Aryl sulfatase and glucuronidase inhibitor, preparation method thereof and application of inhibitor

A technology of arylsulfatase and glucuronidase, which is applied in the medical field, can solve the problems of expensive inhibitors and high half-inhibitory concentrations, and achieve the effects of low price, good effect and simple operation

Inactive Publication Date: 2020-12-22
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, STX64 and D-Sacchuric acid, 1,4-lactone are two commonly used inhibitors, which are used to inhibit arylsulfatase and glucuronidase respectively, but the inhibitors are expensive and the half-inhibitory concentration is relatively high.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Take two 3mL Tris-HCl buffer solution (pH=5.8) in two glass test tubes, denoted as test tube 1 and test tube 2. Proceed as follows for test tube 1 and test tube 2:

[0027] Test tube 1:

[0028] Add 0.212 U of arylsulfatase to test tube 1, and then pass through NO, so that the concentration of NO in the Tris-HCl buffer solution is 250 μg / L, and then add p-nitrophenol sulfuric acid conjugate according to the standard of 800 μmol / L. The glass test tube was placed in a water bath at 37°C for 1 hour, and then the reaction was terminated by adding 2 mL of 0.5 mol / L sodium hydroxide, using a standard method (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34: 225- 229) Determination of arylsulfatase activity.

[0029] Test tube 2:

[0030] Add 0.045U of glucuronidase to test tube 2, and then pass through NO, so that the concentration of NO in the Tris-HCl buffer solution is 250 μg / L, and then add p-nitrophenol glucuronide according to the sta...

Embodiment 2

[0032] Take two 3mL Tris-HCl buffer solution (pH=5.8) in two glass test tubes, denoted as test tube 1 and test tube 2. Proceed as follows for test tube 1 and test tube 2:

[0033] Test tube 1:

[0034] Add 0.212 U of arylsulfatase to test tube 1, and then pass through NO, so that the concentration of NO in the Tris-HCl buffer solution is 250 μg / L, and then add p-nitrophenol sulfuric acid conjugate according to the standard of 800 μmol / L. Place the glass test tube in a water bath at 37°C for 1 hour, then stop the reaction with 2 mL of 0.5 mol / L sodium hydroxide, and use a standard method (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34: 225-229 ) to measure the activity of arylsulfatase.

[0035] Test tube 2:

[0036] Add 0.045U of glucuronidase to test tube 2, and then pass through NO, so that the concentration of NO in the Tris-HCl buffer solution is 250 μg / L, and then add p-nitrophenol glucuronide according to the standard of 800 μmol / L. ...

Embodiment 3

[0038] Take two 3mL Tris-HCl buffer solution (pH=5.8) in two glass test tubes, denoted as test tube 1 and test tube 2. Proceed as follows for test tube 1 and test tube 2:

[0039] Test tube 1:

[0040] Add 0.212 U of arylsulfatase to test tube 1, then pass through NO, so that the concentration of NO in the Tris-HCl buffer solution is 500 μg / L, and then add p-nitrophenol sulfuric acid conjugate according to the standard of 800 μmol / L. Place the glass test tube in a water bath at 37°C for 1 hour, then stop the reaction with 2 mL of 0.5 mol / L sodium hydroxide, and use a standard method (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34: 225-229 ) to measure the activity of arylsulfatase.

[0041] Test tube 2:

[0042] Add 0.045U of glucuronidase to test tube 2, and then pass through NO, so that the concentration of NO in the Tris-HCl buffer solution is 500 μg / L, and then add p-nitrophenol glucuronide according to the standard of 800 μmol / L. bod...

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Abstract

The invention belongs to the field of medicine, and discloses an aryl sulfatase and glucuronidase inhibitor, a preparation method thereof and application of the inhibitor. The preparation method for the aryl sulfatase and glucuronidase inhibitor comprises the following steps: adding NO or a chemical reactant capable of producing the NO by a reaction into a solvent to obtain a solution, namely thearyl sulfatase and glucuronidase inhibitor. Compared with conventional medical treatment inhibitors STX64, D-Saccharic acid,1,4-lactone and the like, the aryl sulfatase and glucuronidase inhibitor hasthe advantages of low effective inhibition concentration, good effect, simple operation, low cost, rapidness and the like, can perform inhibition of different degrees as needed, and has a wide application prospect in the medical field.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an inhibitor of arylsulfatase and glucuronidase, a preparation method and application thereof. Background technique [0002] Arylsulfatase (arylsulfatase) and glucuronidase (β-glucuronidase) widely exist in various organs of humans and animals, and their important role is to convert natural hormones, such as natural estrogen sulfate conjugates or glucuronidase The acid conjugates are transformed into corresponding natural estrogens. In animals, arylsulfatase and glucuronidase are closely related to the normal physiological functions of the human body. For example, in the urine and blood of patients with breast cancer, rectal cancer, and pancreatic cancer, arylsulfatase and glucuronidase are more active than normal people. Therefore, many drugs that inhibit arylsulfatase and glucuronide have been developed. At present, STX64 and D-Sacchuric acid, 1,4-lactone are two commonly ...

Claims

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Application Information

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IPC IPC(8): A61K33/00A61P35/00
CPCA61K33/00A61P35/00C01B21/24A61K31/4422A61K31/21A61K31/34A61K9/08
Inventor刘则华张俊钟姝姝党志尹华
OwnerSOUTH CHINA UNIV OF TECH