Search results for: aromatase activity
4890 Methylphenidate and Placebo Effect on Brain Activity and Basketball Free Throw: A Randomized Controlled Trial
Authors: Mohammad Khazaei, Reza Rostami, Hasan Gharayagh Zandi, Rouhollah Basatnia, Mahbubeh Ghayour Najafabadi
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Objective: Methylphenidate has been demonstrated to enhance attention and cognitive processes, and placebo treatments have also been found to improve attention and cognitive processes. Additionally, methylphenidate may have positive effects on motion perception and sports performance. Nevertheless, additional research is needed to fully comprehend the neural mechanisms underlying the effects of methylphenidate and placebo on cognitive and motor functions. Methods: In this randomized controlled trial, 18 young semi-professional basketball players aged 18-23 years were randomly and equally assigned to either a Ritalin or Placebo group. The participants performed 20 consecutive free throws; their scores were recorded on a 0-3 scale. The participants’ brain activity was recorded using electroencephalography (EEG) for 5 minutes seated with their eyes closed. The Ritalin group received a 10 mg dose of methylphenidate, while the Placebo group received a 10mg dose of placebo. The EEG was obtained 90 minutes after the drug was administere Results: There was no significant difference in the absolute power of brain waves between the pre-test and post-tests in the Placebo group. However, in the Ritalin group, a significant difference in the absolute power of brain waves was observed in the Theta band (5-6 Hz) and Beta band (21-30 Hz) between pre- and post-tests in Fp2, F8, and Fp1. In these areas, the absolute power of Beta waves was higher during the post-test than during the pre-test. The Placebo group showed a more significant difference in free throw scores than the Ritalin group. Conclusions: In conclusion, these results suggest that Ritalin effect on brain activity in areas associated with attention and cognitive processes, as well as improve basketball free throws. However, there was no significant placebo effect on brain activity performance, but it significantly affected the improvement of free throws. Further research is needed to fully understand the effects of methylphenidate and placebo on cognitive and motor functions.Keywords: methylphenidate, placebo effect, electroencephalography, basketball free throw
Procedia PDF Downloads 794889 2D Fingerprint Performance for PubChem Chemical Database
Authors: Fatimah Zawani Abdullah, Shereena Mohd Arif, Nurul Malim
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The study of molecular similarity search in chemical database is increasingly widespread, especially in the area of drug discovery. Similarity search is an application in the field of Chemoinformatics to measure the similarity between the molecular structure which is known as the query and the structure of chemical compounds in the database. Similarity search is also one of the approaches in virtual screening which involves computational techniques and scoring the probabilities of activity. The main objective of this work is to determine the best fingerprint when compared to the other five fingerprints selected in this study using PubChem chemical dataset. This paper will discuss the similarity searching process conducted using 6 types of descriptors, which are ECFP4, ECFC4, FCFP4, FCFC4, SRECFC4 and SRFCFC4 on 15 activity classes of PubChem dataset using Tanimoto coefficient to calculate the similarity between the query structures and each of the database structure. The results suggest that ECFP4 performs the best to be used with Tanimoto coefficient in the PubChem dataset.Keywords: 2D fingerprints, Tanimoto, PubChem, similarity searching, chemoinformatics
Procedia PDF Downloads 2934888 Photo-Degradation Black 19 Dye with Synthesized Nano-Sized ZnS
Authors: M. Tabatabaee, R. Mohebat, M. Baranian
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Textile industries produce large volumes of colored dye effluents which are toxic and non-biodegradable. Earlier studies have shown that a wide range of organic substrates can be completely photo mineralized in the presence of photocatalysts and oxidant agents. ZnO and TiO2 are important photocatalysts with high catalytic activity that have attracted much research attention. Zinc sulfide is one of the semiconductor nanomaterials that can be used for the production of optical sensitizers, photocatalysts, electroluminescent materials, optical sensors and for solar energy conversion. The synthesis of ZnS nanoparticles has been tried by various methods and sulfide sources. Elementary sulfur powder, H2S or Na2S are used as sulfide sources for synthesis of ZnS nano particles. Recently, solar energy is has been successfully used for photocatalytic degradation of dye pollutant. Studies have shown that the use of metal oxides or sulfides with ZnO or TiO2 can significantly enhance the photocatalytic activity of them. In this research, Nano-sized zinc sulfide was synthesized successfully by a simple method using thioasetamide as sulfide source in the presence of polyethylene glycol (PEG 2000). X-ray diffraction (XRD) spectroscopy scanning electron microscope (SEM) was used to characterize the structure and morphology synthesized powder. The effect of photocatalytic activity of prepared ZnS and ZnS/ZnO, on degradation of direct Black19 under UV and sunlight irradiation was investigated. The effects of various parameters such as amount of photocatalyst, pH, initial dye concentration and irradiation time on decolorization rate were systematically investigated. Results show that more than 80% of 500 mgL-1 of dye decolorized in 60-min reaction time under UV and solar irradiation in the presence of ZnS nanoparticles. Whereas, mixed ZnS/ZnO (50%) can decolorize more than 80% of dye in the same conditions.Keywords: zinc sulfide, nano articles, photodegradation, solar light
Procedia PDF Downloads 4044887 Protective Effect of Levetiracetam on Aggravation of Memory Impairment in Temporal Lobe Epilepsy by Phenytoin
Authors: Asher John Mohan, Krishna K. L.
