Search results for: SABA inhibitor

Authors: Benarous Khedidja, Yousfi Mohamed

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Infections caused by Candida species manifest in a number of diseases, including candidemia, vulvovaginal candidiasis, endocarditis, and peritonitis. These Candida species have been reported to have lipolytic activity by secretion of lipolytic enzymes such as esterases, lipases and phospholipases. These Extracellular hydrolytic enzymes seem to play an important role in Candida overgrowth. Candidiasis is commonly treated with antimycotics such as clotrimazole and nystatin, which bind to a major component of the fungal cell membrane (ergosterol). This binding forms pores in the membrane that lead to death of the fungus. Due to their secondary effects, scientists have thought of another treatment basing on lipase inhibition but we haven’t found any lipase inhibitors used as candidiasis treatment. In this work, we are interested to lipases inhibitors such as alkaloids as another candidiasis treatment. In the first part, we have proceeded to optimize the alkaloid structures and protein 3D structure using Hyperchem software. Secondly, we have docked inhibitors using Genetic algorithm with GOLD software. The results have shown ten possibilities of binding inhibitor to Candida rugosa lipase (CRL) but only one possibility has been accepted depending on the weakest binding energy.

Keywords: marrubiin, candida rugosa lipase, docking, gold

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Authors: Beenish Saba, Ann D. Christy

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Modern day municipal solid waste landfills are operated and controlled to protect the environment from contaminants during the biological stabilization and degradation of the solid waste. They are equipped with liners, caps, gas and leachate collection systems. Landfill gas is passively or actively collected and can be used as bio fuel after necessary purification, but leachate treatment is the more difficult challenge. Leachate, if not recirculated in a bioreactor landfill system, is typically transported to a local wastewater treatment plant for treatment. These plants are designed for sewage treatment, and often charge additional fees for higher strength wastewaters such as leachate if they accept them at all. Different biological, chemical, physical and integrated techniques can be used to treat the leachate. Treating that leachate with simultaneous power production using microbial fuel cells (MFC) technology has been a recent innovation, reported its application in its earliest starting phase. High chemical oxygen demand (COD), ionic strength and salt concentration are some of the characteristics which make leachate an excellent substrate for power production in MFCs. Different materials of electrodes, microbial communities, carbon co-substrates and temperature conditions are some factors that can be optimized to achieve simultaneous power production and treatment. The advantage of the MFC is its dual functionality but lower power production and high costs are the hurdles in its commercialization and more widespread application. The studies so far suggest that landfill leachate MFCs can produce 1.8 mW/m2 with 79% COD removal, while amendment with food leachate or domestic wastewater can increase performance up to 18W/m3 with 90% COD removal. The columbic efficiency is reported to vary between 2-60%. However efforts towards biofilm optimization, efficient electron transport system studies and use of genetic tools can increase the efficiency of the MFC and can determine its future potential in treating landfill leachate.

Keywords: microbial fuel cell, landfill leachate, power generation, MFC

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Authors: Chung-Young Lee, Se-Hee Ahn, Jun-Gu Choi, Youn-Jeong Lee, Hyuk-Joon Kwon, Jae-Hong Kim

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A/chicken/Korea/01310/2001 (H9N2) (01310) was passaged through embryonated chicken eggs (ECEs) by 20 times (01310-E20), and it has been used for an inactivated oil emulsion vaccine in Korea. After sequential passages, 01310-E20 showed higher pathogenicity in ECEs and acquired multiple mutations including a potential N-glycosylation at position 133 (H3 numbering) in HA and 18aa-deletion in NA stalk. To evaluate the effect of these mutations on the mammalian pathogenicity and resistance to non-specific inhibitors, we generated four PR8-derived recombinant viruses with different combinations of HA and NA from 01310-E2 and 01310-E20 (rH2N2, rH2N20, rH20N2, and rH20N20). According to our results, recombinant viruses containing 01310 E20 HA showed higher growth property in MDCK cells and higher virulence on mice than those containing 01310 E2 HA regardless of NA. The hemagglutination activity of rH20N20 was less inhibited by egg white and mouse lung extract than that of other recombinant viruses. Thus, the increased pathogenicity of 01310-E20 may be related to both higher replication efficiency and resistance to non-specific inhibitors in mice.

Keywords: avian influenza virus, egg adaptation, H9N2, N-glycosylation, stalk deletion of neuraminidase

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Authors: N. A. Kazemi Sefat, M. M. Mohammadi, J. Hadjati, S. Talebi, M. Ajami, H. Daneshvar

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Colorectal cancer metastases result in a significant number of cancer related deaths. Histone deacetylase (HDAC) inhibitors induce growth arrest and apoptosis in a variety of human cancer cells. Sodium butyrate (SB) is a short chain fatty acid, belongs to HDAC inhibitors which is released in the colonic lumen as a consequence of fiber fermentation. In this study, we are about to assess the effect of sodium butyrate on HCT116 human colorectal carcinoma cell line. The viability of cells was measured by microscopic morphologic study and MTT assay. After 48 hours, treatments more than 10 mM lead to cell injury in HCT116 by increasing cell granulation and decreasing cell adhesion (p>0.05). After 72 hours, treatments at 10 mM and more lead to significant cell injury (p<0.05). Our results may suggest that the gene expression which is contributed in cell proliferation and apoptosis has been changed under pressure of HDAC inhibition.

