Search results for: drug reaction with eosinophilia and systemic symptoms

Authors: Abdorrasoul Malekpour, Mohammad Ghorbani Mojtaba Mortazavi, Mohammadreza Fattahi, Mohammad Hassan Meshkibaf, Ali Fakhrzad, Saeid Salehi, Saeideh Zahedi, Amir Ahmadimoghaddam, Parviz Farzadnia Dr., Mohammadreza Hajyani Asl Bs

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Hepatitis B as an infectious disease has eight main genotypes (A–H). The aim of this study is to Bioinformatically identify Rare Codon Clusters (RCC) in proteins structure of HBV. For detection of protein family accession numbers (Pfam) of HBV proteins; used of uni-prot database and Pfam search tool were used. Obtained Pfam IDs were analyzed in Sherlocc program and RCCs in HBV proteins were detected. In further, the structures of TrEMBL entries proteins studied in PDB database and 3D structures of the HBV proteins and locations of RCCs were visualized and studied using Swiss PDB Viewer software. Pfam search tool have found nine significant hits and 0 insignificant hits in 3 frames. Results of Pfams studied in the Sherlocc program show this program not identified RCCs in the external core antigen (PF08290) and truncated HBeAg protein (PF08290). By contrast the RCCs become identified in Hepatitis core antigen (PF00906) Large envelope protein S (PF00695), X protein (PF00739), DNA polymerase (viral) N-terminal domain (PF00242) and Protein P (Pf00336). In HBV genome, seven RCC identified that found in hepatitis core antigen, large envelope protein S and DNA polymerase proteins and proteins structures of TrEMBL entries sequences that reported in Sherlocc program outputs are not complete. Based on situation of RCC in structure of HBV proteins, it suggested those RCCs are important in HBV life cycle. We hoped that this study provide a new and deep perspective in protein research and drug design for treatment of HBV.

Keywords: rare codon clusters, hepatitis B virus, bioinformatic study, infectious disease

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Authors: Checkfaith I. Aizebeoje, Temitope O. Lawal, Bolanle A. Adeniyi

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The overuse and abuse of antibiotics in treating zoonotic infections in humans and opportunistic infections in rabbit has contributed to the increase in antimicrobial drug resistance, therefore, an alternative to antibiotics is needed in treating these infections. The study was carried out to determine the antimicrobial activity of lactic acid bacteria (LAB) isolated from rabbit’s faeces against multidrug-resistant (MDR) pathogens isolated from the same rabbit. Twelve faecal samples and twelve swabs from fur samples were randomly collected aseptically from apparently healthy rabbits from Ajibode, Ibadan and University of Ibadan research farm in Ibadan, Oyo state, Nigeria. Lactic acid bacteria and multidrug-resistant pathogens were isolated using appropriate agar media and identified by partial sequencing of the 16SrRNA gene. Antibiotic susceptibility pattern of isolated bacteria and LAB were determined by the agar diffusion method. The antibacterial activity of the LAB against the test pathogens was determined using the agar overlay and agar diffusion methods. The pathogens Myroides gitamensis, Citrobacter rodentium, Acinetobacter johnsonii, Enterobacter oryzendophyticus and Serratia marcescens as well as twenty-eight (28) species of LAB belonging to Acetobacter and Lactobacillus genera were identified and characterized. Lactobacillus plantarum had the highest (60.71%) occurrence of the LAB. Viable cells and cell free supernatant (CFS) of isolated LAB inhibited the growth of the test organisms with the largest zone of inhibition (40 mm) produced by Lactobacillus plantarum against Citrobacter rodentium. This study showed that LAB from rabbit possess considerable antibacterial activity against multidrug-resistant bacteria from the same environment.

Keywords: antibacterial activities, cell-free supernatant, lactic acid bacteria; multidrug-resistant pathogens, rabbits’ faeces

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Authors: Rauza Sukma Rita, Katsuya Dezaki, Yuko Maejima, Toshihiko Yada

Abstract:

Oxytocin is a nine-amino acid peptide synthesized in the paraventricular nucleus (PVN) and supraoptic nucleus (SON) of the hypothalamus. Oxytocin promotes contraction of the uterus during birth and milk ejection during breast feeding. Although oxytocin receptors are found predominantly in the breasts and uterus of females, many tissues and organs express oxytocin receptors, including the pituitary, heart, kidney, thymus, vascular endothelium, adipocytes, osteoblasts, adrenal gland, pancreatic islets, and many cell lines. On the other hand, in pancreatic islets, oxytocin receptors are expressed in both α-cells and β-cells with stronger expression in α- cells. However, to our knowledge there are no reports yet about the effect of oxytocin on cytosolic calcium reaction on α and β-cell. This study aims to investigate the effect of oxytocin on α-cells and β-cells and its oscillation pattern. Islet of Langerhans from wild type mice were isolated by collagenase digestion. Isolated and dissociated single cells either α-cells or β-cells on coverslips were mounted in an open chamber and superfused in HKRB. Cytosolic concentration ([Ca2+]i) in single cells were measured by fura-2 microfluorimetry. After measurement of [Ca2+]i, α-cells were identified by subsequent immunocytochemical staining using an anti-glucagon antiserum. In β-cells, the [Ca2+]i increase in response to oxytocin was observed only under 8.3 mM glucose condition, whereas in α-cells, [Ca2+]i an increase induced by oxytocin was observed in both 2.8 mM and 8.3 mM glucose. The oscillation incidence was induced more frequently in β-cells compared to α-cells. In conclusion, the present study demonstrated that oxytocin directly interacts with both α-cells and β-cells and induces increase of [Ca2+]i and its specific patterns.

Keywords: α-cells, β-cells, cytosolic calcium concentration, oscillation, oxytocin

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Authors: M. Ardelean, F. Manea, A. Pop, J. Schoonman

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The presence of pharmaceuticals in the environment and especially in water has gained increasing attention. They are included in emerging class of pollutants, and for most of them, legal limits have not been set-up due to their impact on human health and ecosystem was not determined and/or there is not the advanced analytical method for their quantification. In this context, the development of various advanced analytical methods for the quantification of pharmaceuticals in water is required. The electrochemical methods are known to exhibit the great potential for high-performance analytical methods but their performance is in direct relation to the electrode material and the operating techniques. In this study, two types of carbon-based electrodes materials, i.e., boron-doped diamond (BDD) and carbon nanofiber (CNF)-epoxy composite electrodes have been investigated through voltammetric techniques for the detection of naproxen in water. The comparative electrochemical behavior of naproxen (NPX) on both BDD and CNF electrodes was studied by cyclic voltammetry, and the well-defined peak corresponding to NPX oxidation was found for each electrode. NPX oxidation occurred on BDD electrode at the potential value of about +1.4 V/SCE (saturated calomel electrode) and at about +1.2 V/SCE for CNF electrode. The sensitivities for NPX detection were similar for both carbon-based electrode and thus, CNF electrode exhibited superiority in relation to the detection potential. Differential-pulsed voltammetry (DPV) and square-wave voltammetry (SWV) techniques were exploited to improve the electroanalytical performance for the NPX detection, and the best results related to the sensitivity of 9.959 µA·µM^-1 were achieved using DPV. In addition, the simultaneous detection of NPX and fluoxetine -a very common antidepressive drug, also present in water, was studied using CNF electrode and very good results were obtained. The detection potential values that allowed a good separation of the detection signals together with the good sensitivities were appropriate for the simultaneous detection of both tested pharmaceuticals. These results reclaim CNF electrode as a valuable tool for the individual/simultaneous detection of pharmaceuticals in water.

