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Novel method for preparing catalpol medicament composition containing the same and uses thereof

A new method and composition technology, applied in the preparation of catalpol and its pharmaceutical composition and application field, can solve the problems such as yield decline, separation and purification difficulties, easy oxidation of catalpol, etc.

Inactive Publication Date: 2008-07-16
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the easy oxidation of catalpol during the heating and extraction process, the yield decreased; at the same time, due to the use of a large amount of ethanol solution, more impurities were raised, which increased the difficulty of separation and purification in the later stage
Rehmannia glutinosa has the functions of clearing away heat and nourishing yin, cooling blood and stopping bleeding. Domestic research on the biological activity of catalpol contained in it mainly focuses on the effect on blood sugar, and there is no application and mechanism research on Parkinson's disease and Alzheimer's disease. report

Method used

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  • Novel method for preparing catalpol medicament composition containing the same and uses thereof
  • Novel method for preparing catalpol medicament composition containing the same and uses thereof
  • Novel method for preparing catalpol medicament composition containing the same and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The preparation method of catalpol:

[0038] Add 100 kilograms of dry rehmannia glutinosa (Rehmannia glutinosa Libosch.) into the rotary grid of a flat-rotating continuous countercurrent extractor, add 10 times of 80% ethanol solution, and percolate at room temperature, and control the percolation flow rate to be 20ml / min; extract the rehmannia glutinosa Libosch. The solution was concentrated under reduced pressure to extractum, dispersed with water according to the amount of extract: water (1:2.5), and extracted with 5 times the amount of petroleum ether and 5 times the amount of ethyl acetate to remove impurities; the aqueous solution was added to H103 macroporous adsorption On the resin column, the ratio of the extract to the dry resin is 1:25. After fully absorbing for 2 hours, wash with water until the color is light, and replace it with 5000ml gradient washes of 10%, 20%, 30%, 50%, and 80% ethanol solutions. 80% ethanol fraction was collected; the collected fracti...

Embodiment 2

[0062] Effects of Catalpol on Parkinson's Disease Cell Model:

[0063] 1 Cell Morphological Analysis and Immunohistochemical Methods

[0064] ① Culture of pure neurons in mouse midbrain

[0065] KM mouse embryos with a gestational age of 14 days were removed under aseptic operation, the ventral midbrain was isolated, and then gently mechanically blown in DMEM / F12 to break up the tissue. The cell suspension after mechanical separation was centrifuged at 1500r for 10min to remove tissue cell debris. The supernatant was discarded, and the resuspended cells were counted and seeded into poly-lysine (20 μg / ml) pre-coated 24-well culture plates at a cell seeding density of 5×10 5 / hole. In this study, DMEM / F12 plus 10% inactivated fetal bovine serum, 100U / ml penicillin and 100U / ml streptomycin were used as cell culture medium. After 48 hours of cell culture, 10 μM Mβ-arabinofuranoside (β-D-arabinofuranoside) was added to inhibit glial cell proliferation. After another 48 hours, ...

Embodiment 3

[0071] Effects of catalpol on animal models of Parkinson's disease:

[0072] ICR mice (male), ten weeks old, were randomly divided into 3 groups. Blank control group, model group and catalpol treatment group. In the first 1-7 days, the mice in the blank control group and the catalpol-treated group were injected with normal saline; the mice in the Parkinson's model group were injected with MPTP (30 mg / kg). On days 8-14, catalpol (15 mg / kg) was intraperitoneally injected into catalpol-treated mice, and normal saline was injected intraperitoneally into mice in the other two groups. 24 hours after the last drug injection, the chest was opened, perfused, and the brain was removed after anesthesia.

[0073] The experimental results are as shown, a large number of TH-ir positive neurons can be seen in the substantia nigra pars compacta (Figure 5) of the control group injected with normal saline, arranged in a dense network; compared with the control group, the injection of MPTP Th...

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Abstract

The invention relates to a new preparation method of catalpol of general formula (I), wherein R1 is a monosaccharide; R3, R4, R5 and R8 are H; while R6 is OH and R7 is -OCH2OH. The invention also relates to the application of the compound and the drug combination thereof in the prevention and treatment of Alzheimer disease and Parkinson disease, which provides the new preparation method of the compound and the drug combination thereof for researching and developing new drugs against the Alzheimer disease and the Parkinson disease, being beneficial to further develop natural pharmaceutical resources.

Description

technical field [0001] The present invention relates to a new preparation method of catalpol and its application in anti-Parkinson's disease and senile dementia. Background technique [0002] Rehmannia glutinosa Libosch. is a plant of Scrophulariaceae, mainly distributed in Henan Province, and also produced in Liaoning, Hebei, Shandong and Zhejiang. The use of fresh or dried roots of Rehmannia glutinosa as medicine was first recorded in "Shen Nong's Materia Medica", and it is also recorded in many modern classics. Fresh Rehmannia glutinosa is cold in nature, sweet and bitter in taste, and has the functions of clearing heat and cooling blood, moisturizing dryness and promoting body fluid; dried Rehmannia glutinosa is cold in nature, sweet and bitter in taste, has the functions of clearing heat and nourishing yin, cooling blood and stopping bleeding. The chemical components of Rehmannia glutinosa mainly contain iridoids, stachyose, β-sitosterol, mannitol, campesterol and argi...

Claims

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Application Information

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IPC IPC(8): C07H17/04A61K31/7048A61P25/28A61P25/16
Inventor 姜波姜涛包永明赵荣国毕静安利佳
Owner DALIAN UNIV OF TECH
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