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Bacterial quorum sensing inhibitor and antibacterial application thereof

A quorum sensing system and bacterial technology, applied in the field of microorganisms, can solve the problems of no antibacterial agents and low antibiotics

Inactive Publication Date: 2015-07-22
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Falkalindiol is relatively safe and has anti-cancer, anti-inflammatory, analgesic, anti-melanoma growth, anti-fungal, and anti-bacterial effects, but the detection of these activities does not involve animal experiments
[0009] Falkalindiol has antibacterial effect on Gram-positive bacteria Staphylococcus aureus, and Fakalindiol has weak antibacterial effect on Gram-negative bacteria Mycobacterium, Salmonella, Pseudomonas aeruginosa, etc., but Since the minimum inhibitory concentration of fakalindiol is too low compared to the current traditional antibiotics, there is no research on it as an antibacterial agent

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Purification and identification of the traditional Chinese medicine notopterygium falcarindiol

[0020] Preparation method of methanol crude extract: grind notopterygium rhizomes and weigh 10 g of powder, extract each 2.5 g of powder with 200 mL of methanol, sonicate for 1 h and soak for 24 h; filter paper to obtain the leachate, and evaporate the filtrate to dryness with a rotary evaporator and weighed; re-dissolved with 30 mL of methanol and then filtered to remove insoluble matter with a homemade cotton filter; evaporated the filtrate again and weighed.

[0021] The preparation method of the compound: after the above-mentioned extract is stirred evenly with an appropriate amount of silica gel H, it is separated by vacuum liquid chromatography column chromatography, and the eluent petroleum ether, dichloromethane, dichloromethane:methanol (100: 1), dichloromethane:methanol (50:1), dichloromethane:methanol (20:1), and methanol were washed separately, and eac...

Embodiment 2

[0028] Example 2: Quorum Sensing Inhibition Activity Test of Fakalindiol against Violet Bacillus

[0029]Violet bacteria screening model CV026 composition and method: Cool 19 mL of melted solid LB medium to 40°C, add 600 μL overnight cultured violaceum CV026 bacterial liquid, 15 μL signal molecule hexanoyl homoserine at a concentration of 500 μmol / L ester (C6-HSL) and 15 μL of kanamycin at a concentration of 30 mg / mL, and mix them into a Petri dish. After the plate is solidified, punch holes with a sterilized hole puncher, add 5 μL of compound to each hole, incubate in a 30°C incubator for 12 hours, and observe the growth of bacteria around the sample hole. If the compound is a quorum sensing inhibitor, it can inhibit the production of violacein, and it will appear as a turbid but opaque circle on the agar plate; the larger the turbid circle, the higher the activity of the compound.

[0030] Experimental results: compared with the positive control furanone C 30 (6.5 μg), 6.5...

Embodiment 3

[0031] Embodiment 3: Quorum sensing inhibitory activity test of anti-Pseudomonas aeruginosa of fakalindiol

[0032] Inhibition of Pseudomonas aeruginosa AHL quorum sensing system:

[0033] Components and methods of Pseudomonas aeruginosa detection model QSIS2: 17.5 mL of melted solid LB medium was cooled to 40°C, 2 mL of 60% sucrose was added, 250 μL of Pseudomonas aeruginosa QSIS2 cultured overnight, 8 μL signal molecule 3-oxolauroyl homoserine lactone (3-oxo-C12-HSL) at a concentration of 100 μmol / L, 200 μL of a viable bacterial stain red tetrazolium at a concentration of 5% (w / v) TTC and 32 μL of gentamicin at a concentration of 50 mg / mL, mix well and pour into a petri dish. After the plate is solidified, punch holes with a sterilized hole puncher, add 5 μL of compounds of different concentrations to each hole, place them in an incubator at 37°C, and observe the growth of bacteria around the sample holes. If the compound has quorum sensing inhibitory activity, a red bacte...

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PUM

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Abstract

The invention relates to antibacterial application of small molecular bacterial quorum sensing inhibitor Falcarindiol in the condition of no inhibition on bacteria growth concentration (subinhibitory concentration). The active compound has a broad-spectrum bacterial quorum sensing resistant activity, can inhibit bacterial virulence in subinhibitory concentration, reduces the harm of bacteria to the host, and can prevent and treat quorum sensing bacterial infections. The compound can play the role of inhibition of bacterial virulence in subinhibitory concentration, so that pressure for survival of pathogenic bacteria is not brought, drug resistance is not easy to produce, the antibacterial application of the small molecular bacterial quorum sensing inhibitor Falcarindiol in the condition of no inhibition on bacteria growth concentration (subinhibitory concentration) is different from application of killing bacteria and bacteria growth inhibition of other antibacterial agent, is also is different from the antibacterial application of bacteria growth inhibition of Falcarindiol with the bacteria concentration (the use final concentration is greater than the minimum bacteriostasis concentration), and is a new antibacterial application. The antibacterial application of the small molecular bacterial quorum sensing inhibitor Falcarindiol in the condition of no inhibition on bacteria growth concentration (subinhibitory concentration) has the advantages that: raw materials are easy to get, compound separation and purification are simple and easy to control, security is high, use concentration is low, and drug resistance is easy to produce, and the like, so that the Falcarindiol can be used in preparation of a new antibacterial agent.

Description

technical field [0001] The invention belongs to the field of microorganisms, and relates to the antibacterial application of a compound falcarindiol with a wide range of sources as a bacterial quorum sensing inhibitor. Background technique [0002] Bacterial drug resistance is a worldwide problem. The purpose of current antimicrobial agents is to kill bacteria or inhibit the growth of bacteria. Under this huge selection pressure, a large number of multiplication of drug-resistant bacteria has been produced. Therefore, traditional antibiotics are unlikely to solve the problem of drug resistance. [0003] Another current antibacterial strategy is the anti-virulence strategy, that is, it does not aim at killing or inhibiting the growth of bacteria, and directly inhibits the growth of bacterial virulence factors without inhibiting the growth of bacteria. Expression, lock the bacteria in avirulent or low-virulence state, lose or reduce the ability to harm the host. On the othe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/045A61P31/04A01N31/02A01P1/00
Inventor 于文功宫倩红郑红达宋阳
Owner OCEAN UNIV OF CHINA
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