Keywords: boron-doped diamond electrode, carbon nanofiber-epoxy composite electrode, emerging pollutans, pharmaceuticals

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Authors: Chettyparambil Lalchand Thejalakshmi, Sonal Sabu Edattukaran

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Hair loss is one of the main issues that contemporary society is dealing with. It can be attributable to a wide range of factors, listing from one's genetic composition and the anxiety we experience on a daily basis. Telogen effluvium [TE] is a condition that causes temporary hair loss after a stressor that might shock the body and cause the hair follicles to temporarily rest, leading to hair loss. Most frequently, women are the ones who bring up these difficulties. Extreme illness or trauma, an emotional or important life event, rapid weight loss and crash dieting, a severe scalp skin problem, a new medication, or ceasing hormone therapy are examples of potential causes. Men frequently do not notice hair thinning with time, but women with long hair may be easily identified when shedding, which can occasionally result in bias because women tend to be more concerned with aesthetics and beauty standards of the society, and approach frequently with the concerns .The woman, who formerly possessed a full head of hair, is worried about the hair loss from her scalp . There are several cases of hair loss reported every day, and Telogen effluvium is said to be the most prevalent one of them all without any hereditary risk factors. While the patient has loss in hair volume, baldness is not the result of this problem . The exponentially growing Dermatology and Aesthetic medical division has discovered that this problem is the most common and also the easiest to cure since it is feasible for these people to regrow their hair, unlike those who have scarring alopecia, in which the follicle itself is damaged and non-viable. Telogen effluvium comes in two different forms: acute and chronic. Acute TE occurs in all the age groups with a hair loss of less than three months, while chronic TE is more common in those between the ages of 30 and 60 with a hair loss of more than six months . Both kinds are prevalent throughout all age groups, regardless of the predominance. It takes between three and six months for the lost hair to come back, although this condition is readily reversed by eliminating stresses. After shedding their hair, patients frequently describe having noticeable fringes on their forehead. The current medical treatments for this condition include topical corticosteroids, systemic corticosteroids, minoxidil and finasteride, CNDPA (caffeine, niacinamide, panthenol, dimethicone, and an acrylate polymer) .Individual terminal hair growth was increased by 10% as a result of the innovative intervention CNDPA. Botulinum Toxin A, Scalp Micro Needling, Platelet Rich Plasma Therapy [PRP], and sessions with Multivitamin Mesotherapy Injections are some recently enhanced techniques with partially or completely reversible hair loss. Also, it has been shown that supplements like Nutrafol and Biotin are producing effective outcomes. There is virtually little evidence to support the claim that applying sulfur-rich ingredients to the scalp, such as onion juice, can help TE patients' hair regenerate.

Keywords: dermatology, telogen effluvium, hair loss, modern hair loass treatments

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Authors: Shwadhin Sharma

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As there has been increasing focus on the shorter attention span of the millennials students, there is a relative absence of instructional tools on behavioral assessments in learning information technology skills within the information systems field and textbooks. This study uses project-based learning in which students gain knowledge and skills related to information technology by working on an extended project that allows students to find a real business problem design information systems based on information collected from the company and develop an information system that solves the problem of the company. Eighty students from two sections of the same course engage in the project from the first week of the class till the sixteenth week of the class to deliver a small business information system that allows them to employ all the skills and knowledge that they learned in the class into the systems they are creating. Computer Information Systems related courses are often difficult to understand and process especially for the Under Representative Minorities students who have limited computer or information systems related (academic) experiences. Project-based learning demands constant attention of the students and forces them to apply knowledge learned in the class to a project that helps retaining knowledge. To make sure our assumption is correct, we started with a pre-test and post-test to test the students learning (of skills) based on the project. Our test showed that almost 90% of the students from the two sections scored higher in post-test as compared to pre-test. Based on this premise, we conducted a further survey that measured student’s job-search preparation, knowledge of data analysis, involved with the course, satisfaction with the course, student’s overall reaction the course and students' ability to meet the traditional learning goals related to the course.

Keywords: project-based learning, job-search preparation, satisfaction with course, traditional learning goals

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Authors: Ashirgul Kozhagulova, Ainash Shabdirova, Galym Tokazhanov, Minh Nguyen

Abstract:

The synthetic rocks have been advantageous over the natural rocks in terms of availability and the consistent studying the impact of a particular parameter. The artificial rocks can be fabricated using variety of techniques such as mixing sand and Portland cement or gypsum, firing the mixture of sand and fine powder of borosilicate glass or by in-situ precipitation of calcite solution. In this study, sodium silicate solution has been used as the cementing agent for the quartz sand. The molded soft cylindrical sandstone samples are placed in the gas-tight pressure vessel, where the hardening of the material takes place as the chemical reaction between carbon dioxide and the silicate solution progresses. The vessel allows uniform disperse of carbon dioxide and control over the ambient gas pressure. Current paper shows how the bonding material is initially distributed in the intergranular space and the surface of the sand particles by the usage of Electron Microscopy and the Energy Dispersive Spectroscopy. During the study, the strength of the cement bond as a function of temperature is observed. The impact of cementing agent dosage on the micro and macro characteristics of the sandstone is investigated. The analysis of the cement bond at micro level helps to trace the changes to particles bonding damage after a potential yielding. Shearing behavior and compressional response have been examined resulting in the estimation of the shearing resistance and cohesion force of the sandstone. These are considered to be main input values to the mathematical prediction models of sand production from weak clastic oil reservoir formations.

Keywords: artificial sanstone, cement bond, microstructure, SEM, triaxial shearing

Procedia PDF Downloads 159

Authors: Zinhle Cindi, Collet Dandara, Mpiko Ntsekhe, Edson Makambwa, Miguel Larceda

Abstract:

Background: Warfarin is the most commonly used drug in the management of thromboembolic disease. However, there is a huge variability in the time, number of doses or starting doses for patients to achieve the required international normalised ratio (INR) which is compounded by a narrow therapeutic index. Many genetic-association studies have reported on European and Asian populations which have led to the designing of specific algorithms that are now being used to assist in warfarin dosing. However, very few or no studies have looked at the pharmacogenetics of warfarin in African populations, yet, huge differences in dosage requirements to reach the same INR have been observed. Objective: We set out to investigate the distribution of 3 SNPs CYP4F2 c.1347C > T, VKORC1 g.-1639G > A and VKORC1 c.1173C > T among South African Mixed Ancestry (MA) and Black African patients. Methods: DNA was extracted from 383 participants and subsequently genotyped using PCR/RFLP for the CYP4F2 c.1347 (V433M) (rs2108622), VKORC1 g.-1639 (rs9923231) and VKORC1 c.1173 (rs9934438) SNPs. Results: Comparing the Black and MA groups, significant differences were observed in the distribution of the following genotypes; CYP4F2 c.1347C/T (23% vs. 39% p=0.03). All VKORC1 g.-1639G > A genotypes (p < 0.006) and all VKORC1 c.1173C > T genotypes (p < 0.007). Conclusion: CYP4F2 c.1347T (V433M) reduces CYP4F2 protein levels and therefore expected to affect the amount of warfarin needed to block vitamin k recycling. The VKORC1 g-1639A variant alters transcriptional regulation therefore affecting the function of vitamin k epoxide reductase in vitamin k production. The VKORC1 c.1173T variant reduces the enzyme activity of VKORC1 consequently enhancing the effectiveness of warfarin. These are preliminary results; more genetic characterization is required to understand all the genetic determinants affecting how patients respond to warfarin.

