A kind of water-soluble staphylophyllin polymer

A technology of escarpusin and bonding compound, which is applied in the field of water-soluble escarpusin polymer products, can solve the problems of unsatisfactory anti-cancer effect, weak pharmacological effect, weak selectivity, etc., and achieves improved curative effect and good water solubility. , the effect of improving solubility

Active Publication Date: 2019-05-28
FUJIAN HEALTH COLLEGE
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the research hotspot of staphylophyllin is the development of its anti-tumor activity and its inhibitory effect on tumor cells in vitro. However, in the research, some scholars have found that the anti-cancer effect of staphylophyllin in vivo is not ideal. The reasons for the analysis may be as follows Points: 1. Poor solubility; 2. Poor stability; 3. Belonging to flavonoid alcohol compounds, there are many shortcomings such as more targets, weak selectivity, and weak pharmacological effects

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
  • A kind of water-soluble staphylophyllin polymer
  • A kind of water-soluble staphylophyllin polymer
  • A kind of water-soluble staphylophyllin polymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1: Preparation of small molecule γ-polyglutamic acid sodium salt

[0076] Take 100g of biosynthesized polymer γ-polyglutamic acid (γ-PGA, the molecular weight is about 2 million, the synthesis method refers to the existing technical literature [12]) and dissolve it in 500ml distilled water, add 3 times the volume of absolute ethanol, statically The γ-PGA precipitate was obtained, redissolved in water, ultra-filtered to remove insoluble matter, and the precipitate was freeze-dried to obtain white block γ-PGA.

[0077] Take 10g of the above γ-PGA with distilled water to make 2% (2g of PGA add water to 100ml) γ-PGA aqueous solution, adjust the pH to about 2-3 with hydrochloric acid, apply high temperature and high pressure (121°C, 0.1MPa) for 20min, and immediately ice bath Cool, adjust the pH to 7-8 with NaOH, and freeze-dry to obtain the white cotton flocculent small molecule γ-PGA sodium salt. γ-PGA sodium salt was made into 2% γ-PGA sodium salt aqueous solutio...

Embodiment 2

[0078] Example 2: Synthesis of γ-PGA-AMP

[0079] Take staphylophyllin (0.59g, about 1.8mmol) and dissolve it in 20ml dimethyl sulfoxide, stir and dissolve at room temperature, take 0.37g (about 1.8mmol) of dicyclohexylcarbodiimide (DCC), add 0.1gDMAP , then add 180ml of dimethyl sulfoxide solution containing γ-PGA (1.24g, about 9.37mmol), put it in a collector type magnetic stirrer, 40°C, after the reaction is carried out for 3h, TLC is used to monitor the reaction process, and the reaction is carried out for 24h. The monitoring results showed that the staphylocoxine was completely converted into the polymer conjugate. Add 10 times of diethyl ether to the reaction solution to wash, oscillate, and stand overnight at 4°C. The solution is divided into two layers, extracted, and the lower layer of light yellow solution is collected. The γ-PGA-AMP reaction solution was freeze-dried to obtain 1.02 g of a yellow powder product with a yield of 55.7%.

[0080] The polyglutamic acid ...

Embodiment 3

[0089] Embodiment 3: In vitro cytotoxicity test of polyglutamic acid steroid

[0090] Cell lines and culture: Human breast cancer cell MCF-7, human liver cancer cell HepG-2, and human lung cancer cell A549 were cultured in inactivated newborn bovine serum containing 10% by volume, 1x10 5 U•L -1 Penicillin and 100mg•L -1 Streptomycin in RPMI-1640 medium, placed at 37°C, CO 2Cultured in an incubator with a content of 5%. After 2-3 days, replace the medium by centrifugation or subculture, and take the cells in the logarithmic growth phase for experiments.

[0091] Staphylococcus was prepared with serum-free culture medium to a concentration of 200μg•mL -1 The solution is sterilized by filtration with a 0.22μm microporous membrane, ready to use. γ-PGA-AMP is also directly dissolved in serum-free culture medium to make 200μg•mL -1 The concentration required for the solution experiment is sterilized by filtration with a 0.22 μm microporous membrane, and it is ready-to-use. Th...

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

PropertyMeasurementUnit
molecular weightaaaaaaaaaa
molecular weightaaaaaaaaaa
Login to view more

Abstract

The invention discloses a water-soluble ampelopsin polymer. The polymer can be used for treating cancer, inhibiting bacteria, protecting the liver, lowering blood sugar and lowering blood fat and contains composition, namely, PGA-AMP, of a medicine conjugated with a water-soluble polymer selected from poly-1-glutamic acid, poly-d-glutamic acid and poly-d-1-glutamic acid. According to a preparation method of the water-soluble ampelopsin polymer product, polyglutamic acid and ampelopsin react to produce a polyglutamic acid derivative under the action of a condensation agent and a catalyst, the condensation agent is 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride and / or N-hydroxysuccinimide and / or dicyclohexylcarbodiimide, and the catalyst is 4-dimethylamino-pyridine. The polymer can be used for treating cancer, bacterial infection, liver diseases, hyperglycemia and hyperlipidemia.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a water-soluble staphylophyllin polymer product used for treating tumors, inhibiting bacterial infection, protecting the liver, lowering blood sugar and blood fat. Background technique [0002] Stapelin (AMP), also known as dihydromyricetin, dihydromyricetin, Fujian tea, etc., is a polyphenolic hydroxyl dihydroflavonol, which belongs to flavonoids (see formula below). It is rich in resources and has a wide range of sources. It exists in plants such as aconitum grape, Fujian white tea, and vine tea. Its extraction and analysis methods are simple, low in toxicity, and strong in biological activity. Liver, lowering blood sugar, lowering blood fat, enhancing human immunity, anti-tumor and other pharmacological activities. At present, the research hotspot of staphylophyllin is the development of its anti-tumor activity and its inhibitory effect on tumor cells in vitro. However, in...

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
Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/48A61K47/64A61K31/352A61P35/00A61P31/04A61P3/06A61P1/16A61P35/02
CPCA61K31/352C08G69/48
Inventor 吴晓珊倪峰柯加法李泳宁朱扶蓉黄仁杰
Owner FUJIAN HEALTH COLLEGE
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