Novel application of 2,4-dimethoxyl trans-stilben

A kind of technology of dimethoxy trans-stilbene and application, applied in the field of lipid-lowering and anti-senile dementia

Inactive Publication Date: 2010-12-22
THE INST OF BASIC MEDICAL SCI OF CHINESE ACAD OF MEDICAL SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] After checking the prior art literature, there is no report about the l

Method used

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  • Novel application of 2,4-dimethoxyl trans-stilben
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  • Novel application of 2,4-dimethoxyl trans-stilben

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] 2, the preparation of 4-dimethoxy trans stilbene (hereinafter referred to as S3)

[0050]

[0051] Compound 1 (benzylated bromide, 0.1mol) was reacted with slightly excess triethyl phosphite (0.125mol), the oil bath was heated to 120°C, and the reaction took about 3 hours until no gas escaped, and compound 2 (light yellow oily liquid).

[0052] Put the compound 2 (0.02mol) prepared in the previous step reaction in a 100ml round-bottom flask, place the reaction flask in an ice-water bath, add anhydrous tetrahydrofuran, add NaH (0.02mol) under stirring, react for 2 hours, add compound 3 (0.0126mol), after stirring for 2 hours, stir overnight at room temperature.

[0053] The reaction solution was filtered, the filtrate was concentrated until no THF was evaporated, and the solid was recrystallized from a solution of water: methanol at a ratio of 2:1 to obtain white needle crystals, which were compound 4, namely 2,4-dimethoxystilbene (S3 ), this step yield is 80.1%.

...

Embodiment 2

[0057] S3 vs Aβ 25-35 Protective Effect of Intracerebroventricular Injection Induced Memory Deficiency in Mice

[0058] (1) Experimental method

[0059] 1. Experimental animals Balb / c mice, female, 6 weeks old, were purchased from the Institute of Zoology, Chinese Academy of Medical Sciences.

[0060] 2. Drug dosage and grouping Divided into 4 groups: control group, model group, S3 high-dose group (50 mg / kg / day) obtained by using Example 1 of the present invention, S3 low-dose group (25 mg / kg / day). There were 15 animals in each group. Administration method: use 0.5wt% sodium carboxymethyl cellulose as a solvent to prepare the drug suspension of S3, and start intragastric administration from the day of operation, 0.2ml / monkey / day. The control group and the model group were gavaged with the same amount of vehicle.

[0061] 3. Aβ 25-35 Intraventricular injection Animals were kept in a clean animal room of the Institute of Basic Medical Sciences, Chinese Academy of Medical Sc...

Embodiment 3

[0091] S3 to high fat+Aβ 25-35 Protective Effect of Intracerebroventricular Injection Induced Memory Deficiency in Rats

[0092] (1) Experimental method

[0093] 1. Experimental animals: wistar rats, female, 180 g, purchased from the Institute of Zoology, Chinese Academy of Medical Sciences, license number: SCXK (Beijing) 2005-0013.

[0094] 2. Drug dosage and grouping: the animals were divided into 6 groups, which were normal control group, high-fat control group, and model group. The commercially available S3 high-dose group (50mg / kg / day), S3 middle-dose group (25mg / kg / day), S3 low-dose group (12.5mg / kg / day). There were 10 animals in each group.

[0095] 3. Aβ 25-35 Intraventricular injection: Animals were kept in a clean animal room of the Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences, and the feed and drinking water were sterilized. After all the animals were fed with ordinary feed for one week, all the animals were fed with high-fat feed f...

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Abstract

The invention relates to novel application of 2,4-dimethoxyl trans-stilben, in particular to novel application of 2,4-dimethoxyl trans-stilben for cutting fat and resisting senile dementia.

Description

technical field [0001] The invention relates to a new application of 2,4-dimethoxy-trans-stilbene, in particular to the application of 2,4-dimethoxy-trans-stilbene in reducing lipid and resisting senile dementia. Background technique [0002] Cardiovascular and cerebrovascular diseases are the number one killer threatening the health and life of all human beings. In China, about 2.6 million people die of cardiovascular and cerebrovascular diseases every year, and the incidence rate is still rising. Atherosclerosis (AS) can cause coronary heart disease, stroke, myocardial infarction and other diseases. Hyperlipidemia is a major independent risk factor in the pathogenesis of atherosclerosis. Hyperlipidemia refers to the blood total cholesterol (total cholesterol, TC), low density lipoprotein cholesterol (low density lipoprotein-cholestero, LDL-C) and triglyceride levels (triglyceride, TG) are higher than the normal range and / or low levels of high density lipoprotein chole...

Claims

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Application Information

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IPC IPC(8): A61K31/09A61P3/06A61P25/28
Inventor 孙兰李展陈迪华斯建勇阮灿军骆庆峰
Owner THE INST OF BASIC MEDICAL SCI OF CHINESE ACAD OF MEDICAL SCI
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