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Novel bacterial QS (quorum sensing) inhibitors and antibacterial application thereof

A new type of coumarin-based technology, applied in antibacterial drugs, active ingredients of heterocyclic compounds, organic chemistry, etc., can solve problems such as drugs that have not been seen, and achieve the effect of preventing and curing disease infection and reducing group movement

Active Publication Date: 2016-11-16
CHINA UNIV OF PETROLEUM (EAST CHINA)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A detailed study of its active ingredients found that the coumarin compound psoralen and bergamot lactone compound can strongly inhibit the activity of the QS system of Violet Bacillus and Pseudomonas aeruginosa. Pseudomonas QS activity has been reported, so no drug related to it has been seen on the market

Method used

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  • Novel bacterial QS (quorum sensing) inhibitors and antibacterial application thereof
  • Novel bacterial QS (quorum sensing) inhibitors and antibacterial application thereof
  • Novel bacterial QS (quorum sensing) inhibitors and antibacterial application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Purification and structural identification of psoralen and bergamot lactone in Chinese medicine fig leaves

[0020] Preparation method of methanol crude extract: Weigh 1g of raw materials and add 50ml of methanol solution for extraction, ultrasonic for 30 minutes, and then place on a shaker for 48 hours to shake and extract. Filtrate and filter residue were obtained by filtration. The slag was extracted twice with 20 ml of methanol solvent according to the above method to obtain a total of 3 filtrates, which were combined and concentrated in vacuo to obtain a crude extract.

[0021] Separation and purification of the compound: After the above-mentioned crude extract was mixed with an appropriate amount of silica gel H, it was separated by a vacuum silica gel column chromatography, using different proportions of eluent petroleum ether, petroleum ether: dichloromethane (1:5), Petroleum ether: dichloromethane (1:1), dichloromethane, dichloromethane: methanol (1...

Embodiment 2

[0028] Example 2: Analysis of compounds psoralen and bergamot lactone inhibiting QS activity of Violaceum violaceum

[0029] Violet Bacillus Screening Model and Its Method: Violet Bacillus CV026 cultured overnight was diluted to OD with LB liquid medium 600nm =0.1, 10ml per bottle; add 20μl of different concentrations of compounds psoralen and bergamotide, 50μl of signal molecules and 20μl of kanamycin, respectively, put them in a shaker at 28°C and 160rmp for 18h; DMSO solvent as a blank control. After the culture is over, centrifuge at 6000rmp for 10min, suck out the supernatant, redissolve it with 1ml DMSO, and centrifuge again (6000rmp, 10min), pour the supernatant into the marked centrifuge tubes, and take 200μl of the supernatant in turn Add it to a 96-well microplate and measure the absorbance A at 585nm with a microplate reader 585 , to characterize the production of violacein in violaceum violaceum; for the precipitate obtained by second centrifugation, add 1ml of s...

Embodiment 3

[0031] Example 3: Analysis of compounds psoralen and bergamot lactone inhibiting Pseudomonas aeruginosa swarming activity

[0032] Swarming screening method: take 14.8ml of hot melted swarming soft agar medium (glucose 10g; agar powder 5g; peptone 5g; yeast extract powder 2g; dissolve in 1L deionized water, sterilize at 121°C for 20min), After cooling to about 30°C, 200 μl of psoralen and bergamot lactone compound were added thereto, with final concentrations of 40 μg / ml and 160 μg / ml, respectively. Pour it into a flat plate, and after solidification, punch holes with a puncher, and put 2 μl of overnight cultured Pseudomonas aeruginosa PA01 (OD 600nm =0.1) Bacterial solution was added to the wells, incubated at a constant temperature of 37°C for 24 hours, and the phenomenon was observed.

[0033] Experimental results: 40 μg / ml psoralen and 160 μg / ml bergamot lactone can significantly inhibit the cluster movement of Pseudomonas aeruginosa PA01 ( image 3 ), indicating that ps...

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Abstract

The invention relates to novel bacterial QS (quorum sensing) inhibitors and an antibacterial application thereof. Two coumarin compounds including psoralen and bergapten are obtained through separation and identification from fig leaves. Experiments prove for the first time that the compounds have activity of inhibiting Chromobacterium violaceum and pseudomonas aeruginosa QS systems and cannot produce survival pressure to pathogenic bacteria which further produce drug resistance, thereby being novel antibacterial compounds. The novel bacterial QS inhibitors and the antibacterial application thereof have the advantages that raw materials are easily available, a preparation method is easy to implement, and drug resistance and toxic actions are avoided, so that the coumarin compounds have potential to be developed into lead compounds for novel antibacterial drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a novel bacterial quorum sensing inhibitor and its antibacterial application. Background technique [0002] Bacteria are traditionally considered to be non-social organisms. Studies in recent years have found that bacteria can transmit and communicate with each other by secreting, recognizing, and sensing one or more soluble chemical signal molecules, namely autoinducers (AI), which is called bacterial quorum sensing (Quorum sensing, QS) phenomenon. Bacterial QS systems are involved in the regulation of many biological functions, including toxin production, biofilm formation, spore production, antibiotic production, bioluminescence, etc. In recent years, bacterial QS systems have become the focus of pharmaceutical researchers. Antibacterial drugs screened by targeting the bacterial QS system have a completely different mechanism of action from traditional antib...

Claims

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Application Information

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IPC IPC(8): C07D493/04A61K31/37A61P31/04
CPCC07D493/04
Inventor 朱虎孙世伟李慧刘奥戴晓芸卜祥国翁彩虹
Owner CHINA UNIV OF PETROLEUM (EAST CHINA)
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