Search results for: target hiding
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 2729

Search results for: target hiding

1079 Organotin (IV) Based Complexes as Promiscuous Antibacterials: Synthesis in vitro, in Silico Pharmacokinetic, and Docking Studies

Authors: Wajid Rehman, Sirajul Haq, Bakhtiar Muhammad, Syed Fahad Hassan, Amin Badshah, Muhammad Waseem, Fazal Rahim, Obaid-Ur-Rahman Abid, Farzana Latif Ansari, Umer Rashid

Abstract:

Five novel triorganotin (IV) compounds have been synthesized and characterized. The tin atom is penta-coordinated to assume trigonal-bipyramidal geometry. Using in silico derived parameters; the objective of our study is to design and synthesize promiscuous antibacterials potent enough to combat resistance. Among various synthesized organotin (IV) complexes, compound 5 was found as potent antibacterial agent against various bacterial strains. Further lead optimization of drug-like properties was evaluated through in silico predictions. Data mining and computational analysis were utilized to derive compound promiscuity phenomenon to avoid drug attrition rate in designing antibacterials. Xanthine oxidase and human glucose- 6-phosphatase were found as only true positive off-target hits by ChEMBL database and others utilizing similarity ensemble approach. Propensity towards a-3 receptor, human macrophage migration factor and thiazolidinedione were found as false positive off targets with E-value 1/4> 10^-4 for compound 1, 3, and 4. Further, displaying positive drug-drug interaction of compound 1 as uricosuric was validated by all databases and docked protein targets with sequence similarity and compositional matrix alignment via BLAST software. Promiscuity of the compound 5 was further confirmed by in silico binding to different antibacterial targets.

Keywords: antibacterial activity, drug promiscuity, ADMET prediction, metallo-pharmaceutical, antimicrobial resistance

Procedia PDF Downloads 491
1078 Implementing Service Learning in the Health Education Curriculum

Authors: Karen Butler

Abstract:

Johnson C. Smith University, one of the nation’s oldest Historically Black Colleges and Universities, has a strong history of service learning and community service. We first integrated service learning and peer education into health education courses in the spring of 2000. Students enrolled in the classes served as peer educators for the semester. Since then, the program has evolved and expanded but remains an integral part of several courses. The purpose of this session is to describe our program in terms of development, successes, and obstacles, and feedback received. A detailed description of the service learning component in HED 235: Drugs and Drug Education and HED 337: Environmental Health will be provided. These classes are required of our Community Health majors but are also popular electives for students in other disciplines. Three sources of student feedback were used to evaluate and continually modify the component: the SIR II course evaluation, service learning reflection papers, and focus group interviews. Student feedback has been largely positive. When criticism was given, it was thoughtful and constructive – given in the spirit of making it better for the next group. Students consistently agreed that the service learning program increased their awareness of pertinent health issues; that both the service providers and service recipients benefited from the project; and that the goals/issues targeted by the service learning component fit the objectives of the course. Also, evidence of curriculum and learning enhancement was found in the reflection papers and focus group sessions. Service learning sets up a win-win situation. It provides a way to respond to campus and community health needs while enhancing the curriculum, as students learn more by doing things that benefit the health and wellness of others. Service learning is suitable for any health education course and any target audience would welcome the effort.

Keywords: black colleges, community health, health education, service learning

Procedia PDF Downloads 331
1077 Assessment of Forage Utilization for Pasture-Based Livestock Production in Udubo Grazing Reserve, Bauchi State

Authors: Mustapha Saidu, Bilyaminu Mohammed

Abstract:

The study was conducted in Udubo Grazing Reserve between July 2019 and October 2019 to assess forage utilization for pasture-based livestock production in reserve. The grazing land was cross-divided into grids, where 15 coordinates were selected as the sample points. Grids of one-kilometer interval were made. The grids were systematically selected 1 grid after 7 grids. 1 × 1-meter quadrat was made at the coordinate of the selected grids for measurement, estimation, and sample collection. The results of the study indicated that Zornia glochidiatah has the highest percent of species composition (42%), while Mitracarpus hirtus has the lowest percent (0.1%). Urochloa mosambicensis has 48 percent of height removed and 27 percent used by weight, Zornia glochidiata 60 percent of height removed and 57 percent used by weight, Alysicapus veginalis has 55 percent of height removed, and 40 percent used by weight, and Cenchrus biflorus has 40 percent of height removed and 28 percent used by weight. The target is 50 percent utilization of forage by weight during a grazing period as well as at the end of the grazing season. The study found that Orochloa mosambicensis, Alysicarpus veginalis, and Cenchrus biflorus had lower percent by weight which is normal, while Zornia glochidiata had a higher percent by weight which is an indication of danger. The study recommends that the identification of key plant species in pasture and rangeland is critical to implementing a successful grazing management plan. There should be collective action and promotion of historically generated grazing knowledge through public and private advocacies.

Keywords: forage, grazing reserve, live stock, pasture, plant species

Procedia PDF Downloads 66
1076 Creating Risk Maps on the Spatiotemporal Occurrence of Agricultural Insecticides in Sub-Saharan Africa

Authors: Chantal Hendriks, Harry Gibson, Anna Trett, Penny Hancock, Catherine Moyes

Abstract:

The use of modern inputs for crop protection, such as insecticides, is strongly underestimated in Sub-Saharan Africa. Several studies measured toxic concentrations of insecticides in fruits, vegetables and fish that were cultivated in Sub-Saharan Africa. The use of agricultural insecticides has impact on human and environmental health, but it also has the potential to impact on insecticide resistance in malaria transmitting mosquitos. To analyse associations between historic use of agricultural insecticides and the distribution of insecticide resistance through space and time, the use and environmental fate of agricultural insecticides needs to be mapped through the same time period. However, data on the use and environmental fate of agricultural insecticides in Africa are limited and therefore risk maps on the spatiotemporal occurrence of agricultural insecticides are created using environmental data. Environmental data on crop density and crop type were used to select the areas that most likely receive insecticides. These areas were verified by a literature review and expert knowledge. Pesticide fate models were compared to select most dominant processes that are involved in the environmental fate of insecticides and that can be mapped at a continental scale. The selected processes include: surface runoff, erosion, infiltration, volatilization and the storing and filtering capacity of soils. The processes indicate the risk for insecticide accumulation in soil, water, sediment and air. A compilation of all available data for traces of insecticides in the environment was used to validate the maps. The risk maps can result in space and time specific measures that reduce the risk of insecticide exposure to non-target organisms.

Keywords: crop protection, pesticide fate, tropics, insecticide resistance

Procedia PDF Downloads 131
1075 Links Between Maternal Trauma, Response to Distress, and Toddler Internalizing and Externalizing Behaviors: A Mediational Analysis

Authors: Zena Ebrahim, Susan Woodhouse

Abstract:

Previous research shows that mothers’ experiences of trauma are linked to their child’s later socioemotional functioning. However, the mechanisms involved are not well understood. One potential mediator is maternal insensitive responses to child distress. This study examined the link between maternal trauma, mothers’ responses to toddler distress, and toddlers’ socioemotional outcomes among a socioeconomically diverse sample of 110 mothers and their 12- to 35-month-old toddlers. It was hypothesized that a mother’s difficulty in responding sensitively to her child’s distress would mediate the relations between maternal trauma and child internalizing and externalizing behaviors. Two mediational models were tested to examine non-supportive responses to distress as a potential mediator of the relation between maternal trauma and toddler mental health outcomes; one model focused on predicting child internalizing symptoms and the other focused on predicting child externalizing symptoms. Measures included assessment of maternal trauma (Life Stressor Checklist-Revised), mothers’ responses to child distress (Coping with Toddlers’ Negative Emotions Scale), and toddler socioemotional functioning (Infant-Toddler Social and Emotional Assessment). Results revealed that the relations between maternal trauma and toddler symptoms (internalizing and externalizing symptoms) were mediated by maternal non-supportive response to child distress for both internalizing and externalizing domains of child mental health. Findings suggest the importance of early intervention for trauma-exposed mothers and target areas for parenting interventions.