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Objectives: (1) To assess the extent of memory impairment induced by Phenytoin (PHT) at normal and reduced dose on temporal lobe epileptic mice. (2) To evaluate the protective effect of Levetiracetam (LEV) on aggravation of memory impairment in temporal lobe epileptic mice by PHT. Materials and Methods: Albino mice of either sex (n=36) were used for the study for a period of 64 days. Convulsions were induced by intraperitoneal administration of pilocarpine 280 mg/kg on every 6th day. Radial arm maze (RAM) was employed to evaluate the memory impairment activity on every 7th day. The anticonvulsant and memory impairment activity were assessed in PHT normal and reduced doses both alone and in combination with LEV. RAM error scores and convulsive scores were the parameters considered for this study. Brain acetylcholine esterase and glutamate were determined along with histopathological studies of frontal cortex. Results: Administration of PHT for 64 days on mice has shown aggravation of memory impairment activity on temporal lobe epileptic mice. Although the reduction in PHT dose was found to decrease the degree of memory impairment the same decreased the anticonvulsant potency. The combination with LEV not only brought about the correction of impaired memory but also replaced the loss of potency due to the reduction of the dose of the antiepileptic drug employed. These findings were confirmed with enzyme and neurotransmitter levels in addition to histopathological studies. Conclusion: This study thus builds a foundation in combining a nootropic anticonvulsant with an antiepileptic drug to curb the adverse effect of memory impairment associated with temporal lobe epilepsy. However further extensive research is a must for the practical incorporation of this approach into disease therapy.Keywords: anti-epileptic drug, Phenytoin, memory impairment, Pilocarpine
Procedia PDF Downloads 3164886 Synergistic and Antagonistic Interactions between Garlic Extracts and Metformin in Diabetes Treatment
Authors: Ikram Elsiddig, Yacouba Djamila, Amna Hamad
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Abstract—The worldwide increasing of using herbs in form of medicine with or without prescription medications potentiates the interactions between herbal products and conventional medicines; due to more research for herb-drug interactions are needed. for a long time hyperglycemia had been treated with several medicinal plants. A. sativum, belonging to the Liliaceae family is well known for its medicinal uses in African traditional medicine, it used for treating of many human diseases mainly diabetes, high cholesterol and high blood pressure. The purpose of this study is to determine the interaction effect between A. sativum bulb extracts and metformin drug used in diabetes treatment. The in vitro and in vivo evaluation were conducted by glucose reuptake using isolated rats hemidiaphgrams tissue and by estimate glucose tolerance in glucose-loaded wistar albino rats. The results showed that, petroleum ether, chloroform and ethyl acetate extracts were found to have activity of glucose uptake in isolated rats hemidiaphgrams of 24.11 mg/g, 19.07 mg/g and 15.66 mg/g compared to metformin drug of 17 mg/g. These activity were reducded to 17.8 mg/g, 13.59 mg/g and 14.46 mg/g after combination with metformin, metformin itself reduced to 13.59 mg/g, 14.46 mg/g and 12.71 mg/g in comination with chloroform and ethyl acetate. These decrease in activity could be due to herbal–drug interaction between the extracts of A. sativum bulb and metformin drug. The interaction between A. sativum extract and metformin was also shown by in vivo study on the induced hyperglycemic rats. The glucose level after administered of 200 mg/kg was found to be increase with 47.2 % and 17.7% at first and second hour compared to the increase of blood glucose in the control group of 82.6% and76.7%.. At fourth hour the glucose level was became less than normal with 3.4% compared to control which continue to increase with 68.2%. Dose of 400 mg/kg at first hour showed increase in blood glucose of 31.5 %, at second and fourth hours the glucose level was became less than normal with decrease of 3.2 % and 30.4%. After combination the activity was found to be less than that of extract at both high and low dose, whereas, at first and second hour, the glucose level was found to be increase with 50.4% and 21.2%, at fourth hour the glucose level was became less than normal with 14%. Therefore A. sativum could be a potential source for anti-diabetic when it used alone, and it is significant important to use the garlic extract alone instead of combined with Metformin drug in diabetes- treatment.Keywords: Antagonistic, Garlic, Metformin, Synergistic
Procedia PDF Downloads 1814885 Telomerase, a Biomarker in Oral Cancer Cell Proliferation and Tool for Its Prevention at Initial Stage
Authors: Shaista Suhail
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As cancer populations is increasing sharply, the incidence of oral squamous cell carcinoma (OSCC) has also been expected to increase. Oral carcinogenesis is a highly complex, multistep process which involves accumulation of genetic alterations that lead to the induction of proteins promoting cell growth (encoded by oncogenes), increased enzymatic (telomerase) activity promoting cancer cell proliferation. The global increase in frequency and mortality, as well as the poor prognosis of oral squamous cell carcinoma, has intensified current research efforts in the field of prevention and early detection of this disease. The advances in the understanding of the molecular basis of oral cancer should help in the identification of new markers. The study of the carcinogenic process of the oral cancer, including continued analysis of new genetic alterations, along with their temporal sequencing during initiation, promotion and progression, will allow us to identify new diagnostic and prognostic factors, which will provide a promising basis for the application of more rational and efficient treatments. Telomerase activity has been readily found in most cancer biopsies, in premalignant lesions or germ cells. Activity of telomerase is generally absent in normal tissues. It is known to be induced upon immortalization or malignant transformation of human cells such as in oral cancer cells. Maintenance of telomeres plays an essential role during transformation of precancer to malignant stage. Mammalian telomeres, a specialized nucleoprotein structures are composed of large conctamers of the guanine-rich sequence 5_-TTAGGG-3_. The roles of telomeres in regulating both stability of genome and replicative immortality seem to contribute in essential ways in cancer initiation and progression. It is concluded that activity of telomerase can be used as a biomarker for diagnosis of malignant oral cancer and a target for inactivation in chemotherapy or gene therapy. Its expression will also prove to be an important diagnostic tool as well as a novel target for cancer therapy. The activation of telomerase may be an important step in tumorgenesis which can be controlled by inactivating its activity during chemotherapy. The expression and activity of telomerase are indispensable for cancer development. There are no drugs which can effect extremely to treat oral cancers. There is a general call for new emerging drugs or methods that are highly effective towards cancer treatment, possess low toxicity, and have a minor environment impact. Some novel natural products also offer opportunities for innovation in drug discovery. Natural compounds isolated from medicinal plants, as rich sources of novel anticancer drugs, have been of increasing interest with some enzyme (telomerase) blockage property. The alarming reports of cancer cases increase the awareness amongst the clinicians and researchers pertaining to investigate newer drug with low toxicity.Keywords: oral carcinoma, telomere, telomerase, blockage
