Preparation method and application of nanoparticles capable of inhibiting Aβ polypeptide aggregation and scavenging active oxygen

A nanoparticle, active oxygen technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, powder delivery, etc., can solve the problems of low water solubility and low bioavailability of resveratrol, and achieve a stable product system, Improves biological activity and reduces oxidative damage

Inactive Publication Date: 2020-11-27
JIANGXI AGRICULTURAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In order to overcome the shortcomings and deficiencies of the above-mentioned prior art, the primary purpose of the present invention is to provide a nanoparticle that can inhibit the aggregation of Aβ polypeptide induced by metal ions and scavenge active oxygen, in order to solve the problem of low water solubility of resveratrol in polyphenols and Disadvantages such as low bioavailability

Method used

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  • Preparation method and application of nanoparticles capable of inhibiting Aβ polypeptide aggregation and scavenging active oxygen
  • Preparation method and application of nanoparticles capable of inhibiting Aβ polypeptide aggregation and scavenging active oxygen
  • Preparation method and application of nanoparticles capable of inhibiting Aβ polypeptide aggregation and scavenging active oxygen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1 Preparation of resveratrol nano-selenium

[0039] 1) Weigh 0.173 g of sodium selenite, dilute to 10 mL with distilled water to prepare 0.1 mol / L storage solution; at the same time, weigh 0.143 g of resveratrol, dilute to 25 mL with 60% ethanol to prepare 0.025 mol / L storage solution; weigh 0.0378g of sodium borohydride, and dilute to 10 mL with distilled water to prepare a 0.1 mol / L storage solution.

[0040] 2) Mix 0.2 mL sodium selenite stock solution with different proportions of resveratrol, stir at 400 rpm / min, adjust the reaction temperature range to 25-50 °C, and the pH range to 2-12. Gradually add different proportions of sodium borohydride dropwise, and continue stirring for 10 to 60 minutes. The molar ratios of sodium selenite to resveratrol or sodium borohydride are 1:1, 1:2, 1:3, 1:4, 1:5, 1:6, 1:7, 1:8, respectively. Among them, at 35°C and pH 6, the sample with a molar ratio of sodium selenite to resveratrol of 1:4 was the most stable, whil...

Embodiment 2

[0041] Example 2 Inhibitory Effect of Resveratrol Nano-Selenium on Aβ42 Polypeptide Aggregation Induced by Metal Ions

[0042] Take 35 μM Aβ42 polypeptide and 70 μM CuCl 2 and different concentrations of resveratrol and the resveratrol nano-selenium prepared in Example 1 were incubated for 0-5 days. Take 50 μL from the incubation solution every day and mix it with 200 μL 15 μM ThT and incubate in the dark for 15 min. The fluorescence intensity of ThT was detected on a fluorescence spectrophotometer. ThT has an excitation wavelength of 440 nm and an emission wavelength of 490 nm. Experimental results such as figure 2 As shown, resveratrol could not significantly inhibit the aggregation of Aβ42 polypeptide induced by metal ions, and ThT fluorescence remained at a relatively high intensity. As the concentration of resveratrol nano-selenium increases, the fluorescence of ThT decreases, and the lag period of metal ion-induced Aβ42 polypeptide aggregation also prolongs, indicat...

Embodiment 3

[0043] Example 3 Effect of Resveratrol Nano-Selenium on Metal Ion-Induced Aβ42 Aggregation Form

[0044] Take 35 μM Aβ42 and 70 μM CuCl 2 and different concentrations of resveratrol and the resveratrol nano-selenium prepared in Example 1 were incubated for 3 days. Take 10 μL of the incubation solution and drop it on the copper grid, let it dry for 10 minutes, then add 5 μL of 1.5% (w / v) phosphotungstic acid dropwise for staining. Then, the effects of resveratrol nano-selenium on metal ion-induced Aβ42 aggregation morphology were observed on the transmission electron microscope. Experimental results such as image 3As shown, metal ions can induce Aβ42 aggregation, and blocky Aβ42 aggregates can be observed. Resveratrol could not significantly inhibit the aggregation of Aβ42 polypeptide induced by metal ions, while resveratrol nano-selenium could significantly inhibit the aggregation of Aβ42 polypeptide induced by metal ions, and only a small amount of aggregation was observe...

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Abstract

The invention relates to the field of preparation of nano-selenium medicines, and specifically discloses a preparation method and application of nanoparticles capable of inhibiting Aβ polypeptide aggregation and removing active oxygen. The nano particle is nano selenium modified by resveratrol. Resveratrol has the ability to scavenge reactive oxygen species, but its water solubility is low and its ability to inhibit metal ion-induced Aβ aggregation is weak. The resveratrol nano-selenium prepared by the present invention, compared with resveratrol as a modifier, resveratrol nano-selenium can not only inhibit the aggregation of Aβ induced by metal ions, but also has the effect of scavenging active oxygen, which can be applied to the preparation of Anti-Alzheimer's syndrome drugs. The product system in the invention is simple, the method is simple and convenient, and the product can be directly stored and used. The nano-selenium selected in the present invention greatly improves the problems of low water solubility and low bioavailability of resveratrol, and increases the ability of resveratrol to inhibit the aggregation of Aβ induced by metal ions.

Description

technical field [0001] The invention relates to the field of nano-selenium medicine preparation, in particular to a resveratrol nano-selenium medicine and its preparation method and application. Background technique [0002] Alzheimer's disease (AD) is a common neurodegenerative disease, and its clinical manifestations are mainly the decline of memory function and cognitive ability. In China, with the increasing problem of population aging, the incidence of AD has also increased significantly. Because the severity of AD has greatly affected the quality of life of patients and their families, the development of AD drugs is very necessary and urgent. The main pathological features of AD are amyloid plaques and fibrillary tangles in neuronal cells found in the brain. Among them, amyloid plaque is a well-established neuropathological sign of AD. Aβ polypeptide is the main component of amyloid plaques. Although the pathogenic mechanism of AD is not yet clear, the amyloid depo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K33/04A61K31/05
CPCA61K9/14A61K31/05A61K33/04A61P25/28A61P39/06A61K2300/00
Inventor 杨丽聪郑国栋
Owner JIANGXI AGRICULTURAL UNIVERSITY
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