Keywords: algorithms, pharmacogenetics, thromboembolic disease, warfarin

Procedia PDF Downloads 248

Authors: Devadrita Dey Sarkar

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Oxidosqualene cyclase is a membrane bound enzyme in which helps in the formation of steroid scaffold in higher organisms. In a highly selective cyclization reaction oxidosqualene cyclase forms LANOSTEROL with seven chiral centres starting from the linear substrate 2,3-oxidosqualene. In humans OSC in cholesterol biosynthesis it represents a target for the discovery of novel anticholesteraemic drugs that could complement the widely used statins. The enzyme oxidosqualene: lanosterol cyclase (OSC) represents a novel target for the treatment of hypercholesterolemia. OSC catalyzes the cyclization of the linear 2,3-monoepoxysqualene to lanosterol, the initial four-ringed sterol intermediate in the cholesterol biosynthetic pathway. OSC also catalyzes the formation of 24(S), 25-epoxycholesterol, a ligand activator of the liver X receptor. Inhibition of OSC reduces cholesterol biosynthesis and selectively enhances 24(S),25-epoxycholesterol synthesis. Through this dual mechanism, OSC inhibition decreases plasma levels of low-density lipoprotein (LDL)-cholesterol and prevents cholesterol deposition within macrophages. The recent crystallization of OSC identifies the mechanism of action for this complex enzyme, setting the stage for the design of OSC inhibitors with improved pharmacological properties for cholesterol lowering and treatment of atherosclerosis. While studying and designing the inhibitor of oxidosqulene cyclase, I worked on the pdb id of 1w6k which was the most worked on pdb id and I used several methods, techniques and softwares to identify and validate the top most molecules which could be acting as an inhibitor for oxidosqualene cyclase. Thus, by partial blockage of this enzyme, both an inhibition of lanosterol and subsequently cholesterol formation as well as a concomitant effect on HMG-CoA reductase can be achieved. Both effects complement each other and lead to an effective control of cholesterol biosynthesis. It is therefore concluded that 2,3-oxidosqualene cyclase plays a crucial role in the regulation of intracellular cholesterol homeostasis. 2,3-Oxidosqualene cyclase inhibitors offer an attractive approach for novel lipid-lowering agents.

Keywords: anticholesteraemic, crystallization, statins, homeostasis

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Authors: H. Shamoradifar, B. Teimuri, P. Parvaresh, S. Mohammadi

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One of the main characteristics of Heavy Water Moderated Reactors is their high production of plutonium. This article demonstrates the possibility of reduction of plutonium and other actinides in Heavy Water Research Reactor. Among the many ways for reducing plutonium production in a heavy water reactor, in this research, changing the fuel from natural Uranium fuel to Thorium-Uranium mixed fuel was focused. The main fissile nucleus in Thorium-Uranium fuels is U-233 which would be produced after neutron absorption by Th-232, so the Thorium-Uranium fuels have some known advantages compared to the Uranium fuels. Due to this fact, four Thorium-Uranium fuels with different compositions ratios were chosen in our simulations; a) 10% UO₂-90% THO₂ (enriched= 20%); b) 15% UO₂-85% THO₂ (enriched= 10%); c) 30% UO₂-70% THO₂ (enriched= 5%); d) 35% UO₂-65% THO₂ (enriched= 3.7%). The natural Uranium Oxide (UO₂) is considered as the reference fuel, in other words all of the calculated data are compared with the related data from Uranium fuel. Neutronic parameters were calculated and used as the comparison parameters. All calculations were performed by Monte Carol (MCNPX2.6) steady state reaction rate calculation linked to a deterministic depletion calculation (CINDER90). The obtained computational data showed that Thorium-Uranium fuels with four different fissile compositions ratios can satisfy the safety and operating requirements for Heavy Water Research Reactor. Furthermore, Thorium-Uranium fuels have a very good proliferation resistance and consume less fissile material than uranium fuels at the same reactor operation time. Using mixed Thorium-Uranium fuels reduced the long-lived α emitter, high radiotoxic wastes and the radio toxicity level of spent fuel.

Keywords: Heavy Water Reactor, Burn up, Minor Actinides, Neutronic Calculation

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Authors: Joana Gato, Ahmed Abotabekh, Panayoti Bachkangi

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Introduction: Oestrogen is an essential gonadal hormone that plays a vital role in the reproductive system of women1. The average age of menopause in the UK is 512. Women who go through premature menopause should be offered Hormone replacement therapy (HRT). Similarly, women who undergo surgical menopause should be offered HRT, unless contraindicated, depending on the indication of their surgery2,3. Aim: To assess if the patients in our department are counselled regarding HRT after surgical treatment and if HRT was prescribed. Methodology: A retrospective audit in a busy district hospital, examining all the patients who had a hysterectomy. The audit examined if HRT was discussed pre-operatively, prescribed on discharge and if a follow up was arranged. For women with contraindication to HRT, the audit assessed if the reasons were discussed pre-operatively and communicated to the Inclusion criteria: woman having a total or subtotal hysterectomy, with or without bilateral salpingo-ophorectomy (BSO), between April and September 2022. Exclusion criteria: woman having a vaginal hysterectomy. Results: 40 patients in total had hysterectomy; 27 (68%) were under the age of 51. 15 out of 27 patients bad BSO. 9 women were prescribed HRT, but 8 were offered HRT immediately, and 1 of them were offered a follow up. Of women who underwent surgical menopause, 7 were not given any HRT. The HRT choice was diverse, however, the majority was prescribed oral HRT. 40% of women undergoing surgical menopause did not have a discussion about HRT prior to their surgery. In postmenopausal women (n=13; 33%), still two were given HRT for preexisting menopausal symptoms. Discussion: Only 59% of the pre-menopausal patients had oophorectomy, therefore undergoing surgical menopause. Of these, 44% were not given any HRT, and 40% had no discussion about HRT prior to surgery. Interestingly, the majority of these women have no obvious contraindication to HRT. The choice of HRT was diverse, but the majority was commenced on oral HRT. Our unit is still working towards meeting all the NICE guidance standards of offering HRT and information prior to surgery to women planning to undergo surgical menopause. Conclusion: Starting HRT at the onset of menopause has been shown to improve quality of life and reduce the risk of cardiovascular disease and osteoporotic fractures4. Our unit still has scope for improvement to comply with the current NICE guidance. All pre-menopausal women undergoing surgical menopause should have a discussion regarding HRT prior to surgery and be offered it if there are no contraindications. This discussion should be clearly documented in the notes. At the time of this report, some of the patients have not yet had a follow up, which we recognize as a limitation to our audit.