Keywords: colorectal cancer, sodium butyrate, cytotoxicity, MTT

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Authors: Nneka Nkechi Uchegbu, Temitope Omolayo Fasuan

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This study investigated how to reduce bio-compounds and amino acids in V. amygdalina leaf during processing as a functional food ingredient. Fresh V. amygdalina leaf was processed using thermal oil-aqueous mixtures (soybean oil: aqueous and palm oil: aqueous) at 1:40 and 130 (v/v), respectively. Results indicated that the hot soybean oil-aqueous mixture was the most effective in preserving the bio-compounds and amino acids with retention potentials of 80.95% of the bio-compounds at the rate of 90-100%. Hot palm oil-aqueous mixture retained 61.90% of the bio-compounds at the rate of 90-100% and hot aqueous retained 9.52% of the bio-compounds at the same rate. During the debittering process, seven new bio-compounds were formed in the leaves treated with hot soybean oil-aqueous mixture, six in palm oil-aqueous mixture, and only four in hot aqueous leaves. The bio-compounds in the treated leaves have potential functions as antitumor, antioxidants, antihistaminic, anti-ovarian cancer, anti-inflammatory, antiarthritic, hepatoprotective, antihistaminic, haemolytic 5-α reductase inhibitor, nt, immune-stimulant, diuretic, antiandrogenic, and anaemiagenic. Alkaloids and polyphenols were retained at the rate of 81.34-98.50% using oil: aqueous mixture while aqueous recorded the rate of 33.47-41.46%. Most of the essential amino acids were retained at a rate above 90% through the aid of oil. The process is scalable and could be employed for domestic and industrial applications.

Keywords: V. amygdalina leaf, bio-compounds, oil-aqueous mixture, amino acids

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Authors: A. Asselah, A. Khalfi, M. A.Toumi, A.Tazerouti

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The study of the corrosion inhibition of a standard carbon steel "API 5L grade X70" by two biodegradable anionic surfactants derived from fatty acids by photo sulfochlorination, called sodium lauryl methyl ester sulfonates and sodium palmityl methyl ester sulfonates was carried. A solution at 2.5 g/l NaCl saturated with carbon dioxide is used as a corrosive medium. The gravimetric and electrochemical technics (stationary and transient) were used in order to quantify the rate of corrosion and to evaluate the electrochemical inhibition efficiency, thus the nature of the mode of action of the inhibitor, in addition to a surface characterization by scanning electron microscopy (MEB) coupled to energy dispersive X-ray spectroscopy (EDX). The variation of the concentration and the temperature were examined, and the mode of adsorption of these inhibitors on the surface of the metal was established by assigning it the appropriate isotherm and determining the corresponding thermodynamic parameters. The MEB-EDX allowed the visualization of good adhesion of the protective film formed by the surfactants to the surface of the steel. The corrosion inhibition was evaluated at around 93% for sodium lauryl methyl ester sulfonate surfactant at 20 ppm and 87.2% at 50 ppm for sodium palmityl methyl ester sulfonate surfactant.

Keywords: carbon steel, oilfield, corrosion, anionic surfactants

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Authors: Saba Nuzhat

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The present ethnographic study examines how domestic violence and authoritative knowledge affect the reproductive health of females; in terms of contraceptive behavior and induced abortion. This qualitative study has been conducted by collecting in depth informal interviews and case studies of 12 female respondents living in an urban slum of Keraniganj, located Dhaka city. The study depicts how multivariable factors are linked to a woman’s ability to contracept and make abortion decisions in a cultural context where being a wife infers to submission, limited mobility, sexual availability, and restricted autonomy on her own reproduction health. This study shows how violence is being normalized and socially acceptable, every time women do not adhere to go through expected gender roles. The study primarily explores the subjective experiences and perceptions of the females about contraceptive behavior as well as abortions from a medical anthropological perspective. A number of salient examples are highlighted into this paper where women who go through abortion or adopt various measures of contraceptives get highly influenced by authoritative knowledge or under the pressure of male dominance. The lack of female autonomy or prevalence of domestic violence challenges the gender equality of Bangladeshi society and female sovereignty in accessing sexual or reproductive rights. This paper remarks the significance of medical anthropological research that helps to understand the intricate interrelationship between authoritative knowledge and male dominance with female reproductive health in order to reduce women’s risk of experiencing domestic violence and to promote reproductive health autonomy for themselves for espousing contraceptive behaviors and abortion decisions.

Keywords: abortion, authoritative knowledge, contraception, domestic violence, reproductive health

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Authors: Saba Didarataee, Abbas Ali Khodadadi, Yadollah Mortazavi, Fatemeh Mousavi

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Photocatalytic water splitting is one of the most attractive alternative methods for hydrogen evolution. A variety of nanoparticle engineering techniques were introduced to improve the activity of semiconductor photocatalysts. Among these methods, heterojunction formation is an appealing method due to its ability to effectively preventing electron-hole recombination and improving photocatalytic activity. Reaching an optimal ratio of the two target semiconductors for the formation of heterojunctions is still an open question. Considering environmental issues as well as the cost and availability, ZnS and ZnO are frequently studied as potential choices. In this study, first, the ZnS nanoparticle was synthesized in a hydrothermal process; the formation of ZnS nanorods with a diameter of 14-30 nm was confirmed by field emission scanning electron microscope (FESEM). Then two different methods, partial oxidation and chemical precipitation were employed to construct ZnS/ZnO core-shell heterojunction. X-ray diffraction (XRD), BET, and diffuse reflectance spectroscopy (DRS) analysis were carried out to determine crystallite phase, surface area, and bandgap of photocatalysts. Furthermore, the temperature of oxidation was specified by a temperature programmed oxidation (TPO) and was fixed at 510℃, at which mild oxidation occurred. The bandgap was calculated by the Kubelka-Munk method and decreased by increasing oxide content from 3.53 (pure ZnS) to 3.18 (pure ZnO). The optimal samples were determined by testing the photocatalytic activity of hydrogen evolution in a quartz photoreactor with side irradiation of UVC lamps with a wavelength of 254 nm. In both procedures, it was observed that the photocatalytic activity of the ZnS/ZnO composite was sensibly higher than the pure ZnS and ZnO, which is attributed to forming a type-II heterostructure. The best ratio of oxide to sulfide was 0.24 and 0.37 in partial oxidation and chemical precipitation, respectively. The highest hydrogen evolution was 1081 µmol/gr.h, gained from partial oxidizing of ZnS nanoparticles at 510℃ for 30 minutes.

Keywords: heterostructure, hydrogen, partial oxidation, photocatalyst, water splitting, ZnS

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Authors: Drashti G. Daraji, Rosa E. Moo-Puc, Hitesh D. Patel

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Substituted 2-Thioimidazole analogues have been synthesized and confirmed by advanced spectroscopic techniques. Among them, ten compounds have been selected and evaluated for their in vitro anti-cancer activity at the National Cancer Institute (NCI) for testing against a panel of 60 different human tumor cell lines derived from nine neoplastic cancer types. Furthermore, synthesized compounds were tested for their in vitro antiprotozoal activity, and none of them exhibited significant potency against antiprotozoans. It was observed that the tested all compounds seem effective on the UACC-62 melanoma cancer cell line as compared to other cancer cell lines and also exhibited the least potent in the Non-Small Cell Lung Cancer cell line in one-dose screening. In silico studies of these derivatives were carried out by molecular docking techniques and Absorption, Distribution, Metabolism, and Excretion (ADME) using Schrödinger software to find potent B-Raf kinase inhibitor (PDB ID: 3OG7). All the compounds have been performed for docking study; Compound D4 has a good docking score for melanoma cancer as compared with other.

Keywords: anticancer activity, cancer cell line, 2-thio imidazole, one-dose assay, molecular docking

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Authors: M. Sorahi Nobar, V. Niknam, H. Ebrahimzadeh, H. Soltanloo

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Fusarium graminearum is one of the most destructive crop diseases in the world. Infection occurs during the flowering period in warm and humid conditions. It causes reduction in yield. Moreover, harvested grain is often contaminated with mycotoxins and its acetylated derivatives. Fusarium mycotoxines are potent inhibitor of protein synthesis, and thereby presents hazards for both human and animal health. A rapid production of reactive oxygen intermediates, primarily superoxide and hydrogen peroxide at the site of attempted infection considered as key feature underlying successful pathogen recognition. Here, we compared the time course activity of superoxide dismutase (SOD) as a first line of defenses against ROS- induced oxidative burst between FHB- resistant Sumai3 and susceptible Falat at 48, 96 and 144 hours after infection. Our results showed that Sumai3 SOD activity increased with time and reached the highest-level 4 days after infection while in susceptible cultivar Falat, SOD activity decreased during the first 96 h. after infection. Decreased was followed by an increased at 6 days after infection. According to our results rapid induction of SOD activity in resistant cultivar may play an important role in resistance against FHB in wheat.

Keywords: Fusarium graminearum, mycotoxins, resistant cultivar, superoxide dismutase

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Authors: Emmanuel Kamal Aziz Saba, Gihan Abd El-Lateif Younis El-Tantawi, Mohammed Hamdy Zahran, Ibrahim Khalil Ibrahim, Mohammed Abd El-Salam Shehata, Hussein Al-Moghazy Sultan, Medhat

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Pelvic floor electrophysiological tests are essential for assessment of patients with obstructed defecation. The present study was conducted to determine the different patterns of pelvic floor electrophysiology that are associated with obstructed defecation. The present cross sectional study included 25 patients with obstructed defecation. A control group of 20 apparently healthy subjects were included. All patients were subjected to history taking, clinical examination, proctosigmoidoscopy, lateral proctography (evacuation proctography), dynamic pelvic magnetic resonance imaging, anal manometry and electrophysiological studies. Electrophysiological studies were including pudendal nerve motor conduction study, pudendo-anal reflex, needle electromyography of external anal sphincter and puborectalis muscles, pudendal somatosensory evoked potential and tibial somatosensory evoked potential. The control group was subjected to electrophysiological studies which included pudendal nerve motor conduction study, pudendo-anal reflex, pudendal somatosensory evoked potential and tibial somatosensory evoked potential. The most common pelvic floor electrodiagnostic pattern characteristics of obstructed defecation was pudendal neuropathy, denervation and anismus of external anal sphincter and puborectalis with complete interference pattern of external anal sphincter and puborectalis at squeezing and cough and no localized defect in external anal sphincter. In conclusion, there were characteristic pelvic floor electrodiagnostic patterns associated with obstructed defecation.

Keywords: obstructed defecation, pudendal nerve terminal motor latency, pudendoanal reflex, sphincter electromyography

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Authors: M. E. Abalaka, S. Y. Daniyan, S. O. Adeyemo, D. Damisa

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Gold nanoparticles (AuNPs) have gained increasing interest in recent times. This is greatly due to their special features, which include unusual optical and electronic properties, high stability and biological compatibility, controllable morphology and size dispersion, and easy surface functionalization. In typical synthesis, AuNPs were produced by reduction of gold salt AuCl4 in an appropriate solvent. A stabilizing agent was added to prevent the particles from aggregating. The antibacterial activity of different sizes of gold nanoparticles was investigated against Staphylococcus aureus, Salmonella typhi and Pseudomonas pneumonia using the disk diffusion method in a Müeller–Hinton Agar. The Au-NPs were effective against all bacteria tested. That the Au-NPs were successfully synthesized in suspension and were used to study the antibacterial activity of the two medicinal plants against some bacterial pathogens suggests that Au-NPs can be employed as an effective bacteria inhibitor and may be an effective tool in medical field. The study clearly showed that the Au-NPs exhibiting inhibition towards the tested pathogenic bacteria in vitro could have the same effects in vivo and thus may be useful in the medical field if well researched into.

Keywords: gold nanoparticles, Gomphrena celesioides, Prunus amygdalus, pathogens

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Authors: Alyaa Ahmed Farid, Aida Ismail, Ibrahim Rabia, Azza Fahmy, Azza El Amir

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This study was designed for assessment of 3 types of Cysteine protease inhibitors (CPIs) fluromethylketone (FMK), vinyl sulfone (VS) and sodium nitro prussid (SNP), to define which of them is the best? The experiments aimed to define the protective power of each inhibitor alone or combined with PZQ for curing S. mansoni infection in mice. In vitro, treated S. mansoni adult worms recorded a mortality rate after 1 hr of exposure to 500 ppm of FMK, VS and SNP as 75, 70 and 60%, while, treated cercaria recorded 75, 60 and 50%, respectively. FMK+PZQ treatment recorded the maximum reduction in worm burden (97.2% at 5 wk PI). VS treatment alone or combined with PZQ increases IgM, total IgG, IgG2 and IgG4 levels. In EM study of worm tegument, while only detachment of spines was observed in PZQ treated group, the completely implanted spines were reported in the degenerated tegument of adult worms in all groups treated with CPIs. Treatment with VS+PZQ increased Igs levels but, its effect was different on worm reduction. So, it is not enough to eliminate the infection and FMK+PZQ considered the antischistosomicidal drug of choice.

Keywords: praziquantel, fluromethylketone, vinyl sulfone, worm burden, immunoglobulin pattern

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Authors: Wenxing Chen, Guangying Chen, Yin Lu, Shile Huang

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Cryptotanshinone (CPT), a fat-soluble tanshinone from Salvia miltiorrhiza Bunge, has been demonstrated to inhibit mTOR pathway, resulting in inhibition of cancer cell proliferation. However, the molecular mechanism how CPT acts on mTOR is unknown. Here, cancer cells expressing rapamycin-resistant mutant mTOR are also sensitive to CPT, while phosphorylation of AMPK and TSC2 was activated, suggesting that CPT inhibition of mTOR maybe due to activating upstream of mTOR, AMPK, but not directly binding to and inhibiting mTOR. Further results indicated that Compound C, inhibitor of AMPK, could partially reversed CPT inhibition effect on cancer cells, and dominant-negative AMPK in cancer cells conferred resistance to CPT inhibition of 4EBP1 and phosphorylation of S6K1, as well as sh-AMPK. Furthermore, compared with MEF cells with AMPK positive, MEF cells with AMPK knock out are less sensitive to CPT by the findings that 4E-BP1 and phosphorylation of S6K1 express comparatively much. Furthermore, downexpression of TSC2 slightly recovered expression of 4EBP1 and phosphorylation of S6K1, while co-immunoprecipitation of TSC2 did not affect expression of TSC1 by CPT. Collectively, the above-mentioned results suggest that CPT inhibited mTOR pathway mostly was due to activation of AMPK-TSC2 pathway rather than specific inhibition of mTOR and then induction of subsequent lethal cellular effect.

Keywords: cryptotanshinone, AMPK, TSC2, mTOR, cancer cells

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Authors: Roland Tolulope Loto, Cleophas Akintoye Loto, Abimbola Patricia Popoola

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The inhibiting action of 2-dimethylamine on the electrochemical behaviour of austenitic stainless steel (type 304) in dilute hydrochloric was evaluated through weight-loss method, open circuit potential measurement and potentiodynamic polarization tests at specific concentrations of the organic compound. Results obtained reveal that the compound performed effectively giving a maximum inhibition efficiency of 79% at 12.5% concentration from weight loss analysis and 80.9% at 12.5% concentration from polarization tests. The average corrosion potential of -321 mV was obtained the same concentration from other tests which is well within passivation potentials on the steel thus, providing good protection against corrosion in the acid solutions. 2-dimethylamine acted through physiochemical interaction at the steel/solution interface from thermodynamic calculations and obeyed the Langmuir adsorption isotherm. The values of the inhibition efficiency determined from the three methods are in reasonably good agreement. Polarization studies showed that the compounds behaved as cathodic type inhibitor.

Keywords: corrosion, 2-dimethylamine, inhibition, adsorption, hydrochloric acid, steel

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Authors: Nety Trisnawaty, Mirna Febriani

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The use of stainless steel wires in the field of dentistry is widely used, especially for orthodontic and prosthodontic treatment using stainless steel wire. The oral cavity is the ideal environment for corrosion, which can be caused by saliva. Prevention of corrosion on stainless steel wires can be done by using an organic or non-organic corrosion inhibitor. One of the organic inhibitors that can be used to prevent corrosion is black tea leaves extracts. To explain the comparison of chromium ions release for stainlees steel between artificial saliva and black tea leaves extracts. In this research we used artificial saliva, black tea leaves extracts, stainless steel wire and using Atomic Absorption Spectrophometric testing machine. The samples were soaked for 1, 3, 7 and 14 days in the artificial saliva and black tea leaves extracts. The results showed the difference of chromium ion release soaked in artificial saliva and black tea leaves extracts on days 1, 3, 7 and 14. Statistically, calculation with independent T-test with p < 0,05 showed a significant difference. The longer the duration of days, the more ion chromium were released. The conclusion of this study shows that black tea leaves extracts can inhibit the corrosion rate of stainless steel wires.

Keywords: chromium ion, stainless steel, artificial saliva, black tea leaves extracts

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Authors: Madhu Patial, Dharam Pal, Jagdish Kumar, H. K. Chaudhary

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Doubled haploid breeding serves as a useful technique in wheat improvement by providing instant and complete homozygosity. Of the various techniques employed for haploid production chromosome elimination has a large scale practical application in wheat improvement. Barclay (1975) initiated the technique in wheat by crossing wheat variety Chinese spring with Hordeum bulbosum, but due to presence of the dominant crossability inhibitor genes Kr7 and Kr2 in many wheat varieties, the technique was however genotypic specific. The discovery of wheat X maize system of haploid production being genotype non-specific is quite successful but still maize needs to be grown in greenhouse to coincide flowering with wheat crop. Recently, wheat X Imperate cylindrica has been identified as a new chromosome mediated DH approach for efficient haploid induction. An experiment to use this technique in wheat was set up by crossing six F1s and two three way F1s with Imperata cylindrica. The data was recorded for the three component traits of haploid induction viz., seed formation, embryo formation and regeneration frequency. Variation among wheat F1s was observed and higher frequency for all the traits were recorded in cross HD 2997/2*FL-8/DONSK-POLL and KLE/BER/2*FL-8/DONSK-POLL.

Keywords: wheat, haploid, imperata cylindrica, chromosome elimination technique

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Authors: Pauline Nyssen, Ange Mouithys-Mickalad, Maryse Hoebeke

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Inflammation is a complex physiological phenomenon involving chemical and enzymatic mechanisms. Polymorphonuclear neutrophil leukocytes (PMNs) play an important role by producing reactive oxygen species (ROS) and releasing myeloperoxidase (MPO), a pro-oxidant enzyme. Released both in the phagolysosome and the extracellular medium, MPO produces during its peroxidase and halogenation cycles oxidant species, including hypochlorous acid, involved in the destruction of pathogen agents, like bacteria or viruses. Inflammatory pathologies, like rheumatoid arthritis, atherosclerosis induce an excessive stimulation of the PMNs and, therefore, an uncontrolled release of ROS and MPO in the extracellular medium, causing severe damages to the surrounding tissues and biomolecules such as proteins, lipids, and DNA. The treatment of chronic inflammatory pathologies remains a challenge. For many years, MPO has been used as a target for the development of effective treatments. Numerous studies have been focused on the design of new drugs presenting more efficient MPO inhibitory properties. However, some designed inhibitors can be toxic. An alternative consists of assessing the potential inhibitory action of clinically-known molecules, having antioxidant activity. Propofol, 2,6-diisopropyl phenol, which is used as an intravenous anesthetic agent, meets these requirements. Besides its anesthetic action employed to induce a sedative state during surgery or in intensive care units, propofol and its injectable form Diprivan indeed present antioxidant properties and act as ROS and free radical scavengers. A study has also evidenced the ability of propofol to inhibit the formation of the neutrophil extracellular traps fibers, which are important to trap pathogen microorganisms during the inflammation process. The aim of this study was to investigate the potential inhibitory action mechanism of propofol and Diprivan on MPO activity. To go into the anti-inflammatory action of propofol in-depth, two of its oxidative derivatives, 2,6-diisopropyl-1,4-p-benzoquinone (PPFQ) and 3,5,3’,5’-tetra isopropyl-(4,4’)-diphenoquinone (PPFDQ), were studied regarding their inhibitory action. Specific immunological extraction followed by enzyme detection (SIEFED) and molecular modeling have evidenced the low anti-catalytic action of propofol. Stopped-flow absorption spectroscopy and direct MPO activity analysis have proved that propofol acts as a reversible MPO inhibitor by interacting as a reductive substrate in the peroxidase cycle and promoting the accumulation of redox compound II. Overall, Diprivan exhibited a weaker inhibitory action than the active molecule propofol. In contrast, PPFQ seemed to bind and obstruct the enzyme active site, preventing the trigger of the MPO oxidant cycles. PPFQ induced a better chlorination cycle inhibition at basic and neutral pH in comparison to propofol. PPFDQ did not show any MPO inhibition activity. The three interest molecules have also demonstrated their inhibition ability on an important step of the inflammation pathway, the PMNs superoxide anions production, thanks to EPR spectroscopy and chemiluminescence. In conclusion, propofol presents an interesting immunomodulatory activity by acting as a reductive substrate in the peroxidase cycle of MPO, slowing down its activity, whereas PPFQ acts more as an anti-catalytic substrate. Although PPFDQ has no impact on MPO, it can act on the inflammation process by inhibiting the superoxide anions production by PMNs.

Keywords: Diprivan, inhibitor, myeloperoxidase, propofol, spectroscopy

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Authors: Samira Ghizellaoui, Manel Boumagoura

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Calcium carbonate precipitation is a widespread problem, especially in hard water systems. The main water supply that supplies the city of Constantine with drinking water is underground water called Hamma water. This water has a very high hardness of around 590 mg/L CaCO₃. This leads to the formation of scale, consisting mainly of calcium carbonate, which can be responsible for the clogging of valves and the deterioration of equipment (water heaters, washing machines and encrustations in the pipes). Plant extracts used as scale inhibitors have attracted the attention of several researchers. In recent years, green inhibitors have attracted great interest because they are biodegradable, non-toxic and do not affect the environment. The aim of our work is to evaluate the effectiveness of a chemical antiscale treatment in the presence of three green inhibitors: gallicacid; quercetin; alginate, and three mixtures: (gallic acid-quercetin); (quercetin-alginate); (gallic acid-alginate). The results show that the inhibitory effect is manifested from an addition of 1mg/L of gallic acid, 10 mg/L of quercetin, 0.2 mg/L of alginate, 0.4mg/L of (gallic acid-quercetin), 2mg/L of (quercetin-alginate) and 0.4 mg/L of (gallic acid-alginate). On the other hand, 100 mg/L (Drinking water standard) of Ca2+is reached for partial softening at 4 mg/L of gallic acid, 40 mg/L of quercetin, 0.6mg/L of alginate, 4mg/L of (gallic acid-quercetin), 10mg/L of (quercetin-alginate) and 1.6 mg/L of (gallic acid-alginate).

