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Cationic iridium complex as well as preparation method and application thereof

A technology of iridium complexes and cations, applied in the field of biomedicine, can solve problems such as the lack of research on the application of spinal cord injury repair, and achieve the effect of promoting neurite growth, repair, and branch formation

Active Publication Date: 2022-01-11
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, so far, no Ir(III) complex has been synthesized and reported to have antioxidant effects, and its application in spinal cord injury repair has not been studied.

Method used

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  • Cationic iridium complex as well as preparation method and application thereof
  • Cationic iridium complex as well as preparation method and application thereof
  • Cationic iridium complex as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Preparation and Characterization of Cationic Iridium Complex (D79)

[0047] A preparation method of cationic iridium complex, comprising the steps of:

[0048] (1) Synthesis of (pyridin-2-yl)amide hydrazone: 2-cyanopyridine (5.2 g, 0.05 mol) was slowly heated and melted, and then hydrazine monohydrate (2.6 mL, 2.7 g, 0.05 mol) was added to obtain a cloudy mixture. Add ethanol (2.5mL), stir overnight to form a gel-like product, evaporate the solvent under reduced pressure, suspend in petroleum ether (25mL), cool in an ice bath, filter, and purify by recrystallization from toluene to obtain (pyridin-2-yl)amide Hydrazone (5.3g, 77.4%);

[0049] (2) Synthesis of 3FPHtz ligand: Take (pyridin-2-yl)amide hydrazone (1.0g, 7.5mmol), place it in a flame-dried, nitrogen-purged 50mL Schlenk tube, add sodium carbonate (0.8g, 7.5mmol ), heated at 35±2°C for 5 minutes, added 7.5 mL of dry dimethylacetamide (DMAA) and 2.5 mL of dry tetrahydrofuran (THF), then cooled to 0°C ...

Embodiment 2

[0053] Example 2 Research on the Scavenging Ability of D79 to Oxygen Free Radicals

[0054] The free radical scavenging ability of D79 was determined by ABTS method and DPPH method, as follows:

[0055] (1) React ABTS stock solution (5mmol / L, dissolved in PBS) with manganese oxide solution to form ABTS free radicals (ABTS•+);

[0056] (2) Mix different concentrations of D79 with the ABTS radical solution in step (1);

[0057] (3) The absorbance at 734 nm was detected within 120 min using a cell imaging multimode reader (Cytation 5, BioTek Instruments Inc.).

[0058] Test results such as Figure 5 shown. The results showed that D79 significantly inhibited the formation of ABTS free radicals in a time- and dose-dependent manner, indicating that D79 had a high activity of scavenging ROS, so it could be used as an effective free radical scavenger to prevent ROS damage to neurons.

[0059] Furthermore, the in vitro free radical scavenging test of DPPH (1,1-diphenyl-2-pichydrazi...

Embodiment 3

[0060] Example 3 Toxicity of D79 to neuronal cells

[0061] (1) Sprague-Dawley (SD) rat brain hippocampal tissue was taken, added with 0.25% trypsin, and digested at 37°C for 15 minutes;

[0062] (2) After terminating the trypsin action with bovine serum albumin, wash the tissue and grind it gently;

[0063] (3) Seed the isolated hippocampal neurons at a concentration of 20,000 cells / mL in a 35 mm culture dish (Costar, Cambridge, MA) with DMEM medium containing 10% fetal bovine serum and 10% nutrient mixture F-12 (with glutamine, Gibco, Carlsbad, CA, Cat# 12430054) at 37°C, 95% O 2 , 5% CO 2 Cultivate and cultivate in the incubator for 24h;

[0064] (4) Replace the original medium with Neurobasal medium containing 5% B-27 (Gibco), and place at 37°C, 95% O 2 , 5% CO 2 Cultivate in the incubator for 24h;

[0065] (5) After cell adhesion, add different concentrations of D79 to each well and incubate for another 24 hours;

[0066] (6) CCK8 kit (Abnova (Walnut, CA)) was used...

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Abstract

The invention relates to a cationic iridium complex as well as a preparation method and application thereof. The cationic iridium complex disclosed by the invention is obtained by substituting one (eta<5>-Me5C5)Ir(III)Cl structure in [(eta<5>-Me5C5)Ir(III)Cl]2(mu<2>-Cl)2 with 3fPhtz. In-vitro and in-vivo experiments are combined to prove that the cationic iridium complex disclosed by the invention can be used for promoting the repair of spinal cord injury by removing oxygen free radicals and reducing oxidative stress reaction after spinal cord injury, so a new research direction and a new drug source are provided for drug-assisted treatment of spinal cord injury.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, in particular to a cationic iridium complex and its preparation method and application. Background technique [0002] Spinal cord injury (SCI) is the change of structure and function of spinal cord tissue caused by external force, resulting in temporary or permanent loss of motor, sensory and autonomic nerve functions below the level of injury. Its pathophysiological process is often divided into primary injury and secondary injury. Among them, oxidative stress (Oxidative Stress, OS) is one of the main mechanisms of secondary damage. OS refers to a state of imbalance between oxidation and anti-oxidation in the body, which tends to oxidize, leading to inflammatory infiltration of neutrophils, increased secretion of proteases, and production of a large number of oxidative intermediates. [0003] Under normal circumstances, the oxidative substances and antioxidant substances produced in the bo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P25/28A61P39/06
CPCC07F15/0033A61P25/28A61P39/06
Inventor 纪志盛高贵彬马彦明张国威林宏生
Owner JINAN UNIVERSITY
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