Search results for: scaling inhibition

Authors: Hari Bezwada, Michelle Cheon, Ryan Divan, Hannah Escritor, Michelle Kagramian, Isha Korgaonkar, Maya MacAdams, Udgita Pamidigantam, Richard Pilny, Eleanor Race, Angadh Singh, Nathan Zhang, LeeAnn Nguyen, Fina Liotta

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Malaria is a deadly disease caused by the Plasmodium parasite, which continues to develop resistance to current antimalarial drugs. In this research project, the effectiveness of numerous thiazole derivatives was explored in inhibiting the PfPKG, a crucial part of the Plasmodium life cycle. This study involved the synthesis of six thiazole-derived amides to inhibit the PfPKG pathway. Nuclear Magnetic Resonance (NMR) spectroscopy and Infrared (IR) spectroscopy were used to characterize these compounds. Furthermore, AutoDocking software was used to predict binding affinities of these thiazole-derived amides in silico. In silico, compound 6 exhibited the highest predicted binding affinity to PfPKG, while compound 5 had the lowest affinity. Compounds 1-4 displayed varying degrees of predicted binding affinity. In-vitro, it was found that compound 4 had the best percent inhibition, while compound 5 had the worst percent inhibition. Overall, all six compounds had weak inhibition (approximately 30-39% at 10 μM), but these results provide a foundation for future drug discovery experiments.

Keywords: Medicinal Chemistry, Malaria, drug discovery, PfPKG, Thiazole, Plasmodium

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Authors: Nihar Ranjan, Derrick Watkins, Dev P. Arya

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Current methods in the study of antibiotic activity of ribosome targeted antibiotics are dependent on cell based bacterial inhibition assays or various forms of ribosomal binding assays. These assays are typically independent of each other and little direct correlation between the ribosomal binding and bacterial inhibition is established with the complementary assay. We have developed novel high-throughput capable assays for ribosome targeted drug discovery. One such assay examines the compounds ability to bind to a model ribosomal RNA A-site. We have also coupled this assay to other functional orthogonal assays. Such analysis can provide valuable understanding of the relationships between two complementary drug screening methods and could be used as standard analysis to correlate the affinity of a compound for its target and the effect the compound has on a cell.

Keywords: bacterial resistance, aminoglycosides, screening, drugs

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Authors: Muhammad A. Ado, Intan S. Ismail, Hasanah M. Ghazali, Faridah Abas

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In this study, we have investigated the phytochemical constituents of soluble fractions of dichloromethane (DCM) of methanolic leaves extract of the Callicarpa maingayi. The phytochemicals investigation has resulted in the isolation of three triterpenoids (euscaphic acid (1), arjunic acid (2), and ursolic acid (3)) together with two flavones apigenin (4) and acacetin (5)), two phytosterols (stigmasterol 3-O-β-glycopyranoside (6) and sitosterol 3-O-β-glycopyranoside (7)), and one fatty acid (n-hexacosanoic acid (8)). Six (6) compounds isolated from this species were isolated for the first time (1, 2, 3, 4, 5, and 8). Their structures were elucidated and identified by spectral methods of one and two-dimensional NMR techniques, gas chromatography-mass spectrometry, and comparison with the previously reported literature. The biological activity of three compounds (1-3) was carried out on acetylcholinesterase inhibition activity. Compound (3) was found to displayed good inhibition against AChE with an IC₅₀ value of 21.5 ± 0.022 μM.

Keywords: acetylcholinesterase, Callicarpa maingayi, euscaphic acid, ursolic acid

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Authors: Ahmad Alazemi, M. Sherif El-Eskandrany, Mohamad Kishk, Thanyan AlOnaizi, Ahmad Alduweesh, Shorouq Abdullaleel

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Arc melting technique followed by top-down approach, using a high-energy ball milling technique were employed to synthesize nanocrystalline of Cu50(Zr50-xNix)50 (x = 0, 10, 20 and 30 at.%) powder particles. The end-products of the alloy powders obtained after 50 h of the ball milling time were uniform in composition and had spherical-like morphology with an average particle size of 0.75 µm in diameter. The powders, which consisted of nanocrystalline grains with an average grain size of 10 nm in diameter, were used as feedstock materials for double face coating of stainless (SUS304) sheets, using cold spraying process. The coating materials enjoyed nanocrystalline structure and uniform composition. Biofilms were grown on 20-mm2 SUS304 sheets coated coupons inoculated with 1.5 × 108 CFU ml−1 E. coli. Significant biofilm inhibition was recorded in the nanoparticles coated coupons in comparison to non-coated SUS304 coupon. In conclusion, this study demonstrates that formation of biofilms can be significantly inhibited by Cu-based alloys especially in case of high (Ni) content. The inhibition of biofilm formation by nanocrystalline powders of Cu-based provides a practical approach to achieve the inhibition of biofilms formed by an emerging pathogen.

Keywords: biofilm, Cu, E.coli, FE-HRTEM/EDS, nanomaterials, nanocrystalline

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Authors: Weeraya Samnuknit, Apichat Boontawan

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A vacuum fractionation technique was introduced to remove ethanol from fermentation broth. The effect of initial glucose and ethanol concentrations were investigated for specific productivity. The inhibitory ethanol concentration was observed at 100 g/L. In order to increase the fermentation performance, the ethanol product was removed as soon as it is produced. The broth was boiled at 35°C by reducing the pressure to 65 mBar. The ethanol/water vapor was fractionated for up to 90 wt% before leaving the column. Ethanol concentration in the broth was kept lower than 25 g/L, thus minimized the product inhibition effect to the yeast cells. For batch extractive fermentation, a high substrate utilization rate was obtained at 26.6 g/L.h and most of glucose was consumed within 21 h. For repeated-batch extractive fermentation, addition of glucose was carried out up to 9 times and ethanol was produced more than 8-fold higher than batch fermentation.

