Evaluation Of Inhibitory Effect Research Articles

Helichrysum stoechas (L.) Moench reduces body weight gain and modulates mood disorders via inhibition of silent information regulator 1 (SIRT1) by arzanol.

The prevalence of obesity is steadily rising, making safe and more efficient anti-obesity treatments an urgent medical need. Growing evidence correlates obesity and comorbidities, including anxiety and depression, with the development of a low-grade inflammation in peripheral and central tissues. We hypothesized that attenuating neuroinflammation might reduce weight gain and improve mood. We investigated the efficacy of a methanolic extract from Helichrysum stoechas (L.) Moench (HSE), well-known for its anti-inflammatory properties, and its main constituent arzanol (AZL). HPLC-ESI-MS2 and HPLC-UV were used to characterize the extract. HSE effects on mood and feeding behavior was assessed in mice. The mechanism of action of HSE and AZL was investigated in hippocampus samples and SH-SY5Y cells by western blotting and immunofluorescence. Oral administration of HSE for 3 weeks limited weight gain with no significant decrease in food intake. HSE produced an anxiolytic-like and antidepressant-like phenotype comparable to diazepam and amitriptyline, respectively, in the absence of locomotor and cognitive impairments and induced neuroprotective effects in glutamate-exposed SH-SY5Y cells. A dose-dependent reduction of SIRT1 expression was detected in SH-SY5Y cells and in hippocampal samples from HSE-treated mice. The inhibition of the SIRT1-FoxO1 pathway was induced in the hypothalamus. Molecular docking studies proposed a mechanism of SIRT1 inhibition by AZL, confirmed by the evaluation of inhibitory effects on SIRT1 enzymatic activity. HSE limited weight gain and comorbidities through an AZL-mediated SIRT1 inhibition. These activities indicate HSE an innovative therapeutic perspective for obesity and associated mood disorders.

Evaluation of Inhibitory Effect and Mechanism of Euphorbia Factor L3 against Phytophthora capsici

Phytophthora capsici is a highly destructive phytopathogenic oomycete with a broad host range and is responsible for tremendous losses. Euphorbia factor L3 (EFL3) is a natural plant-derived compound that has been widely studied in medicine and cosmetic applications. In this study, the sensitivity of 105 P. capsici isolates to EFL3 was determined, and the biological activity and physiological effects of EFL3 against P. capsici were investigated. The median effective concentration (EC50) values for EFL3 inhibition mycelial growth and spore germination ranged from 0.66 to 8.94 μg/mL (mean, 2.96 ± 0.91 μg/mL) and 1.63 to 13.16 μg/mL (mean, 5.30 ± 1.64 μg/mL), respectively. EFL3 treatment resulted in cell wall and cell membrane damage of P. capsici, which was revealed by morphological and ultrastructural observations, propidium iodide (PI) and calcofluor white (CFW) staining, and measurements of relative conductivity as well as malondialdehyde (MDA) and glycerol contents. In addition, the contents of phospholipid and cellulose, which are the major components of cell membrane and cell wall, were significantly reduced following EFL3 treatment. Furthermore, EFL3 provided protective as well as curative efficacies against P. capsici on detached tomato leaves and pepper seedlings in vivo. These data show that EFL3 exhibits strong inhibitory activity against P. capsici, thereby suggesting that it could be an effective alternative for controlling P. capsici-induced diseases.

Evaluation of inhibitory effect of alpha-amylase and alpha-glucosidase by interaction phenolic compounds, soluble fiber, and protein extracted from green lentils

Evaluation of inhibitory effect of alpha-amylase and alpha-glucosidase by interaction phenolic compounds, soluble fiber, and protein extracted from green lentils

Involvement of aldehyde oxidase in the metabolism of aromatic and aliphatic aldehyde-odorants in the mouse olfactory epithelium