Keywords: hormone replacement therapy, menopause, premature ovarian insufficiency, surgical management

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Authors: Sid Ahmed Ziane

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This paper argues for Johnson's financial responsiveness to the rise of Black Power and its advocate, 'Stokely Carmichael' in 1966. John H. Johnson was a Black businessman and the owner of Ebony magazine, one of the widely read Black magazines in the U.S. His magazine, however, was designed only to promoting Black fashion, aesthetic, marketing, and consumerism. In mid-1966, the mainstream of the Civil Rights movement was heading into two distinct camps when some of its advocates, led by Stokely Carmichael, began to question the slow pace of the Civil Rights and sought to pursue a more radical approach to bring about upheaval to the Black community. Their new approach, however, propelled the national media into paying close attention to their activities, their new methods, and their radical orientations. In fact, the major White-oriented media discredited Carmichael and distorted his public image via sensational stories and race-mongering reports. However, the Black owned outlets such as The Liberator advocated his agendas, whereas other magazines such as The Crisis rejected them. Based on such oral sources and Ebony’s online issues, this paper adds and argues that Johnson had also responded to the rise of Black Power and Carmichael. This reaction had, in fact, aimed at scooping and selling Carmichael and his new orientation as well as advertising him in his magazine to attract the readers who showed a strong tendency to hear and read about the heyday and even the ferment of Black Power. This paper is part of an ongoing project which aims at framing our understanding of how the Black print media and the modern Black liberation struggle were correlated and could shape each other by appraising their agendas, milestones, and their pivotal figures.

Keywords: Black power, Ebony magazine, John Johson, Stokely Carmichael

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Authors: Jahangir Ahmad Rather, Emad A. Khudaish, Ahsanulhaq Qurashi, Palanisamy Kannan

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Chemical modification and assembling of fullerenes are fundamentally important for the application of fullerenes as functional molecules and in molecular devices and organic electronic devices. We have synthesized fullerene nanorods C60NRs conjugate via liquid-liquid interface and the synthesized C60NRs was characterized by FTIR spectroscopy, field emission electron microscopy (FESEM) and X-ray diffraction techniques. The C60NRs were immobilized on glassy carbon electrode via surface bound diazonium salts as an impact strategy. This method involves electrografting of p–nitrophenyl to give GCE–Ph–NO2 and then the terminal nitro-group was chemically reduced to GCE–Ph–NH2 in a presence of sodium borohydride/gold–polyaniline nanocomposite (NaBH4/Au–PANI). The Au–PANI composite was synthesized and characterized by FTIR, UV-vis, SEM and EDX techniques. The C60NRs were immobilized on GCE–Ph–NH2 via amination reaction which involves N-H addition across a π-bond on [60] fullerene. The immobilized C60NRs/GCE was subjected to electrochemical reduction in 1.0 M KOH to yield ERC60NRs/GCE sensor. The developed sensor shows high electrocatalytic activity for the detection of ethylparaben (EP) over a concentration range from 0.01 to 0.52 µM with a detection limit (LOD) 3.8 nM. The amount of EP present in the nourishing repair cream (OlAY®) was determined by standard addition method at the developed ERC60NRs/GCE sensor. The total concentration of EP was found to be 0.011 µM (0.1%) and is within the permissible limit of 0.19 % EP in cosmetics according to the European scientific committee (SCCS) on consumer safety on 22 March 2011 (SCCS/1348/11).

Keywords: diazonium salt reduction, ethylparaben (EP), endocrine disruptor, fullerene nanorods (C60NRs), gold–polyaniline nanocomposite (Au–PANI)

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Authors: Tamer M. Shehata

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Objective: Currently, mucoadhesive microparticles acquired a high interest in both research and pharmaceutical technology fields. Recently, BÜCHI lunched its latest fourth generation nano spray dryer B-90 used for nanoparticle production. B-90 offers an elegant technology combined particle engineering and drying in one step. In our laboratory, we successfully developed a new formulation for metformin hydrochloride, mucoadhesive microparticles utilizing B-90 technology for treatment of type 2-diabetis. Method: Gelatin or sodium alginate, natural occurring polymers with mucoadhesive properties, solely or in combination was used in our formulation trials. Preformulation studies (atomization head mesh size, flow rate, head temperature, polymer solution viscosity and surface tension) and postformulation characters (particle size, flowability, surface scan and dissolution profile) were evaluated. Finally, hypoglycemic effect of the selected formula was evaluated in streptozotocin-induced diabetic rats. Spray head with 7 µm hole, flow rate of 3.5 mL/min and head temperature 120 ºC were selected. Polymer viscosity was less than 11.5 cP with surface tension less than 70.1 dyne/cm. Result: Discrete, non aggregated particles and free flowing powders with particle size was less than 2000 nm were obtained. Gelatin and sodium alginate combination in ratio 1:3 were successfully sustained the in vitro release profile of the drug. Hypoglycemic evaluation of the previous formula, showed a significant reduction of blood glucose level over 24 h. Conclusion: B-90 technology can open a new era of , mucoadhesive microparticles preparation offering convenient dosage form that can enhance compliance of type 2 diabetic patients.

Keywords: mucoadhesive, microparticles, technology, diabetis

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Authors: Shahnaz Haque, Anand Shukla, Sunita Singh, Anil Kem

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Introduction: Diabetes Mellitus is a chronic metabolic disease affecting millions worldwide. Metformin is the most commonly prescribed first line oral hypoglycemic drug for type 2 diabetes mellitus, but due to progressive worsening of blood glucose control during the natural history of type 2 diabetes, combination therapy usually becomes necessary. Objective: This study was designed to assess the treatment satisfaction between Sitagliptin versus Pioglitazone added to Metformin in patients with type 2 diabetes mellitus (T2DM). Methods: We conducted a prospective, open label, randomized, parallel group study in SIMS, Hapur, U.P. Eligible patients fulfilling inclusion criteria were randomized into two groups having 25 patients in each group using tab Sitagliptin 100mg, tab Pioglitazone 30mg added to ongoing tab Metformin (500mg) therapy for 16 weeks. The follow-up visits were on weeks 4,12 and 16. Result: 16 weeks later, addition of Sitagliptin 100mg compared to that of Pioglitazone 30 mg to ongoing Metformin therapy provided similar glycosylated hemoglobin (HbA1c) lowering efficacy in patients with T2DM with inadequate glycemic control on metformin monotherapy. Change in HbA1c in group1 was -0.656±0.21%(p<0.0001) whereas in group2 was -0.748±0.35%(p<0.0001). Hence decrease in HbA1c from baseline was more in group2. Both treatments were well tolerated with negligible risk of hypoglycaemia. Weight loss was observed with Sitagliptin in contrast to weight gain seen in Pioglitazone. Conclusion: In this study, Sitagliptin 100 mg along with metformin therapy in comparison to pioglitazone 30 mg plus metformin therapy was both effective, well-tolerated and improved glycemic control in both the groups. Addition of pioglitazone had cause oedema and weight gain to the patients whereas sitagliptin caused weight loss in its patients.