Keywords: ethanol, extractive fermentation, product inhibition, vacuum fractionation

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Authors: Houneïda Benbouzid, Houria Berrebbah, Mohammed-Réda Djebar

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The toxicological impacts of the increasing number of synthetic compounds present in the aquatic environment are assessed predominantly in laboratory studies where test organisms are exposed to a range of concentrations of single compounds. The bio-indicator Paramecium sp., characterized by a short life cycle, rapid multiplication and normal behavior that may be affected by the presence of pollutants. We therefore investigated the inhibitory effect of a newly synthesized acaricide: the chlorfenapyr tested at concentrations of 250, 300, and 350 µM on a pure culture of Paramecium sp. during 6 day. Paramecia treated with different concentrations of Chlorfenapyr illustrate strong inhibition of cell growth from the second day of treatment. Low levels of glutathione, increased glutathione S-transferase and the decrease in respiratory metabolism, recorded in the presence of different concentrations of Chlorfenapyr, involve the activation of detoxification system.

Keywords: Paramecium sp., chlorfenapyr, oxidative enzymes, detoxification

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Authors: Kok-Chong Yong

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Poly(butadiene-co-acrylonitrile)-polyaniline Dodecylbenzenesulfonate [NBR-PAni.DBSA] blends with useful electrical conductivity (up to 0.1 S/cm) were prepared and their corrosion inhibiting behaviours for carbon steel were successfully assessed for the first time. The level of compatibility between NBR and PAni.DBSA was enhanced through the introduction of 1.0 wt % hydroquinone. As found from both total immersion and electrochemical corrosion tests, NBR-PAni.DBSA blends with 10.0-30.0 wt% of PAni.DBSA content exhibited the best corrosion inhibiting behaviour for carbon steel, either in acid or artificial brine environment. On the other hand, blends consisting of very low and very high PAni.DBSA contents (i.e. ≤ 5.0 wt % and ≥ 40.0 wt %) showed significantly poorer corrosion inhibiting behaviour for carbon steel.

Keywords: conductive rubber, nitrile rubber, polyaniline, carbon steel, corrosion inhibition

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Authors: Adebisi Adunola Demehin, Wanlaya Thamnarak, Jaruwan Chatwichien, Chatchakorn Eurtivong, Kiattawee Choowongkomon, Somsak Ruchirawat, Nopporn Thasana

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The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein involved in cellular signalling processes and, its aberrant activity is crucial in the development of many cancers such as lung cancer. Selaginellaceae are fern allies that have long been used in Chinese traditional medicine to treat various cancer types, especially lung cancer. Biflavonoids, the major secondary metabolites in Selaginellaceae, have numerous pharmacological activities, including anti-cancer and anti-inflammatory. For instance, amentoflavone induces a cytotoxic effect in the human NSCLC cell line via the inhibition of PARP-1. However, to the best of our knowledge, there are no studies on biflavonoids as EGFR inhibitors. Thus, this study aims to investigate the EGFR inhibitory activities of biflavonoids isolated from Selaginella siamensis and Selaginella bryopteris. Amentoflavone, tetrahydroamentoflavone, sciadopitysin, robustaflavone, robustaflavone-4-methylether, delicaflavone, and chrysocauloflavone were isolated from the ethyl-acetate extract of the whole plants. The structures were determined using NMR spectroscopy and mass spectrometry. In vitro study was conducted to evaluate their cytotoxicity against A549, HEPG2, and T47D human cancer cell lines using the MTT assay. In addition, a target-based assay was performed to investigate their EGFR inhibitory activity using the kinase inhibition assay. Finally, a molecular docking study was conducted to predict the binding modes of the compounds. Robustaflavone-4-methylether and delicaflavone showed the best cytotoxic activity on all the cell lines with IC50 (µM) values of 18.9 ± 2.1 and 22.7 ± 3.3 on A549, respectively. Of these biflavonoids, delicaflavone showed the most potent EGFR inhibitory activity with an 84% relative inhibition at 0.02 nM using erlotinib as a positive control. Robustaflavone-4-methylether showed a 78% inhibition at 0.15 nM. The docking scores obtained from the molecular docking study correlated with the kinase inhibition assay. Robustaflavone-4-methylether and delicaflavone had a docking score of 72.0 and 86.5, respectively. The inhibitory activity of delicaflavone seemed to be linked with the C2”=C3” and 3-O-4”’ linkage pattern. Thus, this study suggests that the structural features of these compounds could serve as a basis for developing new EGFR-TK inhibitors.

Keywords: anticancer, biflavonoids, EGFR, molecular docking, Selaginellaceae

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Authors: Kabrambam D. Singh, Dinabandhu Sahoo, Yallappa Rajashekar

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Evolution has caused many insects to develop resistance to several synthetic insecticides. This problem along with the persisting concern regarding the health and environmental safety issues of the existing synthetic insecticides has urged the scientific fraternity to look for a new plant-based natural insecticide with inherent eco-friendly nature. Colocasia esculenta var. esculenta (L.) Schott (Araceae family) is widely grown throughout the South- East Asian Countries for its edible corms and leaves. Various physico-chemical and spectroscopic techniques (IR, 1H NMR, 13C NMR and Mass) were used for the isolation and characterization of isolated bioactive molecule named 2, 3-dimethylmaleic anhydride (3, 4-dimethyl-2, 5-furandione). This compound was found to be highly toxic, even at low concentration, against several storage grain pests when used as biofumigant. Experimental studies on the mode of action of 2, 3-dimethylmaleic anhydride revealed that the biofumigant act as inhibitor of acetylcholinesterase enzyme in cockroach and stored grain insects. The knockdown activity of bioactive compound is concurrent with in vivo inhibition of AChE; at KD99 dosage of bioactive molecule showed more than 90% inhibition of AChE activity in test insects. The molecule proved to affect the antioxidant enzyme system; superoxide dismutase (SOD), and catalase (CAT) and also found to decrease reduced glutathione (GSH) level in the treated insects. The above results indicate involvement of inhibition of AChE activity and oxidative imbalance as the potential mode of action of 2, 3-dimethylmaleic anhydride. In addition, the study reveals computational docking programs elaborate the possible interaction of 2, 3-dimethylmaleic anhydride with enzyme acetylcholinesterase (AChE) of Periplaneta americana. Finally, the results represent that toxicity of 2, 3-dimethylmaleic anhydride might be associated with inhibition of AChE activity and oxidative imbalance.