Xenobiotic-metabolizing enzymes (XMEs) expressed in the olfactory epithelium (OE) are known to metabolize odorants. Aldehyde oxidase (AOX) recognizes a wide range of substrates among which are substrates with aldehyde groups. Some of these AOX substrates are odorants, such as benzaldehyde and n-octanal. One of the mouse AOX isoforms, namely AOX2 (mAOX2), was shown to be specifically expressed in mouse OE but its role to metabolize odorants in this tissue remains unexplored. In this study, we investigated the involvement of mouse AOX isoforms in the oxidative metabolism of aldehyde-odorants in the OE. Mouse OE extracts effectively metabolized aromatic and aliphatic aldehyde-odorants. Gene expression analysis revealed that not only mAOX2 but also the mAOX3 isoform is expressed in the OE. Furthermore, evaluation of inhibitory effects using the purified recombinant enzymes led us to identify specific inhibitors of each isoform, namely chlorpromazine, 17β-estradiol, menadione, norharmane, and raloxifene. Using these specific inhibitors, we defined the contribution of mAOX2 and mAOX3 to the metabolism of aldehyde-odorants in the mouse OE. Taken together, these findings demonstrate that mAOX2 and mAOX3 are responsible for the oxidation of aromatic and aliphatic aldehyde-odorants in the mouse OE, implying their involvement in odor perception.

Study on Spontaneous Combustion Characteristics of Coal Samples with Different Pre-oxidized Temperatures in Secondary Oxidation Process

ABSTRACT The paper used thermogravimetric experiments to study the spontaneous combustion characteristics of coal samples with different pre-oxidized temperatures during the secondary oxidation process and focused on the calculation of kinetic parameters during the oxygen-absorbing and weight-increasing stage. The results showed that the total reaction course of spontaneous combustion of raw coal and pre-oxidized coal were similar; the difference in pre-oxidized temperature only had a greater impact on the critical temperature and dry cracking temperature of the coal sample, and then had a greater impact on the water evaporation and desorption stage and the oxygen-absorbing and weight-increasing stage. And the oxygen-absorbing and weight-increasing stage had a more violent reaction than the water evaporation and desorption stage. In the oxygen-absorbing and weight-increasing stage, the difference of pre-oxidized temperature had little effect on the reaction mechanism of each coal sample. The reaction functions all followed the Jander equation, and the mechanism was three-dimensional diffusion. The energy of activation of pre-oxidized coal samples was smaller than that of raw coal, and decreased with the rise of pre-oxidized temperature. When the pre-oxidized temperature was less than 160°C, the pre-factor of the pre-oxidized coal was larger than that of the raw coal, and when the pre-oxidized temperature was greater than 160°C, the pre-exponential factor of the pre-oxidized coal was smaller than that of the raw coal. The research results can lay a foundation for the subsequent prediction of coal spontaneous combustion reaction process, determination of critical spontaneous combustion conditions and evaluation of inhibitory effect. At the same time, it can also be used as a reference and supplement for the existing research on coal oxidation kinetic parameters.

Assessment of the Substance Antioxidative Profile by Hyaluronan, Cu(II) and Ascorbate.

In the minireview presented here, the authors discuss the evaluation of inhibitory effect of substances in the phases of initiation and propagation of high-molar-mass hyaluronan oxidative degradation. The experimental approach should be considered as original since on using a simple experimental assay it is possible to prove both the so-called “preventive” and “chain-breaking” antioxidant activity of investigated water-soluble endo- or exogenous substances.

Homology Modelling and Virtual Screening of 3-deoxy-D-mannooctulosonic Acid Transferase of Aeromonas hydrophila as a Potential Target for Novel Natural Inhibitory Compounds

Background: The fish pathogen Aeromonas hydrophila is fast acquiring resistance to commonly employed antibiotics in aquaculture. This development has compelled the aquaculture sector to identify and develop new therapeutics to manage the pathogen. Methods: In this study, the protein 3-deoxy-d-manno-2-octulosonic acid (Kdo) transferase of A. hydrophila involved in the biosynthesis of the cell wall was studied in-silico as a potential drug target to control this pathogen. The three-dimensional structure of Kdo transferase was predicted by homology modelling using the Modellar 9.15. A total of 7682 natural compounds and 55 known Gram-negative bacterial inhibitors were virtually screened. Laboratory evaluation of inhibitory effects of identified inhibitors against A. hydrophila was performed using extracts from tea leaves and Astragalus by standard disc diffusion method. Results: A molecular model of putative virulence factor Kdo was derived by homology modelling. Eleven compounds were found to be potential inhibitors of Kdo. Among natural compounds, LArabinose and Flavan-3,4-diol were identified as the putative therapeutic agents. In the disc diffusion test, the zones of inhibition were observed at 2 mg/ml concentrations for tea leaves extracts and 8 mg/ml for Astragalus, suggesting the inhibitory effects of these extracts. Conclusion: The study shows the utility of essential enzymes such as the protein Kdo transferase as a putative drug target and the potential application of natural compounds in the control of pathogens in aquaculture without the need to use synthetic antimicrobial compounds.

