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

A technology of phloroglucinol and antibacterial drugs, applied to phloroglucinol derivatives and the application field in the preparation of antibacterial drugs, can solve problems such as lack of in-depth research, and achieve low eukaryotic cell toxicity and significant antibacterial activity. Effect

Active Publication Date: 2019-07-19
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.

Method used

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

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The separation, extraction and structural identification of phloroglucinol derivatives comprises the following steps:

[0030] (1) Weigh 8 kg of dried myrtle (Myrtus communis Linn.) branches and leaves, pulverize into a coarse powder with a pulverizer, extract 4 times with 95% (w / w) ethanol percolation, 25 L each time, combine the percolation liquid and decompress Concentrated to no alcohol smell, the total extract obtained 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.

[0031] (2) Carry out silica gel column chromatography on the petroleum ether extraction part, using petroleum ether-ethyl acetate as the eluent, according to the volume ratio of petroleum ether and ethyl acetate: 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 to obt...

Embodiment 2

[0048] Inhibitory effects of (±) Myrtucyclitone C and (±) Myrtucyclitone D on 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, the above strains were purchased 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) Dissolv...

Embodiment 3

[0061] Effects of (±) Myrtucyclitone C and (±) Myrtucyclitone D on normal cells

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PUM

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Abstract

The invention discloses phloroglucinol derivatives and an application of same in preparation of antibacterial drugs. The phloroglucinol derivatives are (+ / -) Myrtucyclitone C and (+ / -) Myrtucyclitone D, wherein the structures are represented as the formula (I). The (+ / -) Myrtucyclitone C and the (+ / -) Myrtucyclitone D are cyclopolyketone-phloroglucinol-cyclopolyketone trimers, which are composed of 38 carbon atoms, wherein one cyclopolyketone fragment is subjected to rearrangement. The phloroglucinol derivatives are chemical entities having novel framework structures. The compounds show significant antibacterial activity to staphylococcus aureus, methicillin-resistant staphylococcus aureus and vancomycin intermediate-resistant staphylococcus aureus even in low concentration and meanwhile have very low toxicity to eukaryotic cells.

Description

technical field [0001] The invention belongs to the field of natural medicines and chemical medicines, in particular to a phloroglucinol derivative 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 val...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/08A61K31/352A61P31/04
CPCC07D493/08
Inventor 王磊叶文才程民井
Owner JINAN UNIVERSITY
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