Keywords: 2, 3-dimethylmaleic anhydride, Colocasia esculenta var. esculenta (L.) Schott, Biofumigant, acetylcholinesterase, antioxidant enzyme, molecular docking

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Authors: Iman Adnan Annon, Kadhim F. Alsultan

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This study investigate the internal corrosion of low carbon steel pipelines in the crude oil, as well as prepare and use natural and locally available plant as a natural corrosion inhibiter, the nature extraction achieved by two types of solvents in order to show the solvent effect on inhibition process, the first being distilled water and the second is diethyl ether. FT-IR spectra and using a chemical reagents achieved to detection the presence of many active groups and the presence of tannins, phenols, and alkaloids in the natural extraction. Some experiments were achieved to estimate the performance of a new inhibitor, one of these tests include corrosion measurement by simple immersion in crude oil within and without inhibitors which added in different amounts 30,40,50and 60 ppm at tow temperature 300 and 323k, where the best inhibition efficiencies which get when added the inhibitors in a critical amounts or closest to it, since for the aqueous extract (EB-A) the inhibition efficiency reached (94.4) and (86.71)% at 300 and 323k respectively, and for diethyl ether extract (EB-D) reached (82.87) and (84.6)% at 300 and 323k respectively. Optical microscopy examination have been conducted to evaluate the corrosion nature where it show a clear difference in the topography of the immersed samples surface after add the inhibitors at two temperatures. The results show that the new corrosion inhibitor is not only equivalent to a chemical inhibitor but has greatly improvement properties such as: high efficiency, low cost, non-toxic, easily to produce, and nonpolluting as compared with chemical inhibitor.

Keywords: corrosion in pipeline, inhibitors, crude oil, carbon steel, types of solvent

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Authors: G. Ozturk, B. Demirci

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It is well known that essential oils used for therapeutic purposes for many years. In this study, five different Pharmacopoeia grade essential oils (Achillea millefolium L., Pimpinella anisum L., Matricaria recutita L., Eucalyptus globulus L., Salvia officinalis L.) which obtained from commercial sources were evaluated for chemical compositions, synergistic antimicrobial activities, and lipoxygenase enzyme inhibitions. Volatile components were determined by gas chromatography/flame ionization detector and gas chromatography/mass spectrometer, simultaneously. The potential antimicrobial activity of essential oils was tested against oral pathogenic standard strains such as Streptococcus mutans, Streptococcus sanguinis, Staphylococcus aureus, Corynebacterium striatum, Candida albicans and Candida krusei by broth microdilution methods. Ciprofloxacin and ketoconazole were used positive controls. It has been observed that the essential oils tested have average inhibitory antimicrobial activity against oral pathogens with a Minimum Inhibition Concentration of 20-0.625 mg/mL. The active essential oils have been combined with antibiotics and synergistic effects have been evaluated by Checkerboard method. ƩFIC values were determined. In combination with antibiotics M. recutita essential oil has been shown to have a synergistic effect against S. aureus in combination with tetracycline (ƩFIC 0.46). In addition, 5-LOX inhibitory activity was measured by modifying the spectrophotometric method developed by Baylac and Racine. As a result, 5-LOX % inhibition of S. officinalis, E. globulus and M. recutita were calculated as 34.0 ± 6.66, 72.7 ± 2.78 and 27.7 ± 0.60, respectively.

Keywords: antimicrobial activity, essential oils, synergistic activity, 5-lipoxygenase inhibition

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Authors: Shanakr Bhattarai, V. S. Tiwari, Barak Akabayov

Abstract:

The plummeting number of infections and death is due to the development of drug-resistant bacteria. In addition, the number of approved antibiotic drugs by the Food and Drug Administration (FDA) is insufficient. Therefore, developing new drugs and finding novel targets for central metabolic pathways in bacteria is urgently needed. One of the promising targets is DNA replication machinery which consists of many essential proteins and enzymes. DnaG primase is an essential enzyme and a central part of the DNA replication machinery. DnaG primase synthesizes short RNA primers that initiate the Okazaki fragments by the lagging strand DNA polymerase. Therefore, it is reasonable to assume that inhibition of primase activity will stall DNA replication and prevent bacterial proliferation. We did the expression and purification of eight different bacterial DnaGs (Mycobacterium tuberculosis(Mtb), Bacillus anthracis (Ba), Mycobacterium smegmatis (Msmeg), Francisella tularencis (Ft), Vibrio cholerae (Vc) and Yersinia pestis (Yp), Staphylococcus aureus(Saureus), Escherichia coli(Ecoli)) followed by the radioactive activity assay. After obtaining the pure and active protein DnaG, we synthesized the inhibitors for them. The inhibitors were divided into five different groups, each containing five molecules, and the cocktail inhibition assay was performed against each DnaGs. The groups of molecules inhibiting the DnaGs were further tested with individual molecules belonging to inhibiting groups. Each molecule showing inhibition was titrated against the corresponding DnaGs to find IC50. We got a molecule(VS167) that acted as broad inhibitors, inhibiting all eight DnaGs. Molecules VS180 and VS186 inhibited seven DnaGs (except Saureus). Similarly, two molecules(VS 173, VS176) inhibited five DnaGs (Mtb, Ba, Ft, Yp, Ecoli). VS261 inhibited four DnaGs (Mtb, Ba, Ft, Vc). MS50 inhibited Ba and Vc DnaGs. And some of the inhibitors inhibited only one DnaGs. Thus we found the broad and specific inhibitors for different bacterial DnaGs, and their Structure-activity analysis(SAR) was done. Further, We tried to explain the similarities among the enzyme DnaGs from different bacteria based on their inhibition pattern.