Evaluation of Inhibitory Effects of Caffeine on Human Carcinoma Cells

One of the world's most consumed medications is caffeine which is available in the vast majority of beverages. Previously, some effects of caffeine have been evaluated including its inhibitory effect on cancer cells. But, the influence of caffeine on esophagus carcinoma squamous cells (CSC) and head and neck carcinoma cells still has not well understood. Herein, the relation between different amounts of caffeine with the proliferation rate of human esophagus carcinoma squamous cell line KYSE-30 as well as human head and neck carcinoma cell line HN5 was evaluated. Furthermore, concentrations of caffeine were adjusted and their effect on cells were studied. The inhibitory effects of caffeine on cells were measured using the conventional colorimetric MTT assay after 3 and 7 day of incubation. Our findings are suggested that caffeine has a significant inhibitory effect on both cell lines at the concentrations of 20, 50, and 70 milli-mol (mmol). The result shows that caffeine can prevent the proliferation of carcinoma cells and it is a perfect candidate for therapeutic applications.

Imidazolium based ionic liquid derivatives; synthesis and evaluation of inhibitory effect on mild steel corrosion in hydrochloric acid solution

Imidazolium bearing ionic liquids (ILs), 3-hexadecyl-1-methyl-1H-imidazol-3-ium bromide [C16M1Im] [Br] and 3-hexadecyl-1,2-dimethyl-1H-imidazol-3-ium bromide [C16M2Im] [Br] have been synthesized. These compounds were evaluated for corrosion resistance of mild steel in 1M HCl solution by gravimetric and electrochemical studies. The results were noticed that the inhibition efficiency, has enhanced due to a rise in the concentration of inhibitor. Further, it is observed that [C16M2Im] [Br] inhibition efficiency better than [C16M1Im] [Br] due to the increased alkyl substituents. Polarization study reveals that the used inhibitors behave as a mixed type, but predominantly exhibited the anodic inhibitive effect. The inhibitors adsorbed on the metal surface obeys Langmuir adsorption isotherm. Surface topography examined using an Atomic Force Microscope (AFM) and a Scanning Electron Microscope (SEM) with EDAX analyses. The formation of the Fe-inhibitor complex on mild steel surface has been confirmed by UV-Visible spectroscopy.

Evaluation of inhibitory effect and feasible utilization of dilute acid-pretreated rice straws on succinate production by metabolically engineered Escherichia coli AS1600a

This work demonstrated a pioneer work in the pre-treatment of rice straw by phosphoric acid (H3PO4) for succinate production. The optimized pre-treatment condition of rice straw was at 121 °C for 30 min with 2 N H3PO4. With this condition, total sugar concentration of 31.2 g/L with the highest hemicellulose saccharification yield of 94% was obtained. The physicochemical analysis of the pre-treated rice straw showed significant changes in its structure thus enhancing enzymatic saccharification. Succinate concentrations of 78.5 and 63.8 g/L were produced from hydrolysate liquor (L) and solid fraction (S) of the pre-treated rice straw respectively, with a comparable yield of 86% by E. coli AS1600a. Use of a combined L + S fraction in simultaneous saccharification and fermentation (LS + SSF) further improved succinate production at a concentration and yield of 85.6 g/L and 90% respectively. The results suggested that H3PO4 pre-treated rice straw may be utilized for economical succinate production by E. coli AS1600a.

Preparation of honokiol nanoparticles by liquid antisolvent precipitation technique, characterization, pharmacokinetics, and evaluation of inhibitory effect on HepG2 cells.