Keywords: water, scaling, calcium carbonate, green inhibitor

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Authors: Reza Eslami-Farsani, Hamed Khosravi, Saba Fayazzadeh

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Lightweight and efficient structures have the aim to enhance the efficiency of the components in various industries. Toward this end, composites are one of the most widely used materials because of durability, high strength and modulus, and low weight. One type of the advanced composites is grid-stiffened composite (GSC) structures which have been extensively considered in aerospace, automotive, and aircraft industries. They are one of the top candidates for replacing some of the traditional components which are used here. Although there are a good number of published surveys on the design aspects and fabrication of GSC structures, little systematic work has been reported on their material modification to improve their properties, to our knowledge. Matrix modification using nanoparticles is an effective method to enhance the flexural properties of the fibrous composites. In the present study, a silane coupling agent (3-glycidoxypropyltrimethoxysilane/3-GPTS) was introduced onto the silica (SiO2) nanoparticle surface and its effects on the three-point flexural response of isogrid E-glass/epoxy composites were assessed. Based on the fourier transform infrared spectrometer (FTIR) spectra, it was inferred that the 3-GPTS coupling agent was successfully grafted onto the surface of SiO2 nanoparticles after modification. Flexural test revealed an improvement of 16%, 14%, and 36% in stiffness, maximum load and energy absorption of the isogrid specimen filled with 3 wt.% 3-GPTS/SiO2 compared to the neat one. It would be worth mentioning that in these structures, a considerable energy absorption was observed after the primary failure related to the load peak. Also, 3-GPTMS functionalization had a positive effect on the flexural behavior of the multiscale isogrid composites. In conclusion, this study suggests that the addition of modified silica nanoparticles is a promising method to improve the flexural properties of the grid-stiffened fibrous composite structures.

Keywords: isogrid-stiffened composite panels, silica nanoparticles, surface modification, flexural properties, energy absorption

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Authors: Hany M. Abd El-Lateef

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Two novel Schiff bases, 5-bromo-2-[(E)-(pyridin-3-ylimino) methyl] phenol (HBSAP) and 5-bromo-2-[(E)-(quinolin-8-ylimino) methyl] phenol (HBSAQ) have been synthesized. They have been characterized by elemental analysis and spectroscopic techniques (UV–Vis, IR and NMR). Moreover, the molecular structure of HBSAP and HBSAQ compounds are determined by single crystal X-ray diffraction technique. The inhibition activity of HBSAP and HBSAQ for carbon steel in 3.5 %NaCl+0.1 M HCl for both short and long immersion time, at different temperatures (20-50 ºC), was investigated using electrochemistry and surface characterization. The potentiodynamic polarization shows that the inhibitors molecule is more adsorbed on the cathodic sites. Its efficiency increases with increasing inhibitor concentrations (92.8 % at the optimal concentration of 10-3 M for HBSAQ). Adsorption of the inhibitors on the carbon steel surface was found to obey Langmuir’s adsorption isotherm with physical/chemical nature of the adsorption, as it is shown also by scanning electron microscopy. Further, the electronic structural calculations using quantum chemical methods were found to be in a good agreement with the results of the experimental studies.

Keywords: carbon steel, Schiff bases, corrosion inhibition, SEM, electrochemical techniques

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Authors: Reza Eslami-Farsani, Hamed Khosravi, Saba Fayazzadeh

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Lightweight and efficient structures have the aim to enhance the efficiency of the components in various industries. Toward this end, composites are one of the most widely used materials because of durability, high strength and modulus, and low weight. One type of the advanced composites is grid-stiffened composite (GSC) structures, which have been extensively considered in aerospace, automotive, and aircraft industries. They are one of the top candidates for replacing some of the traditional components, which are used here. Although there are a good number of published surveys on the design aspects and fabrication of GSC structures, little systematic work has been reported on their material modification to improve their properties, to our knowledge. Matrix modification using nanoparticles is an effective method to enhance the flexural properties of the fibrous composites. In the present study, a silane-coupling agent (3-glycidoxypropyltrimethoxysilane/3-GPTS) was introduced onto the silica (SiO2) nanoparticle surface and its effects on the three-point flexural response of isogrid E-glass/epoxy composites were assessed. Based on the fourier transform infrared spectrometer (FTIR) spectra, it was inferred that the 3-GPTS coupling agent was successfully grafted onto the surface of SiO2 nanoparticles after modification. Flexural test revealed an improvement of 16%, 14%, and 36% in stiffness, maximum load and energy absorption of the isogrid specimen filled with 3 wt.% 3-GPTS/SiO2 compared to the neat one. It would be worth mentioning that in these structures, considerable energy absorption was observed after the primary failure related to the load peak. In addition, 3-GPTMS functionalization had a positive effect on the flexural behavior of the multiscale isogrid composites. In conclusion, this study suggests that the addition of modified silica nanoparticles is a promising method to improve the flexural properties of the grid-stiffened fibrous composite structures.

Keywords: isogrid-stiffened composite panels, silica nanoparticles, surface modification, flexural properties

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Authors: Wissam Saliba, Mandy Nicholson

