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Myrtleone compound and its application in the preparation of antibacterial drugs

A technology of antibacterial drugs and compounds, applied in the field of phytochemistry, can solve the problems of small side effects, the active ingredients and the mechanism of action are not clear, and achieve the effect of strong inhibitory activity and good antibacterial activity

Active Publication Date: 2017-02-22
GUANGZHOU LEADER BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, many studies have shown that drying the leaves to make tea or decocting them in boiling water can be used to treat insomnia, urticaria, dysentery, uterine bleeding and other diseases. The efficacy is excellent and the side effects are small, but its active ingredients and mechanism of action are not yet clear

Method used

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  • Myrtleone compound and its application in the preparation of antibacterial drugs
  • Myrtleone compound and its application in the preparation of antibacterial drugs
  • Myrtleone compound and its application in the preparation of antibacterial drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the separation and purification of compound rhodomyrtosone B and tomentosone C

[0023] The organic solvents used in the separation and extraction, such as chloroform, ethyl acetate, methanol, ethanol, acetone, n-hexane, dichloromethane, etc., have been re-distilled, and other organic solvents used in small amounts are analytically pure; the deuterated reagent is Qingdao Tenglong The product of Microwave Technology Co., Ltd.; the medium pressure preparative chromatography (Dr Flash II) was produced by Shanghai Lisui Chemical Technology Co., Ltd., and the HPLC liquid chromatograph was produced by Tianjin Lanbo Experimental Instrument Equipment Co., Ltd.

[0024] 13 kg of dried myrtle (Rhodomyrtus tomentosa) leaves were pulverized, extracted 3 times with a volume fraction of 95% ethanol aqueous solution, each time for 5 days, and the extracts were combined and concentrated under reduced pressure to obtain 1.8 kg of extract; alkane, ethyl acetate extracted th...

Embodiment 2

[0036] Embodiment 2: the antibacterial activity evaluation of compound

[0037] In this embodiment, the minimum inhibitory concentration (MIC) of the anti-MRSA activity of the sample will be determined by the resazurin chromogenic method. In the test, the 96-well plate dilution titer technique will be used to simultaneously determine the minimum inhibitory concentration (MIC) of various substances.

[0038] First, mix 7.5 mL of indicator solution (100 μg / mL resazurin aqueous solution) with 5 mL of the bacteria solution to be tested (10 8 CFU / mL) and mix well, and add 100 μL of mixed bacterial solution to all test wells in columns 1 to 8. Then add 100 μL of the DMSO solution (16-500 μg / mL) of the sample to be tested into each plate well in the first column in turn, after mixing evenly, take out 100 μL of the solution and transfer it to the corresponding plate well in the second column, and use the same method Doubling dilutions to column 8. Finally, put the orifice plate wit...

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PUM

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Abstract

The invention discloses a myrtle ketone compound and an application thereof in preparation of antibacterial medicines. A compound rhodomyrtosone B (shown in a formula 2) and a compound tomentosone C (shown in a formula 1) are separated from myrtle, and the two compounds have high antibacterial activities, particularly have high inhibitory activity on methicillin-resistant staphylococcus aureus. Therefore, a foundation is laid for developing the compounds into novel drug bacteria resistant lead compounds and launching the compounds on the market. The structural formula is as shown in the specification.

Description

[0001] Technical field: [0002] The invention belongs to the field of phytochemistry, and in particular relates to myrtleone compounds B and C and their application in the preparation of antibacterial drugs. [0003] Background technique: [0004] Methicillin-resistant Staphylococcus aureus (MRSA), since it was first discovered by Jevons in England in 1961, has accounted for an increasing proportion of Staphylococcus aureus infections, and has been increasing since the mid-1980s The 1%-5% of the infection has rapidly increased to the current 60%-70%, and the degree of infection has become more and more serious. It has become one of the important pathogenic bacteria for hospital and community infection. At present, MRSA is resistant to commonly used antibiotics in clinic, and has become a multi-drug resistant pathogen that seriously threatens human health. Its infection is almost all over the world, and it can be transmitted between livestock and human beings, leading to bacter...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04C07D311/82A61P31/04
CPCC07D493/04
Inventor 邱声祥刘洪新谭海波袁尧朱春福徐志防
Owner GUANGZHOU LEADER BIO TECH
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