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Application of benzoylated phaeophyceae polysaccharide for preparing medicines for treating Parkinson disease

A technology for benzoylation of fucoidan and Parkinson's disease, which can be used in drug combinations, pharmaceutical formulations, nervous system diseases, etc., and can solve problems such as adverse reactions, limited application and promotion

Inactive Publication Date: 2011-01-12
QINGDAO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the shortcomings of the prior art. In view of the common adverse reactions of traditional anti-PD drugs, which seriously limit its application and promotion, it aims to provide a kind of benzoylated fucoidan in the preparation of PD treatment. Application in Kinson's Disease Drugs

Method used

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  • Application of benzoylated phaeophyceae polysaccharide for preparing medicines for treating Parkinson disease
  • Application of benzoylated phaeophyceae polysaccharide for preparing medicines for treating Parkinson disease
  • Application of benzoylated phaeophyceae polysaccharide for preparing medicines for treating Parkinson disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1: Preparation of benzoylated fucoidan (PF)

[0017] 1. Synthesis of PF

[0018] Weigh 2g of natural fucoidan (derived from kelp) and dissolve it in 80ml of formamide, stir at 80°C for 30min, dissolve 20g of phthalic anhydride in 1% N-bromosuccinimide (NBS ) into 100ml of formamide, dropwise added to the fucoidan solution, and reacted for 6 hours; after the reaction, pour out the reaction solution, precipitate with 85% alcohol, wash the precipitate with 95% alcohol for 1-2 times, and dissolve the precipitate in 100 -200ml distilled water, 3600 Dalton (Da) dialysis bag tap water dialysis for 2 days, distilled water dialysis for 1 day, concentrated and freeze-dried, recorded as PF. Whether the benzoylation was successful was detected by infrared (IR) spectrum.

[0019] 2. Determination of phthalic acid group content

[0020] Preparation of phthalate standard curve: Accurately weigh 50mg of phthalic acid, prepare 10ml solution with saturated NaOH, take 3, 2, ...

Embodiment 2

[0026] Example 2: PF can counteract the toxic effect of neurotoxin 6-OHDA

[0027] 1. MTT assay for cell viability

[0028] MES23.5 dopaminergic cells in the logarithmic growth phase (gifted by Prof. Le Weidong, Baylor College of Medicine, Houston, USA), were blown to make a single-cell suspension, centrifuged, and diluted with complete medium to 2×10 5 cells / ml cell suspension, inoculated in 96-well plate with 200 μl per well, placed at 37°C, 5% CO 2 cultured in an incubator. Add PF (1 mg / ml, 0.1 mg / ml, 0.01 mg / ml, 0.001 mg / ml) and 6-OHDA ( 100 μmol / L) for 24 hours. Then 20 μl of 5 mg / ml 3-(4,5-dimethylthiazole-2)-2,5-diphenyltetrazolium bromide (MTT) was added to each well, and cultured in a 37° C. incubator for 4 hours. After the supernatant was discarded, 200 μl of dimethyl sulfoxide (DMSO) was added to each well, and an automatic enzyme label reader (R-T-2100C, Shenzhen Redu Company) was used for colorimetry (main wavelength 573nm, secondary wavelength 630nm), and the...

Embodiment 3

[0054] Example 3: PF can counteract the toxic effects of high iron

[0055] 1. MTT assay for cell viability

[0056] MES23.5 dopaminergic cells in the logarithmic growth phase were blown and blown to make a single-cell suspension, centrifuged, and diluted with complete medium to 2×10 5 cells / ml cell suspension, inoculated in 96-well plate with 200 μl per well, placed at 37°C, 5% CO 2 cultured in an incubator. After adherence, PF (1 mg / ml) and iron (1 mmol / L) were added to co-culture for 24 hours. Then 20 μl of 5 mg / ml MTT was added to each well, and cultured in a 37° C. incubator for 4 hours. After discarding the supernatant, add 200 μl of DMSO to each well, measure the absorbance value with an automatic microplate reader (primary wavelength 573 nm, secondary wavelength 630 nm), and calculate the survival rate of MES23.5 cells in each group.

[0057] Cell survival rate=(absorbance value of experimental group-absorbance value of blank group) / (absorbance value of negative co...

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Abstract

The invention relates to application of benzoylated phaeophyceae polysaccharide for preparing medicines for treating Parkinson disease, which is characterized in that 1mg / ml of the benzoylated phaeophyceae polysaccharide has the action on protecting nerves and can resist the cell damage induced by neurotoxin 6-hydroxy dopamine and high ferrum and reduce the generation of reactive oxygen substances in the cells induced by the neurotoxin 6-hydroxy dopamine and high ferrum; the benzoylated phaeophyceae polysaccharide is prepared from natural phaeophyceae polysaccharide by benzoylation; the natural phaeophyceae polysaccharide comes from other phaeophyceaes of kelp seaweeds or gulfweeds, sea mustards, sargassum fusiforme, sargassum thunbergii kuntze, sargassum kjellmanianum, kelp, and the like; the phaeophyceae polysaccharide has the advantages of rich sources and high safety; and the phaeophyceae polysaccharide has the protection action on the cell damage induced by neurotoxin and high ferrum. The invention has an important application value on developing a novel I-class natural medicine for treating Parkinson disease in China.

Description

Technical field: [0001] The present invention relates to the application of benzoylated fucoidan in the preparation of drugs for the treatment of Parkinson's disease, in particular to the use of benzoylated fucoidan in the treatment of Parkinson's disease, which can resist the toxic effects of neurotoxins and high iron on dopaminergic neurons application. It belongs to the field of medical technology. Background technique: [0002] With the intensification of the aging process of the world population, neurodegenerative diseases have become one of the diseases that seriously endanger human health. Parkinson's disease (PD) is the second most common neurodegenerative disease after senile dementia. reduce. The pathogenesis of PD has not yet been studied clearly, and high iron in the substantia nigra is an important reason for the death of dopaminergic neurons. PD will not only affect the quality of life of the patient, but also cause a huge mental and economic burden to the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/737A61P25/16A61P25/00
Inventor 谢俊霞张全斌姜宏宋宁
Owner QINGDAO UNIV
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