BackgroundHonokiol is a bioactive lignanoid and has been utilized in traditional Chinese medicine for a long time. It exhibits several pharmacological properties, such as anticancer effects, anti-inflammatory effects, and antianxiety effects. However, the poor aqueous solubility of honokiol has impeded clinical applications.Materials and methodsIn the present study, we adopted the liquid antisolvent precipitation (LAP) technique to prepare nanoparticles of honokiol for enhancement of solubility and bioavailability. Moreover, the honokiol nanoparticles obtained were investigated and evaluated in terms of morphology, physicochemical properties, saturation solubility, dissolution in vitro, bioavailability in vivo, toxicity, and the inhibitory effect on growth of HepG2 cells.ResultsThe obtained honokiol nanoparticles existed nearly in spherical shape and could be turned into amorphous structure by the LAP method. Moreover, the solubility of the honokiol nanoparticles was extremely higher than that of free honokiol, and the nanoparticle dissolution rate was also higher than that of free honokiol, which was about 20.41 times and 26.2 times than that of free honokiol in artificial gastric juice and in artificial intestinal juice. The area under the curve [AUC(0–t)] value of honokiol nanoparticles was about 6.52 times greater than that of free honokiol; therefore, the honokiol nanoparticles had a higher bioavailability than free honokiol but were innoxious to the organs of rats. Additionally, the honokiol nanoparticles exhibited a higher inhibition of HepG2 cells due to their lower IC50 compared to free honokiol.ConclusionHonokiol nanoparticles have high solubility and bioavailability, and can become a new oral drug formulation and produce a better response for its clinical applications.

Betulinic acid derivatives: a new class of α-glucosidase inhibitors and LPS-stimulated nitric oxide production inhibition on mouse macrophage RAW 264.7 cells

Chemical manipulation studies were conducted on betulinic acid (1), twenty-one new rationally designed analogues of 1 with modifications at C-28 were synthesized for their evaluation of inhibitory effects on α-glucosidase and LPS-stimulated nitric oxide production in mouse macrophage RAW 264.7 cells. Compound 2 (IC50 = 5.4 μM) exhibited an almost 1.4-fold increase in α-glucosidase inhibitory activity on yeast α-glucosidase while analogues 5 (IC50 16.4 μM) and 11 (IC50 16.6 μM) exhibited a 2-fold enhanced inhibitory activity on NO-production than betulinic acid.

Evaluation of inhibitory effect of caffeine on bone morphogenesis in pregnancy in a model of rat embryos

Evaluation of inhibitory effect of caffeine on bone morphogenesis in pregnancy in a model of rat embryos

Evaluation of Inhibitory Effect by Adaptation Measures for Red Soil Runoff from Farmland due to Heavy Rainfall

As the climate begins changing due to global warming, heavy rainfalls have become more frequent. These are, in turn, increasing the red soil runoff that has increasingly damaged the marine products and tourist industries. Over 85% of all such runoff is from farmland. Working with local farmers, we conducted field experiments in Ginoza Village in Okinawa’s Matsuda district to better understand the inhibitory effects on red soil runoff of different potential adaptation measures. Effectiveness of the adaptation methods conducted are discussed based on the obtained results. Further, a physical model is presented for simply estimating the sediment volume due to soil erosion by using the grain size distribution. The model can give a good agreement with the measured maximum particle sizes of the red soils discharged from farmland.

In vitro inhibitory effect of piperlonguminine isolated from Piper longum on human cytochrome P450 1A2

Piperlonguminine (PL), a major alkaloid isolated from Piper longum fruits, shows several biological activities including anti-tumor, anti-hyperlipidemic and anti-inflammatory effects. Although there have been studies of the biological effects of PL, the potential drug-interaction effect of PL following evaluation of inhibitory effects of cytochrome P450 (CYP) activities was not investigated. Here, to investigate the inhibitory effects of PL on the activities of CYP isoforms, CYP inhibition assays were conducted using a cocktail of probe substrates in pooled human liver microsome (HLMs) and human recombinant cDNA-expressed CYP. PL strongly inhibited CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 8.8 μM, as NADPH-independent inhibition, while other CYPs were not significantly inhibited. A Lineweaver-Burk plot resulted in the inhibition mechanism of PL being divided into two different modes, reversible competitive inhibition in a low concentration range of 0-16 μM with a Ki value of 1.39 μM and uncompetitive inhibitory behavior at a high concentration range of 16-40 μM. In addition, PL only decreased CYP 1A2-catalyzed phenacetin O-deethylase activity with IC50 values of 10.0 μM in human recombinant cDNA-expressed 1A2, not 1A1. Overall, this is the first investigation of potential herb-drug interactions associated with PL conducted by identifying the competitive inhibitory effects of PL on CYP1A2 in HLMs.

