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Chitinase inhibitor and application thereof

A technology of chitinase and inhibitors, applied in the direction of insecticides, anti-inflammatory agents, biocides, etc., can solve the problems of abnormal molting, death, and developmental stagnation of insects, and achieve a wide range of anti-allergic and asthma effects

Active Publication Date: 2018-08-31
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Inhibition of nematode chitinase causes developmental arrest
In addition, down-regulating or knocking out insect chitinase will lead to abnormal molt and death of insects

Method used

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  • Chitinase inhibitor and application thereof
  • Chitinase inhibitor and application thereof
  • Chitinase inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Taking chitinases SmChiA, SmChiB, AfChiB1, CeChtI, OvChtI, OfChtI, OfChtII-C2, OfChi-h, HsChit1 and AMCase as targets, 75 compounds listed in Table 1 and Table 2 were screened for inhibitors. Specific steps are as follows:

[0045] Positive control: Set up 3 parallel positive controls. Under the condition of 30℃ reaction temperature and 100μL reaction system, 2nmol / L chitinase and 50μmol / L substrate (MU-(GlcNAc) 2 ) was incubated in 20mmol / L pH 6.0 phosphate buffer for 30min, then 100μL 0.5mol / L sodium carbonate solution was added to terminate the reaction, and the reaction solution was excited with 360nm wavelength excitation light to measure the absorbance value at 450nm wavelength.

[0046] Experimental group: set up 3 parallel experimental groups. Under the condition of 30℃ reaction temperature and 100μL reaction system, 2nmol / L chitinase and 50μmol / L substrate (MU-(GlcNAc) 2 ) and the compounds corresponding to the concentrations in Tables 1 and 2 were incubated...

Embodiment 2

[0051] Inhibition constant K i determination

[0052] SmChiA, SmChiB, OfChi-h, HsChit1 and AMCase: MU-(GlcNAc) 2 As substrates, three groups of substrate concentration gradients were set up for the reaction, and the final concentrations were 15 μM, 30 μM and 50 μM, respectively. OvChtI: MU-(GlcNAc) 3 As substrates, three sets of substrate concentration gradients were set up for the reaction, and the final concentrations were 5 μM, 10 μM and 20 μM, respectively. Under each group of substrate concentrations, multiple groups of suitable compound concentration gradients were taken to measure the inhibitory activity. The reaction system was 100 μL, the buffer environment was 20 mM phosphate buffer, pH 6.0, the final enzyme concentration was 2 nM, the reaction temperature was 30 ° C, the reaction time was 30 min, and then 100 μL of 0.5 M sodium carbonate solution was added to terminate the reaction, and the released MU After being excited by 360nm excitation light, the absorbanc...

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Abstract

The invention discloses a chitinase inhibitor and application thereof. The chitinase inhibitor is first-bit and third-bit derivatives of 2-amino-pyridino-piperidine. The structural formula of the chitinase inhibitor is formula I as shown in the specification. On the basis of inhibition effects and selectivity, the inhibition effect is evaluated and studied for the inhibition activity of compounds,and in all 75 compounds after secondary screening, the first-bit and third-bit derivatives of 2-amino-pyridino-piperidine have certain inhibition activity upon chitinase of human beings, onchocerca volvulus, caenorhabditis elegans, asiatic corn borer, aspergillus fumigates and serratia marcescens. In a word, the first-bit and third-bit derivatives of 2-amino-pyridino-piperidine, which are disclosed by the invention, have wide application prospects in fields such as biology and chemicobiology.

Description

technical field [0001] The invention belongs to the field of biotechnology, and specifically relates to the application of 1- and 3-position derivative compounds of 2-amino-bipyridopyrimidine as chitinase inhibitors. Background technique [0002] Chitin is a natural linear linear polysaccharide with N-acetyl-β-D-glucosamine (GlcNAc) as the basic unit and connected by β-1,4 glycosidic bonds. As an important structural component, chitin is abundantly present in the cell walls of fungi and diatoms, the shells of mollusks, the egg shells of nematodes, and the exoskeletons of crustaceans and insects, and the dynamic balance of its synthesis and hydrolysis is crucial for these organisms. growth and development are extremely important. Chitinase Cht (chitinase) from the glycosyl hydrolase 18 family is involved in bacterial nutrient uptake, fungal cell wall remodeling, insect molting development, and human lung immune regulation processes. Early studies on chitinase inhibitors fou...

Claims

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Application Information

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IPC IPC(8): C07D471/14A61P31/04A61P31/10A61P37/08A61P11/06A01P7/04A01P5/00A61P29/00
CPCA61P11/06A61P29/00A61P31/04A61P31/10A61P37/08C07D471/14
Inventor 杨青姜熙刘田杨君屈明博
Owner DALIAN UNIV OF TECH
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