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A kind of phloroglucinol compound and its application in the preparation of antibacterial drugs

A technology for phloroglucinol and antibacterial drugs, applied to phloroglucinol compounds and the application field in preparing antibacterial drugs, can solve problems such as insufficient research and achieve low eukaryotic cell toxicity, significant antibacterial activity, active effect

Active Publication Date: 2019-02-19
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current research on the chemical constituents of myrtle phloroglucinol is not in-depth, and only less than 20 compounds have been reported.
Therefore, its antibacterial active ingredients need to be further explored

Method used

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  • A kind of phloroglucinol compound and its application in the preparation of antibacterial drugs
  • A kind of phloroglucinol compound and its application in the preparation of antibacterial drugs
  • A kind of phloroglucinol compound and its application in the preparation of antibacterial drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Extraction, separation and structural identification of the compound of Example 1

[0031] (1) Take 8 kg of dried myrtle branches and leaves, pulverize them into coarse powder, extract 4 times by percolation with 95% (w / w) ethanol, each 25 L, combine the percolation liquid and concentrate under reduced pressure to no alcohol smell, The obtained total extract is about 1.2kg. The extract was suspended with water and then extracted with petroleum ether to obtain 389 g of petroleum ether extraction fractions.

[0032] (2) Carry out silica gel column chromatography on the petroleum ether extraction part prepared in step (1), using petroleum ether-ethyl acetate as eluent, according to the volume ratio of petroleum ether and ethyl acetate is 100:0, 100:1 , 100:3, 100:5, 100:7, 100:10, 100:30, 100:50, 100:100 and 0:100 elution gradients were eluted, analyzed by thin layer chromatography (TLC) and combined Similar fractions were obtained to obtain 10 main fractions Fr.1-Fr.10....

Embodiment 2

[0048] The inhibitory effect of embodiment 2 (+) Myrtucyclitones A-B and (-) Myrtucyclitones A-B to various bacteria

[0049] Staphylococcus aureus S.aureus ATCC29213, methicillin-resistant Staphylococcus aureus S.aureusATCC33591 (MRSA), vancomycin-intermediate resistant Staphylococcus aureus S.aureus Mu50 (VISA), Staphylococcus epidermidis S.epidermidis ATCC12228, E. faecalis ATCC29212, E. faecium 13-01, Escherichia coli ATCC25922, Ps. aeruginosa Ps. Aeruginosa, all from the Institute of Pharmaceutical Biotechnology, Chinese Academy of Medical Sciences.

[0050] The minimum inhibitory concentration (MIC) of the compound's antibacterial effect in vitro was determined by the broth micro-doubling dilution method, and the specific operation method was as follows:

[0051] (1) Bacterial culture: Cultivate the experimental bacteria with Mueller-Hinton (MH) broth medium, when it grows for 8-12h to about 0.5 Mcfarland concentration (1 × 10 8 CFU) for backup.

[0052] (2) Dissolve t...

Embodiment 3

[0058] The influence of embodiment 3 (+) Myrtucyclitones A-B and (-) Myrtucyclitones A-B on normal cells

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PUM

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Abstract

The present invention discloses a new phloroglucinol compound and applications of the new phloroglucinol compound in preparation of antibacterial drugs, wherein the structure of the new phloroglucinol compound is represented by a formula I, the new phloroglucinol compound comprises two pairs of enantiomers, and the enantiomers are named (+) Myrtucyclitone A, (-) Myrtucyclitone A, (+) Myrtucyclitone B and (-) Myrtucyclitone B. According to the present invention, the compound has the novel structure, has significant antibacterial activity, can strongly resist Methicillin-resistant Staphylococcus aureus and Vancomycinintermediate-resistant staphylococcus aureus compared to ampicillin and ceftazidime, provides low cytotoxicity to normal cells so as to indicate the good medicinal prospect of the compound, and can be used for preparing antibacterial drugs. The formula I is defined in the specification.

Description

technical field [0001] The invention belongs to the field of natural medicines and chemical medicines, in particular to a phloroglucinol compound and its application in the preparation of antibacterial medicines. Background technique [0002] Bacterial infection is common disease and frequently-occurring disease. At present, clinical drug-resistant bacterial infections are becoming more and more serious, and bacterial drug resistance is showing a trend towards multidrug resistance. Methicillin-resistant Staphylococcus aureus (MRSA), ampicillin-resistant Streptococcus pneumoniae (PRSP), and multidrug-resistant Drug-resistant tuberculosis (MDR-TB) is spreading rapidly. The increasing number of drug-resistant bacterial infections and the gradual increase in mortality indicate that traditional antibacterial drugs can no longer meet the needs of modern clinical treatment. Therefore, the research and development of new antibacterial drugs has important clinical application value...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/22A61K31/352A61P31/04
CPCC07B2200/07C07D493/22Y02A50/30
Inventor 王磊叶文才刘超
Owner JINAN UNIVERSITY
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