Search results for: compound exercises
1187 Synthesis and Biological Evaluation of Some Benzoxazole Derivatives as Inhibitors of Acetylcholinesterase / Butyrylcholinesterase and Tyrosinase
Authors: Ozlem Temiz-Arpaci, Meryem Tasci, Fatma Sezer Senol, İlkay Erdogan Orhan
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Alzheimer’s disease (AD), a neurodegenerative disorder characterized by a progressive deterioration of memory and cognition, occurs more frequently in elderly people. Current treatment approaches in this disease with the major therapeutic strategy are based on the AChE and BChE inhibition. On the other hand, tyrosinase inhibition has become a target for the treatment of Parkinson’s disease (PD) since this enzyme may play a role in neuromelanin formation in the human brain and could be critical in the formation of dopamine neurotoxicity associated with neurodegeneration linked to PD. Also benzoxazoles are structural isosteres of natural nucleotides that can interact with biopolymers so that benzoxazoles showed a lot of different biological activities. In this study, a series of 2,5-disubstituted-benzoxazole derivatives were synthesized and were evaluated as possible inhibitors of acetylcholinesterase (AChE) / butyrylcholinesterase (BChE) and tyrosinase. The results demonstrated that the compounds exhibited a weak spectrum of AChE / BChE inhibitory activity ranging between 3.92% - 54.32% except compound 8 which showed no activity against AChE and compound 4 which showed no activity against BChE at the specified molar concentrations. Also, the compounds indicated lower than tyrosinase inhibitory activity of ranging between 8.14% - 22.90% to that of reference (kojic acid).Keywords: AChE and BChE inhibition, Alzheimer’s disease, benzoxazoles, tyrosinase inhibition
Procedia PDF Downloads 3411186 Effect of Core Stability Exercises on Trunk Muscle Balance in Healthy Adult Individuals
Authors: Amira A. A. Abdallah, Amir A. Beltagi
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Background: Core stability training has recently attracted attention for improving muscle balance and optimizing performance in healthy and unhealthy individuals. Purpose: This study investigated the effect of beginner’s core stability exercises on trunk flexors’/extensors’ peak torque ratio and trunk flexors’ and extensors’ peak torques. Methods: Thirty five healthy individuals participated in the study. They were randomly assigned to two groups; experimental “group I, n=20” and control “group II, n=15”. Their mean age, weight and height were 20.7±2.4 vs. 20.3±0.61 years, 66.5±12.1 vs. 68.57±12.2 kg and 166.7±7.8 vs. 164.28 ±7.59 cm. for group I vs. group II. Data were collected using the Biodex Isokinetic system. The participants were tested twice; before and after a 6-week period during which group I performed a core stability training program. Results: The 2x2 Mixed Design ANOVA revealed that there were no significant differences (p>0.025) in the trunk flexors’/extensors’ peak torque ratio between the pre-test and post-test conditions for either group. Moreover, there were no significant differences (p>0.025) in the trunk flexion/extension ratios between both groups at either condition. However, the 2x2 Mixed Design MANOVA revealed significant increases (p<0.025) in the trunk flexors’ and extensors’ peak torques in the post-test condition compared with the pre-test in group I with no significant differences (p>0.025) in group II. Moreover, there was a significant increase (p<0.025) in the trunk flexors’ peak torque only in group I compared with group II in the post-test condition with no significant differences in the other conditions. Interpretation/Conclusion: The improvement in muscle performance indicated by the increase in the trunk flexors’ and extensors’ peak torques in the experimental group recommends including core stability training in the exercise programs that aim to improve muscle performance.Keywords: core stability, isokinetic, trunk muscles, muscle balance
Procedia PDF Downloads 2601185 Synthesis of Erlotinib Analogues, Conjugation of BSA to Erlotinib Alcohol and Their Anti-Cancer Activity against NSCLC
Authors: Ramalingam Boobalan, Chinpiao Chen, Jui-I. Chiao
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A series of erlotinib analogues that have structural modification at 6,7-alkoxyl positions is efficiently synthesized. The key reactions that involved in synthesis are one-pot oxime formation-dehydration for the formation of nitrile, quinazoline ring formation reaction between aniline and o-cyanoaniline via formamidine intermediate, Fe/NH4Cl catalyzed reduction-hetereocyclization-reductive ring opening reaction for the formation of o-aminobenzamide, high yielding seal tube reactions for O-demethylation, sodium iodide substitution, ammonia substitution. The in vitro anti-tumor activity of synthesized compounds is studied in two non-small cell lung cancer (NSCLC) cell lines (A549 and H1975). Among the synthesized compounds, the iodo compound 6 (ETN-6) exhibits higher anti-cancer activity compared to erlotinib. An efficient method is developed for the conjugation of erlotinib analogue-4, alcohol compound, with protein, bovine serum albumin (BSA), via succinic acid linker. The in vitro anti-tumor activity of the protein attached erlotinib analogue, 8 (ETN-4-Suc-BSA), showed stronger inhibitory activity in both A549 and H1975 NSCLC cell lines.Keywords: anti-cancer, BSA, EGFR, Erlotinib
Procedia PDF Downloads 3301184 Clinical Prediction Rules for Using Open Kinetic Chain Exercise in Treatment of Knee Osteoarthritis
Authors: Mohamed Aly, Aliaa Rehan Youssef, Emad Sawerees, Mounir Guirgis
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Relevance: Osteoarthritis (OA) is the most common degenerative disease seen in all populations. It causes disability and substantial socioeconomic burden. Evidence supports that exercise are the most effective conservative treatment for patients with OA. Therapists experience and clinical judgment play major role in exercise prescription and scientific evidence for this regard is lacking. The development of clinical prediction rules to identify patients who are most likely benefit from exercise may help solving this dilemma. Purpose: This study investigated whether body mass index and functional ability at baseline can predict patients’ response to a selected exercise program. Approach: Fifty-six patients, aged 35 to 65 years, completed an exercise program consisting of open kinetic chain strengthening and passive stretching exercises. The program was given for 3 sessions per week, 45 minutes per session, for 6 weeks Evaluation: At baseline and post treatment, pain severity was assessed using the numerical pain rating scale, whereas functional ability was being assessed by step test (ST), time up and go test (TUG) and 50 feet time walk test (50 FTW). After completing the program, global rate of change (GROC) score of greater than 4 was used to categorize patients as successful and non-successful. Thirty-eight patients (68%) had successful response to the intervention. Logistic regression showed that BMI and 50 FTW test were the only significant predictors. Based on the results, patients with BMI less than 34.71 kg/m2 and 50 FTW test less than 25.64 sec are 68% to 89% more likely to benefit from the exercise program. Conclusions: Clinicians should consider the described strengthening and flexibility exercise program for patents with BMI less than 34.7 Kg/m2 and 50 FTW faster than 25.6 seconds. The validity of these predictors should be investigated for other exercise.Keywords: clinical prediction rule, knee osteoarthritis, physical therapy exercises, validity
