, 1 time / d, for 7 consecutive days. Animals had free access to food and water during the experiment. One hour after the last administration, the mice were placed in a container with a diameter of about 18cm, a water depth of 18cm, and a water temperature of 25°C. The swimming time of the mice was 6 minutes. Struggling ceases, or the animal is buoyant with only small limb movements to keep the head above water). The experimental results are shown in Table 2.

[0052] Table 2. Effects on the immobility time of forced swimming in mice (n=10, ±S)

[...

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Abstract

The invention discloses applications of a stilbene compounds for preparing medicaments for preventing and treating depression, wherein the stilbene compounds can be used as an effective active component to prepare the medicaments for preventing and treating depression. The stilbene compounds are mixtures containing ore or both of piceatannol or piceatannol 3'-O-beta-D-glucopyranoside, and used in the medicaments for preventing and treating endogenous depression, and / or reactive depression, and / or masked depression, and / or depression using learning difficulty as a characteristic; and / or secondary depression caused by medicaments, and / or secondary depression caused by body diseases, and / or postnatal depression, and / or involutional melancholia, and / or depressive neurosis. By a Konmin mouse tail suspension test, a swimming force test and a chronic stress sucrose preference determination experiment, the stilbene compounds can substantially raises disappointed time of mouse tail suspension and motionless time of forced swimming, has substantial resistant effect for interest deprivation symptom caused by chronic stress, and has a substantial antidepressant effect.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a new application of a stilbene compound in the preparation of drugs for preventing and treating depression. Background technique [0002] Depression is a common mood disorder, which can be caused by various reasons. The main clinical feature is marked and persistent low mood, and the low mood is not commensurate with the situation. In severe cases, suicidal thoughts and behaviors may appear. According to the statistics of the World Health Organization, depression has become the fourth largest disease in the world, and it is estimated that by 2020, it may become the second largest disease in the world after coronary heart disease, accounting for 15% of the global disease burden. According to expert statistics, patients with depression account for 4-8% of the total population in my country, and more than 800,000 people commit suicide due to depression. [...

Claims

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Application Information

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IPC IPC(8): A61K31/7034A61K31/05A61P25/24
Inventor 龚云麒陈锦锌刘一丹方芳
Owner KPC PHARM INC
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