Keywords: DNA replication, DnaG, okazaki fragments, antibiotic drugs

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Authors: Khalida Boutemak, Nasssima Benali, Nadji Moulai-Mostefa

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Effect of enzyme on the yield and chemical composition of Artemisia campestris essential oil is reported in the present study. It was demonstrated that enzyme facilitated the extraction of essential oil with increase in oil yield and did not affect any noticeable change in flavour profile of the volatile oil. Essential oil was tested for antibacterial activity using Escherichia coli; which was extremely sensitive against control with the largest inhibition (29mm), whereas Staphylococcus aureus was the most sensitive against essential oil obtained from enzymatic pre-treatment with the largest inhibition zone (25mm). The antioxidant activity of the essential oil with hemicellulase pre-treatment (EO2) and control sample (EO1) was determined through reducing power. It was significantly lower than the standard drug (vitamin C) in this order: vitamin C˃EO2˃EO1.

Keywords: Artemisia campestris, enzyme pre-treatment, hemicellulase, antibacterial activity, antioxidant activity

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Authors: Barrera C. Monserrat, Sierra-Alvarez Reyes, Pat-Espadas Aurora, Moreno Andrade Ivan

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Antimony is a toxic and carcinogenic metalloid considered a pollutant of priority interest by the United States Environmental Protection Agency. It is present in the environment in two oxidation states: antimonite (Sb (III)) and antimony (Sb (V)). Sb (III) is toxic to several aquatic organisms, but the potential inhibitory effect of Sb species for microorganisms has not been extensively evaluated. The fate and possible toxic impact of antimony on aerobic and anaerobic wastewater treatment systems are unknown. For this reason, the objective of this study was to evaluate the microbial toxicity of Sb (V) and Sb (III) in aerobic and anaerobic environments. Sb(V) and Sb(III) were used as potassium hexahydroxoantimonate (V) and potassium antimony tartrate, respectively (Sigma-Aldrich). The toxic effect of both Sb species in anaerobic environments was evaluated on methanogenic activity and the inhibition of hydrogen production of microorganisms from a wastewater treatment bioreactor. For the methanogenic activity, batch experiments were carried out in 160 mL serological bottles; each bottle contained basal mineral medium (100 mL), inoculum (1.5 g of VSS/L), acetate (2.56 g/L) as substrate, and variable concentrations of Sb (V) or Sb (III). Duplicate bioassays were incubated at 30 ± 2°C on an orbital shaker (105 rpm) in the dark. Methane production was monitored by gas chromatography. The hydrogen production inhibition tests were carried out in glass bottles with a working volume of 0.36 L. Glucose (50 g/L) was used as a substrate, pretreated inoculum (5 g VSS/L), mineral medium and varying concentrations of the two species of antimony. The bottles were kept under stirring and at a temperature of 35°C in an AMPTSII device that recorded hydrogen production. The toxicity of Sb on aerobic microorganisms (from a wastewater activated sludge treatment plant) was tested with a Microtox standardized toxicity test and respirometry. Results showed that Sb (III) is more toxic than Sb (V) for methanogenic microorganisms. Sb (V) caused a 50% decrease in methanogenic activity at 250 mg/L. In contrast, exposure to Sb (III) resulted in a 50% inhibition at a concentration of only 11 mg/L, and an almost complete inhibition (95%) at 25 mg/L. For hydrogen-producing microorganisms, Sb (III) and Sb (V) inhibited 50% of this production with 12.6 mg/L and 87.7 mg/L, respectively. The results for aerobic environments showed that 500 mg/L of Sb (V) do not inhibit the Allivibrio fischeri (Microtox) activity or specific oxygen uptake rate of activated sludge. In the case of Sb (III), this caused a loss of 50% of the respiration of the microorganisms at concentrations below 40 mg/L. The results obtained indicate that the toxicity of the antimony will depend on the speciation of this metalloid and that Sb (III) has a significantly higher inhibitory potential compared to Sb (V). It was shown that anaerobic microorganisms can reduce Sb (V) to Sb (III). Acknowledgments: This work was funded in part by grants from the UA-CONACYT Binational Consortium for the Regional Scientific Development and Innovation (CAZMEX), the National Institute of Health (NIH ES- 04940), and PAPIIT-DGAPA-UNAM (IN105220).

Keywords: aerobic inhibition, antimony reduction, hydrogen inhibition, methanogenic toxicity

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Authors: A. Y. Benabdellah, W. Lakhdari, A. Dahliz, Y. Bouchikh, A. Soud, R. M'lik, H. Hammi

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The direct comparison tests on the culture medium, between Trichoderma sp. and Fusarium oxysporum f. sp. radicis-lycopersici revealed that the latest one could inhibit the growth of F. oxysporum mycelial over than 40% compared to the control and that after four days of incubation at 26° C. Moreover, beyond this period and at the end of six days, Trichoderma sp. invading the colonies of F. oxysporum on what it sporule, thus revealing its power is highly myco-parasitic. Almost similar results were obtained against Alternaria solani is also a pathogen which is not causing a lot of damage, but we found it more sensitive to Trichoderma sp. with a percentage of inhibition more than 50%. So due to the in vitro test of Trichoderma sp. against these aggressive pathogens by direct contact has been found that can inhibit their mycelial growth with high speed and a high inhibition rate.

