Beta-sitosterol derivative as well as preparation method and application thereof

A technology of β-sitosterol and its derivatives, which is applied in the field of β-sitosterol derivatives and its preparation, can solve the problem of the solubility of β-sitosterol and the specific combination of β-sitosterol derivatives and avidin to construct nanoparticles, etc. problems, to achieve good clinical application prospects, convenient blood vessel administration, and convenient preparation of pharmaceutical dosage forms

Active Publication Date: 2020-07-17
湖南省中医药研究院
View PDF2 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The most important thing is that so far, there has been no report of improving the solubility of β-sitosterol throu

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Beta-sitosterol derivative as well as preparation method and application thereof
  • Beta-sitosterol derivative as well as preparation method and application thereof
  • Beta-sitosterol derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1 Preparation of β-sitosterol derivatives (B-BS) of the present invention

[0037] Dissolve β-sitosterol (0.15mmol) in 60ml of DMSO, under the action of dehydrating agent DCC (3.0mmol) and catalyst DMAP (3.0mmol), stir at 0°C for 6h; then add β-sitosterol at a molar ratio of 1:3 For biotin (B), raise the temperature from the ice bath to room temperature 25°C, and stir overnight in the dark. Concentrate the filtrate, recrystallize with glacial ether or isopropanol, purify by chromatography or preparative liquid phase, and freeze-dry to obtain the β-sitosterol derivative B-BS (yield is about 48%). The ion peak identified by mass spectrometry [M+H ] + For: 642.1.

[0038] 1 HNMR (400MHz, DMSO): The characteristic peaks of biotin: 10.76-10.82 (NH, 2H, broad peak), 4.47-4.65 (2C-H, 2H), 2.80-3.10 (CH 2 , 2H), 3.24(CH, 1H), 2.32(CH 2 , 2H), 1.23-1.68 (3CH 2 , 6H); The characteristic peak of β-sitosterol: 0.85-0.88 (4CH 3 , 12H), 0.99-1.03 (CH 3 , 3H), 1.08-...

Embodiment 2

[0042] Preparation of embodiment 2β-sitosterol derivative avidin nanoparticles

[0043] Get the β-sitosterol derivative (B-BS) that is equivalent to β-sitosterol 5g and prepare through embodiment 1, be dissolved in a small amount of DMSO or ethanol earlier, dilute with water for injection then, add sodium chloride 1.0g, then Add equimolar avidin (the assembly of B-BS and avidin can be assembled according to various molar ratios of 1-4:1, such as figure 2 shown), stir evenly at room temperature to obtain composite β-sitosterol derivative avidin nanoparticles, characterized by transmission electron microscopy, its nanometer size is about 25nm (such as image 3 shown).

Embodiment 3

[0044] The preparation of embodiment 3β sitosterol derivatives injection

[0045] Take the β-sitosterol derivative (B-BS) prepared by Example 1 in an amount equal to 30 g of β-sitosterol, dissolve it in water for injection, add 5.0 g of sodium chloride and stir evenly, dilute hydrochloric acid to adjust the pH=5.0, and then add 0.5% activated carbon for injection, keep the temperature at 60°C for 30 minutes, after decarbonization, add water for injection to the filtrate to 1000ml, filter through a 0.22μm sterile filter membrane, pack 2ml / branch into glass curved neck ampoules, melt seal, and circulate at 100°C Steam damp heat sterilization for 40 minutes, and then label and store.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention belongs to the technical field of biological medicines, and discloses a beta-sitosterol derivative as well as a preparation method and application thereof. The beta-sitosterol derivativecan be assembled with avidin to form nanoparticles. Animal tests prove that the beta-sitosterol derivative and the nano-drug thereof can obviously reduce the sleep latency time of mice, significantlyimprove the sleep time and the subthreshold hypnotic sleep rate of the mice, can effectively improve the sleep quality of the mice, and can be used for further preparing drugs or health products forimproving the sleep quality.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a β-sitosterol derivative and a preparation method and application thereof. Background technique [0002] Due to the influence of factors such as work pressure, social competition, and population aging, 45.4% of the population in our country has sleep disorders, which is directly proportional to anxiety disorders. About 35% of people in the United States have had sleep disorders, 17% of patients believe that insomnia seriously affects their lives, and 85% of patients believe that they have not received effective treatment. Sleep disorders seriously affect people's quality of life and work efficiency. Studies have shown that sleep disorders can lead to physical and mental retardation, memory loss, and decreased immunity. Persistent sleep disturbance is a risk factor for depressed patients and one of the early clinical symptoms of schizophrenia and other mental dis...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): C07J43/00C07J9/00A61K31/58A61K47/54A61K9/51A61P25/20A23L33/11
CPCA23V2002/00A61K9/5123A61K47/545A61P25/20C07J9/00C07J43/003A23V2200/31
Inventor 万丹郭新红张水寒曹科曾宏亮彭咏波李雄周融融
Owner 湖南省中医药研究院
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap