Aryl sulfatase and glucoside aldehydic acid enzyme inhibitor, preparation method therefor and application of aryl sulfatase and glucoside aldehydic acid enzyme inhibitor

An aryl sulfatase and glucuronidase technology, applied in the medical field, can solve the problems of expensive inhibitors and high 50% inhibitory concentration

Inactive Publication Date: 2021-03-05
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 50% inhibitory concentration is high

Method used

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  • Aryl sulfatase and glucoside aldehydic acid enzyme inhibitor, preparation method therefor and application of aryl sulfatase and glucoside aldehydic acid enzyme inhibitor
  • Aryl sulfatase and glucoside aldehydic acid enzyme inhibitor, preparation method therefor and application of aryl sulfatase and glucoside aldehydic acid enzyme inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] 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:

[0021] Test tube 1:

[0022] Add 4.02U of arylsulfatase to test tube 1, then add sodium hypochlorite (0.28mol / L) so that the concentration of hypochlorite in the Tris-HCl buffer solution is 20μmol / L, and then add paranitrate according to the standard of 800μmol / L phenol-sulfuric acid conjugates, the glass test tube was placed in a 37 ° C water bath for 1 hour, and then the reaction was terminated by adding 2 mL of 0.5 mol / L sodium hydroxide, using standard methods (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34:225-229) assay for arylsulfatase activity.

[0023] Test tube 2:

[0024] Add 3.29U of glucuronidase to test tube 2, then add sodium hypochlorite (0.28mol / L), so that the concentration of hypochlorite in the Tris-HCl buffer solution is 20 μmol / L, and then add par...

Embodiment 2

[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 4.02U of arylsulfatase to test tube 1, then add sodium hypochlorite (0.28mol / L) so that the concentration of hypochlorite in the Tris-HCl buffer solution is 100μmol / L, and then add paranitrate according to the standard of 800μmol / L phenol-sulfuric acid conjugates, the glass test tube was placed in a 37 ° C water bath for 1 hour, and then the reaction was terminated by adding 2 mL of 0.5 mol / L sodium hydroxide, using standard methods (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34:225-229) assay for arylsulfatase activity.

[0029] Test tube 2:

[0030] Add 3.29U of glucuronidase to test tube 2, then add sodium hypochlorite (0.28mol / L), so that the concentration of hypochlorite in the Tris-HCl buffer solution is 100 μmol / L, and then add p...

Embodiment 3

[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 4.02U of arylsulfatase to test tube 1, then add sodium hypochlorite (0.28mol / L), so that the concentration of hypochlorite in the Tris-HCl buffer solution is 200μmol / L, and then add p-Nitrate according to the standard of 800μmol / L phenol-sulfuric acid conjugates, the glass test tube was placed in a 37 ° C water bath for 1 hour, and then the reaction was terminated by adding 2 mL of 0.5 mol / L sodium hydroxide, using standard methods (refer to Tabatabai and Bremner, Soil Science Society of America Journal, 1970, 34:225-229) assay for arylsulfatase activity.

[0035] Test tube 2:

[0036] Add 3.29U of glucuronidase in test tube 2, then add sodium hypochlorite (0.28mol / L), so that the concentration of hypochlorite in the Tris-HCl buffer solution is 200 μmol / L, and then add pa...

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Abstract

The invention belongs to the field of medicine and discloses an aryl sulfatase and glucoside aldehydic acid enzyme inhibitor, a preparation method therefor and application of the aryl sulfatase and glucoside aldehydic acid enzyme inhibitor. The preparation method for the aryl sulfatase and glucoside aldehydic acid enzyme inhibitor comprises the following step: adding hypochlorous acid or hypochlorite into a solvent so as to obtain a solution, thereby preparing the aryl sulfatase and glucoside aldehydic acid enzyme inhibitor. Compared with the conventional medical-treatment inhibitor STX64 andinhibitors such as D-Sacchuric acid and 1,4-lactone, the aryl sulfatase and glucoside aldehydic acid enzyme inhibitor has the advantages that the effective inhibition concentration effect is good, inhibition of different degrees can be carried out as required, and the inhibitor has the advantages of simplicity in operation, low cost, rapidness and the like and has a certain application prospect inthe field of medicine.

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): A61K33/20A61K33/00A61K33/06A61P35/00
CPCA61K33/00A61K33/06A61K33/20A61P35/00
Inventor刘则华钟姝姝张俊党志
OwnerSOUTH CHINA UNIV OF TECH