Keywords: Trichoderma sp., Fusarium oxysporum f. sp. radicis-lycopersici, Alternaria solani, biological control, antagonist

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Authors: Ambrish Singh

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The corrosion inhibition performance of pyran (AP) and benzimidazole (BI) derivatives on J55 steel in 3.5% NaCl solution saturated with CO₂ was investigated by electrochemical, weight loss, surface characterization, and theoretical studies. The electrochemical studies included electrochemical impedance spectroscopy (EIS), potentiodynamic polarization (PDP), electrochemical frequency modulation (EFM), and electrochemical frequency modulation trend (EFMT). Surface characterization was done using contact angle, scanning electron microscopy (SEM), and atomic force microscopy (AFM) techniques. DFT and molecular dynamics (MD) studies were done using Gaussian and Materials Studio softwares. All the studies suggested the good inhibition by the synthesized inhibitors on J55 steel in 3.5% NaCl solution saturated with CO₂ due to the formation of a protective film on the surface. Molecular dynamic simulation was applied to search for the most stable configuration and adsorption energies for the interaction of the inhibitors with Fe (110) surface.

Keywords: corrosion, inhibitor, EFM, AFM, DFT, MD

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Authors: Pao-Huei Chen, Shu-Mei Lin, Yih-Ming Weng, Zer-Ran Yu, Be-Jen Wang

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Pancreatic α-amylase and intestinal α-glucosidase are the critical enzymes for the breakdown of complex carbohydrates into di- or mono-saccharide, which play an important role in modulating postprandial blood sugars. Angiotensin converting enzyme (ACE) converts inactive angiotensin-I into active angiotensin-II, which subsequently increase blood pressure through triggering vasoconstriction and aldosterone secretion. Thus, inhibition of carbohydrate-digestion enzymes and ACE will help the management of blood glucose and blood pressure, respectively. Studies showed Pleurotus citrinopileatus (PC), an edible mushroom and commonly cultured in oriental countries, exerted anticancer, immune improving, antioxidative, hypoglycemic and hypolipidemic effects. Previous studies also showed various molecular weights (MW) fractioned from extracts may affect biological activities due to varying contents of bioactive components. Thus, the objective of this study is to investigate the in vitro antioxidant, hypoglycemic and hypotenstive effects and distribution of active compounds of various MWs of cold water extract from P. citrinopileatus (CWEPC). CWEPC was fractioned into four various MW fractions, PC-I (＜1 kDa), PC-II (1-3.5 kDa), PC-III (3.5-10 kDa), and PC-IV (＞10 kDa), using an ultrafiltration system. The physiological activities, including antioxidant activities, the inhibition capabilities of pancreatic α-amylase, intestinal α-glucosidase, and hypertension-linked ACE, and the active components, including polysaccharides, protein, and phenolic contents, of CWEPC and four fractions were determined. The results showed that fractions with lower MW exerted a higher antioxidant activity (p<0.05), which was positively correlated to the levels of total phenols. In contrast, the inhibition effects on the activities of α-amylase, α-glucosidase, and ACE of PC-IV fraction were significantly higher than CWEPC and the other three low MW fractions (< 10 kDa), which was more related to protein contents. The inhibition capability of CWEPC and PC-IV on α-amylase activity was 1/13.4 to 1/2.7 relative to that of acarbose (positive control), respectively. However, the inhibitory ability of PC-IV on α-glucosidase (IC50 = 0.5 mg/mL) was significantly higher than acarbose (IC50 = 1.7 mg/mL). Kinetic data revealed that PC-IV fraction followed a non-competitive inhibition on α-glucosidase activity. In conclusion, the distribution of various bioactive components contribute to the functions of different MW fractions on oxidative stress prevention, and blood pressure and glucose modulation.

Keywords: α-Amylase, angiotensin converting enzyme, α-Glucosidase, Pleurotus citrinopileatus

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Authors: A. Al-Rifaie, Z. W. Guan, S. W. Jones

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This paper presents a method for modelling and analysing end plate beam-to-column connections to obtain the quasi-static behaviour using non-linear dynamic explicit integration. In addition to its importance to study the static behaviour of a structural member, quasi-static behaviour is largely needed to be compared with the dynamic behaviour of such members in order to investigate the dynamic effect by proposing dynamic increase factors (DIFs). The beam-to-column bolted connections contain various contact surfaces at which the implicit procedure may have difficulties converging, resulting in a large number of iterations. Contrary, explicit procedure could deal effectively with complex contacts without converging problems. Hence, finite element modelling using ABAQUS/explicit is used in this study to address the dynamic effect may be produced using explicit procedure. Also, the effect of loading rate and mass scaling are discussed to investigate their effect on the time of analysis. The results show that the explicit procedure is valuable to model the end plate beam-to-column connections in terms of failure mode, load-displacement relationships. Also, it is concluded that loading rate and mass scaling should be carefully selected to avoid the dynamic effect in the solution.

Keywords: quasi-static, end plate, finite elements, connections

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Authors: Mohit Wadhawan, Sushma Rathaur

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Lymphatic filariasis, also called elephantiasis is a tropical disease afflicting over 120 million people in 81 countries worldwide. Existing anti filarial drugs are effective against the larval stages of filarial parasites which call for an urgent need of drugs which are macrofilaricidal. Identification of molecular targets crucial for survival of filarial parasites is a prerequisite for drug designing. Prolyl oligopeptidase (POP) is one such crucial enzyme involved in the maturation and degradation of neuropeptides and peptide hormones. We have identified this peptidase in the bovine filarial parasite, Setaria cervi. Effect of inhibition of POP on the proteome profile of filarial parasite has been discussed in this study. Filarial parasites were exposed to Z-pro-prolinal (ZPP), a specific POP inhibitor for 8 h and the motility and viability of the parasites was observed. It significantly reduced the motility and viability of the parasites. To study the proteome profile, the cytosolic, endoplasmic reticulum (ER) and mitochondrial extracts of the adult female parasites were subjected to 2-dimensional electrophoresis. As analyzed by the PD-Quest software, the ZPP caused the alteration in the different subcellular proteins, and the significantly altered proteins were identified using MALDI-MS/MS spectrometry. The major proteins identified were found to play important role in diverse biological functions like signaling, redox regulation, energy metabolism, stress response, and cytoskeleton formation. Moreover, we found upregulation in the calcium binding proteins such as calreticulin, calponin, and calpain-6 suggesting that POP inhibition regulates calcium release. This relates to earlier reports that POP plays non-catalytic role in inositol 1,4,5-trisphosphate (IP3) signaling inducing release of calcium from ER. Taken together, the data demonstrated that inhibition of prolyl oligopeptidase alter the overall proteome signifying its role in survival of the filarial parasites. Thus this study provides a basis for the use of POP as a chemotherapeutic target for the treatment of lymphatic filariasis.

Keywords: lymphatic filariasis, setaria cervi, prolyl oligopeptidase, proteomics

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Authors: Dimitra Sygkridou, Andreas Rapsomanikis, Elias Stathatos, Polycarpos Falaras, Evangelos Vitoratos

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At the present work highly transparent strip type quasi-solid state dye-sensitized solar cells (DSSCs) were fabricated through inkjet printing using nanocomposite TiO2 inks as raw materials and tested under outdoor illumination conditions. The cells, which can be considered as the structural units of large area modules, were fully characterized electrically and electrochemically and after the evaluation of the received results a large area DSSC module was manufactured. The module design was a sandwich Z-interconnection where the working electrode is deposited on one conductive glass and the counter electrode on a second glass. Silver current collective fingers were printed on the conductive glasses to make the internal electrical connections and the adjacent cells were connected in series and finally insulated using a UV curing resin to protect them from the corrosive (I-/I3-) redox couple of the electrolyte. Finally, outdoor tests were carried out to the fabricated dye-sensitized solar module and its performance data were collected and assessed.

Keywords: dye-sensitized solar devices, inkjet printing, quasi-solid state electrolyte, transparency, up-scaling

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Authors: Chengcao Sun, Cuili Yang, Shujun Li, Ruilin Xue, Yongyong Xi, Liang Wang, Dejia Li

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Backgrounds: A few lines of evidence show that Sulforaphane (SFN) has anti-fibrosis effect in liver tissue via Nrf2-mediated inhibition of TGF-β/Smad signaling. However, its effects on muscular dystrophic fibrosis remain unknown. This work was undertaken to evaluate the effects of SFN on fibrosis in dystrophic muscle. Methods: 3-month-old male mdx mice were treated with SFN by gavage (2 mg/kg body weight per day) for 3 months. Gastrocnemius, tibial anterior and triceps brachii muscles were collected for related analysis. Fibrosis in skeletal muscles was analyzed by Sirius red staining. Histology and morphology of skeletal muscles were investigated by H&E staining. Moreover, the expressions of Nrf2, NQO1, HO-1, and TGF-β/Smad signaling pathway were detected by western blot, qRT-PCR, immunohistochemistry and immunofluorescence assays. Results: Our results demonstrated that SFN treatment significantly decreased and improved morphological features in mdx muscles. Moreover, SFN increased the expression of muscle phase II enzymes NQO1 and HO-1 and significantly decreased the expression of TGF-β1，p-smad2, p-smad3, α-SMA, fibronectin, collagen I, PAI-1, and TIMP-1 in Nrf2 dependent manner. Additionally, SFN significantly decreased the expression of CD45 and TNF-α. Conclusions: Collectively, these results show that SFN can ameliorate muscle fibrosis in mdx mice by Nrf2-induced inhibition of TGF-β/Smad signaling pathway, which indicate Nrf2 may be useful for the treatment of muscular dystrophy.

Keywords: sulforaphane, Nrf2, TGF-β/smad signaling, duchenne muscular dystrophy, fibrosis

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Authors: Naoual Boussoualim, Hayat Trabsa, Iman Krache, Lekhmici Arrar, Abderrahmane Baghiani

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Resistance to antibiotics has emerged following their widespread use; the important mechanism of beta-lactam resistance in bacteria is the production of beta-lactamase. In order to find new bioactive beta-lactamase inhibitors, this study investigated the inhibition effect of the extracts of Anchusa azurea (AA) on a beta-lactamase from Bacillus cereus. The extracts exerted inhibitory effects on beta-lactamase in a dose-dependent manner, the results showed that the crude extract (BrE) and the ethyl acetate extract (AcE) of Anchusa azurea showed a very high inhibitory activity at a concentration of 10 mg, the percentage of inhibition was between 58% and 68%. Not all extracts were as potent as the original inhibitors such as clavulanic acid, the isolation and the structural elucidation of the active constituents in these extracts will provide useful means in the development of beta -lactamase inhibitors.

Keywords: Anchusa azurea, natural product, resistance, antibiotics, beta-lactamase, inhibitors

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Authors: P. Geetha, R. S. D. Wahida Banu

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The crowning advances in Silicon based electronic technology have dominated the computation world for the past decades. The captivating performance of Si devices lies in sustainable scaling down of the physical dimensions, by that increasing device density and improved performance. But, the fundamental limitations due to physical, technological, economical, and manufacture features restrict further miniaturization of Si based devices. The pit falls are due to scaling down of the devices such as process variation, short channel effects, high leakage currents, and reliability concerns. To fix the above-said problems, it is needed either to follow a new concept that will manage the current hitches or to support the available concept with different materials. The new concept is to design spintronics, quantum computation or two terminal molecular devices. Otherwise, presently used well known three terminal devices can be modified with different materials that suits to address the scaling down difficulties. The first approach will occupy in the far future since it needs considerable effort; the second path is a bright light towards the travel. Modelling paves way to know not only the current-voltage characteristics but also the performance of new devices. So, it is desirable to model a new device of suitable gate control and project the its abilities towards capability of handling high current, high power, high frequency, short delay, and high velocity with excellent electronic and optical properties. Carbon nanotube became a thriving material to replace silicon in nano devices. A well-planned optimized utilization of the carbon material leads to many more advantages. The unique nature of this organic material allows the recent developments in almost all fields of applications from an automobile industry to medical science, especially in electronics field-on which the automation industry depends. More research works were being done in this area. This paper reviews the carbon nanotube field effect transistor with various gate configurations, number of channel element, CNT wall configurations and different modelling techniques.

Keywords: array of channels, carbon nanotube field effect transistor, double gate transistor, gate wrap around transistor, modelling, multi-walled CNT, single-walled CNT

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Authors: Amthal Al-Gailani, Olujide Sanni, Thibaut Charpentier, Anne Neville

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Formation of inorganic scale on heat transfer surfaces is a serious problem encountered in industrial, commercial, and domestic heat exchangers and systems. Several industries use potable/groundwater sources such as rivers, lakes, and oceans to use water as a working fluid in heat exchangers and steamers. As potable/surface water contains diverse salt ionic species, the scaling kinetics and deposit morphology are expected to be different from those found in artificially hardened solutions. In this work, scale formation on the heat transfer surfaces from potable water has been studied using a once-through open flow cell under atmospheric pressure. The surface scaling mechanism and deposit morphology are investigated at high surface temperature. Thus the water evaporation process has to be considered. The effect of surface temperature, flow rate, and inhibitor deployment on the thermal resistance and morphology of the scale have been investigated. The study findings show how an increase in surface temperature enhances the crystallization reaction kinetics on the surface. There is an increase in the amount of scale and the resistance to heat transfer. The fluid flow rate also increases the fouling resistance and the thickness of the scale layer.

Keywords: fouling, heat exchanger, thermal resistance, crystallization, potable water

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Authors: Shimaa A. Higazy, Olfat E. El-Azabawy, Ahmed M. Al-Sabagh, Notaila M. Nasser, Eman A. Khamis

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In this work, two novel Schiff base polymers (PSB1 and PSB₂) with extra-high protective barrier features were facilely prepared via Polycondensation reactions. They were applied for the first time as effective corrosion inhibitors in the sour corrosive media of petroleum environments containing hydrogen sulfide (H₂S) gas. For studying the polymers' inhibitive action on the carbon steel, numerous corrosion testing methods including potentiodynamic polarization (PDP), open circuit potential, and electrochemical impedance spectroscopy (EIS) have been employed at various temperatures (298-328 K) in the oil wells formation water with H₂S concentrations of 100, 400, and 700 ppm as aggressive media. The activation energy (Ea) and other thermodynamic parameters were computed to describe the mechanism of adsorption. The corrosion morphological traits and steel samples' surfaces composition were analyzed by field emission scanning electron microscope and energy dispersive X-ray analysis. The PSB2 inhibited sour corrosion more effectively than PSB1 when subjected to electrochemical testing. The 100 ppm concentration of PSB2 exhibited 82.18 % and 81.14 % inhibition efficiencies at 298 K in PDP and EIS measurements, respectively. While at 328 K, the inhibition efficiencies were 61.85 % and 67.4 % at the same dosage and measurements. These poly Schiff bases exhibited fascinating performance as corrosion inhibitors in sour environment. They provide a great corrosion inhibition platform for the sustainable future environment.

Keywords: schiff base polymers, corrosion inhibitors, sour corrosive media, potentiodynamic polarization, H₂S concentrations

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Authors: J. K. D. M. P. Madara, R. B. L. Dharmawickreme, Linu John, Ivee Boiss

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Flemingia vestita, commonly known as ‘Sohphlang’ is an important medicinal plant found in the North-Eastern region of India, which is traditionally recognized for its anthelmintic properties. This study was aimed to evaluate the phytochemical constituents and antibacterial activity of the tuber skin extracts of the plant species. Methanol, acetone, and water were used to obtain the solvent extractions of the skin peel extracts. Concentrated extracts of skin peel were tested using previously established qualitative phytochemical assays. The antibacterial efficacy of methanol tuber skin extract was tested against Gram-negative and positive microorganisms, namely, Klebsiella pneumonia, Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Mycobacterium tuberculosis strains. Agar well diffusion method was employed to determine the zone of inhibition of the plant extracts. Obtained data were statistically analyzed. Methanol extracts of Flemingia vestita were found to be effective against Bacillus subtilis and Mycobacterium tuberculosis at concentrations of 0.5 mg/ml. The reported zone of inhibition for the two strains was 13.3mm ± 0.57 and 16.3mm ± 4.9, respectively. However Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli were resistant to the plant extracts with no zone of inhibition. Alkaloids, glycosides, and phenols were found to be present in aqueous, methanol, and acetone extracts of the plant in qualitative phytochemical analysis.

Keywords: flemingia vestita, antibacterial activity, phytochemical screening, well diffusion method

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Authors: Gabriel S. De Oliveira, Patricia P. Adriani, Christophe Moriseau, Bruce D. Hammock, Felipe S. Chambergo

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Epoxide hydrolases (EHs) are enzymes that are present in all living organisms and catalyze the hydrolysis of epoxides to the corresponding vicinal diols. EHs have high biotechnological interest for the drug design and chemistry transformation for industries. In this study, we describe the identification of substrates and inhibitors of epoxide hydrolase enzyme from the filamentous fungus Trichoderma reesei (TrEH), and these inhibitors showed the fungal growth inhibitory activity. We have used the cloned enzyme and expressed in E. coli to develop the screening in the library of fluorescent substrates with the objective of finding the best substrate to be used in the identification of good inhibitors for the enzyme TrEH. The substrate (3-phenyloxiranyl)-acetic acid cyano-(6-methoxy-naphthalen-2-yl)-methyl ester showed the highest specific activity and was chosen for the next steps of the study. The inhibitors screening was performed in the library with more than three thousand molecules and we could identify the 6 best inhibitors. The IC50 of these molecules were determined in nM and all the best inhibitors have urea or amide in their structure, because It has been recognized that these groups fit well in the hydrolase catalytic pocket of the epoxide hydrolases. Then the growth of T. reesei in PDA medium containing these TrEH inhibitors was tested, and fungal growth inhibition activity was demonstrated with more than 60% of inhibition of fungus growth in the assay with the TrEH inhibitor with the lowest IC50. Understanding how this EH enzyme from T. reesei responds to inhibitors may contribute for the study of fungal metabolism and drug design against pathogenic fungi.

