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A kind of polyphenolic polymer and its application

A polyphenol polymer, polymer technology, applied in the field of medicine, can solve problems such as drug-resistant strains

Active Publication Date: 2020-06-26
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Antibiotics discovered based on this strategy can create selective pressure on bacteria after overuse, leading to the emergence of drug-resistant strains

Method used

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  • A kind of polyphenolic polymer and its application
  • A kind of polyphenolic polymer and its application
  • A kind of polyphenolic polymer and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Separation and Purification of Uncariitannin from Fang Catechu

[0036] a) After pulverizing 2.5 kg of catechu catechu, add 10 times the amount of 80% (V / V) ethanol to extract under reflux for 3 to 5 times, and evaporate the extract under reduced pressure to obtain the extract;

[0037] b) suspending the extract obtained in step a) in water, and extracting with ethyl acetate to obtain the ethyl acetate extraction part and the water part of the catechu catechu extract respectively;

[0038] c) The water portion of the Catechua catechin extract obtained in step b) is separated by an MCI column, and eluted with water, 10%, 20%, 30%, 40%, 50%, 60%, 70%, and 95% ethanol in sequence, After concentration, the activity is tested, and the most active 40% ethanol elution site is selected for further separation

[0039] d) The 40% ethanol elution fraction obtained in step c) is separated with a Sephadex LH-20 column, and eluted with 80% EtOH. After evaporation under red...

Embodiment 2

[0040] Embodiment 2 SEC-RI-LS measures the molecular weight of polyphenol polymer Uncaritannin

[0041]The purity and molecular weight of polyphenolic polymer Uncaritannin were analyzed by Viscotek GPCmax+RI (differential refractive index detector)+LS (light scattering detector) multi-detector GPC / SEC system from Malvern Company. The analysis conditions are as follows: Mobile phase: HCOONH4 / DMF (15mM); Flow rate: 0.7mL / min; Injection volume: 50μL; Chromatographic column: I-MBMMW-3078 (10μM, 300mm L×8.0mm ID); Column temperature: 45 °C; sample solvent: HCOONH4 / DMF (15 mM). The analysis results were calculated by the method of absolute molecular weight. The measurement results are as follows ( figure 2 ):

[0042] Number average molecular weight (M n )=160192

[0043] Weight average molecular weight (M w )=195463

[0044] Z-average molecular weight (M z )=219322

[0045] Polydispersity index (M w / M n ) = 1.22.

Embodiment 3

[0046] Example 3 Under the condition of excessive phloroglucinol, Uncaritannin is acid-degraded, and the main degradation products are identified

[0047] The reaction conditions were as follows: Acetyl chloride (120 mL) was slowly added to methanol (180 mL), followed by Uncariitannin (100 mg), ascorbic acid (250 mg) and phloroglucinol (1.8 g), and reflux at 80°C for 4 h. After the reaction, concentrate under reduced pressure, add water (400ml) to suspend, add ethyl acetate (600ml), extract 5 times, the ethyl acetate extract layer is washed with water until neutral, and concentrate under reduced pressure to obtain a degradation product (2g).

[0048] Take 1 mg of the sample and redissolve it in methanol, filter it through a 0.22 μm microporous membrane, and analyze it by UPLC-PDA-QTOF-MS. The chromatographic conditions are as follows: A: acetonitrile; B: 0.1% formic acid water; the gradient program is: 10-18% A (0-6min), 18-25% A (6-11min), 25-30% A (11-13min ), 30-40% A (13-...

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Abstract

The invention relates to the field of medicine, in particular to a polyphenol polymer and application thereof. The average molecular weight of polyphenol polymer Uncariitannin is between 160000-220000, the polyphenol polymer is prepared by adopting the following method that pale catechu medicinal slices are taken to be smashed to be coarse powder, ethyl alcohol with the concentration being 80% andthe amount being 10 times of the coarse powder is added, the mixture is subjected to heating reflux or cold-soaked extracting for three times, cold-soaked extracting is conducted for 1.5 hours for each time, the extraction liquid is combined and filtered, the filtrate is subjected to vacuum concentration till no alcohol smell exists, extraction is conducted through ethyl acetate, the left water-course after extraction is adsorbed through an MCI column, then the product is eluted by using water, 10% ethyl alcohol ,20% ethyl alcohol, 30% ethyl alcohol, 40% ethyl alcohol, 50% ethyl alcohol, 60%ethyl alcohol, 70% ethyl alcohol and 95% ethyl alcohol sequentially, the product eluted through 40% ethyl alcohol is collected, concentrated and sent to a Sephadex LH-20 chromatographic column, then the product is eluted through 80% ethyl alcohol and analyzed and detected through UPLC, the pure Uncariitannin components displayed through UPLC analysis are combined, and the polyphenol polymer is obtained. The polyphenol polymer can be applied to preparation of drugs for preventing and treating infection of methicillin resistant staphylococcus.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a polyphenol polymer and its application. Background technique [0002] Staphylococcus aureus (Staphylococcus aureus, referred to as Staphylococcus aureus) is the most common pathogen causing human suppurative infection, which can directly cause local suppurative infection, pneumonia, pseudomembranous enteritis, pericarditis, etc., and even systemic infection such as sepsis and sepsis. Infection seriously endangers human life and health. The types of S. aureus infection can be divided into hospital-acquired infection and community-acquired infection, the latter increasing the potential biohazardousness of this pathogen and the possibility of causing infection outbreaks. Antibiotic therapy is the main treatment for Staphylococcus aureus infection, but in recent years, due to the increase in the infection rate of Staphylococcus aureus, the acceleration of drug resistance, and the character...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/84C08G65/38A61P31/04
CPCA61P31/04C07D307/84C08G65/38
Inventor 徐宏喜张洪蒋嘉明郑丹劳远至谭红胜
Owner SHANGHAI UNIV OF T C M
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