Keywords: sitagliptin, pioglitazone, metformin, type 2 diabetes mellitus

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Authors: Antonia Stergiou

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Background: Due to the developmental trajectory of executive function in preschool age, the majority of existing studies investigating the association between acute physical activity and cognitive control have focused on adolescents and adult population. Aim- The aim of this study was to investigate the possible effects of physical activity on the inhibitory control of pre-school children. Methods: This is a prospectively designed study that was conducted in a primary school in Bristol in June 2015. The total number of subjects was n=61 and 20 trials of a modified Eriksen Flanker Task were completed before and after a 30-minutes session of moderate exercise (including both 5 minutes of warm up and cool down). For each test a pre- and post-test assessment took place that included both congruent and incongruent trials. The congruent trials were considered as the control condition and the incongruent trials as those that measure inhibitory control (experimental condition). At the end of the assessment, the participants were instructed to choose the face that described their current feelings between three options (happy, neutral, sad). Results: There was a trend for increased accuracy following moderate exercise, but there was statistical significance (p > .05). However, there was statistically significant improvement in the reaction time following the same type of exercise (p = .005). Face board assessment revealed positive emotions after 30 minutes of moderate exercise. Conclusions: The current study supports findings from previous studies related to the benefits of physical activity on the children’s inhibitory control and provides evidence of those benefits in even younger ages. Further research should take place considering each child individually. Implementation of those findings could result in an improved curriculum in schools with additional time spent on physical education courses.

Keywords: cognitive control, inhibition, physical activity, pre-school children

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Authors: S. Kershaw, P. J. Barry, K. Webb

Abstract:

Background: Cystic Fibrosis (CF) is a chronic lung disease where patients have chronic lung infection punctuated by acute exacerbations that require intermittent intravenous (IV) antibiotics during their lives. With time, peripheral venous access can become difficult and limited. Accessing these veins can become arduous, traumatic, painful and unworkable. A permanent intravascular access device or Port is a small device that is inserted into the central venous system that allows the delivery of medicine eliminating the need for peripheral venous access. Ports represent a convenient and efficient method when venous access is required on a permanent basis however they are also associated with significant vascular complications. Superior Vena Cava Obstruction (SVCO) is a rare but significant vascular complication of ports in this setting. Objective: We aimed to look at a single CF centre’s experience of port-related SVCO over a thirty year period. Methods: Retrospective data was extracted using patient’s notes, electronic radiological reports and local databases over a period in excess of 30 years from 1982 to 2014. Results: 13 patients were identified with SVCO as a result of their port. 11 patients had CF (9 female, 2 male), one male patient had Primary Ciliary Dyskinesia and one female patient had severe Asthma. The mean port function was 1532 days (range 110 – 4049) and the mean age at SVCO was 24 years (range 11.1 to 36.5 years). The most common symptoms were facial oedema (n=8, 61.5%) and dilated veins (n=6, 46.2%). 7 patients had their Ports removed after SVCO. 6 patients underwent attempted stenting (46.2%) and 6 did not. 4 out of the 6 who underwent stenting required/had re-intervention. 3 of the 6 patients who underwent stenting had symptom resolution, however, 4 of the 6 patients who were not stented had symptom resolution also. Symptom resolution was not guaranteed with stenting and required re-intervention in two-thirds. Conclusion: This case series represents the experience of one of the longest established CF units in the UK and represents the largest cohort ever reported in the literature.

Keywords: ports, Superior Vena Cava Obstruction, cystic fibrosis, access devices

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Authors: Ladda Her, Juntip Kanjanasilp, Ratree Sawangjit, Nathorn Chaiyakunapruk

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Cough is the common symptom of the respiratory tract infections or non-infections; the duration of cough indicates a classification and severity of disease. Herbal medicines can be used as the alternative to drugs for relief of cough symptoms from acute and chronic disease. Eucalyptus was used for reducing cough with evidences suggesting it has an active role in reduction of airway inflammation. The present study aims to evaluate efficacy and safety of eucalyptus for relief of cough symptom in respiratory disease. Method: The Cochrane Library, MEDLINE (PubMed), Scopus, CINAHL, Springer, Science direct, ProQuest, and THAILIS databases. From its inception until 01/02/2019 for randomized control trials. We follow for the efficacy and safety of eucalyptus for reducing cough. Methodological quality was evaluated by using the Cochrane risk of bias tool; two reviewers in our team screened eligibility and extracted data. Result: Six studies were included for the review and five studies were included in the meta-analysis, there were 1.911 persons including children (n: 1) and adult (n: 5) studies; for study in children and adult were between 1 and 80 years old, respectively. Eucalyptus was used as mono herb (n: 2) and in combination with other herbs form (n: 4). All of the studies with eucalyptus were compared for efficacy and safety with placebo or standard treatment, Eucalyptus dosage form in studies included capsules, spray, and syrup. Heterogeneity was 32.44 used random effect model (I² = 1.2%, χ² = 1.01; P-value = 0.314). The efficacy of eucalyptus was showed a reduced cough symptom statistically significant (n = 402, RR: 1.40, 95%CI [1.19, 1.65], P-value < 0.0001) when compared with placebo. Adverse events (AEs) were reported mild to moderate intensity with mostly gastrointestinal symptom. The methodological quality of the included trials was overall poor. Conclusion: Eucalyptus appears to be beneficial and safe for relieving in respiratory diseases focus on cough frequency. The evidence was inconclusive due to limited quality trial. Well-designed trials for evaluating the effectiveness in humans, the effectiveness for reducing cough symptom in human is needed. Eucalyptus had safety as monotherapy or in combination with other herbs.

Keywords: cough, eucalyptus, cineole, herbal medicine, systematic review, meta-analysis

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Authors: Fatemeh Rasooli, Behzad Simiari, Pooya Payandemehr, Amir Nejati, Maryam Bahreini, Atefeh Abdollahi

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Introduction: Pain is a complex physiological reaction to tissue injury. In the course of painful procedures such as nerve block, ice has been shown to be a feasible and inexpensive material to control pain. It delays nerve conduction, actives other senses and reduces inflammatory and painful responses. This study assessed the effect of ice in reducing pain caused by needling and infiltration during digital block. Patient satisfaction recorded as a secondary outcome. Methods: This study was designed as a non-blinded randomized clinical trial approved by Tehran University of Medical Sciences Ethical Committee. Informed consent was taken from all the participants who were then randomly divided into two groups. Digital block performed by standard approach in selected patients. Tubes of ice were prepared in gloves and were fragmented at a time of application for circling around the finger. Tubes were applied for 6 minutes before digital nerve block in the site of needling in the case group. Patients in the control group underwent digital nerve block with the conventional method without ice administration. Numeric Rating Scale (NRS) used for grading pain. 0 used for no pain and 10 for the worst pain that patient had experienced until now. Scores were analyzed by Wilcoxon Rank Sum test and compared in case and control groups. Results: 100 patients aged 16-50 years were enrolled. Mean NRS scores with and without ice were 1.5 mm (S.D ± 1.44) and 6.8 mm (S.D ± 1.40) for needling pain and for infiltration pain were 2.7mm ( S.D ±1.65) and 8.5mm ( S.D ± 1.47), respectively (p<0.001). Besides, patients’ satisfactions were significantly higher in the ice group (p<0.001). Conclusion: Application of ice for 6 minutes significantly reduced pain of needling and infiltration in digital nerve block; thus, it seems to be a feasible and inexpensive material which acts effectively to decrease pain and stress before the procedure.

Keywords: digital block, ice, needle, pain

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Authors: O. V. Vyazovska

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Behavioral efficiency is one of the main principles to be successful in nature. Accuracy of visual discrimination is determined by the attention, learning experience, and memory. In the experimental condition, pigeons’ responses to visual stimuli presented on the screen of the monitor are behaviorally manifested by pecking or not pecking the stimulus, by the number of pecking, reaction time, etc. The higher the probability of rewarding is, the more likely pigeons will respond to the stimulus. We trained 8 pigeons (Columba livia) on a stagewise go/no-go visual discrimination task.16 visual stimuli were created from all possible combinations of four binary dimensions: brightness (dark/bright), size (large/small), line orientation (vertical/horizontal), and shape (circle/square). In the first stage, we presented S+ and 4 S-stimuli: the first that differed in all 4-dimensional values from S+, the second with brightness dimension sharing with S+, the third sharing brightness and orientation with S+, the fourth sharing brightness, orientation and size. Then all 16 stimuli were added. Pigeons rejected correctly 6-8 of 11 new added S-stimuli at the beginning of the second stage. The results revealed that pigeons’ behavior at the beginning of the second stage was controlled by probabilities of rewarding for 4 dimensions learned in the first stage. More or fewer mistakes with dimension discrimination at the beginning of the second stage depended on the number S- stimuli sharing the dimension with S+ in the first stage. A significant inverse correlation between the number of S- stimuli sharing dimension values with S+ in the first stage and the dimensional learning rate at the beginning of the second stage was found. Pigeons were more confident in discrimination of shape and size dimensions. They made mistakes at the beginning of the second stage, which were not associated with these dimensions. Thus, the received results help elucidate the principles of dimensional stimulus control during learning compound multidimensional visual stimuli.

Keywords: visual go/no go discrimination, selective attention, dimensional stimulus control, pigeon

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Authors: Michał Lidner, Zbigniew SzcześNiak

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The ability to estimate blast load overpressure properly plays an important role in safety design of buildings. The issue of studying of blast loading on structural elements has been explored for many years. However, in many literature reports shock wave overpressure is estimated with simplified triangular or exponential distribution in time. This indicates some errors when comparing real and numerical reaction of elements. Nonetheless, it is possible to further improve setting similar to the real blast load overpressure function versus time. The paper presents a method of numerical analysis of the phenomenon of the air shock wave propagation. It uses Finite Volume Method and takes into account energy losses due to a heat transfer with respect to an adiabatic process rule. A system of three equations (conservation of mass, momentum and energy) describes the flow of a volume of gaseous medium in the area remote from building compartments, which can inhibit the movement of gas. For validation three cases of a shock wave flow were analyzed: a free field explosion, an explosion inside a steel insusceptible tube (the 1D case) and an explosion inside insusceptible cube (the 3D case). The results of numerical analysis were compared with the literature reports. Values of impulse, pressure, and its duration were studied. Finally, an overall good convergence of numerical results with experiments was achieved. Also the most important parameters were well reflected. Additionally analyses of dynamic response of one of considered structural element were made.

Keywords: adiabatic process, air shock wave, explosive, finite volume method

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Authors: Alexis Winfield, Carly Sugar, Barbara Fenesi

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The COVID-19 pandemic uprooted regular routines forcing many children to learn from home, requiring many adults to work from home, and cutting families off from support outside the home. Public health restrictions associated with the pandemic caused widespread psychological distress, including depression and anxiety, increased fear, panic, and stress. These trends are particularly concerning for families raising neuroatypical children, such as those with Attention-Deficit Hyperactivity Disorder (ADHD), as these children are already more likely than their typically developing peers to experience comorbid mental health issues and to experience greater distress when required to stay indoors. Families with children who have ADHD are also at greater risk for experiencing heightened familial stress due to the challenges associated with managing ADHD behavioural symptoms, greater parental discord and divorce, and greater financial difficulties compared to other families. The current study engaged families comprised of at least one child diagnosed with ADHD to elucidate 1) the unique ways that the COVID-19 pandemic affected their mental health and 2) the specific barriers these families faced to maintaining optimal mental wellbeing. A total of 33 participants (15 parent-child dyads) engaged in virtual interviews. Content analysis revealed that the most frequently identified mental health effects for families were increased child anxiety and disconnectedness, as well as deteriorating parental mental health. The most frequently identified barriers to maintaining optimal mental well-being were lack of routine, lack of social interaction and social support, and uncertainty and fear. Findings underscore areas of need during times of large-scale social isolation, bring voice to the families of children with ADHD, and contribute to our understanding of the pandemic’s impact on the wellbeing of vulnerable families. This work contributes to a growing body of research aimed at creating safeguards to support mental wellbeing for vulnerable families during times of crisis.

Keywords: attention-deficit hyperactivity disorder, COVID-19, mental health, vulnerable families

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Authors: S. B. Otieno1, F. Were, A. Afullo, K. Waza

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Background: Multi drug resistance HIV has emerged rendering the current conventional treatment of HIV ineffective. There is a need for new treatment regime which is cheap, effective and not prone to resistance development by HIV. Methods: In randomized clinical study of 68 HIV positive children 3 – 15 years to asses the efficacy of yeast selenium in HIV/AIDS patients, 50μ yeast selenium was administered to 34 children while in matched control of 34 were put on placebo. Blood samples and weight of the both groups which were taken every 3 months intervals up to 6 months, were analyzed by ELIZA for CD4T cells, the data was analyzed by SPSS version 16, WAZ scores were analyzed by Epi Info version 6. Results: No significant difference in age { χ2 (1, 62) =0.03, p =0.853}, cause of morbidity between test and controls {χ2 (1, 65) = 5.87, p= 0.015} and on condition of foster parents {χ2 ( 1,63) = 5.57, p= 0.0172} was observed. Children on selenium showed progressive improvement of WAZ and significant difference at six months {F (5,12) = =5.758, P=0.006}, and weight gain of up to 4.1 kilograms in six months, and significant CD4 T cell count increase t= -2.943, p<0.05 compared to matched controls t = -1.258 p> 0.05. CD4 T cell count increased among all age groups on test 3-5 years (+ 267.1),5-8 years (+200.3) 9-15 years (+71.2) cells/mm3 and in matched controls a decrease 3-5 years (-71), 5-8 years (-125) and 9-13 years (-10.1) cells/mm3 . No significant difference inCD4 T cell count between boys {F (2, 32) = 1.531 p= 0.232} and between boys {F (2, 49) = 1.040, p= 0.361} on test and between boys and girls {F (5, 81) = 1.379, p= 0.241} on test. Similarly no significant difference between boys and girls were observed {F (5, 86) = 1.168, p= 0.332}.In the test group there was significant positive correlation β =252.23 between weight for age (WAZ), and CD4 T Cell Count p=0.007, R2= 0.252, F< 0.05. In matched controls no significant correlation between weight gain and CD4 T cell count change was observed at six months p > 0.05. No positive correlation β =-138.23 was observed between CD4T Cell count, WAZ, p=0.934, R2 =0.0337 F >0.05. Majority (96.78%) of children on test either remained or progressed to WHO immunological stage I. Conclusion: From this study it can be concluded that yeast Selenium is effective in slowing the progress of HIV 1 in children from WHO clinical stage I by improving CD4 T cell count and hence the immunity.