Procedia PDF Downloads 4221183 The Effect of Taekwondo on Plantar Pressure Distribution and Arch Index
Authors: Maryam Kakavand, Samira Entezari, Sara Khoshjamalfekri, Raghad Mimar
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The objective of this study is 1) to compare elite female and beginner taekwondo players in terms of plantar pressure distribution, vertical ground reaction force, contact area, mean pressure, and right and left longitudinal arches, and 2) to compare preferred and non-preferred limbs among elite players. To the best of authors’ knowledge, as of yet, there is no information available about the plantar pressure distribution and arch index among taekwondo players. Material and Methods: An analytical-comparative research method is applied. Therefore seven elite athletes and eight novice athletes were selected. The emed-C50 platform was used to assess plantar pressure distribution, vertical ground reaction force, contact area, mean pressure of different areas, and planter longitudinal arch in a second step protocol. Independent t-test and dependent t-test were used at a level of 0.05 to compare the elites and beginners' right and left feet, and preferred and non-preferred limbs among elite athletes, respectively. Results: In comparing the right and left limbs of elite and beginner groups, findings indicate that there is only a significant difference in the mean pressure of the first metatarsal of the right foot. Findings also showed a significant difference in the contact area of the toes 3, 4, 5 regions between elites’ preferred and non-preferred limbs. However, no significant difference was found between the two groups’ right and left limbs and elites’ preferred and non-preferred limbs in terms of pressure distribution, vertical ground reaction force, and arch index. Conclusion: It seems that taekwondo exercises have affected pressure distribution patterns among advanced players causing some differences in their planter pressure distribution pattern when compared to that of beginners. Therefore, taekwondo exercises may be a factor contributing to asymmetry performance in preferred and non-preferred limbs.Keywords: planter pressure, arch index, taekwondo, elite
Procedia PDF Downloads 1541182 Excavation of Phylogenetically Diverse Bioactive Actinobacteria from Unexplored Regions of Sundarbans Mangrove Ecosystem for Mining of Economically Important Antimicrobial Compounds
Authors: Sohan Sengupta, Arnab Pramanik, Abhrajyoti Ghosh, Maitree Bhattacharyya
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Newly emerged phyto-pathogens and multi drug resistance have been threating the world for last few decades. Actinomycetes, the most endowed group of microorganisms isolated from unexplored regions of the world may be the ultimate solution to these problems. Thus the aim of this study was to isolate several bioactive actinomycetes strains capable of producing antimicrobial secondary metabolite from Sundarbans, the only mangrove tiger land of the world. Fifty four actinomycetes were isolated and analyzed for antimicrobial activity against fifteen test organisms including three phytopathogens. Nine morphologically distinct and biologically active isolates were subjected to polyphasic identification study. 16s rDNA sequencing indicated eight isolates to reveal maximum similarity to the genus streptomyces, whereas one isolate presented only 93.57% similarity with Streptomyces albogriseolus NRRL B-1305T. Seventy-one carbon sources and twenty-three chemical sources utilization assay revealed their metabolic relatedness. Among these nine isolates three specific strains were found to have notably higher degree of antimicrobial potential effective in a broader range including phyto-pathogenic fungus. PCR base whole genome screen for PKS and NRPS genes, confirmed the occurrence of bio-synthetic gene cluster in some of the isolates for novel antibiotic production. Finally the strain SMS_SU21, which showed antimicrobial activity with MIC value of 0.05 mg ml-1and antioxidant activity with IC50 value of 0.242±0.33 mg ml-1 was detected to be the most potential one. True prospective of this strain was evaluated utilizing GC-MS and the bioactive compound responsible for antimicrobial activity was purified and characterized. Rare bioactive actinomycetes were isolated from unexplored heritage site. Diversity of the biosynthetic gene cluster for antimicrobial compound production has also been evaluated. Antimicrobial compound SU21-C has been identified and purified which is active against a broad range of pathogens.Keywords: actinomycetes, sundarbans, antimicrobial, pks nrps, phyto-pathogens, GC-MS
Procedia PDF Downloads 5051181 Experimental and Theoretical Approach, Hirshfeld Surface, Reduced Density Gradient, Molecular Docking of a Thiourea Derivative
Authors: Noureddine Benharkat, Abdelkader Chouaih, Nourdine Boukabcha
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A thiourea derivative compound was synthesized and subjected to structural analysis using single-crystal X-ray diffraction (XRD). The crystallographic data unveiled its crystallization in the P21/c space group within the monoclinic system. Examination of the dihedral angles indicated a notable non-planar structure. To support and interpret these resulats, density functional theory (DFT) calculations were conducted utilizing the B3LYP functional along with a 6–311 G (d, p) basis set. Additionally, to assess the contribution of intermolecular interactions, Hirshfeld surface analysis and 2D fingerprint plots were employed. Various types of interactions, whether weak intramolecular or intermolecular, within a molecule can significantly impact its stability. The distinctive signature of non-covalent interactions can be detected solely through electron density analysis. The NCI-RDG analysis was employed to investigate both repulsive and attractive van der Waals interactions while also calculating the energies associated with intermolecular interactions and their characteristics. Additionally, a molecular docking study was studied to explain the structure-activity relationship, revealing that the title compound exhibited an affinity energy of -6.8 kcal/mol when docked with B-DNA (1BNA).Keywords: computational chemistry, density functional theory, crystallography, molecular docking, molecular structure, powder x-ray diffraction, single crystal x-ray diffraction
Procedia PDF Downloads 601180 Efficiency of Virtual Reality Exercises with Nintendo Wii System on Balance and Independence in Motor Functions in Hemiparetic Patients: A Randomized Controlled Study
Authors: Ayça Utkan Karasu, Elif Balevi Batur, Gülçin Kaymak Karataş