Evaluation of inhibitory effects of some Iranian plants against Phytophthora drechsleri

Evaluation of inhibitory effects of some Iranian plants against Phytophthora drechsleri

Evaluation of inhibitory effect of chamomile alcoholic extract on the growth and production of certain factors of Staphylococcus aureus

Investigation of the alcoholic extract of chamomile against growth and production of catalase, Dnase and haemolysin of Staphylococcus aureus (ATCC29213) were the aims of this study In this study, German chamomile was prepared from Tehran agricultural researches center. Extraction was performed by ethanol 85 (Maceration method) then solvent is removed by vacuum distillation system (concentrated extract). For initial screening of antibacterial property of the concentrated extract and determination of the mean diameter of growth inhibition zone of the MIC concentration, agar well diffusion assay were used. One ml of the concentrated extract was dried at 50°C within 24 hours. Its dried weight per ml was then measured. Dried extract powder is used for determination of Minimal Inhibitory Concentration (MIC) & Minimal Bactericidal Concentration (MBC) by using of the tube dilution method in broth media. In order to investigate the enzymatic activities, bacteria were treated by MIC (sub-inhibitory Concentrations, SIC) of extract for 24 hours as well as control tube (without extract). Catalase activity on 3% H2O2 by Iodometric & KMnO4 titration method, Dnase activity by culture of the treated bacteria and control tube on Dnase agar plate and comparison of nucleic acid precipitated zones and haemolysin activity in supernatant of the bacterial suspensions against sheep RBC for tests and control tube were performed and compared. All results were repeated three times and were analyzed by SPSS software. Our results were as follows: -Mean dry weight: 83.8±0.002 mg/ml -MIC: 2.615 mg/ml -MBC: 5.23 mg/ml -SIC: 1.35 mg/ml -SIC: 0.653 mg/ml -Inhibitory zone of MIC: 15±1.2 mm In concentration 1.35 mg/ml of extract 28-34% was decreased. Haemolysin activity: In concentration 0.653 mg/ml of extract 12-14% was decreased In concentration 1.35 mg/ml of extract 79-84% was decreased Catalase activity: In concentration 0.653 mg/ml of extract 34-38% was decreased In concentration 1.35 mg/ml of extract 71-74% was decreased Dnase activity: In concentration 0.653 mg/ml of extract 46-50% was decreased Although some of the concentrations of the chamomile alcoholic extract showed pronounced antibacterial activity on the Staphylococcus aureus; but its introduction as an antibacterial compound requires more information.

Allosteric inhibitors of chemoattractant receptors: opportunities and pitfalls

Given the central role of chemokines in infection, inflammation and immunity, chemokine receptors are a prime target for pharmacological intervention, and more so after the recent approval of chemokine receptor inhibitors for HIV. Allosteric inhibitors offer a largely unexploited opportunity to interfere with and modulate chemokine receptor activation and signaling. In addition to characterizing binding mode as a first step to understanding the specific mechanism underlying drug action, allosteric inhibitors pose new questions concerning different phases in drug discovery and pharmacological characterization, including the identification of appropriate screening tests, the evaluation of inhibitory effects on different signaling pathways and the implications of agonist- and signaling pathway-dependent inhibition for overall in vivo efficacy.

Evaluation of inhibitory effect and apoptosis induction of Zyzyphus Jujube on tumor cell lines, an in vitro preliminary study

In the present study, water extract of dried fruit of Zyzyphus Jujube was tested for its possible anticancer effect and induction of apoptosis on human tumor cell lines, HEp-2, HeLa and Jurkat cell lines. The inhibitory effect of water extract of this fruit on cell proliferation was assessed by MTT colorimetric assay. The induction of apoptosis of this extract was analyzed by DNA fragmentation analysis. Zyzyphus Jujube extract showed inhibitory effects on mentioned cell lines. Jurkat leukemic line was found the most sensitive cells with IC50 of 0.1 mug mL(-1). Our study also showed a typical DNA laddering in this cell line. The present study showed cytotoxic activity of Zyzyphus Jujube on tumor cells. Although Zyzyphus Jujube has useful compounds for medical applications.