A quercetin-modified nano-sulfur and its preparation method and application in anti-Alzheimer's disease drugs

A technology of quercetin and nano-sulfur, which is applied in the direction of drug combination, drug delivery, and medical preparations of non-active ingredients, etc., can solve the problems of reducing drug efficacy and low blood-brain barrier penetration, and achieve improved drug efficacy and inhibition Effects of endoplasmic reticulum stress, ease of storage and use

Active Publication Date: 2020-06-16
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

General AD treatment drugs have low penetration ability to the blood-brain barrier (BBB), thus limiting their effect on the brain of patients and reducing drug efficacy

Method used

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  • A quercetin-modified nano-sulfur and its preparation method and application in anti-Alzheimer's disease drugs
  • A quercetin-modified nano-sulfur and its preparation method and application in anti-Alzheimer's disease drugs
  • A quercetin-modified nano-sulfur and its preparation method and application in anti-Alzheimer's disease drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] This embodiment provides a quercetin-modified nano-sulfur and a preparation method thereof, and a pharmaceutical preparation containing the quercetin-modified nano-sulfur and a preparation method thereof.

[0050] A quercetin-modified nano sulfur and its preparation method:

[0051] Mix 2.5 mL of 4 mM quercetin aqueous solution and 2.5 mL of 100 mM methionine aqueous solution, add 2 mL of 0.1 M vitamin C (Vc) aqueous solution, and then slowly drop 5 mL of 10 mM under ultrasonic conditions Sodium thiosulfate solution, the mixed solution was obtained, and the reaction was observed. The color of the solution changed from transparent to light white. The ultrasonic reaction was continued for 20 minutes. The precipitate was obtained by centrifugation and washed three times with distilled water to obtain quercetin-modified nano-sulfur (Qc@SNPs ).

[0052] A pharmaceutical preparation containing the above-mentioned quercetin-modified nano-sulfur and a preparation method thereof:

[00...

Embodiment 2

[0058] This embodiment provides a quercetin-modified nano-sulfur and a preparation method thereof, and a pharmaceutical preparation containing the quercetin-modified nano-sulfur and a preparation method thereof.

[0059] Mix 2.5 mL of a 3.2 mM quercetin aqueous solution and 2.4 mL of a 50 mM methionine aqueous solution, add 1.8 mL of a 0.05 M vitamin C (Vc) aqueous solution, and then slowly drip 5 mL under ultrasonic conditions. 6mM sodium thiosulfate solution to obtain a mixed solution, the reaction was observed, the color of the solution changed from transparent to light white, the ultrasonic reaction was continued for 15 minutes, the precipitate was obtained by centrifugation, and washed with distilled water three times to obtain quercetin-modified nano-sulfur (Qc @SNPs).

[0060] A pharmaceutical preparation containing the above-mentioned quercetin-modified nano-sulfur and a preparation method thereof:

[0061] Add 30 mL of 0.16 mM quercetin-modified nano-sulfur aqueous solution...

Embodiment 3

[0063] This embodiment provides a quercetin-modified nano-sulfur and a preparation method thereof, and a pharmaceutical preparation containing the quercetin-modified nano-sulfur and a preparation method thereof.

[0064] Mix 2.5 mL of 5 mM quercetin aqueous solution and 2.5 mL of 180 mM methionine aqueous solution, add 2 mL of 0.3 M vitamin C (Vc) aqueous solution, and then slowly drop 5 mL of 15 mM under ultrasonic conditions Sodium thiosulfate solution, the mixed solution was obtained, and the reaction was observed. The color of the solution changed from transparent to light white. The ultrasonic reaction was continued for 30 minutes, the precipitate was obtained by centrifugation, and washed with distilled water three times to obtain quercetin-modified nano-sulfur (Qc@SNPs ).

[0065] A pharmaceutical preparation containing the above-mentioned quercetin-modified nano-sulfur and a preparation method thereof:

[0066] Add 30 mL of a 0.3mM quercetin-modified nanosulfur aqueous solut...

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Abstract

The invention belongs to the technical field of preparation of drugs, and specifically relates to quercetin-modified nano sulfur as well as a preparation method and application thereof to an anti-AD (Alzheimer's Disease) drug. According to the preparation method disclosed by the invention, quercetin is modified on nano sulfur by utilizing the microsize and a high surface energy effect of nano sulfur, not only a function of the quercetin for reducing endoplasmic reticulum stress in cells of the quercetin is utilized, but also the water solubility is improved, so that quercetin-modified nano sulfur integrating high biocompatibility and an AD treatment effect is obtained. The quercetin-modified nano sulfur is further embedded in a microbubble shell prepared from alpha-butyl cyanoacrylate by adopting a one-pot method, so that a drug preparation containing quercetin-modified nano sulfur is prepared; microbubbles of the drug preparation can be destroyed under ultrasonic action, sonoporationcan be generated, a blood brain barrier can be temporarily opened, and quercetin-modified nano sulfur can further enter the brain by penetrating through the blood brain barrier so as to take a treatment effect, so that high brain targeting performance is obtained. The preparation method of the drug preparation is simple, and products are convenient to preserve and use.

Description

Technical field [0001] The invention belongs to the technical field of medicine preparation, and specifically relates to a quercetin-modified nano-sulfur, a preparation method thereof, and application in anti-Alzheimer's disease medicine. Background technique [0002] Alzheimer's disease (AD) is a common neurodegenerative disease. Because its pathogenesis is very complicated, its therapeutic drugs are very limited, and treatment is still difficult. At present, the pathogenesis of Alzheimer's disease is generally recognized in two points. First, the abnormal accumulation of amyloid (Aβ) is believed to be closely related to the pathogenesis of AD. Second, the endoplasmic reticulum is an important organelle, responsible for protein processing and folding, such as the formation of disulfide bonds and protein glycosylation. However, when the internal and external environment of the cell is disturbed, the unfolded protein response (UPR) or misfolded protein will accumulate in the en...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/55A61K33/04A61P25/28A61K9/127A61K47/32A61K41/00A61K31/352
CPCA61K9/0009A61K9/1273A61K31/352A61K33/04A61K41/0028A61K47/32A61K47/55A61P25/28A61K2300/00
Inventor 刘杰谢文杰
Owner JINAN UNIVERSITY
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