Arylsulfatase and beta-glucuronidase inhibitor as well as preparation method and application thereof

A technology of aryl sulfatase and glucuronidase, which is applied in the medical field and can solve the problems of high price of inhibitors and the like

Pending Publication Date: 2021-03-23
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

Method used

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  • Arylsulfatase and beta-glucuronidase inhibitor as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] 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:

[0020] Test tube 1:

[0021] Add 0.336U of arylsulfatase to test tube 1, then add peracetic acid solution (solubility is 2mol / L), so that the concentration of peracetic acid in Tris-HCl buffer is 10μmol / L, and then press 800μmol / L Add the p-nitrophenol sulfuric acid conjugate according to the standard, place the glass test tube in a water bath at 37°C to react for 1 hour, then add 2 mL of 0.5 mol / L sodium hydroxide to terminate the reaction, and use the standard method (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34:225-229) assay for arylsulfatase activity.

[0022] Test tube 2:

[0023] Add 0.180 U of glucuronidase in test tube 2, then add peracetic acid solution (solubility is 2mol / L), so that the concentration of peracetic acid in Tris-HCl buffer solution is 10 μmol...

Embodiment 2

[0025] 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:

[0026] Test tube 1:

[0027] Add 0.336U of arylsulfatase to test tube 1, then add peracetic acid solution (solubility is 2mol / L), so that the concentration of peracetic acid in Tris-HCl buffer solution is 50μmol / L, and then press 800μmol / L Add the p-nitrophenol sulfuric acid conjugate according to the standard, place the glass test tube in a water bath at 37°C to react for 1 hour, then add 2 mL of 0.5 mol / L sodium hydroxide to terminate the reaction, and use the standard method (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34:225-229) assay for arylsulfatase activity.

[0028] Test tube 2:

[0029] Add 0.180 U of glucuronidase in test tube 2, then add peracetic acid solution (solubility is 2mol / L), so that the concentration of peracetic acid in Tris-HCl buffer solution i...

Embodiment 3

[0031] 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:

[0032] Test tube 1:

[0033] Add 0.336U of arylsulfatase to test tube 1, then add peracetic acid solution (solubility is 2mol / L), so that the concentration of peracetic acid in Tris-HCl buffer is 100μmol / L, and then press 800μmol / L Add the p-nitrophenol sulfuric acid conjugate according to the standard, place the glass test tube in a water bath at 37°C to react for 1 hour, then add 2 mL of 0.5 mol / L sodium hydroxide to terminate the reaction, and use the standard method (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34:225-229) assay for arylsulfatase activity.

[0034] Test tube 2:

[0035] Add 0.180U of glucuronidase to test tube 2, then add peracetic acid solution (solubility is 2mol / L), so that the concentration of peracetic acid in Tris-HCl buffer solution is 100 μmo...

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Abstract

The invention belongs to the field of medicine, and discloses an arylsulfatase and beta-glucuronidase inhibitor as well as a preparation method and application thereof. The preparation method of the arylsulfatase and beta-glucuronidase inhibitor comprises the following steps of adding peracetic acid into a solvent to obtain a solution, namely the arylsulfatase and beta-glucuronidase inhibitor. Compared with conventional medical treatment inhibitors such as STX64 and D-Sacchuric acid, 1, 4-lactone and the like, the arylsulfatase and beta-glucuronidase inhibitor has the advantages of being goodin effective inhibition concentration effect, capable of achieving inhibition of different degrees according to needs, easy to operate, low in cost, rapid and the like, and has a certain 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, a number of inhibitors of arylsulfatase and glucuronide have been developed. At present, STX64 and D-Sacchuric acid, 1,4-lactone are two commonl...

Claims

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Application Information

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IPC IPC(8): A61K31/327A61P35/00
CPCA61K31/327A61P35/00
Inventor刘则华钟姝姝张俊党志
OwnerSOUTH CHINA UNIV OF TECH