Procedia PDF Downloads 1754884 Alumina Supported Copper-manganese Catalysts for Combustion of Exhaust Gases: Catalysts Characterization
Authors: Krasimir I. Ivanov, Elitsa N. Kolentsova, Dimitar Y. Dimitrov, Georgi V. Avdeev, Tatyana T. Tabakova
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In recent research copper and manganese systems were found to be the most active in CO and organic compounds oxidation among the base catalysts. The mixed copper manganese oxide has been widely studied in oxidation reactions because of their higher activity at low temperatures in comparison with single oxide catalysts. The results showed that the formation of spinel CuxMn3−xO4 in the oxidized catalyst is responsible for the activity even at room temperature. That is why most of the investigations are focused on the hopcalite catalyst (CuMn2O4) as the best copper-manganese catalyst. Now it’s known that this is true only for CO oxidation, but not for mixture of CO and VOCs. The purpose of this study is to investigate the alumina supported copper-manganese catalysts with different Cu/Mn molar ratio in terms of oxidation of CO, methanol and dimethyl ether. The catalysts were prepared by impregnation of γ-Al2O3 with copper and manganese nitrates and the catalytic activity measurements were carried out in continuous flow equipment with a four-channel isothermal stainless steel reactor. Gas mixtures on the input and output of the reactor were analyzed with a gas chromatograph, equipped with FID and TCD detectors. The texture characteristics were determined by low-temperature (- 196 oС) nitrogen adsorption in a Quantachrome Instruments NOVA 1200e (USA) specific surface area&pore analyzer. Thermal, XRD and TPR analyses were performed. It was established that the active component of the mixed Cu-Mn/γ–alumina catalysts strongly depends on the Cu/Mn molar ratio. Highly active alumina supported Cu-Mn catalysts for CO, methanol and DME oxidation were synthesized. While the hopcalite is the best catalyst for CO oxidation, the best compromise for simultaneous oxidation of all components is the catalyst with Cu/Mn molar ratio 1:5.Keywords: supported copper-manganese catalysts, CO, VOCs oxidation, combustion of exhaust gases
Procedia PDF Downloads 2854883 Antibacterial Activity of Nisin: Comparison the Role of Free and Encapsulated Nisin to Control Staphylococcus Aureus Inoculated in Minced Beef
Authors: Zh. Ghasemi, S. Nouri Saeedlou, A. Ghasemi, SL. Nasiri, P. Ayremlou, P. Mahasti
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The use of nisin is successfully used as antibacterial agent in various food products. Although the conclusions of the previous studies were that nisin is not very effective in meat environments. The reduced antimicrobial efficacy of nisin when applied in food has been frequently observed. The aim of this study is to evaluate the potential of free and encapsulated nisin to inhibit the growth of staphylococcus aureus in minced beef. The minimum inhibitory concentration (MIC) of nisin is determined against S. aureus using the agar dilution method. Nisin is encapsulated by spray drying, and encapsulation efficiency, mass yield and total solids content values are 47.79%, 61%, and 96.41 respectively. The study in vitro release kinetics shows highest release of nisin from zein capsules is obtained after 72 hour. This work shows that an appropriate delivery system is necessary to obtain desirable effect of nisin in meat and meat product.Keywords: nisin, encapsulation, Staphylococcus aureus, minced beef, antibacterial activity
Procedia PDF Downloads 2914882 Reducing Power Consumption in Network on Chip Using Scramble Techniques
Authors: Vinayaga Jagadessh Raja, R. Ganesan, S. Ramesh Kumar
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An ever more significant fraction of the overall power dissipation of a network-on-chip (NoC) based system on- chip (SoC) is due to the interconnection scheme. In information, as equipment shrinks, the power contributes of NoC links starts to compete with that of NoC routers. In this paper, we propose the use of clock gating in the data encoding techniques as a viable way to reduce both power dissipation and time consumption of NoC links. The projected scramble scheme exploits the wormhole switching techniques. That is, flits are scramble by the network interface (NI) before they are injected in the network and are decoded by the target NI. This makes the scheme transparent to the underlying network since the encoder and decoder logic is integrated in the NI and no modification of the routers structural design is required. We review the projected scramble scheme on a set of representative data streams (both synthetic and extracted from real applications) showing that it is possible to reduce the power contribution of both the self-switching activity and the coupling switching activity in inter-routers links.Keywords: Xilinx 12.1, power consumption, Encoder, NOC
Procedia PDF Downloads 4004881 Comparative Study of Outcomes of Nonfixation of Mesh versus Fixation in Laparoscopic Total Extra Peritoneal (TEP) Repair of Inguinal Hernia: A Prospective Randomized Controlled Trial
Authors: Raman Sharma, S. K. Jain
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Aims and Objectives: Fixation of the mesh during laparoscopic total extraperitoneal (TEP) repair of inguinal hernia is thought to be necessary to prevent recurrence. However, mesh fixation may increase surgical complications and postoperative pain. Our objective was to compare the outcomes of nonfixation with fixation of polypropylene mesh by metal tacks during TEP repair of inguinal hernia. Methods: Forty patients aged 18 to72 years with inguinal hernia were included who underwent laparoscopic TEP repair of inguinal hernia with (n=20) or without (n=20) fixation of the mesh. The outcomes were operative duration, postoperative pain score, cost, in-hospital stay, time to return to normal activity, and complications. Results: Patients in whom the mesh was not fixed had shorter mean operating time (p < 0.05). We found no difference between groups in the postoperative pain score, incidence of recurrence, in-hospital stay, time to return to normal activity and complications (P > 0.05). Moreover, a net cost savings was realized for each hernia repair performed without stapled mesh. Conclusions: TEP repair without mesh fixation resulted in the shorter operating time and lower operative cost with no difference between groups in the postoperative pain score, incidence of recurrence, in-hospital stay, time to return to normal activity and complications. All this contribute to make TEP repair without mesh fixation a better choice for repair of uncomplicated inguinal hernia, especially in developing nations with scarce resources.Keywords: postoperative pain score, inguinal hernia, nonfixation of mesh, total extra peritoneal (TEP)
Procedia PDF Downloads 3434880 Evaluation of Phytochemical and Antidiarrhoeal Activity of Butanol Fraction of Terminalia avicennioides Leaf in Swiss Albino Rats
Authors: Fatima Mohammed Musa, J. B. Ameh, S. A. Ado, O. S. Olonitola
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The study was undertaken to evaluate the phytochemical constituents of extracts of Terminalia avicennioides leaf and the antidiarrhoeal effect of n-butanol fraction of the leaf extract in Swiss albino rats infected with Salmonella Typhimurium and Escherichia coli. Ethanol crude extract of Terminalia avicennioides leaf was dissolved in 1.5 liters of sterile distilled water. The extract solution was partitioned with 250 ml each of chloroform, ethyl acetate and n-butanol solvents (1:1v/v) to obtain soluble fractions from the extract. The leaf extract and its fractions were screened for the presence of phytocompounds using standard analytical methods. The antidirrhoeal activity of n-butanol fraction was evaluated in Swiss albino rats using standard methods. The results of phytochemical screening of extract of Terminalia avicennioides leaf and its fractions, revealed the presence of carbohydrates, alkaloids, tannins, flavonoids, saponins, steroids, triterpens, glycosides and phenols. The results of in vivo activity showed that 60 % of each group of rats infected with 2.0 x 108 cfu/ml viable cells of S. Typhimurium and 2.0 x109 cfu/ml viable cells of E. coli manifested the symptoms of diarrhoea, 72 hours after the rats were challenged with bacteria. Other symptoms observed among the infected animals included, loss of appetite, loss of weight, general body weakness and 40 % mortality in S. Typhimurium infected non treated group of rats. Similarly, 60 %, and 20 % mortality was observed among E. coli infected none treated and E. coli infected antibiotic (metronidazole) treated groups of rats respectively. However, there was a reduction in the number of infected rats defecating watery stools over time among all the infected rats that were treated with n-butanol fraction of the leaf extract and mortality was also not observed in the group, indicating high efficacy of n-butanol fraction of T. avicennioides leaf. The results also indicated that n-butanol can be used as alternative source of antidiarrhoeal agent in the treatment of diarrhoea caused by Salmonella Typhimurium and Escherichia coli. In the light of this, there is a need for further research on the mechanism of action of the candidate fraction of T. avicennioides leaf which could be responsible for the observed in vivo antibacterial activity.Keywords: antidirrhoeal effect, phytochemical constituents, swiss albino rats, terminalia avicennioides
Procedia PDF Downloads 3824879 Development of 4-Allylpyrocatechol Loaded Self-Nanoemulsifying Drug Delivery System for Enhancing Water Solubility and Antibacterial Activity against Oral Pathogenic Bacteria
Authors: Pimpak Phumat, Sakornrat Khongkhunthian, Thomas Rades, Anette Müllertz, Siriporn Okonogi
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Self-nanoemulsifying drug delivery systems (SNEDDS) containing 4-allylpyrocatechol (AP) extracted from Piper betle were developed to enhance water solubility of AP by using modeling and design (MODDE) program. The amount of AP in each SNEDDS formulation was determined by using high-performance liquid chromatography. The formulation consisted of 20% Miglyol®812N, 40 % Kolliphor®RH40, 30 % Maisine®35-1 and 10 % ethanol was found to be the best SNEDDS that provided the highest loading capacity of AP. (141.48±15.64 mg/g SNEDDS). The system also showed miscibility with water. The particle shape and size of the AP-SNEDDS after dispersing in water was investigated by using a transmission electron microscope and photon correlation spectrophotometer, respectively. The results showed that they were a spherical shape, having a particle size of 34.27 ± 1.14 nm with a narrow size distribution of 0.17 ± 0.04. The particles showed negative zeta potential with a value of -21.66 ± 2.09 mV. Antibacterial activity of AP-SNEDDS containing 1.5 mg/mL of AP was investigated against Streptococcus intermedius. The effect of this system on S. intermedius cells was observed by a scanning electron microscope (SEM). The results from SEM revealed that the bacterial cells were obviously destroyed. Killing kinetic study of AP-SNEDDS was carried out. It was found that the killing rate of AP-SNEDDS against S. intermedius was dose-dependent and the bacterial reduction was 79.86 ± 0.45 % within 30 min. In comparison with chlorhexidine (CHX), AP-SNEDDS showed similar antibacterial effects against S. intermedius. It is concluded that SNEDDS is a potential system for enhancing water solubility of AP. The antibacterial study reveals that AP-SNEDDS can be a promising system to treat bacterial infection caused by S. intermedius.Keywords: SNEDDS, 4-allylpyrocathecol, solubility, antibacterial activity, Streptococcus intermedius
Procedia PDF Downloads 1194878 Assessment of the Psychoemotional State and Quality of Life at Women Teachers of the Senior Age Group
Authors: Meruyert Burumbayeva, Aiman Mussina, Gulnoza Aldabekova, Aiymtory Abildaeva, Gulshat Yerdenova, Aigul Kairgeldina
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this article introduces results of a research which purpose is evaluation the quality of life, the psychophysiological status, expressiveness of uneasiness at women teachers of the senior age group. At a research of quality of life of teachers the lowest values have been received from the indicators of the general state of health, vital activity, role emotional functioning and mental health. Every second woman-teacher noted high personal uneasiness; every third woman-teacher noted moderate situational uneasiness, confirming the existence of a professional stress. Revealed the interrelation between alarming conditions and a decrease in a mental component of health. Moreover, there was revealed exhaustion signs at low activity values that indicate a high tension of labor process.Keywords: expressiveness of uneasiness, quality of life, psychophysiological status, component of health
Procedia PDF Downloads 2924877 Accelerator Mass Spectrometry Analysis of Isotopes of Plutonium in PM₂.₅
Authors: C. G. Mendez-Garcia, E. T. Romero-Guzman, H. Hernandez-Mendoza, C. Solis, E. Chavez-Lomeli, E. Chamizo, R. Garcia-Tenorio
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Plutonium is present in different concentrations in the environment and biological samples related to nuclear weapons testing, nuclear waste recycling and accidental discharges of nuclear plants. This radioisotope is considered the most radiotoxic substance, particularly when it enters the human body through inhalation of powders insoluble or aerosols. This is the main reason of the determination of the concentration of this radioisotope in the atmosphere. Besides that, the isotopic ratio of ²⁴⁰Pu/²³⁹Pu provides information about the origin of the source. PM₂.₅ sampling was carried out in the Metropolitan Zone of the Valley of Mexico (MZVM) from February 18th to March 17th in 2015 on quartz filter. There have been significant developments recently due to the establishment of new methods for sample preparation and accurate measurement to detect ultra trace levels as the plutonium is found in the environment. The accelerator mass spectrometry (AMS) is a technique that allows measuring levels of detection around of femtograms (10-15 g). The AMS determinations include the chemical isolation of Pu. The Pu separation involved an acidic digestion and a radiochemical purification using an anion exchange resin. Finally, the source is prepared, when Pu is pressed in the corresponding cathodes. According to the author's knowledge on these aerosols showed variations on the ²³⁵U/²³⁸U ratio of the natural value, suggesting that could be an anthropogenic source altering it. The determination of the concentration of the isotopes of Pu can be a useful tool in order the clarify this presence in the atmosphere. The first results showed a mean value of activity concentration of ²³⁹Pu of 280 nBq m⁻³ thus the ²⁴⁰Pu/²³⁹Pu was 0.025 corresponding to the weapon production source; these results corroborate that there is an anthropogenic influence that is increasing the concentration of radioactive material in PM₂.₅. According to the author's knowledge in Total Suspended Particles (TSP) have been reported activity concentrations of ²³⁹⁺²⁴⁰Pu around few tens of nBq m⁻³ and 0.17 of ²⁴⁰Pu/²³⁹Pu ratios. The preliminary results in MZVM show high activity concentrations of isotopes of Pu (40 and 700 nBq m⁻³) and low ²⁴⁰Pu/²³⁹Pu ratio than reported. These results are in the order of the activity concentrations of Pu in weapons-grade of high purity.Keywords: aerosols, fallout, mass spectrometry, radiochemistry, tracer, ²⁴⁰Pu/²³⁹Pu ratio
Procedia PDF Downloads 1674876 Good Marketing is an Important Factor for the Success of the Institution
Authors: Maamar Moumena
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the Follower of the movement of international competition finds that the success of Japanese companies to break into global markets and win a competitive edge and meet the challenges of this competition, due primarily to the adoption of these companies to the modern concept of marketing, and possession of sophisticated marketing systems, with a focus on pricing policy. The institution's ability to produce goods and services be limited unless accompanied by an effective marketing effort. So the satisfaction of the consumer needs efficiently and effectiveness are unwarranted economic and social presence in the market, and ensure the continuity and achieve their goals, and this can only be achieved through marketing activity, where he activity facet which translates the output of the institution and its presence in the form of financial compensation, and that the inclusion of and marketing function within the functions of the institution and awarded each of gravity reflects the extent of their importance in the conduct of the future of the institution, and depending on excellence in performance and a good application of the basic concepts of marketing and primarily make the consumer focus of attention, so the pleasing of the consumer and earn his allegiance reflects the success of an organization.Keywords: competition, marketing, institution, consumer
Procedia PDF Downloads 2824875 Synthesis, Characterization and Antibacterial Screening of 3-Hydroxy-2-[3-(2/3/4-Methoxybenzoyl)Thioureido]Butyric Acid
Authors: M. S. M. Yusof, R. Ramli, S. K. C. Soh, N. Ismail, N. Ngah
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This study presents the synthesis of a series of methoxybenzoylthiourea amino acid derivatives. The compounds were obtained from the reactions between 2/3/4-methoxybenzoyl isothiocyanate with threonine. All of the compounds were characterized via mass spectrometry, 1H and 13C NMR spectrometry, UV-Vis spectrophotometer and FT-IR spectroscopy. Mass spectra for all of the compounds showed the presence of molecular ion [M]+ peaks at m/z 312, which are in agreement to the calculated molecular weight. For 1H NMR spectra, the presence of OCH3, C=S-NH and C=O-NH protons were observed within range of δH 3.8-4.0 ppm, 11.1-11.5 ppm and 10.0-11.5 ppm, respectively. 13C NMR spectra in all compounds displayed the presence of OCH3, C=O-NH, C=O-OH and C=S carbon resonances within range of δC 55.0-57.0 ppm, 165.0-168.0 ppm, 170.0-171.0 ppm and 180.0-182.0 ppm, respectively. In UV spectra, two absorption bands have been observed and both were assigned to the n-π* and π-π* transitions. Six vibrational modes of v(N-H), v(O-H), v(C=O-OH), v(C=O-NH), v(C=C) aromatic and v(C=S) appeared in the FT-IR spectra within the range of 3241-3467 cm-1, 2976-3302 cm-1, 1720-1768 cm-1, 1655-1672 cm-1, 1519-1525 cm-1 and 754-763 cm-1, respectively. The antibacterial activity for all of the compounds was screened against Staphylococcus aureus, Staphylococcus epidermidis, Salmonella typhimurium and Escherichia coli. However, no activity was observed.Keywords: methoxybenzoyl isothiocyanate, amino acid, threonine, antibacterial
Procedia PDF Downloads 3324874 Hepatoprotective Assessment of L-Ascorbate 1-(2-Hydroxyethyl)-4,6-Dimethyl-1, 2-Dihydropyrimidine-2-On Exposure to Carbon Tetrachloride
Authors: Nail Nazarov, Alexandra Vyshtakalyuk, Vyacheslav Semenov, Irina Galyametdinova, Vladimir Zobov, Vladimir Reznik
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Among hepatic pyrimidine used as a means of stimulating protein synthesis and recovery of liver cells in her damaged toxic and infectious etiology. When an experimental toxic hepatitis hepatoprotective activity detected some pyrimidine derivatives. There are literature data on oksimetiluratcila hepatoprotective effect. For analogs of pyrimidine nucleobases - drugs Methyluracilum pentoxy and hepatoprotective effect of weakly expressed. According to the American scientists broad spectrum of biological activity, including hepatoprotective properties, have a 2,4-dioxo-5-arilidenimino uracils. Influenced Xymedon medicinal preparation (1- (beta-hydroxyethyl) -4,6-dimethyl-1,2-dihydro-2-oksopirimidin) developed as a means of stimulating the regeneration of tissue revealed increased activity of microsomal oxidases human liver. In studies on the model of toxic liver damage in rats have shown hepatoprotective effect xymedon and stimulating its impact on the recovery of the liver tissue. Hepatoprotective properties of the new compound in the series of pyrimidine derivatives L-ascorbate 1-(2-hydroxyethyl)-4,6-dimethyl-1,2-dihydropirimidine-2-one synthesized on the basis Xymedon preparation were firstly investigated on rats under the carbon tetrachloride action. It was shown the differences of biochemical parameters from the reference value and severity of structural-morphological liver violations decreased in comparison with control group under the influence of the compound injected before exposure carbon tetrachloride. Hepatoprotective properties of the investigated compound were more pronounced in comparison with Xymedon.Keywords: hepatoprotectors, pyrimidine derivatives, toxic liver damage, xymedon
Procedia PDF Downloads 4254873 A Ti₃C₂O₂ Supported Single Atom, Trifunctional Catalyst for Electrochemical Reactions
Authors: Zhanzhao Fu, Chongyi Ling, Jinlan Wang
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Water splitting and rechargeable air-based batteries are emerging as new renewable energy storage and conversion technologies. However, the discovery of suitable catalysts with high activity and low cost remains a great challenge. In this work, we report a single-atom trifunctional catalyst, namely Ti₃C₂O₂ supported single Pd atom (Pd1@Ti₃C₂O₂), for the hydrogen evolution reaction (HER), oxygen evolution reaction (OER) and oxygen reduction reaction (ORR). This catalyst is selected from 12 candidates and possesses low overpotentials of 0.22 V, 0.31 V and 0.34 V for the HER, OER and ORR, respectively, making it an excellent electrocatalyst for both overall water splitting and rechargeable air-based batteries. The superior OER and ORR performance originates from the optimal d band center of the supported Pd atom. Moreover, the excellent activity can be maintained even if the single Pd atoms aggregate into small clusters. This work offers new opportunities for advancing the renewable energy storage and conversion technologies and paves a new way for the development of multifunctional electrocatalysts.Keywords: DFT, SACs, OER, ORR, HER
Procedia PDF Downloads 764872 Autonomic Nervous System Changes Associated with Rheumatoid Arthritis: Clinical and Electrophysiological Study
Authors: Emmanuel Kamal Aziz Saba, Hussein Al-Moghazy Sultan
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The aim of this study was to evaluate clinically and electro physiologically the autonomic nervous system changes associated with rheumatoid arthritis (RA). The present study included 25 patients with RA [22 women (88%)] and 30 apparently healthy control subjects [27 women (90%)]. A thorough clinical examination was carried out. Disease activity and functional disability were assessed. Tests for assessment of autonomic functions include active and passive orthostatic stress tests, and sympathetic skin response (SSR). The presence of abnormality in 2 tests or more was a clue for the presence of autonomic neuropathy (AN). Sural sensory nerve conduction study and posterior tibial motor nerve conduction study were done. There was a statistically significant decrease in standing systolic and diastolic blood pressure (BP) components of the active orthostatic stress test and SSR amplitude as well as statistically significant prolongation of SSR latency of RA patients when compared to control. Three patients (12%) had clinical symptoms suggestive of AN; increased to 14 patients (56 %) when orthostatic stress tests and SSR were utilized. There were no statistically significant differences between patients with different disease activity score 28 with 4 variables grades of RA activity and SSR latency and amplitude. There were no statistically significant differences between patients with different Stanford Health Assessment Questionnaire Disability Index grades of RA functional disability and SSR latency and amplitude. In conclusion, autonomic neuropathy is a common extra-articular manifestation of RA affecting sympathetic and parasympathetic fibers.Keywords: autonomic neuropathy, orthostatic stress test, rheumatoid arthritis, sympathetic skin response
Procedia PDF Downloads 3594871 Time Driven Activity Based Costing Capability to Improve Logistics Performance: Application in Manufacturing Context
Authors: Siham Rahoui, Amr Mahfouz, Amr Arisha
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In a highly competitive environment characterised by uncertainty and disruptions, such as the recent COVID-19 outbreak, supply chains (SC) face the challenge of maintaining their cost at minimum levels while continuing to provide customers with high-quality products and services. More importantly, businesses in such an economic context strive to maintain survival by keeping the cost of undertaken activities (such as logistics) low and in-house. To do so, managers need to understand the costs associated with different products and services in order to have a clear vision of the SC performance, maintain profitability levels, and make strategic decisions. In this context, SC literature explored different costing models that sought to determine the costs of undertaking supply chain-related activities. While some cost accounting techniques have been extensively explored in the SC context, more contributions are needed to explore the potential of time driven activity-based costing (TDABC). More specifically, more applications are needed in the manufacturing context of the SC, where the debate is ongoing. The aim of the study is to assess the capability of the technique to assess the operational performance of the logistics function. Through a case study methodology applied to a manufacturing company operating in the automotive industry, TDABC evaluates the efficiency of the current configuration and its logistics processes. The study shows that monitoring the process efficiency and cost efficiency leads to strategic decisions that contributed to improve the overall efficiency of the logistics processes.Keywords: efficiency, operational performance, supply chain costing, time driven activity based costing
Procedia PDF Downloads 1654870 Recovery of an Area Degraded by Gullies in the Municipality of Monte Alto (SP), Brazil
Authors: Layane Sara Vieira, Paulo Egidio Bernardo, Roberto Saverio Souza Costa
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Anthropogenic occupations and agricultural explorations without concern for the preservation and sustainability of the activity result in soil degradation that can make rural activity unfeasible. The objective of this work was to characterize and evaluate the recovery costs of an area degraded by major erosion (gully) in the municipality of Monte Alto (SP). Topographic characterization was carried out by means of a planialtimetric survey with a total station. The contours of the gully, internal area, slope height, contribution area, volume, and costs of operations for the recovery of the gully were delimited. The results obtained showed that the gully has a length of 145.56 m, a maximum width of 36.61 m, and a gap of 19.48 m. The external area of the gully is 1,039.8741 m², and the internal area is 119.3470 m². The calculated volume was 3,282.63 m³. The intervention area for breaking slopes was measured at 8,471.29 m², requiring the construction of 19 terraces in this area, vertically spaced at 2.8 m. The estimated costs for mechanical recovery of the gully were R$ 19,167.84 (US$ 3.657,98).Keywords: erosion, volumetric assessment, soil degradation, terraces
Procedia PDF Downloads 1064869 Nanocomposite Metal Material: Study of Antimicrobial and Catalytic Properties
Authors: Roman J. Jedrzejczyk, Damian K. Chlebda, Anna Dziedzicka, Rafal Wazny, Agnieszka Domka, Maciej Sitarz, Przemyslaw J. Jodlowski
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The aim of this study was to obtain antimicrobial material based on thin zirconium dioxide coatings on structured reactors doped with metal nanoparticles using the sonochemical sol-gel method. As a result, dense, uniform zirconium dioxide films were obtained on the kanthal sheets which can be used as support materials in antimicrobial converters with sophisticated shapes. The material was characterised by physicochemical methods, such as AFM, SEM, EDX, XRF, XRD, XPS and in situ Raman and DRIFT spectroscopy. In terms of antimicrobial activity, the material was tested by ATP/AMP method using model microbes isolated from the real systems. The results show that the material can be potentially used in the market as a good candidate for active package and as active bulkheads of climatic systems. The mechanical tests showed that the developed method is an efficient way to obtain durable converters with high antimicrobial activity against fungi and bacteria.Keywords: antimicrobial properties, kanthal steel, nanocomposite, zirconium oxide
Procedia PDF Downloads 2014868 Constraint-Directed Techniques for Transport Scheduling with Capacity Restrictions of Automotive Manufacturing Components
Authors: Martha Ndeley, John Ikome
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In this paper, we expand the scope of constraint-directed techniques to deal with the case of transportation schedule with capacity restrictions where the scheduling problem includes alternative activities. That is, not only does the scheduling problem consist of determining when an activity is to be executed, but also determining which set of alternative activities is to be executed at all level of transportation from input to output. Such problems encompass both alternative resource problems and alternative process plan problems. We formulate a constraint-based representation of alternative activities to model problems containing such choices. We then extend existing constraint-directed scheduling heuristic commitment techniques and propagators to reason directly about the fact that an activity does not necessarily have to exist in a final transportation schedule without being completed. Tentative results show that an algorithm using a novel texture-based heuristic commitment technique propagators achieves the best overall performance of the techniques tested.Keywords: production, transportation, scheduling, integrated
Procedia PDF Downloads 3624867 Screening of Antiviral Compounds in Medicinal Plants: Non-Volatiles
Authors: Tomas Drevinskas, Ruta Mickiene, Audrius Maruska, Nicola Tiso, Algirdas Salomskas, Raimundas Lelesius, Agneta Karpovaite, Ona Ragazinskiene, Loreta Kubiliene
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Antiviral effect of substances accumulated by plants and natural products is known to ethno-pharmacy and modern day medicine. Antiviral properties are usually assigned to volatile compounds and polyphenols. This research work is divided into several parts and the task of this part was to investigate potential plants, potential substances and potential preparation conditions that can be used for the preparation of antiviral agents. Sixteen different medicinal plants, their parts and two types of propolis were selected for screening. Firstly, extraction conditions of non-volatile compounds were investigated: 3 pre-selected plants were extracted with 5 different ethanol – water mixtures (96%, 75%, 60%, 40%, 20 %, vol.) and bidistilled water. Total phenolic content, total flavonoid content and radical scavenging activity was determined. The results indicated that optimal extrahent is 40%, vol. of ethanol – water mixture. Further investigations were performed with the extrahent of 40%, vol. ethanol – water mixture. All 16 of selected plants, their parts and two types of propolis were extracted using selected extrahent. Determined total phenolic content, total flavonoid content and radical scavenging activity indicated that extracts of Origanum Vulgare L., Mentha piperita L., Geranium macrorrhizum L., Melissa officinalis L. and Desmodium canadence L. contains highest amount of extractable phenolic compounds (7.31, 5.48, 7.88, 8.02 and 7.16 rutin equivalents (mg/ ml) respectively), flavonoid content (2.14, 2.23, 2.49, 0.79 and 1.51 rutin equivalents (mg/ml) respectively) and radical scavenging activity (11.98, 8.72, 13.47, 13.22 and 12.22 rutin equivalents (mg/ml) respectively). Composition of the extracts is analyzed using HPLC.Keywords: antiviral effect, plants, propolis, phenols
Procedia PDF Downloads 3244866 Synthesis, Characterization and Cytotoxic Effect of Eu2O3-doped ZnO Nanostructures
Authors: Otilia R. Vasile, Florina C. Ilie, Irina F. Nicoara, Cristina D. Ghitulica, Roxana Trusca, Ovidiu Oprea, Vasile A. Surdu, Bogdan S. Vasile, Ecaterina Adronescu
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In this work ZnO nanostructures (nanopowders and nanostars) have been synthesized via a simple sol-gel method. The used methods for synthesizing the nanostructures involve two steps as follows: (1) precipitation of zinc acetate precursor for the synthesis of ZnO nanopowders and zinc chloride precursor for the synthesis of ZnO nanostars and (2) addition of Eu2O3 in different concentrations (1%, 3%, and 5%) using europium acetate as precursor. Detailed crystalline parameters for each of the synthetized species were analysed using X-ray diffraction. Structural transitions were also discussed. The structure and morphology of the as-prepared ZnO nanopowders and nanostars were investigated by electron microscopy. TEM investigations have shown an average particle size range from 23 to 29 nm and polyhedral and spherical morphology with tendency to form aggregates for nanopowders. For nanostars structures, a star-like morphology could be observed. Cytotoxicity tests on MG-63 cell lines were also performed. Photocatalytic activity of ZnO nanopowders have reached higher values compared to ZnO nanostars.Keywords: cytotoxicity, photocatalytic activity, TEM, ZnO
Procedia PDF Downloads 5614865 Influence of Pine Wood Ash as Pozzolanic Material on Compressive Strength of a Concrete
Authors: M. I. Nicolas, J. C. Cruz, Ysmael Verde, A.Yeladaqui-Tello
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The manufacture of Portland cement has revolutionized the construction industry since the nineteenth century; however, the high cost and large amount of energy required on its manufacturing encouraged, from the seventies, the search of alternative materials to replace it partially or completely. Among the materials studied to replace the cement are the ashes. In the city of Chetumal, south of the Yucatan Peninsula in Mexico, there are no natural sources of pozzolanic ash. In the present study, the cementitious properties of artificial ash resulting from the combustion of waste pine wood were analyzed. The ash obtained was sieved through the screen and No.200 a fraction was analyzed using the technique of X-ray diffraction; with the aim of identifying the crystalline phases and particle sizes of pozzolanic material by the Debye-Scherrer equation. From the characterization of materials, mixtures for a concrete of f'c = 250 kg / cm2 were designed with the method ACI 211.1; for the pattern mixture and for partial replacements of Portland cement by 5%, 10% and 12% pine wood ash mixture. Simple resistance to axial compression of specimens prepared with each concrete mixture, at 3, 14 and 28 days of curing was evaluated. Pozzolanic activity was observed in the ash obtained, checking the presence of crystalline silica (SiO2 of 40.24 nm) and alumina (Al2O3 of 35.08 nm). At 28 days of curing, the specimens prepared with a 5% ash, reached a compression resistance 63% higher than design; for specimens with 10% ash, was 45%; and for specimens with 12% ash, only 36%. Compared to Pattern mixture, which after 28 days showed a f'c = 423.13 kg/cm2, the specimens reached only 97%, 86% and 82% of the compression resistance, for mixtures containing 5%, 10% ash and 12% respectively. The pozzolanic activity of pine wood ash influences the compression resistance, which indicates that it can replace up to 12% of Portland cement by ash without compromising its design strength, however, there is a decrease in strength compared to the pattern concrete.Keywords: concrete, pine wood ash, pozzolanic activity, X-ray
Procedia PDF Downloads 4564864 Formulation and Evaluation of Curcumin-Zn (II) Microparticulate Drug Delivery System for Antimalarial Activity
Authors: M. R. Aher, R. B. Laware, G. S. Asane, B. S. Kuchekar
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Objective: Studies have shown that a new combination therapy with Artemisinin derivatives and curcumin is unique, with potential advantages over known ACTs. In present study an attempt was made to prepare microparticulate drug delivery system of Curcumin-Zn complex and evaluate it in combination with artemether for antimalarial activity. Material and method: Curcumin Zn complex was prepared and encapsulated using sodium alginate. Microparticles thus obtained are further coated with various enteric polymers at different coating thickness to control the release. Microparticles are evaluated for encapsulation efficiency, drug loading and in vitro drug release. Roentgenographic Studies was conducted in rabbits with BaSO 4 tagged formulation. Optimized formulation was screened for antimalarial activity using P. berghei-infected mice survival test and % paracetemia inhibition, alone (three oral dose of 5mg/day) and in combination with arthemether (i.p. 500, 1000 and 1500µg). Curcumin-Zn(II) was estimated in serum after oral administration to rats by using spectroflurometry. Result: Microparticles coated with Cellulose acetate phthalate showed most satisfactory and controlled release with 479 min time for 60% drug release. X-ray images taken at different time intervals confirmed the retention of formulation