Keywords: selenium, HIV, AIDS, WAZ

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Authors: Praveen Adusumilli, Meher Lakshmi Konatam, Sadashivudu Gundeti, Stalin Bala

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The invention of trastuzumab has changed the treatment of breast cancer and lives of many patients all over the world. Despite many patients getting benefitted from the drug, it is out of reach for most of the patients. There is very limited real world data regarding the epidemiology and clinical outcome of Her2neu positive breast cancer patients. Materials and Methods: This is a retrospective analysis of breast cancer patients presenting to a tertiary care cancer centre in Southern India from 2007 to2013. All early and locally advanced breast cancer patients, who were Her2neu 3+ on IHC are included in the study and evaluated in terms of epidemiology, 3-year disease free survival (DFS)and 5-year overall survival(OS). Chemotherapy regimens used were-FAC 6 cycles or AC 4 cycles followed by 12 cycles of weekly paclitaxel . Trastuzumab was given after 6 cycles of FAC or weekly with paclitaxel followed by 3weekly maintenance until 1 year. Results: Over the period of this study there were 885 newly diagnosed cases of carcinoma breast, of which 242 (27%) were Her2neu positive, 360(40%) were hormone receptor positive, and 212(24%) were triple negative. A total of 71(8%) were Her2neu equivocal of which only 10 patients got FISH test done. Of the 212 newly diagnosed patients, only 74 (29%) opted to have standard of care therapy with trastuzumab at our centre, out of which 52(24%), 8(3%), received under insurance, paying basis respectively. 14(9%) patients received the care as part of clinical trial program (ALTTO trial). 7 (9.72%) patients developed decrease of ejection fraction by greater than 10%, requiring stoppage of trastuzumab out of which 5 were restarted in 2 months. Patients receiving trastuzumab along with chemotherapy had longer 3year DFS 92% vs. 60% (p value<0.0001) when compared to chemotherapy alone. 5 year OS was 87% vs 44% (p-value <0.0001) compared to chemotherapy alone. Conclusion: Trastuzumab with chemotherapy improves the DFS and OS in Her2neu positive patients. The biggest constraint is the cost of the treatment and absence of universal health security net to treat all patients with this diagnosis.

Keywords: breast cancer, Her 2 neu positive, real world data, Trastuzumab

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Authors: Branka Milicic Stanic, Romana Mijovic

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In primary hyperparathyroidism, an increased risk of developing cardiovascular disease may exist due to increased activity of the renin-angiotensin-aldosterone system (RAAS). In adenomatous altered tissue of parathyroid gland, compared to normal tissue, there are two to fourfold increase in the expression of type 1 angiotensin II receptors. As there is a clear evidence of the independent role of aldosterone on the cardiovascular system, the aim of this study was to evaluate the existence of an association between aldosterone secretion and parathyroid hormone in patients with primary hyperparathyroidism. This study included 48 patients with elevated parathyroid hormone who had come to the Departement of Nuclear Medicine, Clinical Center of Vojvodina, for Parathyroid Scintigraphy. The control group consisted of 30 healthy subjects who matched age and gender to the study group. All the results were statistically processed by statistical package STATISTICA 14 (Statsoft Inc,Tulsa, OK, USA). The survey was conducted between February 2017 and April 2018 at the Departement of Nuclear Medicine and at the Departement for Endocinology Diagnoistics, in Clinical Center of Vojvodina, Novi Sad. Compared to the control group, the study group had statistically significantly higher values of aldosterone (p=0.028), total calcium (p=0.01), ionized calcium (p=0.003) and parathyroid hormone (N-TACT PTH) (p=0.00), while statistically a significant lower levels in the study group were for phosphorus (p=0.003) and vitamin D (p=0.04). A linear correlation analysis in the study group revealed a statistically significant degree of positive correlation between renin and N-TACT PTH (r=0.688, p<0.05); renin and calcium (r=0.673, p<0.05) and renin and ionized calcium (r=0.641, p<0.05). Serum aldosterone and parathyroid hormone levels (N-TACT) were correlated positively in patients with primary hyperparathyroidism (r=0.509, p<0.05). According to the linear correlation analysis in the control group, aldosterone showed no positive correlation with N-TACT PTH (r=-0.285, p>0.05), as well as total and ionized calcium (r=-0.200, p>0.05; r=-0.313, p>0.05). In multivariate regression analysis of the study group, the strongest predictive variable of aldosterone secretion was N-TACT PTH (p=0.011). Aldosterone correlated positively to PTH levels in patients with primary hyperparathyroidism, and the fact is that in these patients aldosterone might be a key mediator of cardiovascular symptoms. All this knowledge should help to find new treatments to prevent cardiovascular disease.

Keywords: aldosterone, hyperparathyroidism, parathyroid hormone, parathyroid gland

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Authors: Parastoo Parhizkar, Jaber Yaghini, Omid Fakheran

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Background: Third molar surgery is often associated with postoperative problems which cause serious impediments on daily activities and quality of life. Steroidal anti-inflammatory drugs may decrease these common post-operative complications. The purpose of this review is evaluating the available evidence regarding the efficacy of corticosteroids used as adjunctive therapy for patients undergoing third molar surgery. Methods: PubMed, Google scholar, Scopus, web of science, clinicaltrials.gov, scirus.com, Cochrane central register for controlled trials, LILACS, OpenGrey, centerwatch, isrctn, who.int and ebsco were searched without restrictions regarding the year of publication. Randomized clinical trials assessing patient-reported outcomes in patients undergoing surgical therapy, were eligible for inclusion. Study quality was assessed using the CONSORT-checklist. No meta-analysis was performed. Results: A total of twelve Randomized Clinical Trials were included in this study. Methylprednisolone and Dexamethasone may decrease postoperative side effects such as pain, trismus and edema. Based on the results both of them could improve patients’ satisfaction, and there is no significant difference between these two types of corticosteroids regarding the patient centered outcomes (p > 0.05). Intralesional and intravenous injection of Dexamethasone showed an equivalent result, with statistically significant better results (P < 0.05) in comparison with the oral treatment. Conclusion: various types of corticosteroids can enhance the patient’s satisfaction following third molar surgery. However, there is no significant difference between Dexamethasone, Prednisolone and Methylprednisolone groups in this regard. Comparing the various administration routs, local injection of Dexamethasone is quite simple, painless and cost-effective adjunctive therapy with better drug efficacy.

Keywords: third molar surgery, corticosteroids, patient-reported outcomes, health related quality of life

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Authors: Abhishek Pandey

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Ibuprofen and Acetaminophen is widely used as prescription & non-prescription medicine. Ibuprofen mainly used in the treatment of mild to moderate pain related to headache, migraine, postoperative condition and in the management of spondylitis, osteoarthritis and rheumatoid arthritis. Acetaminophen is used as an analgesic and antipyretic drug. Ibuprofen having high tendency of sticking to punches of tablet punching machine while Acetaminophen is not ordinarily compressible to tablet formulation because Acetaminophen crystals are very hard and brittle in nature and fracture very easily when compressed producing capping and laminating tablet defects therefore wet granulation method is used to make them compressible. The aim of study was to prepare Ibuprofen and Acetaminophen tablets by direct compression and top spray granulation technique. In this Investigation tablets were prepared by using directly compressible grade excipients. Dibasic calcium phosphate, lactose anhydrous (DCL21), microcrystalline cellulose (Avicel PH 101). In order to obtain best or optimized formulation, nine different formulations were generated among them batch F7, F8, F9 shows good results and within the acceptable limit. Formulation (F7) selected as optimize product on the basis of dissolution study. Furtherly, directly compressible granules of both drugs were prepared by using top spray granulation technique in fluidized bed processor equipment and compressed .In order to obtain best product process optimization was carried out by performing four trials in which various parameters like inlet air temperature, spray rate, peristaltic pump rpm, % LOD, properties of granules, blending time and hardness were optimized. Batch T3 coined as optimized batch on the basis physical & chemical evaluation. Finally formulations prepared by both techniques were compared.