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Secretory carcinoma (SC) is a rare type of salivary gland cancer. It was first realized as a distinct type of malignancy in 2010and wasinitially termed “mammary analogue secretory carcinoma” because of similarities with secretory breast cancer. The name was later changed to SC. Most SCs originate in parotid glands, and most harbour a rare gene mutation: ETV6-NTRK3. This mutation is rare in common cancers and common in rare cancers; it is present in most secretory carcinomas. Disease outcomes for SC are usually described as favourable as many cases of SC are lowgrade (LG), and cancer growth is slow. In early stages, localized therapy is usually indicated (surgery and/or radiation). Despitea favourable prognosis, a sub-set of casescan be much more aggressive.These cases tend to be of high-grade(HG).HG casesare associated with a poorer prognosis.Management of such cases can be challenging due to limited evidence for effective systemic therapy options. This case report describes the clinical management of a 46-year-oldmale patient with a unique case of SC. He was initially diagnosed with a low/intermediate grade carcinoma of the left parotid gland in 2009; he was treated with surgery and adjuvant radiation. Surgical pathology favoured primary salivary adenocarcinoma, and 2 lymph nodes were positive for malignancy. SC was not yet realized as a distinct type of cancerat the time of diagnosis, and the pathology reportvalidated this gap by stating that the specimen lacked features of the defined types of salivary carcinoma.Slow-growing pulmonary nodules were identified in 2017. In 2020, approximately 11 years after the initial diagnosis, the patient presented with malignant pleural effusion. Pathology from a pleural biopsy was consistent with metastatic poorly differentiated cancer of likely parotid origin, likely mammary analogue secretory carcinoma. The specimen was sent for Next Generation Sequencing (NGS); ETV6-NTRK3 gene fusion was confirmed, and systemic therapy was initiated.One cycle ofcarboplatin/paclitaxel was given in June 2020. He was switched to Larotrectinib (NTRK inhibitor (NTRKi)) later that month. Larotrectinib continued for approximately 9 months, with discontinuation in March 2021 due to disease progression. A second-generation NTRKi (Selitrectinib) was accessed and prescribedthrough a single patient study. Selitrectinib was well tolerated. The patient experienced a complete radiological response within~4 months. Disease progression occurred once again in October 2021. Progression was slow, and Selitrectinib continuedwhile the medical team performed a thorough search for additional treatment options. In January 2022, a liver lesion biopsy was performed, and NGS showed an NTRKG623R solvent-front resistance mutation. Various treatment pathways were considered. The patient pursuedanother investigational NTRKi through a clinical trial, and Selitrectinib was discontinued in July 2022. Excellent performance status was maintained throughout the entire course of treatment.It can be concluded that NTRK inhibitors provided satisfactory treatment efficacy and tolerance for this patient with high-grade transformation and NTRK gene fusion cancer. In the future, more clinical research is needed on systemic treatment options for high-grade transformations in NTRK gene fusion SCs.

Keywords: secretory carcinoma, high-grade transformations, NTRK gene fusion, NTRK inhibitor

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Authors: Ibrahim M. Labouta, Marwa H. El-Wakil, Hayam M. Ashour, Ahmed M. Hassan, Manal N. Saudi

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The receptor tyrosine kinase c-Met is an attractive target for therapeutic treatment of cancers nowadays. Among the wide variety of heterocycles that have been explored for developing c-Met kinase inhibitors, the 1,2,4-triazines have been rarely investigated, although they are well known in the literature to possess antitumor activities. Herein we describe the design and synthesis of a novel series of 1,2,4-triazine derivatives possessing N-acylarylhydrazone moiety and another series combining the 1,2,4-triazine scaffold to the well-known anticancer drug 6-MP in order to explore their “double-drug” effect. The synthesized compounds were evaluated for their in vitro antitumor activity against three c-Met addicted cancer cell lines (A549, HT-29 and MKN-45). Most compounds showed moderate to excellent antiproliferative activity and four compounds showed potent inhibitory activity more than the reference drug Foretinib against one or more cancer cell lines. The obtained results revealed that the potent compounds are highly selective to A549 (lung adenocarcinoma) cancer cell line. The c-Met kinase inhibitory activity of the potent derivatives is still under investigation. The present study clearly demonstrates that the 1,2,4-triazine core ring exhibits promising antitumor activity with potential c-Met kinase inhibitory activity.

Keywords: 1, 2, 4-triazine, antitumor, c-Met inhibitor, double-drug

Procedia PDF Downloads 313

Authors: Rajiv Arora

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Biodiesel may be economical if produced from inexpensive feedstock which commonly contains high level of free fatty acids (FFA) as an inhibitor in production of methyl ester. In this study, a two-step process for biodiesel production from high FFA spent bleach earth oil in a batch reactor is developed. Oil sample extracted from spent bleaching earth (SBE) was utilized for biodiesel process. In the first step, FFA of the SBE oil was reduced to 1.91% through sulfuric acid catalyzed esterification. In the second step, the product prepared from the first esterification process was carried out transesterification with an alkaline catalyst. The influence of four variables on conversion efficiency to methyl ester, i.e., methanol/ SBE oil molar ratio, catalyst amount, reaction temperature and reaction time, was studied in the second stage. The optimum process variables in the transesterification were methanol/oil molar ratio 6:1, heterogeneous catalyst conc. 5 wt %, reaction temperature 65 °C and reaction time 60 minutes to produce biodiesel. Major fuel properties of SBE biodiesel were measured to comply with ASTM and EN standards. Therefore, an optimized process for production of biodiesel from a low-cost high FFA source was accomplished.

Keywords: biodiesel, esterification, free fatty acids, residual oil, spent bleaching earth, transesterification

Procedia PDF Downloads 153

Authors: Seham Alsaif, Susan Wray

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Obesity is a worldwide disorder influencing women’s health and childbearing. There is a close relation between obesity and pregnancy related complications. Dyslipidemia and adipokine dysregulation are core environmental changes that may mechanistically link these complications with obesity in pregnant women. We have previously found that visfatin has a relaxant effect on mouse, rat and human myometrial contractility. We hypothesised that visfatin inhibits mouse myometrial contractility through the NAD+ pathway. This study was designed to examine the mechanism of action of visfatin on myometrial contractility. To examine the NAD+ pathway, FK866 which is a potent inhibitor of NAD+ biosynthesis was used. Methods: Myometrial strips from term pregnant mice were dissected, superfused with physiological saline and the effects of visfatin (10nM) on oxytocin-induced contractions (0.5nM) alone and after the infusion of FK866 (10uM) were studied. After regular contractions were established, contractility was examined for control (100%) and test response at 37 °C for 10 min each. Results: FK866 was found to inhibit the effect of visfatin on myometrial contractility (the AUC increased from 89±2% of control, P=0.0009 for visfatin alone to 97±4% of control, P>0.05 for visfatin combined with FK866, n=8). In conclusion, NAD+ pathway appears to be involved in the mechanism of action of visfatin on mouse myometrium. This could have a role in making new targets to prevent obesity-related complications.

