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Application of AgDT compound

A technology of drugs and structural formulas, applied in the field of medicinal chemistry, which can solve the problem that the mechanism of action has not been fully elucidated.

Inactive Publication Date: 2018-07-20
GUANGZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, silver ion compounds have also been confirmed to have anti-tumor activity, but their specific mechanism of action has not yet been fully elucidated.

Method used

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  • Application of AgDT compound
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: AgDT induces changes in the amount of ubiquitinated proteins in tumor cells

[0040] After different concentrations of AgDT (0.31, 0.63, 1.25, 2.5 μM) were applied to A549 and H1299 cells for 6 hours, the cells were collected to extract total protein, and Western Blot was performed to detect the expression of Ub, K48-, and GAPDH. The results showed that AgDT significantly inhibited protein degradation. See results figure 1 .

[0041] Western Blot method: 1. Configure the gel required for SDS-PAGE. First configure the lower part of the separating gel in an appropriate proportion, slowly add the configured separating gel into the gap between the equipped glass splints, and then add an appropriate amount of double-distilled water to seal; after the lower part of the separating gel is solidified, pour off the upper layer of double-distilled water and slowly add the configured Insert the comb after the good upper thickening gel, and wait for the upper thickenin...

Embodiment 2

[0042] Example 2: Effect of AgDT on proteasome exogenous specific substrate GFPu and ubiquitinated protein

[0043] After treating GFPu-HEK-293 cells (stable GFPu transfection) with different concentrations of AgDT for 12h, the cells were collected to extract total protein, and Western Blot immunoblotting (see Example 1) or fluorescent microscope in situ photographing was performed to detect Ub and GFPu. Express the situation. The results showed that AgDT significantly inhibited proteasome function. See results figure 2 .

Embodiment 3

[0044] Example 3: Effect of AgDT on proteolytic activity of 20S proteasome

[0045] Different concentrations of AgDT acted on the purified 20S proteasome, adding the respective enzymatic substrates Z-LLE-AMC, Boc-LRR-AMC and Suc-LLVYAMC to detect caspase-like, trypsin-like and chymotrypsin-like activities, multifunctional A microplate reader (350 / 438nm) was used to detect the fluorescence intensity released by AMC. The results showed that AgDT had no effect on the Chymotrypsin-like enzymatic activity of purified 20S proteasome. See results image 3 (a).

[0046] After treating A549 and H1299 cells with different concentrations of AgDT for 3 hours, the cells were collected to extract the lysate protein, and the respective enzymatic substrates Z-LLE-AMC, Boc-LRR- AMC and Suc-LLVYAMC, multifunctional microplate reader (350 / 438nm) detect the fluorescence intensity released by AMC. The results showed that AgDT had no effect on the Chymotrypsin-like enzymatic activity of intrace...

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PUM

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Abstract

The invention discloses application of [Ag(S2CN(C2H5)2)]6 to preparation of a medicine for preventing and curing tumor as well as application of the [Ag(S2CN(C2H5)2)]6 serving as deubiquitinating enzyme to preparation of a medicine for preventing and treating inflammation, tissue ischemia-reperfusion injury and myocardial hypertrophy diseases. The invention also provides the medicine for preventing and curing tumor, inflammation, tissue ischemia-reperfusion injury and myocardial hypertrophy diseases, which takes the [Ag(S2CN(C2H5)2)]6 as an active component, so that more choices are provided for clinical aspect.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to [Ag(S 2 CN(C 2 h 5 ) 2 )] 6 (abbreviated as AgDT) new application in medicine. Background technique [0002] There are two sets of protein degradation systems in eukaryotic cells. One is the autophagy-lysosome system, which mainly degrades protein aggregates and organelles. It is the ubiquitin-proteasome system (Ubiquitin-proteasome system, UPS), which is the main protein degradation pathway in cells, mediates the degradation of more than 80% of proteins, and regulates many important life activities (see Hershko A, et al., Annu RevBiochem. 1998, 67, 425-479; Mizushima et al., Nature. 2008, 451, 1069-1075). Due to the importance of this system, the 2004 Nobel Prize in Chemistry was awarded to three scientists from Israel and the United States who discovered this system. Due to the increased protein synthesis rate of tumor cells, which are more dependent on the p...

Claims

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Application Information

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IPC IPC(8): A61K33/38A61P35/00A61P29/00A61P9/10A61P9/00
CPCA61K33/38
Inventor 刘金保陈鑫张培全杨倩倩
Owner GUANGZHOU MEDICAL UNIV
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