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Application of Methyl 2-(methylamino)benzoate

A technology of methyl benzoate and methylamino, which is applied in the direction of medical preparations containing active ingredients, antibacterial drugs, organic active ingredients, etc., to achieve the effects of easy access, small effective dose, and small potential side effects

Active Publication Date: 2020-01-17
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the volatile oil of tangerine peel has been confirmed to have biological activities such as antioxidant, antibacterial and antiviral activities. The reports of its antibacterial activity are mainly against Escherichia coli, Staphylococcus aureus, mold, etc. Methyl (methylamino)benzoate is used in the treatment of Pseudomonas aeruginosa infection or combined with traditional antibacterial drugs to prevent and treat Pseudomonas aeruginosa infection

Method used

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  • Application of Methyl 2-(methylamino)benzoate
  • Application of Methyl 2-(methylamino)benzoate
  • Application of Methyl 2-(methylamino)benzoate

Examples

Experimental program
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Effect test

Embodiment 1

[0036] Example 1: Effect of 2-(methylamino)methyl benzoate on the growth of Pseudomonas aeruginosa

[0037] To the Pseudomonas aeruginosa that adds the 2-(methylamino) methyl benzoate effect 48h of different concentrations, the growth curve drawn is as follows figure 1 As shown, different concentrations of PCR-M had no significant inhibition on the growth of Pseudomonas aeruginosa.

Embodiment 2

[0038] Example 2: Effect of methyl 2-(methylamino)benzoate on pyocyanin, elastase, rhamnolipid and biofilm of Pseudomonas aeruginosa

[0039] The inhibitory effect of PCR-M on Pseudomonas aeruginosa was investigated according to the experimental methods of pyocyanin, elastase, rhamnolipid and biofilm, and the results are shown in Table 1. The experimental results showed that the inhibition rates of 2.5mg / mL PCR-M to Pseudomonas aeruginosa pyocyanin, elastase, rhamnolipid and biofilm were 86.4%, 20.5%, 40.5% and 46.8%, respectively. One-way analysis of variance showed that PCR-M had significant inhibitory effect on virulence factors (including pyocyanin, elastase, rhamnolipid) and biofilm formation of Pseudomonas aeruginosa (P<0.05).

[0040] Table 1 is the inhibition of pyocyanin, elastase, rhamnolipid and biofilm of Pseudomonas aeruginosa by 2-(methylamino) methyl benzoate

[0041]

[0042] Among them, different letters * and ** in the table indicate that the differences ...

Embodiment 3

[0043] Embodiment 3: 2-(Methylamino) benzoic acid methyl ester affects the real-time fluorescence quantitative PCR of the genes related to virulence factors and biofilm formation in Pseudomonas aeruginosa quorum sensing system

[0044] Real-time quantitative PCR experiments were used to detect the regulation of PCR-M on the transcription level of genes related to the quorum sensing system of Pseudomonas aeruginosa. The genes with significant changes were as follows: figure 2 shown.

[0045] The experimental results show that the relative expression levels of genes lasA, pqsA, phzM, mvfR, pelF, lasR, chiC, lasI, lasB, rhlI, rhlR, pslA, rpoS and other genes related to virulence factors or biofilm formation during the growth of Pseudomonas aeruginosa Both were down-regulated, and the difference was extremely significant (P<0.001); this indicates that PCR-M has a significant regulatory effect on the transcription level of the quorum sensing system of Pseudomonas aeruginosa, there...

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Abstract

The invention discloses an application of Methyl 2-(methylamino)benzoate and relates to the technical field of compound use. Methyl 2-(methylamino)benzoate has strong inhibitory activity on the production of Pseudomonas aeruginosa quorum sensing virulence factors and biofilm formation. Experimental results show that Methyl 2-(methylamino)benzoate has no remarkable inhibitory effect on the growth of pseudomonas aeruginosa, but has significant inhibitory effect (p is less than 0.05) on the virulence factors (including pyocyanin, elastase, rhamnolipid) and biofilm formation, can be used in preparation of health products or drugs for preventing and / or treating Pseudomonas aeruginosa infections, and is suitable for large-scale promotion. The effective dose of Methyl 2-(methylamino)benzoatefor inhibiting Pseudomonas aeruginosa quorum sensing is small and the potential side effects are also small, so that Methyl 2-(methylamino)benzoate is safer to use. Methyl 2-(methylamino)benzoate, along with different additives and excipients, can be made into different health products and pharmaceutical dosage forms, and is convenient for people to eat and facilitates clinical applications.

Description

technical field [0001] The present invention relates to the technical field of compounds, more specifically, to the technical field of citrus volatile oil compounds, in particular to the use of methyl 2-(methylamino)benzoate in the preparation of products for preventing and / or treating Pseudomonas aeruginosa infection application. Background technique [0002] Pseudomonas aerginosa (PA) is one of the common opportunistic pathogenic bacteria in nature (existing in water, air, normal human skin, respiratory tract and intestinal tract, etc.), which can cause respiratory system, chronic trauma, urinary tract infection, etc. system, soft tissue and other important system infections of the body, seriously endangering human health. At present, the treatment of Pseudomonas aeruginosa infection is mainly based on the combined use of antibiotics. However, with the abuse of antibiotics, the resistance variation induced by Pseudomonas aeruginosa makes traditional antibacterial drugs no...

Claims

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Application Information

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IPC IPC(8): A61K31/245A61P31/04
CPCA61K31/245A61P31/04
Inventor 陈谷马永凯何倩娴
Owner SOUTH CHINA UNIV OF TECH
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