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Application of 3 [(4 - ((Z)[(2Z) - 4 oxo 2 (phenylimino) - 1, 3 - thiazolidine 5 idene] methyl) phenoxy) methyl] benzoic acid in agent for restraining staphylococcal bacteria

A phenylimino, staphylococcus technology, applied in antibacterial drugs, medical preparations containing active ingredients, organic active ingredients, etc., can solve problems such as easy development of chronic infection and severe infection problems

Inactive Publication Date: 2007-12-26
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

With the frequent use of the above-mentioned medical materials and the abuse of antibiotics, Staphylococcus epidermidis that is resistant to vancomycin and multi-drug resistance has emerged, leading to increasingly serious problems of such nosocomial infections, which are very easy to develop into chronic infections, so there is Urgent need for research and development of new drugs

Method used

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  • Application of 3 [(4 - ((Z)[(2Z) - 4 oxo 2 (phenylimino) - 1, 3 - thiazolidine 5 idene] methyl) phenoxy) methyl] benzoic acid in agent for restraining staphylococcal bacteria
  • Application of 3 [(4 - ((Z)[(2Z) - 4 oxo 2 (phenylimino) - 1, 3 - thiazolidine 5 idene] methyl) phenoxy) methyl] benzoic acid in agent for restraining staphylococcal bacteria
  • Application of 3 [(4 - ((Z)[(2Z) - 4 oxo 2 (phenylimino) - 1, 3 - thiazolidine 5 idene] methyl) phenoxy) methyl] benzoic acid in agent for restraining staphylococcal bacteria

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0013] Preparation Example 1: Construction of Prokaryotic Expression Plasmid of Staphylococcus Epidermidis Tryptophanyl-tRNA Synthetase

[0014] Staphylococcus epidermidis tryptophanyl-tRNA synthetase gene (NC_004461, locus tag: SE0685) acquisition method is as follows:

[0015] Design an NcoI restriction site at the 5′ end of the sense strand primer, and an NheI restriction site at the 5′ end of the antisense strand primer:

[0016] sense:

[0017] 5'-CC CCA TGG AAA CTT TAT TCT CAG GA-3’

[0018] anti-sense:

[0019] 5’-CG GCT AGC TTA TCT TTT TCG ACC TAA GCC C-3’

[0020] The underlined sequence is the restriction site of Nco I, and the sequence in italics is the restriction site of Nhe I.

[0021] The coding gene of Staphylococcus epidermidis tryptophanyl-tRNA synthetase was amplified by PCR using the above primers. Through the digestion reaction of restriction endonuclease (Nco I and Nhe I) and the ligation reaction of T4 DNA ligase, the above gene was connected into...

preparation Embodiment 2

[0022] Preparation Example 2: Expression and Purification of Tryptophanyl-tRNA Synthetase Protein

[0023] Host bacteria: Escherichia coli BL21-DE3

[0024] 1) Pick a single clone colony and inoculate into 5ml LB medium, 37℃×250rpm to OD 600 =1~2;

[0025] 2) Inoculate 10 μl to 5ml LBK medium, add 1M IPTG to a final concentration of 1mM, and induce expression for 4 hours;

[0026] 3) Centrifuge the bacterial cells, resuspend them in PBS, and ultrasonically disrupt them, centrifuge at 12,000 rpm for 5 minutes at 4°C, and take the supernatant; use Invitrogen ProBond TM Purify the protein with Purification System; determine the distribution of the target protein by 12% SDS-PAGE protein electrophoresis analysis. Proteins were quantified by the Bradford method.

Embodiment 1

[0027] Example 1: The effect of compound FDDDC03 on the activity of Staphylococcus epidermidis tryptophanyl-tRNA synthetase and the activity of human tryptophanyl-tRNA synthetase (using two methods for detection):

[0028] 1) Detection of the reduction of the substrate ATP - Kinase-Glo TM Luminescent Kinase Assay Kit (Promega, USA): 2 μg of recombinantly expressed and purified tryptophanyl-tRNA synthetase from Staphylococcus epidermidis and 3 μg of human tryptophanyl-tRNA synthetase were reacted with serially diluted compound FDDDC03 at 25°C for 20 minutes, Then add 100 μM ATP (total reaction volume 50 μL), after 20 minutes at 25 ° C, add the reaction mixture to a 96-well microtiter plate, 50 μL per well, add Kinase-Glo TM 50 μL of Reagent per well was allowed to stand at room temperature for 10 minutes, and the chemiluminescence value was read to indicate the amount of ATP remaining in the reaction. In the experiment, the group without compound was set as the control group....

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Abstract

The present invention belongs to the field of biological medicine, in the concrete, it relates to an application of 3-[(4-{(Z)-[(2Z)-4-keto-2-(phenylimino)-1, 3-thiazolidine-5-subunit] methyl} phenoxy) methyl] benzoic acid. Specially, it relates to application of said compound in preparation of staphylococcus inhibitor and pharmaceutical field. Said compound can effectively and obviously inhibit the growth of staphylococcus epidermidis.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to 3-[(4-{(Z)-[(2Z)-4-oxo-2-(phenylimino)-1,3-thiazolidine-5-ylidene ] methyl} phenoxy group) methyl] benzoic acid purposes, especially relate to the purposes of this compound in staphylococcus inhibitor and pharmaceutical field. Background technique [0002] Staphylococcus is associated with nosocomial infections, especially Staphylococcus aureus and Staphylococcus epidermidis. Staphylococcus epidermidis has become the most important factor of iatrogenic infection in transplant surgery, and the infection caused by it is related to the indwelling of some polymer medical devices, such as venous catheters, pacemakers, cerebrospinal fluid drainage devices, artificial organs, etc. . With the frequent use of the above-mentioned medical materials and the abuse of antibiotics, Staphylococcus epidermidis that is resistant to vancomycin and multi-drug resistance has emerged, which has led to an ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/425A61P31/04
Inventor 于坤千蒋华良吴旸瞿涤沈旭
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI