Application of flavonoid compound to preparation of beta-lactamase inhibitor

A technology of flavonoids and lactamase, which is applied in the field of serine β-lactamase inhibitors, can solve the problems of high price and few types of inhibitors, achieve good inhibitory activity and reduce the difficulty of obtaining

Pending Publication Date: 2022-07-05
MICROBIOLOGY INST OF SHAANXI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commercial inhibitors such as clavulanic acid, sulbactam, and tazobactam mainly have inhibitory activity on class A and class C β-lactamases, and there are fewer inhibitors against class D serine β-lactamases, and the price very expensive technical problem

Method used

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  • Application of flavonoid compound to preparation of beta-lactamase inhibitor
  • Application of flavonoid compound to preparation of beta-lactamase inhibitor
  • Application of flavonoid compound to preparation of beta-lactamase inhibitor

Examples

Experimental program
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Effect test

Embodiment 1

[0042] Embodiment 1: a kind of antibacterial drug composition

[0043] This embodiment discloses an antibacterial drug composition, the composition contains a serine β-lactamase inhibitor and a β-lactam antibiotic, and the serine β-lactamase inhibitor is a flavonoid compound.

[0044] The flavonoid compound described in this example is a combination of quercetin, 3',4',7-trihydroxyflavonoid, fisetin and luteolin.

Embodiment 2

[0045] Example 2: A method for designing the structure of an OXA-48 inhibitor

[0046] The present embodiment provides a method for designing the structure of an OXA-48 inhibitor, which has designed a substance conforming to the following general structural formula:

[0047]

[0048] In the above formula: the 2 and 3 positions contain a double bond; the R1, R2, R3, R4 and R5 are hydroxy substances, and the OXA-48 inhibitory activity of the synthesized compound is measured.

Embodiment 3

[0049] Example 3: Determination of the inhibitory activity of quercetin and its structural analogs on OXA-48 (IC 50 )

[0050] The change of absorbance after OXA-48 serine β-lactamase hydrolyzed the substrate was monitored at a wavelength of 495 nm using cefnitrothiophene as the hydrolysis substrate. Assay buffer is 0.1M PBS (pH 7.0), 30mM NaHCO 3 , the temperature is 25 ℃. The specific method is as follows: incubate the enzyme and inhibitor in the buffer for 30 minutes, so that the inhibitor and the enzyme can fully interact, add the mixture to a 96-well plate, and immediately use a microplate reader to record the absorbance change before the reaction 30s after adding the substrate. Calculate the initial reaction rate. The concentration of substrate and enzyme was kept constant throughout the experiment, the concentration of inhibitor was changed, the percentage inhibition rate at different inhibitor concentrations was calculated, and the IC was calculated by nonlinear fit...

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PUM

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Abstract

The invention provides application of a flavonoid compound to preparation of a serine beta-lactamase inhibitor. Specifically, the flavonoid compound is any one or a combination of more of quercetin, fisetin, luteolin, 3 ', 4', 7-trihydroxyflavone, apigenin, kaempferol and dihydroquercetin, and particularly discloses application of the flavonoid compound in preparation of a D-serine beta-lactamase OXA-48 inhibitor. The flavonoid compound disclosed by the invention is combined with a beta-lactam drug to resist drug-resistant bacteria generating OXA-48.

Description

technical field [0001] The present invention relates to the field of serine beta-lactamase inhibitors, in particular to the use of flavonoids as serine beta-lactamase inhibitors. Background technique [0002] Beta-lactam antibiotics such as penicillins, cephalosporins, and carbapenems are one of the most effective drugs for the treatment of bacterial infections, and they are also the most widely used clinically. However, with the overuse of antibiotics, a variety of multi-drug resistant bacteria have been found clinically, and one of their main drug resistance mechanisms is the expression of β-lactamase, which catalyzes the hydrolysis of the β-lactam ring of antibiotics, thereby rendering the antibiotics ineffective. . According to the amino acid sequence homology of β-lactamase and the mechanism of enzymatic hydrolysis of antibiotics, β-lactamase can be divided into four categories: A-D. Classes A, C and D are serine β-lactamases (SβLs) that hydrolyze antibiotics via seri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K31/407A61K31/496A61P31/04C07D311/30
CPCA61K31/352A61K31/407A61K31/496A61P31/04C07D311/30A61K2300/00
Inventor 万一张月娟高磊秦川张绪王军
Owner MICROBIOLOGY INST OF SHAANXI
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