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Use of l-cysteine ​​ester compounds in inhibiting ndm-1

A technology of cysteine ​​ester and NDM-1, which is applied in the field of pharmacy, can solve the problems of undiscovered L-cysteine ​​ester compounds and achieve the effects of solving drug resistance, eliminating hydrolysis and improving curative effect

Inactive Publication Date: 2016-08-03
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The application of L-cysteine ​​ester compounds in inhibiting bacterial activity has not been found so far

Method used

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  • Use of l-cysteine ​​ester compounds in inhibiting ndm-1
  • Use of l-cysteine ​​ester compounds in inhibiting ndm-1
  • Use of l-cysteine ​​ester compounds in inhibiting ndm-1

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0037] Step 1. Preparation of NDM-1 substrate stock solution

[0038] Imipenem monohydrate (Imipenemmonohydrate, purchased from Sigma Company) was dissolved in 50 mM HEPES (purchased from BioBasie Company), and prepared into a 10 mM substrate stock solution for future use.

[0039] Step 2. Treatment of Compounds

[0040] Compound in 95%DMSO+5%ddH 2 Dissolve in O, and prepare a solution with a concentration of 100mM, then place the prepared compound solution in a 1.5mlep tube, and store it at 4°C for future use.

[0041] Step 3. Preparation of NDM-1 protein buffer

[0042] Dissolve NDM-1 (provided by the MDC protein purification group of our laboratory, see YuGuo, JingWang et al., Astructural view of the antibiotic degradation enzyme NDM-1 from a superbug. Protein & Cell, 2011, 2(5): 384-394 for the preparation method) in protein buffer (pH=6.8) , prepared into 50nM NDM-1 protein buffer, wherein the protein buffer contains 50mM HEPES, 5μM ZnCl 2 (purchased from BioBasic Compa...

Embodiment 1

[0054] Embodiment 1 N-benzyloxycarbonyl-L-cysteine ​​methyl ester inhibits the determination of NDM-1 activity

[0055]

[0056] The N-benzyloxycarbonyl-L-cysteine ​​methyl ester used was purchased from Bailingwei with a purity of 98%.

[0057] N-benzyloxycarbonyl-L-cysteine ​​methyl ester (4 mg) was dissolved in 95% DMSO double distilled water (148.5 μL) to prepare a solution with a concentration of 100 mM, and then the solution was placed in a 1.5 mlep tube, Store at 4°C.

[0058] Then according to the above activity test method step 5 (preliminary screening of compound) and step 6 (IC of compound) 50 Determination of the value) described in the operation. Then take the concentration logarithm of N-benzyloxycarbonyl-L-cysteine ​​methyl ester as the abscissa, and the remaining active fraction of NDM-1 as the ordinate to draw a curve, see image 3 . Finally, according to the curve, using GraphPad Prismversion5.0 software to calculate, the obtained IC 50 The value is 1....

Embodiment 2

[0059] Example 2 Determination of NDM-1 activity inhibited by N-acetyl-L-cysteine ​​methyl ester

[0060]

[0061] The N-acetyl-L-cysteine ​​methyl ester used was purchased from Bailingwei with a purity of 99%.

[0062] N-acetyl-L-cysteine ​​methyl ester (4 mg) was dissolved in 95% DMSO double-distilled water (225.8 μL) to prepare a solution with a concentration of 100 mM, and then the solution was placed in a 1.5 mlep tube, and the Store at 4°C.

[0063] Proceed as described in steps 5 and 6 of the activity test method above. Then take the logarithm of the concentration of N-acetyl-L-cysteine ​​methyl ester as the abscissa, and the remaining active fraction of NDM-1 as the ordinate to draw a curve, see Figure 4 . Finally, according to the curve, the GraphPad Prismversion5.0 software is used to calculate the obtained IC 50 The value is 33.94±2.8 μM.

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Abstract

The invention provides L-cysteine compound of a following general formula for restraining new delhi metallo (NDM)-1 activity in medicine. R1 is hydrogen or aromatic oxygen carbonyl or C1-C4 alkyl acyl, and R2 is C1-C4 alkyl. The compound can well restrain NDM-1 activity.

Description

technical field [0001] The present invention relates to the field of pharmacy, in particular to the use of L-cysteine ​​ester compounds. Background technique [0002] In the 1950s and 1960s, known as the "golden age" of antibiotics, about 7 million people died of infectious diseases worldwide every year, and this figure rose to 20 million by 1999. The main reason for the increase in the fatality rate is the difficulty in medication brought by drug-resistant bacteria. [0003] At present, the problem of bacterial resistance has become very serious. In developed countries, 5% to 10% of hospitalized patients have one or more infections. There are about 2 million patients with nosocomial infection in the United States every year, 90,000 people die, and the economic loss reaches 4.5 billion to 5.7 billion US dollars. In developing countries, the risk of nosocomial infection is 2 to 20 times higher than in developed countries. The incidence rate of nosocomial infection in our ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/27A61K31/223A61P31/04
CPCY02A50/30
Inventor 饶子和陈悦杨诚白翠改郭宇徐寅通李宁宁夏强娄智勇
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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