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Novel iridoid compound with anti-Alzheimer's disease function

A technology of iridoids and compounds, which is applied in the field of iridoids and can solve the problems of unclear anti-senile dementia active substances

Inactive Publication Date: 2009-07-22
BEIJING JOEKAI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Recent studies have reported that Coptidis detoxification decoction (Coptis chinensis, Cortex Phellodendron, Scutellaria baicalensis, Gardenia) with Zhizi formula has the effect of anti-senile dementia [7，8] , but the anti-senile dementia active substance of Huanglian Jiedu Decoction is still unclear and needs further research

Method used

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  • Novel iridoid compound with anti-Alzheimer's disease function
  • Novel iridoid compound with anti-Alzheimer's disease function
  • Novel iridoid compound with anti-Alzheimer's disease function

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0129] Part 1: Extraction and separation of iridoids from Scrophulariaceae

[0130] Get 18 kg of dried root of Scrophulariaceae plant Scrophularia ningpoensis Hemsl, heat and reflux extraction with 60% ethanol, concentrate the extract, use ethyl acetate and n-butanol to carry out equal-volume extraction for 3 times, and the n-butanol extraction part passes through D101 macroporous resin column, gradient elution with water, 30% ethanol, 50% ethanol and 95% ethanol. 50.2 g of the fraction eluted with 50% ethanol was chromatographed on a silica gel column, chloroform-methanol 95:5-70:30 gradient elution, and SN-9 (14 g) was obtained; the subfraction Fr.1-Fr.7 (3.9 g), ODS column, methanol-water 40:60 elution, and reverse HPLC, methanol-water 35:65 elution, to obtain SN-2 (117.1mg), SN-6 (17.9mg), SN-7 (10.1 mg), SN-8 (28.2mg), sub-fraction Fr.5 (6.1g) was eluted by reverse HPLC, methanol-water 50:50 to obtain compound SN-3 (237.6mg), SN-4 (110.1mg ), SN-5 (13.0 mg). 51.4g of t...

Embodiment 2

[0340] Part 1: Extraction and separation of iridoids from Gardenia

[0341] Get 5kg of dried fruit of Gardenia jasminoides Ellis (Gardenia jasminoides Ellis), heat reflux with 60% ethanol to extract, concentrate the extract, suspend the obtained extract in water, pass through a D101 macroporous resin column, wash with water, 30%, 50% , 70% and 95% ethanol gradient elution. The fraction eluted with 50% ethanol was subjected to silica gel column chromatography (200-300 mesh) and eluted with a gradient of chloroform-methanol-water (100:0:0) to methanol. Subfraction Fr7 (9g) was chromatographed by ODS column, methanol-water (10:90-90:10) gradient elution, subfraction Fr.1 was passed through Toyopearl HW-40 column, methanol-water (20:80-80:20 ) gradient elution, followed by reverse HPLC, methanol-water 40:60 elution, purified to obtain GJ-1 (6mg), GJ-4 (28.9mg), GJ-5 (45mg), GJ-6 (22.0mg ); Subfraction Fr.3 was purified by Toyopearl HW-40 column, methanol-water (20:80-80:20) grad...

Embodiment 3

[0431] Example 3: Preparation of pharmaceutical composition in tablet form

[0432] composition:

[0433] Compound SN-1 0.5 g

[0434] Compound SN-2 0.5 g

[0435] 150g compressible starch

[0436] 17% starch slurry appropriate amount

[0437] Magnesium Stearate 1.8g

[0438] Preparation steps: mix SN-1 and SN-2 with starch evenly, add starch slurry to make a soft material, granulate, dry at 80°C, sieve with 12 meshes, add magnesium stearate and mix, single Tablet pressing with a tablet machine, ready to be obtained.

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Abstract

The invention discloses a serial of iridoids compounds with the structural formula (I), the application of the compounds in preparing medicaments applied to the prevention or treatment of nervous system degenerative disorders such as senile dementia and the like, the medical compositions containing the compounds and a preparation method of the compounds. The structural formula is as shown above, wherein, various groups are defined in the instruction.

Description

technical field [0001] The invention relates to the application of a series of iridoid compounds in preventing neurodegenerative diseases such as senile dementia. Using Gardenia and Scrophulariaceae as raw materials, a series of iridoid compounds were obtained by various separation methods, and the activity of anti-senile dementia drugs was screened using transgenic fruit flies as a model. The results showed that these compounds can effectively improve the aging The learning and memory ability of dementia transgenic fruit flies shows that these compounds have obvious effects on treating neurodegenerative diseases such as Alzheimer's disease and have good research and development prospects. Background of the invention [0002] Alzheimer's disease is a degenerative disease of the central nervous system mainly characterized by progressive cognitive impairment and memory impairment [1] . The patient's quality of life is low, the course of the disease is long, and special perso...

Claims

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Application Information

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IPC IPC(8): C07H17/04A61K31/7048A61P25/28
Inventor 姚新生钟毅高昊谢作磊于洋柳婷陈斌袁野戴毅黄蓝
Owner BEIJING JOEKAI BIOTECH
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