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Inhibitor and application thereof in inhibiting chitinase and hexosaminidase activity

A technology of hexosaminidase and chitinase, applied in application, biocides, insecticides, etc., can solve the problem of no report on the biological activity of glycosyl hydrolases

Active Publication Date: 2017-06-16
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The compound phlegmacin B1 is a secondary metabolite secreted by the toadstool Cortinarius odorifer, which is closely related to the color formation of the toadstool. However, so far, there are few reports on the biological activity of the compound phlegmacin B1, especially for glycosyl hydrolases. Biological activity has not been reported

Method used

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  • Inhibitor and application thereof in inhibiting chitinase and hexosaminidase activity
  • Inhibitor and application thereof in inhibiting chitinase and hexosaminidase activity
  • Inhibitor and application thereof in inhibiting chitinase and hexosaminidase activity

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Using chitinase OfChi-h and hexosaminidase OfHex1 as targets, 556 microbial secondary metabolites were screened for inhibitors. Specific steps are as follows:

[0022] Positive control: Set up 2 parallel positive controls. Under the condition of 30℃ reaction temperature and 100μL reaction system, 2nmol / L glycosyl hydrolase and 50μmol / L substrate (OfChi-h: MU-(GlcNAc) 2 ; OfHex1: MU-GlcNAc) was incubated in 20mmol / L pH6.0 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 450nm The absorbance value at the wavelength.

[0023] Experimental group: set up 3 parallel experimental groups. Under the condition of 30℃ reaction temperature and 100μL reaction system, 2nmol / L glycosyl hydrolase and 50μmol / L substrate (OfChi-h: MU-(GlcNAc) 2 ; OfHex1: MU-GlcNAc) and 13ppm compound were incubated in 20mmol / L pH 6.0 phosphate buffer fo...

Embodiment 2

[0028] 1) Absolute configuration identification of compound phlegmacin B1

[0029] Take 500 μL of 100% methanol and add it into the cuvette for circular dichroism scanning, and the result is used as a negative control. The compound phlegmacin B1 was dissolved in 100% methanol to make the final concentration 0.7 μM, and 500 μL was added to a cuvette, and its circular dichroism spectrum was measured in a circular dichroism instrument, and the results were as follows figure 1 As shown in A. The circular dichroism chromatogram measured by the experiment is compared with the circular dichroism chromatogram in the document "Biosynthesisand Stereochemistry of Phlegmacin-Type Fungal Pigments" to obtain the absolute configuration of compound phlegmacin B1, such as figure 1 b. Experimental parameters: optical path 2mm; scanning wavelength 190-350nm; speed 1nm / s; repetition times 3 times.

[0030] 2) Inhibition constant K i determination

[0031] OfChi-h: MU-(GlcNAc) 2 As substrate...

Embodiment 3

[0038] The specific steps of the insecticidal activity evaluation of compound phlegmacin B1 are as follows:

[0039] 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 phlegmacin B1 was dissolved in 5% DMSO at a concentration of 0.5 μM. The larvae of the control group were injected with 2 μL of 5% DMSO, and the larvae of the experimental group were injected with 2 μL of the compound phlegmacin B1 at a concentration of 0.5 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 Figure 4 , where A is the control group, B is the experimental group, and C is the phenotype. The results sho...

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Abstract

The invention discloses application of a compound for efficient inhibition of chitinase OfChi-h and hexosaminidase OfHex1 activity, and relates to application of a compound phlegmacin B1 and its derivatives in inhibiting chitinase OfChi-h and hexosaminidase OfHex1 activity. The used final concentration is not less than 13ppm, under the concentration, the measured inhibition rates are 90.4% and 71.4% respectively, and inhibition constants Ki are 5.5 microM and 26 microM respectively. The invention proves that the compound phlegmacin B1 has good application prospect in the prevention and control of agricultural pests, especially in prevention and control of lepidoptera insects.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to the insecticidal activity of a fungal secondary metabolite. 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. Currently, two types of glycosyl hydrolases are known to be involved in the hydrolysis of chitin, namely chitinases from the glycosyl hydrolase 18 family (EC 3.2.1.14) and chitinases from the glycosyl hydrolase 20 family. β-N-acetyl-D-hexosaminidase (EC 3.2.1.52) with proteolytic activity, the forme...

Claims

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Application Information

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IPC IPC(8): C07C49/755C07C50/38A01N35/06A01P7/04G01N21/31
CPCA01N35/06C07C49/755C07C50/38G01N21/31
Inventor 杨青刘田陈磊段燕伟路新华
Owner DALIAN UNIV OF TECH
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