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Myrtucommulone R and application thereof in preparing antibacterial drug

A technology of antibacterial drugs and antibacterial activity, applied in the field of natural medicine and chemical medicine, can solve the problems of in-depth research and unreported antibacterial effect, and achieve the effect of low eukaryotic cell toxicity and significant antibacterial activity

Active Publication Date: 2017-07-28
JINAN UNIVERSITY +1
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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.
The compound Myrtucommulone R has only been reported as a synthetic product (Angewandte Chemie, International Edition, 2010, 49:2045-2049), and its antibacterial effect has not been reported yet

Method used

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  • Myrtucommulone R and application thereof in preparing antibacterial drug
  • Myrtucommulone R and application thereof in preparing antibacterial drug
  • Myrtucommulone R and application thereof in preparing antibacterial drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Extraction, separation and structure identification of compounds:

[0025] (1) 18 kg of dried branches and leaves of myrtle (Myrtus communis), crushed into coarse powder, extracted 4 times by percolation with 25L 95% (w / w) ethanol, combined percolation liquid and concentrated under reduced pressure until no alcohol smell, to obtain total extract The paste is about 1.9kg. After the total extract was suspended in 5 L of water, it was extracted with 5 L of petroleum ether and repeated 4 times. The extracts were combined and concentrated under reduced pressure to obtain 489 g of petroleum ether extraction fractions.

[0026] (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, and similar fractions were combined aft...

Embodiment 2

[0034] Inhibitory Effects of Myrtucommulone R on Various Bacteria

[0035] Staphylococcus aureus S.aureus ATCC29213, methicillin-resistant Staphylococcus aureus S.aureusATCC33591 (MRSA), vancomycin-intermediate resistant Staphylococcus aureus S.aureus Mu50 (VISA), coagulase-negative staphylococcus S.epidermidis ATCC12228, E.faecalis ATCC29212, vancomycin-resistant Enterococcus faecium ATCC700221, Escherichia coli E.coli ATCC25922, Ps.aeruginosaATCC 27853, the above strains are from Chinese Academy of Medical Sciences Institute of Technology.

[0036]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:

[0037] (1) Bacterial culture: Cultivate the experimental bacteria in trypticase soy broth (TSB), cultivate overnight at 35°C (12-16h) to a Mcfarland concentration of about 0.5 (1×10 8 CFU) for backup.

[0038] (2) The test sample...

Embodiment 3

[0047] Effects of Myrtucommulone R on Normal Cells

[0048] Test method: Human embryonic kidney cells HEK 293 (purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences) were cultured in DMEM medium containing 10% (v / v) fetal bovine serum and double antibodies (penicillin and streptomycin each 100U / ml) to In the logarithmic phase, wash with PBS, digest with 0.25% (w / v) trypsin, then suspend the cells with fresh DMEM medium, adjust the cell density to 1×10 6 cells / ml, spread 96-well plates, 200 μl per well, after the cells adhere to the wall, add samples of different concentrations, at 37°C, 5% CO 2 Co-cultivate under the same conditions for 24 hours. After the culture, add 20μl 5mg / ml MTT solution to each well, continue to incubate for 4h, use a pipette gun to suck out the liquid in the well, add 100μl DMSO to each well, shake gently at room temperature for 10 minutes, and use enzyme labeling The instrument detects the absorbance OD value of each well at a wave...

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Abstract

The invention discloses Myrtucommulone R and application thereof in preparing antibacterial drug. Structure of phloroglucinol tripolymer Myrtucommulone R is shown as a formula I, and Myrtucommulone R is a new natural product. The compound even at low concentration has remarkable antibacterial activity to staphylococcus aureus, methicillin-resistant staphylococcus aureus, vancomycin-intermediate-resistant staphylococcus aureus and vancomycin-resistant enterococcus faecium and has quite low toxicity to eukaryocytes, indicating that the compound has good medicinal prospect and can be applied to preparing an antibacterial drug preparation. The antibacterial drug preparation contains Myrtucommulone R and the balance of medicinal auxiliary materials or other compatible drugs. The antibacterial drug preparation includes various clinical drug dosage forms.

Description

technical field [0001] The invention belongs to the field of natural medicines and chemical medicines, and in particular relates to the antibacterial activity of a phloroglucinol trimer Myrtucommulone R and its application in the preparation of antibacterial medicines. Background technique [0002] Bacterial infection can cause many diseases in human body. At present, clinically, drug-resistant bacterial infections are becoming more and more serious, such as methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and multidrug-resistant Mycobacterium tuberculosis (MDR-TB). Bacterial drug resistance is gradually showing the development trend of multidrug resistance. In recent years, the clinical fatality rate caused by drug-resistant bacterial infection has been increasing year by year, reflecting that traditional antibacterial drugs have been difficult to meet the needs of modern clinical treatment. Therefore, the research ...

Claims

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Application Information

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IPC IPC(8): C07D311/82A61K31/352A61P31/04
CPCC07D311/82
Inventor 叶文才王磊杨信怡卢曦游雪甫陈明
Owner JINAN UNIVERSITY
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