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The aim of this study was to examine the efficiency of virtual reality exercises with Nintendo Wii system on balance and independence in motor functions. This randomized controlled assessor-blinded study included 23 stroke inpatients with hemiparesis all within 12 months poststroke. Patients were randomly assigned to control group (n=11) or experimental group (n=12) via block randomization method. Control group participated in a conventional balance rehabilitation programme. Study group received a four-week balance training programme five times per week with a session duration of 20 minutes in addition to the conventional balance rehabilitation programme. Balance was assessed by the Berg’s balance scale, the functional reach test, the timed up and go test, the postural assessment scale for stroke, the static balance index. Also, displacement of centre of pressure sway and centre of pressure displacement during weight shifting was calculated by Emed-SX system. Independence in motor functions was assessed by The Functional Independence Measure (FIM) ambulation and FIM transfer subscales. The outcome measures were evaluated at baseline, 4th week (posttreatment), 8th week (follow-up). Repeated measures analysis of variance was performed for each of the outcome measure. Significant group time interaction was detected in the scores of the Berg’s balance scale, the functional reach test, eyes open anteroposterior and mediolateral center of pressure sway distance, eyes closed anteroposterior center of pressure sway distance, center of pressure displacement during weight shifting to effected side, unaffected side and total centre of pressure displacement during weight shifting (p < 0.05). Time effect was statistically significant in the scores of the Berg’s balance scale, the functional reach test, the timed up and go test, the postural assessment scale for stroke, the static balance index, eyes open anteroposterior and mediolateral center of pressure sway distance, eyes closed mediolateral center of pressure sway distance, the center of pressure displacement during weight shifting to effected side, the functional independence measure ambulation and transfer scores (p < 0.05). Virtual reality exercises with Nintendo Wii system combined with a conventional balance rehabilitation programme enhances balance performance and independence in motor functions in stroke patients.Keywords: balance, hemiplegia, stroke rehabilitation, virtual reality
Procedia PDF Downloads 2211179 Investigation of the Inhibition Effect of 2,3-Diaminopyridine on Mild Steel Corrosion in Solution Simulating Water of Pores Concrete in Absence and Presence of Chloride Ions
Authors: Fatiha Benghanem, Mokhtar Berarma, Saida Keraghel, Ali Ourari
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Corrosion is the result of the reaction between a material and its environment. Steel in concrete is protected from corrosion by a passive film promoted by concrete alkalinity. For the initiation of corrosion, this protective film must be destroyed and this can be mainly done in two ways: by the attack of chlorides on the steel or by carbonation of the cover concrete due the reaction with carbon dioxide, which causes reduction in the alkalinity of concrete. The literature reports several ways to decrease or to prevent reinforcement corrosion. Among them, the use of corrosion inhibitors has been an envisaged solution. Two approaches are generally used to evaluate the efficiency of inhibitors for concrete application; one uses simulated pore solution testing , and the other uses actual concrete or mortar specimens. Both methods are some times used in conjunction. The aim of this study is to investigate the use of 2,3-diaminopyridine as a corrosion inhibitors of steel in alkaline media which simulate the electrolyte in the concrete pores. The effectiveness of this compound as corrosion inhibitor was investigated by measuring the corrosion potentials, the polarization curves and the corrosion current densities of steel with and without chlorides. The study of corrosion inhibition by this compound led to the conclusion that he has low rates of inhibition in the absence of aggressive ions and high rates in their presence. This type of organic compounds are promoting for the protection of armatures in concrete.Keywords: corrosion, inhibitors, mild steel, conjunction
Procedia PDF Downloads 4411178 The Effect of Aerobics and Yogic Exercise on Selected Physiological and Psychological Variables of Middle-Aged Women
Authors: A. Pallavi, N. Vijay Mohan
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A nation can be economically progressive only when the citizens have sufficient capacity to work efficiently to increase the productivity. So, good health must be regarded as a primary need of the community. This helps the growth and development of the body and the mind, which in turn leads to progress and prosperity of the nation. An optimum growth is a necessity for an efficient existence in a biologically adverse and economically competitive world. It is also necessary for the execution of daily routine work. Yoga is a method or a system for the complete development of the personality in a human being. It can be further elaborated as an all-around and complete development of the body, mind, morality, intellect and soul of a being. Sri Aurobindo defines yoga as 'a methodical effort towards self-perfection by the development of the potentialities in the individual.' Aerobic exercise as any activity that uses large muscle groups, can be maintained continuously, and is rhythmic I nature. It is a type of exercise that overloads the heart and lungs and causes them to work harder than at rest. The important idea behind aerobic exercise today, is to get up and get moving. There are more activities that ever to choose from, whether it is a new activity or an old one. Find something you enjoy doing that keeps our heart rate elevated for a continuous time period and get moving to a healthier life. Middle aged selected and served as the subjects for the purpose of this study. The selected subjects were in the age group of 30 to 40 years. By going through the literature and after consulting the experts in yoga and aerobic training, the investigator had chosen the variables which are specifically related to the middle-aged men. The selected physiological variables are pulse rate, diastolic blood pressure, systolic blood pressure; percent body fat and vital capacity. The selected psychological variables are job anxiety, occupational stress. The study was formulated as a random group design consisting of aerobic exercise and yogic exercises groups. The subjects (N=60) were at random divided into three equal groups of twenty middle-aged men each. The groups were assigned the names as follows: 1. Experimental group I- aerobic exercises group, 2. Experimental group II- yogic exercises, 3. Control group. All the groups were subjected to pre-test prior to the experimental treatment. The experimental groups participated in their respective duration of twenty-four weeks, six days in a week throughout the study. The various tests administered were: prior to training (pre-test), after twelfth week (second test) and twenty-fourth weeks (post-test) of the training schedule.Keywords: pulse rate, diastolic blood pressure, systolic blood pressure; percent body fat and vital capacity, psychological variables, job anxiety, occupational stress, aerobic exercise, yogic exercise
Procedia PDF Downloads 4451177 Experimental Chevreul’s Salt Production Methods on Copper Recovery
Authors: Turan Çalban, Oral Laçin, Abdüsselam Kurtbaş
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The experimental production methods Chevreul’s salt being a intermediate stage product for copper recovery were investigated by dealing with the articles written on this topic. Chevreul’s salt, Cu2SO3.CuSO3.2H2O, being a mixed valence copper sulphite compound has been obtained by using different methods and reagents. Chevreul’s salt has a intense brick-red color. It is a highly stable and expensive salt. The production of Chevreul’s salt plays a key role in hiydrometallurgy. In recent years, researchs on this compound have been intensified. Silva et al. reported that this salt is thermally stable up to 200oC. Çolak et al. precipitated the Chevreul’s salt by using ammonia and sulphur dioxide. Çalban et al. obtained at the optimum conditions by passing SO2 from leach solutions with NH3-(NH4)2SO4. Yeşiryurt and Çalban investigated the optimum precipitation conditions of Chevreul’s salt from synthetic CuSO4 solutions including Na2SO3. Çalban et al. achieved the precipitation of Chevreul’s salt at the optimum conditions by passing SO2 from synthetic CuSO4 solutions. Çalban et al. examined the precipitation conditions of Chevreul’s salt using (NH4)2SO3 from synthetic aqueous CuSO4 solutions. In light of these studies, it can be said that Chevreul’s salt can be produced practically from both a leach solutions including copper and synthetic CuSO4 solutions.Keywords: Chevreul’s salt, ammonia, copper sulpfite, sodium sülfite, optimum conditions
Procedia PDF Downloads 2681176 Control Strategy for Two-Mode Hybrid Electric Vehicle by Using Fuzzy Controller
Authors: Jia-Shiun Chen, Hsiu-Ying Hwang
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Hybrid electric vehicles can reduce pollution and improve fuel economy. Power-split hybrid electric vehicles (HEVs) provide two power paths between the internal combustion engine (ICE) and energy storage system (ESS) through the gears of an electrically variable transmission (EVT). EVT allows ICE to operate independently from vehicle speed all the time. Therefore, the ICE can operate in the efficient region of its characteristic brake specific fuel consumption (BSFC) map. The two-mode powertrain can operate in input-split or compound-split EVT modes and in four different fixed gear configurations. Power-split architecture is advantageous because it combines conventional series and parallel power paths. This research focuses on input-split and compound-split modes in the two-mode power-split powertrain. Fuzzy Logic Control (FLC) for an internal combustion engine (ICE) and PI control for electric machines (EMs) are derived for the urban driving cycle simulation. These control algorithms reduce vehicle fuel consumption and improve ICE efficiency while maintaining the state of charge (SOC) of the energy storage system in an efficient range.Keywords: hybrid electric vehicle, fuel economy, two-mode hybrid, fuzzy control
Procedia PDF Downloads 3841175 An Innovation and Development System for a New Hybrid Composite Technology in Aerospace Industry
Authors: M. Fette, J. P. Wulfsberg, A. Herrmann, R. H. Ladstaetter
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Present and future lightweight design represents an important key to successful implementation of energy-saving, fuel-efficient and environmentally friendly means of transport in the aerospace and automotive industry. In this context the use of carbon fibre reinforced plastics (CFRP) which are distinguished by their outstanding mechanical properties at relatively low weight, promise significant improvements. Due to the reduction of the total mass, with the resulting lowered fuel or energy consumption and CO2 emissions during the operational phase, commercial aircraft and future vehicles will increasingly be made of CFRP. An auspicious technology for the efficient and economic production of high performance thermoset composites and hybrid structures for future lightweight applications is the combination of carbon fibre sheet moulding compound (SMC), tailored continuous carbon fibre reinforcements and metallic components in a one-shot pressing and curing process. This paper deals with a new hybrid composite technology for aerospace industries, which was developed with the help of a universal innovation and development system. This system supports the management of idea generation, the methodical development of innovative technologies and the achievement of the industrial readiness of these technologies.Keywords: development system, hybrid composite, innovation system, prepreg, sheet moulding compound
Procedia PDF Downloads 3401174 Role of Fish Hepatic Aldehyde Oxidase in Oxidative In Vitro Metabolism of Phenanthridine Heterocyclic Aromatic Compound
Authors: Khaled S. Al Salhen
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Aldehyde oxidase is molybdo-flavoenzyme involved in the oxidation of hundreds of endogenous and exogenous and N-heterocyclic compounds and environmental pollutants. Uncharged N-heterocyclic aromatic compounds such phenanthridine are commonly distributed pollutants in soil, air, sediments, surface water and groundwater, and in animal and plant tissues. Phenanthridine as uncharged N-heterocyclic aromatic compound was incubated with partially purified aldehyde oxidase from rainbow trout fish liver. Reversed-phase HLPC method was used to separate the oxidation products from phenanthridine and the metabolite was identified. The 6(5H)-phenanthridinone was identified the major metabolite by partially purified aldehyde oxidase from fish liver. Kinetic constant for the oxidation reactions were determined spectrophotometrically and showed that this substrate has a good affinity (Km = 78 ± 7.6 µM) for hepatic aldehyde oxidase, coupled with a relatively high oxidation rate (0.77± 0.03 nmol/min/mg protein). In addition, the kinetic parameters of hepatic fish aldehyde oxidase towards the phenanthridine substrate indicate that in vitro biotransformation by hepatic fish aldehyde oxidase will be a significant pathway. This study confirms that partially purified aldehyde oxidase from fish liver is indeed the enzyme responsible for the in vitro production 6(5H)-phenanthridinone metabolite as it is a major metabolite by mammalian aldehyde oxidase.Keywords: aldehyde oxidase, fish, phenanthridine, specificity
Procedia PDF Downloads 3641173 Effect of Extracorporeal Shock Wave Therapy on Post Burn Scars
Authors: Mahmoud S. Zaghloul, Mohammed M. Khalaf, Wael N. Thabet, Haidy N. Asham
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Background. Hypertrophic scarring is a difficult problem for burn patients, and scar management is an essential aspect of outpatient burn therapy. Post-burn pathologic scars involve functional and aesthetic limitations that have a dramatic influence on the patient’s quality of life. The aim was to investigate the use of extracorporeal shock wave therapy (ESWT), which targets the fibroblasts in scar tissue, as an effective modality for scar treatment in burn patients. Subjects and methods: forty patients with post-burn scars were assigned randomly into two equal groups; their ages ranged from 20-45 years. The study group received ESWT and traditional physical therapy program (deep friction massage, stretching exercises). The control group received traditional physical therapy program (deep friction massage, stretching exercises). All groups received two sessions per week for six successful weeks. The data were collected before and after the same period of treatment for both groups. Evaluation procedures were carried out to measure scar thickness using ultrasonography and Vancouver Scar Scale (VSS) was completed before and after treatment. Results: Post-treatment results showed that there was a significant improvement difference in scar thickness in both groups in favor of the study group. Percentage of improvement in scar thickness in the study group was 42.55%, while it was 12.15% in the control group. There was also a significant improvement difference between results obtained using VSS in both groups in favor of the study group. Conclusion: ESWT is effective in management of pathologic post burn scars.Keywords: extracorporeal shock wave therapy, post-burn scars, ultrasonography, Vancouver scar scale
Procedia PDF Downloads 2561172 Synthesis and Solubilization of Flurbiprofen Derivatives and Investigation of Their Biological Activities
Authors: Muhammad Mustaqeem, Musa Kaleem Baloch, Irfan Ullah, Ammarah Luqman, Afshan Ahmad
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Flurbiprofen is one of the most potent nonsteroidal anti-inflammatory drugs. It is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrhea. However, its aqueous solubility is very low and hinders the skin permeation. Thus, it is imperative to develop such a drug delivery systems which can improve its aqueous solubility and hence improve the skin permeation and therapeutic compliance. Microemulsions have been also proven to increase the cutaneous absorption of lipophilic drugs as compared to conventional vehicles. Micro-emulsion is thermodynamically stable emulsion that has the capacity to ‘hide/solubilize’ water-insoluble molecules within a continuous oil phase. Therefore, flurbiprofen was converted to Easters through chemical reactions with alcohols such as methanol, ethanol, propanol and butanol. The product was further treated with hydrazine to get hydrazide. The solubility of the parent drug Flurbiprofen and the products were solubilized in microemulsions formed using various surfactants like ionic, non-ionic and zwitterions. It has been concluded that the product was more soluble than the parent compound. The biological activities of these were also investigated. The outcome was very promising and the product was more active than the parent compound. It, therefore, concluded that in this way, we can not only enhance the solubility of the drug and increase its bioactivity, but also reduce the risk of stomach cancer.Keywords: Flurbiprofen, microemulsion, surfactants, hyrazides
Procedia PDF Downloads 2281171 Cytotoxicity of Nano β–Tricalcium Phosphate (β-TCP) on Human Osteoblast (hFOB1.19)
Authors: Jer Ping Ooi, Shah Rizal Bin Kasim, Nor Aini Saidin
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The objective of this study was to synthesize nano-sized β-tricalcium phosphate (β-TCP) powder and assess its cytotoxic effects on human osteoblast (hFOB1.19) by using four cytotoxicity assays, namely, lactose dehydrogenase (LDHe), tetrazolium hydroxide (XTT), neutral red (NR), and sulforhodamine B (SRB) assays. β-tricalcium phosphate (β-TCP) is a calcium phosphate compound commonly used as an implant material. To date, bulk-sized β-TCP is reported to be readily tolerated by the osteogenic cells and body based on in vitro, in vivo experiments and clinical studies. However, to what extent of nano-sized β-TCP will react in models as compared to bulk β-TCP is yet to be investigated. Thus, in this project, the cells were treated with nano β-TCP powder within a range of concentrations from 0 to 1000 μg/mL for 24, 48, and 72 h. The cytotoxicity tests showed that loss of cell viability ( > 50%) was high for hFOB1.19 cells in all assays. Cell cycle and apoptosis analysis of hFOB1.19 cells revealed that 50 μg/mL of the compound led to 30.5% of cells being apoptotic after 72 h of incubation, and the percentage was increased to 58.6% when the concentration was increased to 200 μg/mL. When the incubation time was increased from 24 to 72 h, the percentage of apoptotic cells increased from 17.3% to 58.6% when the hFOB1.19 were exposed with 200 μg/mL of nano β-TCP powder. Thus, both concentration and exposure duration affected the cytotoxicity effects of the nano β-TCP powder on hFOB1.19. We hypothesize that these cytotoxic effects on hFOB1.19 are related to the nano-scale size of the β-TCP.Keywords: β-tricalcium phosphate, hFOB1.19, adipose-derived mesenchymal stem cells, cytotoxicity
Procedia PDF Downloads 3161170 A Novel Small-Molecule Inhibitor of Influenza a Virus Acts by Suppressing PA Endonuclease Activity of the Viral Polymerase
Authors: Shuafeng Yuan, Bojian Zheng
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The RNA-dependent RNA polymerase of influenza a virus comprises conserved and independently folded subdomains with defined functionalities. The N-terminal domain of the PA subunit (PAN) harbors the endonuclease function so that it can serve as a desired target for drug discovery. To identify a class of anti-influenza inhibitors that impedes PAN endonuclease activity, a screening approach that integrated the fluorescence resonance energy transfer based endonuclease inhibitor assay with the DNA gel-based endonuclease inhibitor assay was conducted, followed by the evaluation of antiviral efficacies and potential cytotoxicity of the primary hits in vitro and in vivo. A small-molecule compound ANA-0 was identified as a potent inhibitor against the replication of multiple subtypes of influenza A virus, including H1N1, H3N2, H5N1, H7N7, H7N9 and H9N2, in cell cultures. Combinational treatment of zanamivir and ANA-0 exerted synergistic anti-influenza effect in vitro. Intranasal administration of ANA-0 protected mice from lethal challenge and reduced lung viral loads in H1N1 virus infected BALB/c mice. Docking analyses predicted ANA-0 bound the endonuclease cavity of PAN by interacting with the metal-binding and catalytic residues. In summary, ANA-0 shows potential to be developed to novel anti-influenza agents.Keywords: anti-influenza, novel compound, inhibition of endonuclease, PA
Procedia PDF Downloads 2451169 Investigation of Physical Properties of W-Doped CeO₂ and Mo-Doped CeO₂: A Density Functional Theory Study
Authors: Aicha Bouhlala, Sabah Chettibi
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A systematic investigation on structural, electronic, and magnetic properties of Ce₀.₇₅A₀.₂₅O₂ (A = W, Mo) is performed using first-principles calculations within the framework Full-Potential Linear Augmented Plane Wave (FP-LAPW) method based on the Density Functional Theory (DFT). The exchange-correlation potential has been treated using the generalized gradient approximation (WC-GGA) developed by Wu-Cohen. The host compound CeO2 was doped with transition metal atoms W and Mo in the doping concentration of 25% to replace the Ce atom. In structural properties, the equilibrium lattice constant is observed for the W-doped CeO₂ compound which exists within the value of 5.314 A° and the value of 5.317 A° for Mo-doped CeO2. The present results show that Ce₀.₇₅A₀.₂₅O₂ (A=W, Mo) systems exhibit semiconducting behavior in both spin channels. Although undoped CeO₂ is a non-magnetic semiconductor. The band structure of these doped compounds was plotted and they exhibit direct band gap at the Fermi level (EF) in the majority and minority spin channels. In the magnetic properties, the doped atoms W and Mo play a vital role in increasing the magnetic moments of the supercell and the values of the total magnetic moment are found to be 1.998 μB for Ce₀.₇₅W₀.₂₅O₂ and to be 2.002 μB for Ce₀.₇₅Mo₀.₂₅O₂ compounds. Calculated results indicate that the magneto-electronic properties of the Ce₁₋ₓAₓO₂(A= W, Mo) oxides supply a new way to the experimentalist for the potential applications in spintronics devices.Keywords: FP-LAPW, DFT, CeO₂, properties
Procedia PDF Downloads 2151168 Optical Properties of TlInSe₂<AU> Si̇ngle Crystals
Authors: Gulshan Mammadova
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This paper presents the results of studying the surface microrelief in 2D and 3D models and analyzing the spectroscopy of a three-junction TlInSe₂Keywords: optical properties, dielectric permittivity, real and imaginary dielectric permittivity, optical electrical conductivity
Procedia PDF Downloads 631167 To Study the Effect of Drying Temperature Towards Extraction of Aquilaria subintegra Dry Leaves Using Vacuum Far Infrared
Authors: Tengku Muhammad Rafi Nazmi Bin Tengku Razali, Habsah Alwi
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This article based on effect of temperature towards extraction of Aquilaria Subintegra. Aquilaria Subintegra which its main habitat is in Asia-tropical and particularly often found in its native which is Thailand. There is claim which is Aquilaria Subintegra contains antipyretic properties that helps fight fever. Research nowadays also shown that paracetamol consumed bring bad effect towards consumers. This sample will first dry using Vacuum Far Infrared which provides better drying than conventional oven. Soxhlet extractor used to extract oil from sample. Gas Chromatography Mass Spectrometer used to analyze sample to determine its compound. Objective from this research was to determine the active ingredients that exist in the Aquilaria Subintegra leaves and to determine whether compound of Acetaminophen exist or not inside the leaves. Moisture content from 400C was 80%, 500C was 620% and 600C was 36%. The greater temperature resulting lower moisture content inside sample leaves. 7 components were identified in sample T=400C while only 5 components were identified in sample at T=50C and T=60C. Four components were commonly identified in three sample which is 1n-Hexadecanoic acid, 9,12,15-Octadecatrienoic acid, methyl ester (z,z,z), Vitamin E and Squalene. Further studies are needed with new series of temperature to refine the best results.Keywords: aquilaria subintegra, vacuum far infrared, SOXHLET extractor, gas chromatography mass spectrometer, paracetamol
Procedia PDF Downloads 4841166 Digital Rehabilitation for Navigation Impairment
Authors: Milan N. A. Van Der Kuil, Anne M. A. Visser-Meily, Andrea W. M. Evers, Ineke J. M. Van Der Ham
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Navigation ability is essential for autonomy and mobility in daily life. In patients with acquired brain injury, navigation impairment is frequently impaired; however, in this study, we tested the effectiveness of a serious gaming training protocol as a tool for cognitive rehabilitation to reduce navigation impairment. In total, 38 patients with acquired brain injury and subjective navigation complaints completed the experiment, with a partially blind, randomized control trial design. An objective navigation test was used to construct a strengths and weaknesses profile for each patient. Subsequently, patients received personalized compensation training that matched their strengths and weaknesses by addressing an egocentric or allocentric strategy or a strategy aimed at minimizing the use of landmarks. Participants in the experimental condition received psychoeducation and a home-based rehabilitation game with a series of exercises (e.g., map reading, place finding, and turn memorization). The exercises were developed to stimulate the adoption of more beneficial strategies, according to the compensatory approach. Self-reported navigation ability (wayfinding questionnaire), participation level, and objective navigation performance were measured before and after 1 and 4 weeks after completing the six-week training program. Results indicate that the experimental group significantly improved in subjective navigation ability both 1 and 4 weeks after completion of the training, in comparison to the score before training and the scores of the control group. Similarly, goal attainment showed a significant increase after the first and fourth week after training. Objective navigation performance was not affected by the training. This navigation training protocol provides an effective solution to address navigation impairment after acquired brain injury, with clear improvements in subjective performance and goal attainment of the participants. The outcomes of the training should be re-examined after implementation in a clinical setting.Keywords: spatial navigation, cognitive rehabilitation, serious gaming, acquired brain injury
Procedia PDF Downloads 1761165 Biological Control of Karnal Bunt by Pseudomonas fluorescens
Authors: Geetika Vajpayee, Sugandha Asthana, Pratibha Kumari, Shanthy Sundaram
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Pseudomonas species possess a variety of promising properties of antifungal and growth promoting activities in the wheat plant. In the present study, Pseudomonas fluorescens MTCC-9768 is tested against plant pathogenic fungus Tilletia indica, causing Karnal bunt, a quarantine disease of wheat (Triticum aestivum) affecting kernels of wheat. It is one of the 1/A1 harmful diseases of wheat worldwide under EU legislation. This disease develops in the growth phase by the spreading of microscopically small spores of the fungus (teliospores) being dispersed by the wind. The present chemical fungicidal treatments were reported to reduce teliospores germination, but its effect is questionable since T. indica can survive up to four years in the soil. The fungal growth inhibition tests were performed using Dual Culture Technique, and the results showed inhibition by 82.5%. The interaction of antagonist bacteria-fungus causes changes in the morphology of hyphae, which was observed using Lactophenol cotton blue staining and Scanning Electron Microscopy (SEM). The rounded and swollen ends, called ‘theca’ were observed in interacted fungus as compared to control fungus (without bacterial interaction). This bacterium was tested for its antagonistic activity like protease, cellulose, HCN production, Chitinase, etc. The growth promoting activities showed increase production of IAA in bacteria. The bacterial secondary metabolites were extracted in different solvents for testing its growth inhibiting properties. The characterization and purification of the antifungal compound were done by Thin Layer Chromatography, and Rf value was calculated (Rf value = 0.54) and compared to the standard antifungal compound, 2, 4 DAPG (Rf value = 0.54). Further, the in vivo experiments showed a significant decrease in the severity of disease in the wheat plant due to direct injection method and seed treatment. Our results indicate that the extracted and purified compound from the antagonist bacteria, P. fluorescens MTCC-9768 may be used as a potential biocontrol agent against T. indica. This also concludes that the PGPR properties of the bacteria may be utilized by incorporating it into bio-fertilizers.Keywords: antagonism, Karnal bunt, PGPR, Pseudomonas fluorescens
Procedia PDF Downloads 4041164 Prediction of Boundary Shear Stress with Flood Plains Enlargements
Authors: Spandan Sahu, Amiya Kumar Pati, Kishanjit Kumar Khatua
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The river is our main source of water which is a form of open channel flow and the flow in the open channel provides with many complex phenomena of sciences that need to be tackled such as the critical flow conditions, boundary shear stress, and depth-averaged velocity. The development of society, more or less solely depends upon the flow of rivers. The rivers are major sources of many sediments and specific ingredients which are much essential for human beings. During floods, part of a river is carried by the simple main channel and rest is carried by flood plains. For such compound asymmetric channels, the flow structure becomes complicated due to momentum exchange between the main channel and adjoining flood plains. Distribution of boundary shear in subsections provides us with the concept of momentum transfer between the interface of the main channel and the flood plains. Experimentally, to get better data with accurate results are very complex because of the complexity of the problem. Hence, CES software has been used to tackle the complex processes to determine the shear stresses at different sections of an open channel having asymmetric flood plains on both sides of the main channel, and the results are compared with the symmetric flood plains for various geometrical shapes and flow conditions. Error analysis is also performed to know the degree of accuracy of the model implemented.Keywords: depth average velocity, non prismatic compound channel, relative flow depth, velocity distribution
