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Small molecule inhibitor of protein disulfide isomerase

A technology of disulfide isomerase and small molecule inhibitor, applied in the field of biomedicine, can solve problems such as poor drugability, and achieve the effect of delaying the process of serum agglutination and reducing the amount of serum agglutination

Pending Publication Date: 2020-01-17
FUZHOU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the druggability of these inhibitors is poor, and the search for PDI inhibitors with

Method used

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  • Small molecule inhibitor of protein disulfide isomerase
  • Small molecule inhibitor of protein disulfide isomerase
  • Small molecule inhibitor of protein disulfide isomerase

Examples

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Effect test

Embodiment 1

[0014] Example 1: Isorhamnetin inhibits PDI reduction activity experiment

[0015] (Dabcyl)-GSSG-{E(EDANS)}-NH 2 The two ends of the fluorescent substrate are respectively labeled with a fluorescent group (EDANS) and a quencher group (DABCYL). In the complete substrate molecule, they are very close to each other, and the fluorescence is quenched. When the substrate is reduced by PDI, EDANS is no longer quenched by DABCYL, and then EDANS fluorescence can be detected. The effectiveness of PDI reduction inhibitors can be monitored by changes in the fluorescence intensity of EDANS. According to its principle, a certain concentration of PDI and inhibitors were added to the microwell plate, incubated for 30 min, and then the fluorescent substrate was added, and the fluorescence value of EDANS could be detected with a microplate reader to evaluate the inhibitory effect of the inhibitors on PDI.

[0016] The specific operation steps are as follows:

[0017] The mass concentration o...

Embodiment 2

[0026] Embodiment 2: Isorhamnetin inhibits serum agglutination experiment

[0027] Ca 2+ The addition of EDTA can neutralize the anticoagulant EDTA in the serum, thereby promoting the agglutination of the serum. Agglutination of serum increases the turbidity of the reaction system, with the largest change in the absorbance value at 405 nm. According to its principle, serum and a certain concentration of PDI were added to the microwell plate, then a certain amount of inhibitor was added to react for 10 min, and Ca 2+ Immediately after putting it into a microplate reader to detect the change of the absorbance value at 405nm, the anticoagulant activity of the inhibitor can be evaluated.

[0028] The specific operation steps are as follows:

[0029] The mass concentration of PDI was determined with BCA protein quantification kit, then converted into molar volume, and diluted to 15 μM with buffer. Dilute isorhamnetin and rutin to 1 mM, and prepare 100 mM CaCl 2 solution. Add...

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Abstract

The invention relates to an application of isorhamnetin as a protease disulfide bond isomerase inhibitor. At a molecular level, isorhamnetin can directly interact with the protein disulfide isomeraseand inhibit a reducing activity of the protein disulfide isomerase. The invention also relates to an application of isorhamnetin in antithrombotic treatment.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to compounds and applications of disulfide bond isomerase inhibitors. Background technique [0002] Protein disulfide isomerase (PDI) is a member of the thiol isomerase family (thiol isomerase, TI), which mainly exists in the endoplasmic reticulum (ER) Folding plays a vital role. PDI can act as an oxidoreductase, isomerase, or molecular chaperone. It not only catalyzes the formation of disulfide bonds of new ecological chains in the endoplasmic reticulum and the rearrangement of mismatched disulfide bonds in molecules, but also helps new proteins to fold correctly and plays an important role in maintaining cell homeostasis. [0003] Recent studies have shown that PDI also plays an important role in the process of thrombosis. It can simultaneously regulate the activation of platelets and the activation of the coagulation system, and is a new antithrombotic therapeutic target. In recent...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P7/02A61P9/10
CPCA61K31/352A61P7/02A61P9/10
Inventor 黄明东廖馨源袁彩江龙光
Owner FUZHOU UNIV
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