Keywords: trauma, parenting, child mental health, transgenerational effects of trauma

Procedia PDF Downloads 146
1074 hsa-miR-1204 and hsa-miR-639 Prominent Role in Tamoxifen's Molecular Mechanisms on the EMT Phenomenon in Breast Cancer Patients

Authors: Mahsa Taghavi

Abstract:

In the treatment of breast cancer, tamoxifen is a regularly prescribed medication. The effect of tamoxifen on breast cancer patients' EMT pathways was studied. In this study to see if it had any effect on the cancer cells' resistance to tamoxifen and to look for specific miRNAs associated with EMT. In this work, we used continuous and integrated bioinformatics analysis to choose the optimal GEO datasets. Once we had sorted the gene expression profile, we looked at the mechanism of signaling, the ontology of genes, and the protein interaction of each gene. In the end, we used the GEPIA database to confirm the candidate genes. after that, I investigated critical miRNAs related to candidate genes. There were two gene expression profiles that were categorized into two distinct groups. Using the expression profile of genes that were lowered in the EMT pathway, the first group was examined. The second group represented the polar opposite of the first. A total of 253 genes from the first group and 302 genes from the second group were found to be common. Several genes in the first category were linked to cell death, focal adhesion, and cellular aging. Two genes in the second group were linked to cell death, focal adhesion, and cellular aging. distinct cell cycle stages were observed. Finally, proteins such as MYLK, SOCS3, and STAT5B from the first group and BIRC5, PLK1, and RAPGAP1 from the second group were selected as potential candidates linked to tamoxifen's influence on the EMT pathway. hsa-miR-1204 and hsa-miR-639 have a very close relationship with the candidates genes according to the node degrees and betweenness index. With this, the action of tamoxifen on the EMT pathway was better understood. It's important to learn more about how tamoxifen's target genes and proteins work so that we can better understand the drug.

Keywords: tamoxifen, breast cancer, bioinformatics analysis, EMT, miRNAs

Procedia PDF Downloads 118
1073 Biophysical Consideration in the Interaction of Biological Cell Membranes with Virus Nanofilaments

Authors: Samaneh Farokhirad, Fatemeh Ahmadpoor

Abstract:

Biological membranes are constantly in contact with various filamentous soft nanostructures that either reside on their surface or are being transported between the cell and its environment. In particular, viral infections are determined by the interaction of viruses (such as filovirus) with cell membranes, membrane protein organization (such as cytoskeletal proteins and actin filament bundles) has been proposed to influence the mechanical properties of lipid membranes, and the adhesion of filamentous nanoparticles influence their delivery yield into target cells or tissues. The goal of this research is to integrate the rapidly increasing but still fragmented experimental observations on the adhesion and self-assembly of nanofilaments (including filoviruses, actin filaments, as well as natural and synthetic nanofilaments) on cell membranes into a general, rigorous, and unified knowledge framework. The global outbreak of the coronavirus disease in 2020, which has persisted for over three years, highlights the crucial role that nanofilamentbased delivery systems play in human health. This work will unravel the role of a unique property of all cell membranes, namely flexoelectricity, and the significance of nanofilaments’ flexibility in the adhesion and self-assembly of nanofilaments on cell membranes. This will be achieved utilizing a set of continuum mechanics, statistical mechanics, and molecular dynamics and Monte Carlo simulations. The findings will help address the societal needs to understand biophysical principles that govern the attachment of filoviruses and flexible nanofilaments onto the living cells and provide guidance on the development of nanofilament-based vaccines for a range of diseases, including infectious diseases and cancer.