Keywords: myometrium, obesity, oxytocin, pregnancy, visfatin

Procedia PDF Downloads 150

Authors: K. Biswas, U. H. Armin, S. M. J. Prodhan, J. A. Prithul, S. Sarker, F. Afrin

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Alzheimer’s disease (AD) (a progressive neurodegenerative disorder) is mostly predominant cause of dementia in the elderly. Prolonging the function of acetylcholine by inhibiting both acetylcholinesterase and butyrylcholinesterase is most effective treatment therapy of AD. Traditionally Pterocarpus santalinus L. is widely known for its medicinal use. In this study, in vitro acetylcholinesterase inhibitory activity was investigated and methanolic extract of the plant showed significant activity. To confirm this activity (in vivo), learning and memory enhancing effects were tested in mice. For the test, memory impairment was induced by scopolamine (cholinergic muscarinic receptor antagonist). Anti-amnesic effect of the extract was investigated by the passive avoidance task in mice. The study also includes brain acetylcholinesterase activity. Results proved that scopolamine induced cognitive dysfunction was significantly decreased by administration of the extract solution, in the passive avoidance task and inhibited brain acetylcholinesterase activity. These results suggest that bark extract of Pterocarpus santalinus can be better option for further studies on AD via their acetylcholinesterase inhibitory actions.

Keywords: Pterocarpus santalinus, cholinesterase inhibitor, passive avoidance, Alzheimer’s disease

Procedia PDF Downloads 210

Authors: Azhar Jabareen, Mahmoud Huleihel

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BRCA-1 is a multifunctional tumor suppressor, whose expression is activated by the estrogen (E2)-liganded ERα receptor. The activated ERα is a transcriptional factor which activates various genes either by direct binding to the DNA at E2-responsive elements (EREs) and indirectly associated with a range of alternative non-ERE elements. Interference with BRCA-1 expression and/or functions leads to high risk of breast or/and ovarian cancer. Our lab investigated the involvement of Human T-cell leukemia Virus Type 1 (HTLV-1) in breast cancer, since HTLV-1 Tax was found to strongly inhibit BRCA-1 expression. In addition, long exposure of 12-O-tetradecanoylphorbol-13-acetate (TPA), which is one of the stress-inducing agents activated the HTLV-1 promoter. So here the involvement of TPA in breast cancer had been examined by testing the effect of TPA on BRCA-1 and ERE expression. The results showed that TPA activated both BRCA-1 and ERE expression. In the 12 hours TPA activated the tow promoters more than others time, and after 24 hours the level of the tow promoters was decreased. Tax inhibited BRCA-1 expression but did not succeed to inhibit the effect of TPA. Then the activation of the two promoters was not through ERα pathway because TPA had no effect on ERα binding to the two promoters of the BRCA-1 and ERE. Also, the activation was not via nuclear factor kappa B (NF-κB) pathway because when the inhibitory of NF-κB had been added to the TPA, it still activated the tow promoters. However, it seems that 53BP1 may be involved in TPA activation of these promoters because ectopic high expression of 53BP1 significantly reduced the TPA activity. In addition, in the presence of Bisindolylmaleimide-I (BI)- the inhibitor of Protein Kinase C (PKC)- there was no activation for the two promoters, so the PKC is agonized BRCA-1 and ERE activation.

Keywords: BRCA-1, ERE, HTLV-1, TPA

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Authors: Zahra Tolou-Ghamari

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Introduction: After allogeneic organ transplantation, in order to lower the rate of rejectiontacrolimus is given. In fact, infection is reported as the most complication of tacrolimus that might be associated with higher susceptibility by its’ long term use. Aim: This study aims to review the association between the occurrence of infections after organ transplantation following the administration of tacrolims. Materials and Methods: Scientific literature on the pharmacotherapy of tacrolimus after organ transplantation and infections were searched using PUBMED.Gov (https://pubmed.ncbi.nlm.nih.gov/), Web of Science, and Scopus. Results: In order to prevent acute and chronic rejection, the potent immunosuppressive drug tacrolimus administered as a calcineurin inhibitor after organ transplantation. Its’ most frequent infectious complication is reported as urinary tract infection. Virulent strain of recombinant Literiamonocytogenes, in addition to an increase in bacterial burden in the liver and spleen tissues, was reported in the animal experimental study. The consequence of aggressive events and recipients total area under the cureve exposure to immunosuppressive could be as considered as surrogate markers for individual infection’s risk evaluation. Conclusion: Transplant surgery and duration of hospital stay could determinate the risk of infection during the first month of organ transplantation. Despite administration of antiviral drugs, opportunistic infection such as cytomegalovirus could increase the risk of infection during month 1 to year after transplantation.

Keywords: transplant, infection, tacrolimus, kidney

Procedia PDF Downloads 93

Authors: Fatiha Benghanem, Mokhtar Berarma, Saida Keraghel, Ali Ourari

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Corrosion is the result of the reaction between a material and its environment. Steel in concrete is protected from corrosion by a passive film promoted by concrete alkalinity. For the initiation of corrosion, this protective film must be destroyed and this can be mainly done in two ways: by the attack of chlorides on the steel or by carbonation of the cover concrete due the reaction with carbon dioxide, which causes reduction in the alkalinity of concrete. The literature reports several ways to decrease or to prevent reinforcement corrosion. Among them, the use of corrosion inhibitors has been an envisaged solution. Two approaches are generally used to evaluate the efficiency of inhibitors for concrete application; one uses simulated pore solution testing , and the other uses actual concrete or mortar specimens. Both methods are some times used in conjunction. The aim of this study is to investigate the use of 2,3-diaminopyridine as a corrosion inhibitors of steel in alkaline media which simulate the electrolyte in the concrete pores. The effectiveness of this compound as corrosion inhibitor was investigated by measuring the corrosion potentials, the polarization curves and the corrosion current densities of steel with and without chlorides. The study of corrosion inhibition by this compound led to the conclusion that he has low rates of inhibition in the absence of aggressive ions and high rates in their presence. This type of organic compounds are promoting for the protection of armatures in concrete.

Keywords: corrosion, inhibitors, mild steel, conjunction

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