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Application of berberine and its derivatives as hexosaminidase inhibitors

A technology of hexosaminidase and inhibitor, applied in the application field of inhibitors, can solve problems such as abnormal molting and death of insects

Active Publication Date: 2020-04-14
DALIAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Down-regulation or interference of Hex1 gene expression level will lead to abnormal molt and death of insects

Method used

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  • Application of berberine and its derivatives as hexosaminidase inhibitors
  • Application of berberine and its derivatives as hexosaminidase inhibitors
  • Application of berberine and its derivatives as hexosaminidase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Taking hexosaminidase OfHex1 and HsHexB as targets, 35 compounds listed in Table 1 were screened for inhibitors. Specific steps are as follows:

[0029] Positive control: Set up 2 parallel positive controls. Under the conditions of 30℃ reaction temperature and 100μL reaction system, 2nmol / L glycosyl hydrolase and 50μmol / L substrate (MU-GlcNAc) were incubated in 20mmol / L pH 6.5 phosphate buffer for 30min, and then 100μL 0.5mol / L sodium carbonate solution terminated the reaction, and the reaction solution was excited with excitation light with a wavelength of 360nm, and then the absorbance value at a wavelength of 450nm was measured.

[0030] Experimental group: set up 3 parallel experimental groups. Under the conditions of 30°C reaction temperature and 100 μL reaction system, 2 nmol / L glycosyl hydrolase, 50 μmol / L substrate (MU-GlcNAc) and 10 μM compound were incubated in 20 mmol / L pH 6.5 phosphate buffer for 30 min, Afterwards, 100 μL of 0.5 mol / L sodium carbonate so...

Embodiment 2

[0035]1) Inhibition constant K i determination

[0036] OfHex1: MU-GlcNAc was used as the substrate, and three groups of substrate concentration gradients were set up for the reaction, and the final concentrations were 12.5 μM, 25 μM and 50 μM, respectively. In each group of substrate concentrations, five groups of compound concentration gradients with final concentrations of 5, 2.5, 1.25, 0.625 and 0 μM were taken to measure the inhibitory activity. The reaction system is 100 μL, the buffer environment is 20 mM phosphate buffer, pH 6.5, the final enzyme concentration is 2 nM, the reaction temperature is 30 ° C, the reaction time is 30 min, and then 100 μ L of 0.5 M sodium carbonate solution is added to terminate the reaction, and the released MU After being excited by 360nm excitation light, the absorbance value was measured at a wavelength of 450nm. The data were plotted by Dixon method, and the inhibition constants Ki of Sysu-00021 and Sysu-00679 to OfHex1 were 2 μM and 1...

Embodiment 3

[0038] The specific steps for evaluating the insecticidal activity of the compound Sysu-00021 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. The compound Sysu-00021 was dissolved in 5% DMSO, and the final concentration of the solution was 100 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 Sysu-00021 at a concentration of 100 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 2 , where A is the control group and B is the experimental group. The resul...

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Abstract

The invention discloses application of berberine and a derivative of the berberine as a hexosaminidase inhibitor. The general structure formula of the hexosaminidase inhibitor is shown as I or II; in all screened 35 compounds, the berberine and the derivative of the berberine show certain inhibition activity on hexosaminidase OfHex1; particularly, the suppression rate of Sysu-00021 and Sysu-00679 on the OfHex1 enzyme is respectively 76 percent and 79 percent, and the inhibition constant Ki is respectively 2mu M and 1.8mu M. Compound applicable object determination shows that under the final concentration of 10mu M, the compound shows higher inhibition activity on the hexosaminidase OfHex1; no inhibition activity is shown on the hexosaminidase HsHexB derived from the human. In a word, the berberine and the derivative of the berberine have wide application prospects in the fields of biology, chemicobiology and the like.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to the application of alkaloids and derivatives thereof as hexosaminidase 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. Insect N-acetyl-D-hexosaminidase Hex1 (N-acetyl-D-hexosaminidase) from the glycosyl hydrolase 20 family is an indispensable chitin hydrolase in insect molt and metamorphosis. Down-regulating or disturbing the expression level of Hex1 gene will lead to abnormal molting and deat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N43/90A01P7/04
CPCA01N43/90
Inventor 杨青刘田段燕伟唐静仪屈明博杨君
Owner DALIAN UNIV OF TECH
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