in GI tract. Estimation of curcumin in serum by spectroflurometry showed that drug concentration is maintained in the blood for longer time with tmax of 6 hours. The survival time (40 days post treatment) of mice infected with P. berghei was compared to survival after treatment with either Curcumin-Zn(II) microparticles artemether combination, curcumin-Zn complex and artemether. Oral administration of Curcumin-Zn(II)-artemether prolonged the survival of P.berghei-infected mice. All the mice treated with Curcumin-Zn(II) microparticles (5mg/day) artemether (1000µg) survived for more than 40 days and recovered with no detectable parasitemia. Administration of Curcumin-Zn(II) artemether combination reduced the parasitemia in mice by more than 90% compared to that in control mice for the first 3 days after treatment. Conclusion: Antimalarial activity of the curcumin Zn-artemether combination was more pronounced than mono therapy. A single dose of 1000µg of artemether in curcumin-Zn combination gives complete protection in P. berghei-infected mice. This may reduce the chances of drug resistance in malaria management.Keywords: formulation, microparticulate drug delivery, antimalarial, pharmaceutics
Procedia PDF Downloads 3944863 Facile Fabrication of TiO₂NT/Fe₂O₃@Ag₂CO₃ Nanocomposite and Its Highly Efficient Visible Light Photocatalytic and Antibacterial Activity
Authors: Amal A. Al-Kahlawy, Heba H. El-Maghrabi
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Due to the increasing need to environment protection in real time need to energize new materials are under extensive investigations. Between others, TiO2 nanotubes (TNTs) nanocomposite with iron oxide and silver carbonate, are promising alternatives as high-efficiency visible light photocatalyst due to their unique properties and their superior charge transport properties. Our efforts in this domain aim the construction of novel nanocomposite of TiO2NT/Fe2O3@Ag2CO3. The structure, surface morphology, chemical composition and optical properties were characterized by X-ray diffraction (XRD), Raman, Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), energy dispersive X-ray spectrometer (EDS), transmission electron microscopy (TEM), selected area electron diffraction (SAED) and UV–vis diffuse reflectance spectroscopy (DRS). XRD results confirm the interaction of TiO2-NT with iron oxide. This novel nanocomposite shows remarkably enhanced performance for phenol compounds photodegradation. The experimental data shows a promising photocatalytic activity. In particular, a maximum value of 450 mg/g was removed within 60 min at solar light irradiation with degradation efficiency of 99.5%. The high photocatalytic activity of the nanocomposite is found to be related to the increased adsorption toward chemical species, enhanced light absorption and efficient charge separation and transfer. Finally, the designed TiO2NT/Fe2O3@Ag2CO3 nanocomposite has a great degree of sustainability and could has a potential application for the industrial treatment of wastewater containing toxic organic materials.Keywords: nanocomposite, photocatalyst, solar energy, titanium dioxide nanotubes
Procedia PDF Downloads 2474862 Application of Computational Chemistry for Searching Anticancer Derivatives of 2-Phenazinamines as Bcr-Abl Tyrosine Kinase Inhibitors
Authors: Gajanan M. Sonwane
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The computational studies on 2-phenazinamines with their protein targets have been carried out to design compounds with potential anticancer activity. This strategy of designing compounds possessing selectivity over specific tyrosine kinase has been achieved through G-QSAR and molecular docking studies. The objective of this research has been to design newer 2-phenazinamine derivatives as Bcr-Abl tyrosine kinase inhibitors by G-QSAR, molecular docking studies followed by wet-lab studies along with evaluation of their anticancer potential. Computational chemistry was done by using VLife MDS 4.3 and Autodock 4.2 followed by wet-lab experiments for synthesizing 2-phenazinamine derivatives. The chemical structures of ligands in 2D were drawn by employing Chemdraw 2D Ultra 8.0 and were converted into 3D. These were optimized by using a semi-empirical method called MOPAC. The protein structure was retrieved from RCSC protein data bank as a PDB file. The binding interactions of protein and ligands were done by using PYMOL. The molecular properties of the designed compounds were predicted in silico by using Osiris property explorer. The parent compound 2-phenazinamine was synthesized by reduction of 2, 4-dinitro-N-phenyl-benzenamine in the presence of tin chloride followed by cyclization in the presence of nitrobenzene and magnesium sulfate. The derivatization at the amino function of 2-phenazinamine was performed by treating parent compound with various aldehydes in the presence of dicyclohexylcarbodiimide (DCC) and urea to afford 2-(2-chlorophenyl)-3-(phenazine-2-yl) thiazolidine-4-one. Synthesized 39 novel derivatives of 2-phenazinamine and performed antioxidant activity, anti antiproliferative on the bulb of onion and anticancer activity on cell line showing significant competition with marked blockbuster drug imatinib.Keywords: computer-aided drug design, tyrosin kinases, anticancer, docking
Procedia PDF Downloads 1404861 Protective Effect of the Histamine H3 Receptor Antagonist DL77 in Behavioral Cognitive Deficits Associated with Schizophrenia
Authors: B. Sadek, N. Khan, D. Łażewska, K. Kieć-Kononowicz
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The effects of the non-imidazole histamine H3 receptor (H3R) antagonist DL77 in passive avoidance paradigm (PAP) and novel object recognition (NOR) task in MK801-induced cognitive deficits associated with schizophrenia (CDS) in adult male rats, and applying donepezil (DOZ) as a reference drug were investigated. The results show that acute systemic administration of DL77 (2.5, 5, and 10 mg/kg, i.p.) significantly improved MK801-induced (0.1 mg/kg, i.p.) memory deficits in PAP. The ameliorating activity of DL77 (5 mg/kg, i.p.) in MK801-induced deficits was partly reversed when rats were pretreated with the centrally-acting H2R antagonist zolantidine (ZOL, 10 mg/kg, i.p.) or with the antimuscarinic antagonist scopolamine (SCO, 0.1 mg/kg, i.p.), but not with the CNS penetrant H1R antagonist pyrilamine (PYR, 10 mg/kg, i.p.). Moreover, the memory enhancing effect of DL77 (5 mg/kg, i.p.) in MK801-induced memory deficits in PAP was strongly reversed when rats were pretreated with a combination of ZOL (10 mg/kg, i.p.) and SCO (1.0 mg/kg, i.p.). Furthermore, the significant ameliorative effect of DL77 (5 mg/kg, i.p.) on MK801-induced long-term memory (LTM) impairment in NOR test was comparable to the DOZ-provided memory-enhancing effect, and was abrogated when animals were pretreated with the histamine H3R agonist R-(α)-methylhistamine (RAMH, 10 mg/kg, i.p.). However, DL77(5 mg/kg, i.p.) failed to provide procognitive effect on MK801-induced short-term memory (STM) impairment in NOR test. In addition, DL77 (5 mg/kg) did not alter anxiety levels and locomotor activity of animals naive to elevated-plus maze (EPM), demonstrating that improved performances with DL77 (5 mg/kg) in PAP or NOR are unrelated to changes in emotional responding or spontaneous locomotor activity. These results provide evidence for the potential of H3Rs for the treatment of neurodegenerative disorders related to impaired memory function, e.g. CDS.Keywords: histamine H3 receptor, antagonist, learning, memory impairment, passive avoidance paradigm, novel object recognition
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