Procedia PDF Downloads 1761163 Effect of Core Stability Exercises on Balance between Trunk Muscles in Healthy Adult Subjects
Authors: Amir A. Beltagi, Ahmed R. Abdelbaki
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Background: Core stability training has recently attracted attention for optimizing performance and improving muscle balance for healthy and unhealthy individuals. The purpose of this study was to investigate the effect of beginner’s core stability exercises on the trunk flexors’/extensors’ peak torque ratio and trunk flexors’ and extensors’ peak torques. Methods: Thirty five healthy individuals, randomly assigned into two groups; experimental (group I) and control (group II), participated in the study. Group I involved 20 participants (10 male & 10 female) with mean ±SD age, weight, and height of 20.7±2.4 years, 66.5±12.1 kg and 166.7±7.8 cm respectively. Group II involved 15 participants (6 male & 9 female) with mean ±SD age, weight, and height of 20.3±0.61 years, 68.57±12.2 kg and 164.28 ±7.59 cm respectively. Data were collected using the Biodex Isokinetic system. The participants were tested twice; before and after a 6-week period during which the experimental group performed a core stability training program. Findings: Statistical analysis using the 2x2 Mixed Design ANOVA revealed that there were no significant differences in the trunk flexors’/extensors’ peak torque ratio between the ‘pre’ and ‘post’ tests for either group (p > 0.025). Moreover, there were no significant differences in the trunk flexors’/extensors’ ratios between both groups at either test (p > 0.025). Meanwhile, the 2x2 Mixed Design MANOVA revealed that there were significant differences in the trunk flexors’ and extensors’ peak torques between the ‘pre’ and ‘post’ tests for group I (p < 0.025), while there were no significant differences inbetween for group II (p > 0.025). Moreover, there were no significant differences between both groups for the tested muscles’ peak torques at either test except for that of the trunk flexors at the ‘post’ test only (p < 0.025). Interpretation: The improvement in muscle performance indicated by the increase in the trunk flexors’ and extensors’ peak torques in the experimental group recommends including core stability training in the exercise programs that aim to improve muscle performance.Keywords: core stability, isokinetic, trunk muscles, muscle balance
Procedia PDF Downloads 3121162 Secondary Metabolites Identified from a Pseudoalteromonas rubra Bacterial Strain Isolated from a Fijian Marine Alga
Authors: James Sinclair, Katy Soapi, Brad Carte
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The marine environment has continuously demonstrated to be a rich source of secondary metabolites and bioactive compounds that can address the many pharmaceutical problems facing mankind. The emergence of multidrug resistant pathogens has caused scientists to explore contemporary ways of combating these super bugs. A red-pigmented bacterial strain isolated from a marine alga collected in Fiji was identified to be Pseudoalteromonas rubra from 16s rRNA sequencing. This bacterial strain was cultured using a yeast-peptone media and incubated for five days. The ethyl acetate extract of this bacterium was subjected to chromatographic separation techniques such as vacuum liquid chromatography, flash chromatography, size exclusion chromatography and high-pressure liquid chromatography to yield the pure compound and a number of semi-pure fractions. The crude extract and subsequent purified fractions were analyzed by ultraviolet/visible spectroscopy and mass spectroscopy and was found to contain the compounds ivermectin, stenothricin, cyclo-L-pro-L-val, prodigiosin, mycophenolic acid, phenazine-1-carboxylic acid, eplerenone, staurosporine and pseudoalteromone A. The structure of the pure compound, pseudoalteromone A, was elucidated using NMR 1H, 13C, 1H-1H COSY, HSQC and HMBC spectroscopic data.Keywords: Pseudoalteromonas rubra, Pseudoalteromone A, secondary metabolites, structure elucidation
Procedia PDF Downloads 2131161 Revolutionizing Manufacturing: Embracing Additive Manufacturing with Eggshell Polylactide (PLA) Polymer
Authors: Choy Sonny Yip Hong
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This abstract presents an exploration into the creation of a sustainable bio-polymer compound for additive manufacturing, specifically 3D printing, with a focus on eggshells and polylactide (PLA) polymer. The project initially conducted experiments using a variety of food by-products to create bio-polymers, and promising results were obtained when combining eggshells with PLA polymer. The research journey involved precise measurements, drying of PLA to remove moisture, and the utilization of a filament-making machine to produce 3D printable filaments. The project began with exploratory research and experiments, testing various combinations of food by-products to create bio-polymers. After careful evaluation, it was discovered that eggshells and PLA polymer produced promising results. The initial mixing of the two materials involved heating them just above the melting point. To make the compound 3D printable, the research focused on finding the optimal formulation and production process. The process started with precise measurements of the PLA and eggshell materials. The PLA was placed in a heating oven to remove any absorbed moisture. Handmade testing samples were created to guide the planning for 3D-printed versions. The scrap PLA was recycled and ground into a powdered state. The drying process involved gradual moisture evaporation, which required several hours. The PLA and eggshell materials were then placed into the hopper of a filament-making machine. The machine's four heating elements controlled the temperature of the melted compound mixture, allowing for optimal filament production with accurate and consistent thickness. The filament-making machine extruded the compound, producing filament that could be wound on a wheel. During the testing phase, trials were conducted with different percentages of eggshell in the PLA mixture, including a high percentage (20%). However, poor extrusion results were observed for high eggshell percentage mixtures. Samples were created, and continuous improvement and optimization were pursued to achieve filaments with good performance. To test the 3D printability of the DIY filament, a 3D printer was utilized, set to print the DIY filament smoothly and consistently. Samples were printed and mechanically tested using a universal testing machine to determine their mechanical properties. This testing process allowed for the evaluation of the filament's performance and suitability for additive manufacturing applications. In conclusion, the project explores the creation of a sustainable bio-polymer compound using eggshells and PLA polymer for 3D printing. The research journey involved precise measurements, drying of PLA, and the utilization of a filament-making machine to produce 3D printable filaments. Continuous improvement and optimization were pursued to achieve filaments with good performance. The project's findings contribute to the advancement of additive manufacturing, offering opportunities for design innovation, carbon footprint reduction, supply chain optimization, and collaborative potential. The utilization of eggshell PLA polymer in additive manufacturing has the potential to revolutionize the manufacturing industry, providing a sustainable alternative and enabling the production of intricate and customized products.Keywords: additive manufacturing, 3D printing, eggshell PLA polymer, design innovation, carbon footprint reduction, supply chain optimization, collaborative potential