Keywords: direct compression, top spray granulation, process optimization, blending time

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Authors: Cigdem Karaaslan, Yalcin Duydu, Aylin Ustundag, Can Ozgur Yalcın, Hakan Goker

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Benzazole nucleus is found in the structure of many compounds as anticancer agents. Bendamustine (Alkylating agent), Nocodazole (Mitotic inhibitor), Veliparib (PARP inhibitor), Glasdegib (SMO inhibitor) are clinically used as anticancer therapeutics which bearing benzimidazole moiety. Based on the principle of bioisosterism in the present work, 23 compounds belonging to 2-(3,4-dimethoxy-phenyl) benzazoles and imidazopyridine series were synthesized and evaluated for their anticancer activities. N-(5-Chloro-2-hydroxyphenyl)-3,4-dimethoxybenzamide, was obtained by the amidation of 2-hydroxy-5-chloroaniline with 3,4-dimethoxybenzoic acid by using 1,1'-carbonyldiimidazole. Cyclization of benzamide derivative to benzoxazole, was achieved by p-toluenesulfonic acid. Other 1H-benz (or pyrido) azoles were prepared by the reaction between 2-aminothiophenol, o-phenylenediamine, o-pyridinediamine with sodium metabisulfite adduct of 3,4-dimethoxybenzaldehyde. The NMR assignments of the dimethoxy groups were established by the Nuclear Overhauser Effect Spectroscopy. A compound named, 5(4),7(6)-Dichloro-2-(3,4-dimethoxy) phenyl-1H-benzimidazole, bearing two chlorine atoms at the 5(4) and 7(6) positions of the benzene moiety of benzimidazole was found the most potent analogue, against A549 cells with the GI50 value of 1.5 µg/mL. In addition, 2-(3,4-Dimethoxyphenyl)-5,6-dimethyl-1H-benzimi-dazole showed remarkable cell growth inhibition against MCF-7 and HeLa cells with the GI₅₀ values of 7 and 5.5 µg/mL, respectively. It could be concluded that introduction of di-chloro atoms at the phenyl ring of 2-(3,4-dimethoxyphenyl)-1H-benzimidazoles increase significant cytotoxicity to selected human tumor cell lines in comparison to other all benzazoles synthesized in this study. Unsubstituted 2-(3,4-dimethoxyphenyl) imidazopyridines also gave the good inhibitory profile against A549 and HeLa cells.

Keywords: 3, 4-Dimethoxyphenyl, 1H-benzimidazole, benzazole, imidazopyridine

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Authors: Sylvain Caillol, Maxence Fache, Bernard Boutevin

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Recent years have witnessed an increasing demand on renewable resource-derived polymers owing to increasing environmental concern and restricted availability of petrochemical resources. Thus, a great deal of attention was paid to renewable resources-derived polymers and to thermosetting materials especially, since they are crosslinked polymers and thus cannot be recycled. Also, most of thermosetting materials contain aromatic monomers, able to confer high mechanical and thermal properties to the network. Therefore, the access to biobased, non-harmful, and available aromatic monomers is one of the main challenges of the years to come. Starting from phenols available in large volumes from renewable resources, our team designed platforms of chemicals usable for the synthesis of various polymers. One of these phenols, vanillin, which is readily available from lignin, was more specifically studied. Various aromatic building blocks bearing polymerizable functions were synthesized: epoxy, amine, acid, carbonate, alcohol etc. These vanillin-based monomers can potentially lead to numerous polymers. The example of epoxy thermosets was taken, as there is also the problematic of bisphenol A substitution for these polymers. Materials were prepared from the biobased epoxy monomers obtained from vanillin. Their thermo-mechanical properties were investigated and the effect of the monomer structure was discussed. The properties of the materials prepared were found to be comparable to the current industrial reference, indicating a potential replacement of petrosourced, bisphenol A-based epoxy thermosets by biosourced, vanillin-based ones. The tunability of the final properties was achieved through the choice of monomer and through a well-controlled oligomerization reaction of these monomers. This follows the same strategy than the one currently used in industry, which supports the potential of these vanillin-derived epoxy thermosets as substitutes of their petro-based counterparts.

Keywords: lignin, vanillin, epoxy, amine, carbonate

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Authors: O. F. Elkommos

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Teaching and learning EFL speaking modules is one of the most challenging productive modules for both instructors and learners. In a student-centered interactive communicative language teaching approach, learners and instructors should be aware of the fact that the target language must be taught as/for communication. The student must be empowered by tools that will work on more than one level of their communicative competence. Communicative learning will need a teaching and learning methodology that will address the goal. Teaching turn-taking rules, pragmatic principles and speech acts will enhance students' sociolinguistic competence, strategic competence together with discourse competence. Sociolinguistic competence entails the mastering of speech act conventions and illocutionary acts of refusing, agreeing/disagreeing; emotive acts like, thanking, apologizing, inviting, offering; directives like, ordering, requesting, advising, and hinting, among others. Strategic competence includes enlightening students’ consciousness of the various particular turn-taking systemic rules of organizing techniques of opening and closing conversation, adjacency pairs, interrupting, back-channeling, asking for/giving opinion, agreeing/disagreeing, using natural fillers for pauses, gaps, speaker select, self-select, and silence among others. Students will have the tools to manage a conversation. Students are engaged in opportunities of experiencing the natural language not as a mere extra student talking time but rather an empowerment of knowing and using the strategies. They will have the component items they need to use as well as the opportunity to communicate in the target language using topics of their interest and choice. This enhances students' communicative abilities. Available websites and textbooks now use one or more of these tools of turn-taking or pragmatics. These will be students' support in self-study in their independent learning study hours. This will be their reinforcement practice on e-Learning interactive activities. The students' target is to be able to communicate the intended meaning to an addressee that is in turn able to infer that intended meaning. The combination of these tools will be assertive and encouraging to the student to beat the struggle with what to say, how to say it, and when to say it. Teaching the rules, principles and techniques is an act of awareness raising method engaging students in activities that will lead to their pragmatic discourse competence. The aim of the paper is to show how the suggested pragmatic model will empower students with tools and systems that would support their learning. Supporting students with turn taking rules, speech act theory, applying both to texts and practical analysis and using it in speaking classes empowers students’ pragmatic discourse competence and assists them to understand language and its context. They become more spontaneous and ready to learn the discourse pragmatic dimension of the speaking techniques and suitable content. Students showed a better performance and a good motivation to learn. The model is therefore suggested for speaking modules in EFL classes.

Keywords: communicative competence, EFL, empowering learners, enhance learning, speech acts, teaching speaking, turn taking, learner centred, pragmatics

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