Keywords: virus nanofilaments, cell mechanics, computational biophysics, statistical mechanics

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1072 Feature Selection of Personal Authentication Based on EEG Signal for K-Means Cluster Analysis Using Silhouettes Score

Authors: Jianfeng Hu

Abstract:

Personal authentication based on electroencephalography (EEG) signals is one of the important field for the biometric technology. More and more researchers have used EEG signals as data source for biometric. However, there are some disadvantages for biometrics based on EEG signals. The proposed method employs entropy measures for feature extraction from EEG signals. Four type of entropies measures, sample entropy (SE), fuzzy entropy (FE), approximate entropy (AE) and spectral entropy (PE), were deployed as feature set. In a silhouettes calculation, the distance from each data point in a cluster to all another point within the same cluster and to all other data points in the closest cluster are determined. Thus silhouettes provide a measure of how well a data point was classified when it was assigned to a cluster and the separation between them. This feature renders silhouettes potentially well suited for assessing cluster quality in personal authentication methods. In this study, “silhouettes scores” was used for assessing the cluster quality of k-means clustering algorithm is well suited for comparing the performance of each EEG dataset. The main goals of this study are: (1) to represent each target as a tuple of multiple feature sets, (2) to assign a suitable measure to each feature set, (3) to combine different feature sets, (4) to determine the optimal feature weighting. Using precision/recall evaluations, the effectiveness of feature weighting in clustering was analyzed. EEG data from 22 subjects were collected. Results showed that: (1) It is possible to use fewer electrodes (3-4) for personal authentication. (2) There was the difference between each electrode for personal authentication (p<0.01). (3) There is no significant difference for authentication performance among feature sets (except feature PE). Conclusion: The combination of k-means clustering algorithm and silhouette approach proved to be an accurate method for personal authentication based on EEG signals.

Keywords: personal authentication, K-mean clustering, electroencephalogram, EEG, silhouettes

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1071 The Fabrication of Stress Sensing Based on Artificial Antibodies to Cortisol by Molecular Imprinted Polymer

Authors: Supannika Klangphukhiew, Roongnapa Srichana, Rina Patramanon

Abstract:

Cortisol has been used as a well-known commercial stress biomarker. A homeostasis response to psychological stress is indicated by an increased level of cortisol produced in hypothalamus-pituitary-adrenal (HPA) axis. Chronic psychological stress contributing to the high level of cortisol relates to several health problems. In this study, the cortisol biosensor was fabricated that mimicked the natural receptors. The artificial antibodies were prepared using molecular imprinted polymer technique that can imitate the performance of natural anti-cortisol antibody with high stability. Cortisol-molecular imprinted polymer (cortisol-MIP) was obtained using the multi-step swelling and polymerization protocol with cortisol as a target molecule combining methacrylic acid:acrylamide (2:1) with bisacryloyl-1,2-dihydroxy-1,2-ethylenediamine and ethylenedioxy-N-methylamphetamine as cross-linkers. Cortisol-MIP was integrated to the sensor. It was coated on the disposable screen-printed carbon electrode (SPCE) for portable electrochemical analysis. The physical properties of Cortisol-MIP were characterized by means of electron microscope techniques. The binding characteristics were evaluated via covalent patterns changing in FTIR spectra which were related to voltammetry response. The performance of cortisol-MIP modified SPCE was investigated in terms of detection range, high selectivity with a detection limit of 1.28 ng/ml. The disposable cortisol biosensor represented an application of MIP technique to recognize steroids according to their structures with feasibility and cost-effectiveness that can be developed to use in point-of-care.