Procedia PDF Downloads 721160 Separation, Identification, and Measuring Gossypol in the Cottonseed Oil and Investigating the Performance of Drugs Prepared from the Combination of Plant Extract and Oil in the Treatment of Cutaneous Leishmaniasis Resistant to Drugs
Authors: Sara Taghdisi, M. Mirmohammadi, M. Mokhtarian
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In 2013, the World Health Organization announced the cases of Cutaneous leishmaniasis infection in Iran between 69,000 to 113,000. The most common chemical drugs for Cutaneous leishmaniasis treatment are sodium stibogluconate, and meglumine antimonate, which not only have relatively many side effects, but also some species of the Leishmania genus have become resistant to them .The most prominent compound existing in different parts of the cotton plant is a yellow polyphenol called Gossypol. Gossypol is an extremely valuable compound and has anti-cancer properties. In the current project, Gossypol was extracted with a liquid-liquid extraction method in 120 minutes in the presence of Phosphoric acid from the cotton seed oil of Golestan beach varieties, then got crystallized in darkness using Acetic acid and isolated as Gossypol Acetic acid. The efficiency of the extracted crystal was obtained at 0.12+- 1.28. the cotton plant could be efficient in the treatment of Cutaneous leishmaniasis. The extract of the green-leaf cotton boll of Jargoyeh varieties was tested as an ointment on the target group of patients suffering from Cutaneous leishmaniasis resistant to drugs esistant to drugs by our colleagues in the research team. The results showed the Pearson's correlation coefficient of 0.72 between the two variables of wound diameter and the extract use over time which indicated the positive effect of this extract on the treatment of Cutaneous leishmaniasis was resistant to drugs.Keywords: cottonseed oil, crystallization, gossypol, green-leaf
Procedia PDF Downloads 1091159 The Effect of Aromatherapy Candle as Insecticide from Citrus Extract of Lemongrass (Cymbopogon) to Increase Ae. aegypti Mortality
Authors: Nurul Hidayah, Farida Rahmatika, Fathimah Azzahra, Nesty Herennadia
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Aromatherapy candles are one of the insecticide media that have not been much researched. The active ingredient that is proven to have the effect of insecticide is a citrus extract from lemongrass oil (Cymbopogon). Aromatherapy candles are added by citrus compounds to be insecticidal for Ae. aegypti mosquito that was related to the infectious disease such as dengue fever. This research aims to find out if aromatherapy candles of citrus compounds have an insecticidal effect on Ae. aegypti mosquito. We used true experimental design including posttest only with control group design. The samples are 20 male and female Ae. aegypti mosquitos with aged 1-7 days belong to the inclusion criteria. The subjects were divided into 6 groups, consisting of 1 negative control group and 5 treatment groups with variation concentration are 1%; 2%; 3%; 4%; 5%. Each group will be treated for 2 hours and observed death after 24 hours. Replication in each group is done 4 times. The results were then tested statistically using Kruskal-Wallis and probit test. Mean of death in negative control group, and treatment group 1%; 2%; 3%; 4%; 5% respectively 0; 1; 0.25; 0; 1 and 1 mosquito. The Kruskal-Wallis test in the study group found no significant difference (p = 0.178). The probit analysis showed that LC50 and LC90 were 20.069% and 31.557%. The aromatherapy candle of a citrus compound has an insecticidal effect on the Ae aegypti mosquito.Keywords: Ae. aegypti insecticide, aromatherapy candle, citrus compound, lemongrass oil (Cymbopogon)
Procedia PDF Downloads 1891158 MTT Assay-Guided Isolation of a Cytotoxic Lead from Hedyotis umbellata and Its Mechanism of Action against Non-Small Cell Lung Cancer A549 Cells
Authors: Kirti Hira, A. Sajeli Begum, S. Mahibalan, Poorna Chandra Rao
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Introduction: Cancer is one of the leading causes of death worldwide. Although existing therapy effectively kills cancer cells, they do affect normal growing cells leading to many undesirable side effects. Hence there is need to develop effective as well as safe drug molecules to combat cancer, which is possible through phyto-research. The currently available plant-derived blockbuster drugs are the example for this. In view of this, an investigation was done to identify cytotoxic lead molecules from Hedyotis umbellata (Family Rubiaceae), a widely distributed weed in India. Materials and Methods: The methanolic extract of the whole plant of H. umbellata (MHU), prepared through Soxhlet extraction method was further fractionated with diethyl ether and n-butanol, successively. MHU, ether fraction (EMHU) and butanol fraction (BMHU) were lyophilized and were tested for the cytotoxic effect using 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay against non-small cell lung cancer (NSCLC) A549 cell lines. The potentially active EMHU was subjected to chromatographic purification using normal-phase silica columns, in order to isolate the responsible bioactive compounds. The isolated pure compounds were tested for their cytotoxic effect by MTT assay against A549 cells. Compound-3, which was found to be most active, was characterized using IR, 1H- and 13C-NMR and MS analysis. The study was further extended to decipher the mechanism of action of cytotoxicity of compound-3 against A549 cells through various in vitro cellular models. Cell cycle analysis was done using flow cytometry following PI (Propidium Iodide) staining. Protein analysis was done using Western blot technique. Results: Among MHU, EMHU, and BMHU, the non-polar fraction EMHU demonstrated a significant dose-dependent cytotoxic effect with IC50 of 67.7μg/ml. Chromatography of EMHU yielded seven compounds. MTT assay of isolated compounds explored compound-3 as potentially active one, which inhibited the growth of A549 cells with IC50value of 14.2μM. Further, compound-3 was identified as cedrelopsin, a coumarin derivative having molecular weight of 260. Results of in vitro mechanistic studies explained that cedrelopsin induced cell cycle arrest at G2/M phase and down-regulated the expression of G2/M regulatory proteins such as cyclin B1, cdc2, and cdc25C, dose dependently. This is the first report that explores the cytotoxic mechanism of cedrelopsin. Conclusion: Thus a potential small lead molecule, cedrelopsin isolated from H. umbellata, showing antiproliferative effect mediated by G2/M arrest in A549 cells was discovered. The effect of cedrelopsin against other cancer cell lines followed by in vivo studies can be performed in future to develop a new drug candidate.Keywords: A549, cedrelopsin, G2/M phase, Hedyotis umbellata
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