Inhibition Effect Of Inhibitor Research Articles

Identification of Specific N6-Methyladenosine RNA Demethylase FTO Inhibitors by Single-Quantum-Dot-Based FRET Nanosensors.

The fat mass and obesity-associated enzyme (FTO) can catalyze the demethylation of N6-methyladenosine (m6A) residues in mRNA, regulates the cellular level of m6A modification, and plays a critical role in human obesity and cancers. Herein, we develop a single-quantum-dot (QD)-based fluorescence resonance energy transfer (FRET) sensor for the identification of specific FTO demethylase inhibitors. The FTO-mediated demethylation of m6A can induce the cleavage of demethylated DNA to generate the biotinylated DNA fragments, which may function as capture probes to assemble the Cy5-labeled reporter probes onto the QD surface, enabling the occurrence of FRET between the QD and Cy5. The presence of inhibitors can inhibit the FTO demethylation and consequently abolish FRET between the QD and Cy5. The inhibition effect of inhibitors upon FTO demethylation can be simply evaluated by monitoring the decrease of Cy5 counts. We use this nanosensor to screen several small-molecule inhibitors and identify diacerein as a highly selective inhibitor of FTO. Diacerein can inhibit the demethylation activity of endogenous FTO in HeLa cells. Interestingly, diacerein is neither a structural mimic of 2-oxoglutarate (2-OG) nor a chelator of metal ions, and it can selectively inhibit FTO demethylation by competitively binding the m6A-containing substrate.

Adsorption and inhibitive properties of seroquel drug for the corrosion of zinc in 0.1\xa0M hydrochloric acid solution

Inhibition action of seroquel on corrosion of zinc in 0.1 M HCl solution was investigated using weight loss, electrochemical potentiodynamic polarization and impedance spectroscopic techniques. Corrosion inhibition efficiency showed the positive effect with increase in concentration of inhibitor and with the increase in temperature. Results obtained from all the methods are in good agreement with each other. Inhibition effect of inhibitor is due to the adsorption of seroquel molecule on zinc surface from bulk of the solution and the process of adsorption follows Temkin’s adsorption isotherm. Potentiodynamic polarization studies revealed that seroquel acts as a mixed type of inhibitor. Corrosion inhibition mechanism is explained by activation and thermodynamic parameters. Surface morphology of the corroded metal was studied by scanning electron microscopic studies and FT-IR spectrum of the corrosion product further confirms the process of adsorption of seroquel on metal surface.

Inhibition of the erosion-corrosion of a 90° low alloy steel bend

The inhibition effect of inhibitor on the erosion-corrosion (E-C) of a low alloy steel bend is investigated by weight loss, electrochemical measurements, and surface analysis. It is demonstrated that inhibitor can significantly reduce the E-C rate and effectively inhibit the four components (pure corrosion, pure erosion, corrosion-enhanced erosion, and erosion-enhanced corrosion) of E-C. The inhibition of corrosion is more pronounced than that of erosion. The inhibition efficiencies (IEs) for total E-C, pure erosion, corrosion-enhanced erosion, and erosion-enhanced corrosion at the intrados are higher than that at the extrados of the bend. The lower IEs at the extrados are due to the severe sand particle impact and detrimental hydrodynamics conditions at these positions.

Protection of Aluminium in Acidic Environment and Inhibition Efficiency of Aminophenol-N-Benzylidene - Theoretical and Practical Investigation

Aluminium has a remarkable industrial importance. Aluminium and its alloys are exposed to the action of acid in industrial processes where acid play an important role such as oil well acidizing, acid pickling, acid cleaning and descaling. This can lead to substantial metal loss due to corrosion. The use of inhibitors is one of the most practical options to protect metal from corrosion. Organic and inorganic compounds are usually added to HCl as corrosion inhibitors. The present work is carried out to find the effective inhibitor with minimum concentration but maximum inhibition. The corrosion inhibition effect of o,m,p-Aminophenol-N-Benzylidene (o,m,p-AmphNB) for pure Aluminium in 1M HCl were investigated by means of weight loss, potentiodynamic polarization and electrochemical impedance spectroscopy (EIS). Electrochemical studies were carried out using standard three electrode cell where Calomel electrode act as a reference electrode, Platinum electrode as counter electrode and Aluminium electrode as working electrode. The values of indicates the competitive Chemisorption and physisorption, Potentiodynamic polarization parameters revealed the mixed mode of inhibition with predominance of cathodic inhibition. The EIS showed linear correlation with concentration of inhibitor & Rctl while Cdl inversely correlated. Quantum chemical calculations based on density functional theory (DFT) method were performed on studied inhibitors to ascertain relationship between molecular structure and their inhibition efficiency. Correlation analyses between experimental and theoretical values were performed to conclude that the inhibition effect of inhibitors could be explained in terms of electronic properties.

