Inhibitor Lo-isohexyl for resisting virulence of staphylococcus aureus and formation of biofilms, and application of inhibitor Lo-isohexyl

A staphylococcus and biofilm technology, applied in the direction of local antibacterial agents, medical preparations containing active ingredients, antibacterial drugs, etc., can solve problems such as chronic infection, limited selection of clinical antibacterial drugs, and reduce the sensitivity of antibacterial drugs. Strong inhibitory activity, inhibitory effect on virulence and biofilm formation

Pending Publication Date: 2020-02-21
SHENZHEN NANSHAN DISTRICT PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

With the widespread use of antibacterial drugs, the emergence of drug-resistant bacteria, especially methicillin-resistant Staphylococcus aureus (MRSA), has brought difficulties to clinical treatment.
Vancomycin and linezolid are very few antibacterial drugs that can treat MRSA infection, but more and more Staphylococcus aureus (VISA / hVISA) and linezolid resistance to vancomycin have been found at home and abroad strains, so that the choice of clinical antibacterial drugs is severely limited
In addition, Staphylococcus aureus can also adhere to the surface of human tissue cells or medical implant materials to form a biofilm structure composed of exopolysaccharide adhesion molecules, proteins, teichoic acid and extracellular DNA (eDNA), reducing the Bacteria are sensitive to antibacterial drugs and evade the attack and phagocytosis of host immune cells, resulting in chronic infection and persistent healing

Method used

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  • Inhibitor Lo-isohexyl for resisting virulence of staphylococcus aureus and formation of biofilms, and application of inhibitor Lo-isohexyl
  • Inhibitor Lo-isohexyl for resisting virulence of staphylococcus aureus and formation of biofilms, and application of inhibitor Lo-isohexyl
  • Inhibitor Lo-isohexyl for resisting virulence of staphylococcus aureus and formation of biofilms, and application of inhibitor Lo-isohexyl

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Lo-isohexyl was prepared using the following steps:

[0040]

[0041] The desloratadine reactant (I) is dissolved in an organic solvent, and triethylamine is used as an acid-binding agent, and an organic solution having a reactant (III) is added, wherein the reactant (I) and the reactant (III ) in a molar ratio of 1:1 to 1.5, the two were mixed, stirred and reacted at -5°C to obtain a reaction solution containing Lo-isohexyl. Wherein organic solvent can be a kind of in dichloromethane, chloroform, acetone, acetonitrile, tetrahydrofuran, DMF, pyridine or toluene. Wherein the reactant (III) is obtained through a conventional synthesis reaction.

[0042] After the reaction, the reaction liquid was poured into cold water, fully shaken and separated into layers, the organic layer was extracted, and washed three times with water continuously. The organic layer was dried and set aside. Then filter and evaporate the solvent under reduced pressure to obtain the compound Lo-i...

Embodiment 2

[0044] The compound Lo-isohexyl inhibits the biofilm formation experiment of Staphylococcus aureus.

[0045] Detection of biofilm formation of strains: Staphylococcus aureus strains were cultured overnight in TSB medium at 37°C and 220 rpm / min for 10-12 hours. Dilute the bacterial solution 1:200 (with or without Lo-isohexyl) with TSBG medium (TSB medium + 0.5% glucose), add 200ul per well to a 96-well plate (Costar 3599), and set 3 replicate wells for each strain , and cultured statically at 37°C for 24h. Discard the supernatant, wash with PBS 3 times (200ul / well / time), dry at room temperature, add methanol for fixation for 15min (200ul / well), discard methanol and add 100ul of 0.5% crystal violet staining solution to each well after drying at room temperature. Stain at room temperature for 10 minutes, gently elute the crystal violet staining solution under clean water until the running water is colorless, dry at room temperature and read OD on a microplate reader 570 value. ...

Embodiment 3

[0049] Compound Lo-isohexyl inhibits aureus pigment production and hemolytic activity of Staphylococcus aureus.

[0050] Detection of golden yellow pigment of bacterial strains: cultured with TSB medium at 37° C. for 48 hours (with or without Lo-isohexyl), centrifuged 3 ml of bacterial culture and washed twice with 0.01 M phosphate buffered saline (PBS). After washing the cell pellet with PBS, discard the supernatant, add 300ul methanol (100%) to the cell pellet, pipette the resuspended bacteria solution, shake for 5 minutes after resuspension, centrifuge (12000r / min, centrifuge for 1-2 minutes), and then Aspirate the supernatant extract into a clean EP tube, then add 300-350ul methanol (100%) to the cell pellet, repeat 2 times, suck out the extract each time, and finally extract these 3 times together After mixing about 1ml of the solution thoroughly, take 200ul and add it to a 96-well plate (three duplicate wells), and measure the OD450 value on a microplate reader. The abo...

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Abstract

The invention provides an inhibitor Lo-isohexyl for resisting virulence of staphylococcus aureus and formation of biofilms, and an application of the inhibitor Lo-isohexyl. The inhibitor Lo-isohexyl for resisting virulence of staphylococcus aureus and formation of biofilms has a chemical structural formula shown in a formula (1). The inhibitor Lo-isohexyl for resisting virulence of staphylococcusaureus and formation of biofilms has an inhibition effect on virulence of staphylococcus aureus and formation of biofilms, and can be used for preparing medicaments for inhibiting virulence of staphylococcus aureus and formation of biofilms, or preparing medicaments for treating diseases caused by staphylococcus aureus, or preparing disinfectants of medical apparatus or medical instruments.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to an inhibitor Lo-isohexyl for resisting Staphylococcus aureus virulence and biofilm formation and its application. Background technique [0002] Staphylococcus aureus can infect different parts of the human body and cause a variety of infectious diseases, ranging from common skin diseases such as folliculitis, acne, and stye, to profound and fatal diseases such as pneumonia, endocarditis, osteomyelitis, and other metastatic complications disease. During the process of Staphylococcus aureus invading the host and inducing host infection, it can secrete a variety of virulence factors such as hemolysin, extracellular protease, leukocidin and phenol-soluble protein, etc., thereby assisting its invasion and damage to the host, and then induce disease. With the widespread use of antibacterial drugs, the emergence of drug-resistant bacteria, especially methicillin-resistant Stap...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61K31/4545A61P31/04A61P31/02
CPCC07D401/04A61P31/04A61P31/02
Inventor 郑金鑫余治健邓启文陈重孙翔尚永朋林志伟
Owner SHENZHEN NANSHAN DISTRICT PEOPLES HOSPITAL
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