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Application of nitidine chloride in preparation of urease inhibitor

A technology of chlorinated acanthine and urease inhibitors, which is applied in the field of natural compound applications, can solve the problems of acetohydroxamic acid losing its effect, and achieve the effects of enriching optional types, reducing drug resistance, and good safety

Pending Publication Date: 2021-12-14
遵义医科大学珠海校区
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the effectiveness of existing urease inhibitors is mostly affected by factors such as temperature, time, and pH environment. Therefore, the relatively mature urease inhibitor in China is acetohydroxamic acid, which has the advantages of simple synthesis, low cost, and low toxicity. specialty
However, the main problem is that the long-term use of acetohydroxamic acid will cause the microorganisms to develop adaptability and drug resistance, which will lead to the loss of the effect of acetohydroxamic acid

Method used

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  • Application of nitidine chloride in preparation of urease inhibitor
  • Application of nitidine chloride in preparation of urease inhibitor
  • Application of nitidine chloride in preparation of urease inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: Research on the inhibitory effect of chlorinated diacid on urease

[0038] Mix the canavalia urease solution and a series of concentration test drug solutions, and incubate at 37°C for 20 minutes; add urea solution, and react in the dark for 20 minutes at room temperature; add Berthelot color developing solution in the dark for 10 minutes, Pipette 200 μL of the incubation solution onto a 96-well plate, and measure the absolute value of OD at 595 nm on a microplate reader. Each concentration was done 3 times in parallel. The blank sample was replaced by the solvent of each dilution, and the other operations were the same as above, and the OD blank was measured. Calculate the corresponding OD relative value according to formula 1. According to formula 2, the residual enzyme activity (Residual activity, RA) was obtained, and the corresponding half inhibitory concentration IC was obtained by GraphPad 50 .

[0039] OD 相对 =OD 绝对 –OD 空白 (Formula 1)

[0040]...

Embodiment 2

[0042] Example 2: Research on the type of inhibition of urease by chlorinated double-sided alkaloids

[0043] A certain concentration of cana urease was mixed with a series of concentrations of echinacea chloride solution (0, 25, 50, 100 μM), and incubated at 37° C. for 20 minutes. Then add a series of concentrations of urea solution (0.9375-30mM) at room temperature to react in the dark for 20 minutes, then develop color according to the method of Example 1 and measure the OD 绝对 value and obtain the corresponding OD 相对 value. The solvent of the added substance was used as a blank control, and the parallel determination was performed 3 times. The experiment passes the reciprocal of the reaction speed (1 / V, that is, 1 / OD 相对 ) to the reciprocal (1 / [urea]) of the substrate concentration to make a Lineweaver-Burk diagram, and finally obtain the kinetic parameter K by combining the L-B curve with formula 3 M , v max , and through the L-B curve to obtain the inhibition constant...

Embodiment 3

[0046] Example 3: Kinetic study on the inhibition of urease by chlorinated dihedral

[0047] Take the same volume of a series of concentrations of Echinacea chloride solution (0, 25, 50, 100 μM) and a certain concentration of canavalia urease and mix well, then incubate in a 37°C incubator for 20min, then add an equal volume of urea at room temperature The solution was reacted in the dark for 20 minutes (incubation system) or directly added to an equal volume of urea solution without incubation in an incubator and reacted in the dark for 20 minutes (incubation system). Then pipette the reaction solution into a 1.5mL centrifuge tube at different time intervals (0-30min), then develop color according to the method of Example 1 and measure the OD 绝对 value and obtain the corresponding OD 相对 value. The solvent of the added substance was used as a blank control, and the parallel determination was performed 3 times.

[0048] The OD obtained from the above two reaction systems 相对 ...

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Abstract

The invention belongs to the technical field of application of natural compounds, and discloses application of nitidine chloride in preparation of a urease inhibitor. The nitidine chloride has a remarkable urease inhibition effect, has the characteristics of simple structure, good safety and the like, has good application value and development prospect, and can be used as a urease inhibitor in the fields of plant fertilizers, feed additives, medicines and the like.

Description

technical field [0001] The invention belongs to the technical field of application of natural compounds, and in particular relates to the application of acanthine chloride in the preparation of urease inhibitors. Background technique [0002] Urease, also known as urease or urea amidohydrolase, is a Ni-containing enzyme that widely exists in various organisms and ecological environments. 2+ of metalloenzymes. Urease catalyzes the hydrolysis of urea to ammonia and thus plays an important role in nitrogen metabolism. However, if the activity of urease is too high, the catalytic hydrolysis of urea will be too fast, and a large amount of ammonia gas will be released, which will bring various hazards to agriculture, animal husbandry, the environment and even human health. In agriculture, if the activity of urease is too high, the catalytic hydrolysis of urea will be too fast, and a large amount of ammonia gas will be released, which will seriously reduce the nitrogen utilizatio...

Claims

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Application Information

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IPC IPC(8): A61K31/4741A61P1/00A61P1/04A61P13/04C05G3/90A23K20/132A23K20/121A23K20/116A23K50/10
CPCA61K31/4741A61P1/00A61P1/04A61P13/04C05G3/90A23K20/132A23K20/121A23K20/116A23K50/10
Inventor 鲁强李彩兰刘玫瑰
Owner 遵义医科大学珠海校区
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