Protection of Aluminium in Acidic Environment and Inhibition Efficiency of Aminophenol-N-Benzylidene -Theoretical and Practical Investigation

Aluminium has a remarkable industrial importance. Aluminium and its alloys are exposed to the action of acid in industrial processes where acid play an important role such as oil well acidizing, acid pickling, acid cleaning and descaling. This can lead to substantial metal loss due to corrosion. The use of inhibitors is one of the most practical options to protect metal from corrosion. Organic and inorganic compounds are usually added to HCl as corrosion inhibitors. The present work is carried out to find the effective inhibitor with minimum concentration but maximum inhibition. The corrosion inhibition effect of o,m,p-Aminophenol-N-Benzylidene (o,m,p-AmphNB) for pure Aluminium in 1M HCl were investigated by means of weight loss, potentiodynamic polarization and electrochemical impedance spectroscopy (EIS). Electrochemical studies were carried out using standard three electrode cell where Calomel electrode act as a reference electrode, Platinum electrode as counter electrode and Aluminium electrode as working electrode. The values of ΔGads indicates the competitive Chemisorption and physisorption, Potentiodynamic polarization parameters revealed the mixed mode of inhibition with predominance of cathodic inhibition. The EIS showed linear correlation with concentration of inhibitor & Rctl while Cdl inversely correlated. Quantum chemical calculations based on density functional theory (DFT) method were performed on studied inhibitors to ascertain relationship between molecular structure and their inhibition efficiency. Correlation analyses between experimental and theoretical values were performed to conclude that the inhibition effect of inhibitors could be explained in terms of electronic properties. Figure 1

Electrochemical and theoretical investigation of the inhibitory effect of two Schiff bases of benzaldehyde for the corrosion of aluminium in hydrochloric acid

The corrosion inhibition effect of o-Aminophenol-N-Benzylidene (o-AmphNB) and o-Anisidene-N-Benzylidene (o-AnsNB) for pure Aluminium in 1 M HCl at different concentrations of two different inhibitors were investigated by means of weight loss, potentiodynamic polarization and electrochemical impedance spectroscopy (EIS). The values of ΔGadso revealed that the adsorption mechanism of these molecules on aluminium surface is competitive phenomenon between chemical and physical adsorption. Potentiodynamic polarization parameters revealed the mixed mode of inhibition with predominance of cathodic inhibition. The impedance results showed that with increase in concentration of inhibitor, charge transfer resistance increases while double layer capacitance decreases. Quantum chemical calculations based on density functional theory (DFT) method were performed on o-AmphNB and o-AnsNB to determine the relationship between molecular structures and their inhibition efficiencies. Correlation analysis concluded that the inhibition effect of inhibitors could be explained in terms of electronic properties.

A CIEF-LIF method for simultaneous analysis of multiple protein kinases and screening of inhibitors.

Here, a CIEF-LIF method for multiple protein kinase simultaneous analysis and inhibitors throughput screening with fast rate and low cost is presented. Comparing with CZE, CIEF-LIF exhibited great focusing ability and high separation efficiency for substrate and phosphorylated peptides, and is applicable for multiple kinases simultaneous analysis regardless of their substrate peptides compositions and charge statuses. Thus, highly sensitive analysis for cyclic adenosine 3', 5'-monophosphate-dependent protein kinase (PKA) and cyclin-dependent kinase 1 (CDK1) was achieved in CIEF-LIF analysis with detection sensitivity up to 1.25 mU/μL and 0.4 mU/μL, respectively, two magnitudes higher than that of CZE and comparable with that in nanomaterials or green fluorescent protein-based kinase assay. Moreover, the inhibition effect of inhibitors on multiple kinases could be simultaneously readout in a single electrophoretic run, with half maximal inhibitory concentration of H-89 for PKA and Ro-3306 for CDK1 calculated as 37.0 and 35.9 nM, respectively, consistent with literatures reported. The CIEF-LIF also exhibited strong anti-interference ability in human breast cancer cell lysates analysis and simulators such as forskolin and 3-isobutyl-1-methylxantine assessment. Therefore, CIEF-LIF is desirable for future biological application and clinical diagnostics and drug discovery.