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Application of kasugamycin and derivatives thereof as chitinase inhibitor

A technology of chitinase and kasugamycin, applied in the application, biocide, animal repellent and other directions

Active Publication Date: 2017-10-03
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The biological activity of kasugamycin and its derivatives against the glycosyl hydrolase of the 18 family has not been reported yet. Therefore, the study of kasugamycin as an inhibitor of the glycosyl hydrolase of the 18 family has very positive significance for expanding its application

Method used

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  • Application of kasugamycin and derivatives thereof as chitinase inhibitor
  • Application of kasugamycin and derivatives thereof as chitinase inhibitor
  • Application of kasugamycin and derivatives thereof as chitinase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Using chitinase OfChtI as the target, 556 microbial secondary metabolites were screened for inhibitors. Specific steps are as follows:

[0024] Positive control: Set up 2 parallel positive controls. Under the condition of 30℃ reaction temperature and 100μL reaction system, 2nmol / L glycosyl hydrolase OfChtI and 50μmol / L substrate (MU-(GlcNAc) 2 ) in 20mmol / L pH 6.0 phosphate buffer for 30min, then add 100μL 0.5mol / L sodium carbonate solution to terminate the reaction, and measure the absorbance value at 450nm wavelength after the reaction solution is excited with 360nm wavelength excitation light.

[0025] Experimental group: set up 3 parallel experimental groups. Under the condition of 30℃ reaction temperature and 100μL reaction system, 2nmol / L glycosyl hydrolase OfChtI and 50μmol / L substrate (MU-(GlcNAc) 2 ) and 50 μM compound were incubated in 20 mmol / L pH 6.0 phosphate buffer for 30 min, then 100 μL 0.5 mol / L sodium carbonate solution was added to terminate the re...

Embodiment 2

[0030]1) Half inhibitory concentration IC 50 determination

[0031] OfChtI: MU-(GlcNAc) 2 As a substrate, the substrate concentration was 30 μM. Under the same substrate concentration, eight groups of compound concentration gradients with final concentrations of 200, 100, 50, 25, 12.5, 6.25, 3.125, and 1.5625 μM were used to determine 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 The absorbance value was measured at a wavelength of 450 nm after being excited by 360 nm excitation light. IC obtained after data fitting 50 =14μM, the result is as figure 2 shown.

[0032] 2) Determination of applicable objects of compounds

[0033] GH18: 18 family chitinases from 7 different species were selec...

Embodiment 3

[0035] The specific steps of the insecticidal activity evaluation of the compound Kasugamycin are as follows:

[0036] In the experiment, healthy larvae on the fourth day of the fifth instar were selected as experimental materials, and a control group and an experimental group were set up. Compound Kasugamycin with H 2 O was dissolved at a concentration of 500 μM. Control group larvae were injected with 2 μL of H 2 O, the larvae of the experimental group were injected with 2 μL of the compound Kasugamycin at a concentration of 500 μM. The injected larvae were cultured at 26°C, with a relative humidity of 70%-90%, 16 hours of light per day, and 8 hours of darkness until all of them pupated. During this period, normal larvae, dead larvae, normal pupae, and abnormal pupae Quantities and phenotypes were counted. The statistical results are plotted as image 3 , where A is the control group and B is the experimental group. The results showed that the development of larvae in ...

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Abstract

The invention discloses application of kasugamycin and derivatives thereof as a chitinase inhibitor, and a structural formula of the inhibitor is shown in I. Inhibitory effect, selectivity and insecticidal activity of selected compounds are evaluated in an inhibitory activity research, and the results show that the compound Kasugamycin has an inhibitory effect on OfChtI. When final concentration of usage is not less than 50 [mu]M, the inhibitory rate is 86.4% and the half maximal inhibitory concentration (IC50) value is 14 [mu]M. The kasugamycin and derivatives thereof described in the invention have wide application prospects in the fields of biology and chemical biology, especially in delaying the development of Asian corn borers.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to the application of a fungal secondary metabolite and a derivative thereof as an inhibitor of chitinase. 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. Insect chitinase ChtI (chitinase I) from the glycosyl hydrolase 18 family is an indispensable chitin hydrolase in insect molt and metamorphosis development. Down-regulating or interfering with the expression level of ChtI gene will lead to abnormal molt an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/16A01N43/40A01P7/04
CPCA01N43/16A01N43/40
Inventor 杨青刘田姜熙杨君屈明博
Owner DALIAN UNIV OF TECH
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