Keywords: epoxide hydrolases, fungal growth inhibition, inhibitor, Trichoderma reesei

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Authors: Abdelkader H. El Debani, Huda Gargoum, Awad G. Abdellatif

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The aim of this study is to investigate analgesic and the anti-inflammatory effects Camel Thorn Extract (CTE) in rodents. Male albino mice weighing 20-25 gm. were divided into different groups each of 8 mice. The control was given normal saline i. p., the first group was given normal saline i. p. the 2nd, 3rd, 4th, groups received different doses of CTE (330, 660, and 1300 mg/kg) respectively and the 6th group received 5mg/kg of morphine i. p. All groups (except the control group) were given acetic acid 40 min after receiving the different treatment. The number of writhes was recorded 5 min after acetic acid injection for 15 min and the % of inhibition of writhing were calculated. Different groups of rats weighing 180- 220 gm., were divided into three groups each of 5 rats. At the beginning, the volumes of the right and left paw in animals were measured by using of the plethysmometer. The 1st group was given 660 mg /kg i. p. of CTE, the 2nd group received indomethacin (5 mg/kg i. p.). One hour later, edema was induced by sub planter injection of 0.1 ml of 1 % freshly prepared suspension of carrageenan into the right hind paws of the rats. The volume of the injected paws and contra-lateral paws were measured at 0, 0.5, 1, 2, 3, 4, and 5 hours using plethysmometer. The volume of the left paw of the rat was subtracted from the volume of the right paw of the same animal. Our results showed that 330,660 and 1300 mg/kg produced 14, 49 and 84%of inhibition of writhes, indicating that CTE has a strong analgesic activity. Our data also showed that the % of inhibition of edema at 30, 60, 120, 180, and 240 min was 14,51,71,61, and 56% in the animals given camel thorn extract whereas these figures in animals given endomethacin were 14, 24, 54, 52, and 54%. These results indicate that camel thorn has anti-inflammatory activities. The mechanism of analgesic and anti-inflammatory activities needs further investigations.

Keywords: camel thorn, imdomethacin, morphine, pharmaceutical medicine

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Authors: Neha Parekh, Divya Ladha, Poonam Wadhwani, Nisha Shah

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Nano scaled materials have attracted tremendous interest as corrosion inhibitor due to their high surface area on the metal surfaces. It is well known that the zinc oxide nanoparticles have higher reactivity towards aqueous acidic solution. This work presents a new method to incorporate zinc oxide nanoparticles with white sesame seeds extract (nano-green inhibitor) for corrosion protection of zinc in acidic medium. The morphology of the zinc oxide nanoparticles was investigated by TEM and DLS. The corrosion inhibition efficiency of the green inhibitor and nano-green inhibitor was determined by Gravimetric and electrochemical impedance spectroscopy (EIS) methods. Gravimetric measurements suggested that nano-green inhibitor is more effective than green inhibitor. Furthermore, with the increasing temperature, inhibition efficiency increases for both the inhibitors. In addition, it was established the Temkin adsorption isotherm fits well with the experimental data for both the inhibitors. The effect of temperature and Temkin adsorption isotherm revealed Chemisorption mechanism occurring in the system. The activation energy (Ea) and other thermodynamic parameters for inhibition process were calculated. The data of EIS showed that the charge transfer controls the corrosion process. The surface morphology of zinc metal (specimen) in absence and presence of green inhibitor and nano-green inhibitor were performed using Scanning Electron Microscopy (SEM) and Atomic Force Microscopy (AFM) techniques. The outcomes indicated a formation of a protective layer over zinc metal (specimen).

Keywords: corrosion, green inhibitor, nanoparticles, zinc

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Authors: Małgorzata Drzewiecka, Tomasz Śliwiński, Maciej Radek

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The inhibition of histone deacetyles (HDACs) holds promise as a potential anti-cancer therapy because histone and non-histone protein acetylation is frequently disrupted in cancer, leading to cancer initiation and progression. Additionally, histone deacetylase inhibitors (HDACi) such as class I HDAC inhibitor - valproic acid (VPA) have been shown to enhance the effectiveness of DNA-damaging factors, such as cisplatin or radiation. In this study, we found that, using of VPA in combination with talazoparib (BMN-637 – PARP1 inhibitor – PARPi) and/or Dacarabazine (DTIC - alkylating agent) resulted in increased DNA double strand break (DSB) and reduced survival (while not affecting primary melanocytes )and proliferation of melanoma cells. Furthermore, pharmacologic inhibition of class I HDACs sensitizes melanoma cells to apoptosis following exposure to DTIC and BMN-637. In addition, inhibition of HDAC caused sensitization of melanoma cells to dacarbazine and BMN-637 in melanoma xenografts in vivo. At the mRNA and protein level histone deacetylase inhibitor downregulated RAD51 and FANCD2. This study provides that combining HDACi, alkylating agent and PARPi could potentially enhance the treatment of melanoma, which is known for being one of the most aggressive malignant tumors. The findings presented here point to a scenario in which HDAC via enhancing the HR-dependent repair of DSBs created during the processing of DNA lesions, are essential nodes in the resistance of malignant melanoma cells to methylating agent-based therapies.

Keywords: melanoma, hdac, parp inhibitor, valproic acid

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