Keywords: stress biomarker, cortisol, molecular imprinted polymer, screen-printed carbon electrode

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1070 Genre Hybridity and Postcolonialism in 'Chairil: The Voice of Indonesia's Decolonisation'

Authors: Jack Johnstone

Abstract:

This research presents postcolonial translation as an approach to eradicate traces of colonialism in former colonies. An example of demonstrating postcolonial translation in the Indonesian context is in Hasan Aspahani's Chairil, a biographical narrative and history book based on the personal life of a well-known Indonesian poet and writer, Chairil Anwar (1922-1949) in Dutch occupied Indonesia. This postcolonial translation approach has been applied in the first five chapters on his early years under Dutch colonization, in an attempt to show a postcolonialised TT. This approach aims to demonstrate the postcolonial refutation of the Dutch colonial language to convey the Indonesian setting to target readers. It is also designed to explicate the summary of the book as well as my attempt to apply postcolonial translation as a strategy to reject the Dutch colonial terms in this book. The data conveys 26 important examples of the ST and TT, in consideration of the chosen three factors of culture, forced-Europeanisation, and cross-genre between a biographical narrative and history under categories of Cultural Bound Objects, Politics and Place. However, the 10 selected examples will be analyzed in the Analysis Chapter, which are discussed at word, sentence, and paragraph level. As well, the translation strategies used, namely retention, substitution and specification on four main examples, on the methods utilized to achieve a postcolonialised translation that attempts to 1) examine the way the alteration of the TT can affect the message portrayed within the ST, 2) show the notion of disagreement between the Dutch colonizers and colonized Indonesians on their views on the way Indonesia should be governed and 3) present a translation that reverses the inequality between the superior colonials and inferior Indigenous Indonesians during the Dutch colonial era.

Keywords: Chairil, Dutch colonialism, Indonesia, postcolonial translation

Procedia PDF Downloads 149
1069 Determining the Prevalence and Correlates of Depression among Transgenders of a Developing Country

Authors: Usama Bin Zubair, Muhammad Azeem

Abstract:

Introduction: Depression has been one of the most commonly diagnosed mental health disorders in Pakistan. A Census conducted by the government of Pakistan in 2017 showed that more than 10000 trans-genders live in Pakistan. HIV, illicit substance use and mental health issues, including depression, have been the main health problems faced by them. Trans-gender population has been suffering from depressive illness more than normal population all over the world. Aim: To assess the prevalence of depression among the transgender population and analyze the relationship of socio-demographic factors with depression. Subjects and Methods: The sample population comprised of one hundred and forty-two transgender people of Rawalpindi and Islamabad. Beck depressive inventory II (BDI-II) was used to record the presence and severity of the depressive symptoms. Depressive symptoms were categorized as mild, moderate and severe. Relationship of the age, smoking, family income, illicit substance use and education were studied with the presence of depressive symptoms among these transgender people of twin cities of Pakistan. Results: A total of 142 transgender people were included in the final analysis. The mean age of the study participants was 39.55 ± 6.18. Out of these, 45.1% had no depressive symptoms while 31.7% had mild, 12.7% had moderate and 10.6% had severe depressive symptomatology. After applying the binary logistic regression, we found that the presence of depressive symptoms had a significant association with illicit substance use among the target population. Conclusion: This study showed a high prevalence of depressive symptoms among the transgender population in the twin cities of Pakistan. Use of illicit substances like tobacco, cannabis, opiates, and alcohol should be discouraged to prevent mental health problems.

Keywords: depression, transgender, prevalence, sociodemographic factors

Procedia PDF Downloads 108
1068 Towards Renewable Energy: A Qualitative Study of Biofuel Development Policy in Indonesia

Authors: Arie Yanwar Kapriadi

Abstract:

This research is aiming to develop deeper understanding of the scale of power that shaped the biofuel policy. This research is important for the following reasons. Firstly, this research will enrich the body of literature within the field of political ecology, scale and environmental governance. Secondly, by focussing on energy transition policies, this research offers a critical perspective on how government policy, aimed at delivering low carbon sustainable energy systems, being scaled and implemented through multi variate stakeholders. Finally, the research could help the government of Indonesia as a policy evaluation on delivering low carbon sustainable energy systems at the macro level that (possibility) being unable to be delivered at different scale and instead being perceived differently by different stakeholders. Qualitative method is applied particularly an in depth interview with government officials as well as policy stakeholders outside of government and people in positions of responsibility with regards to policy delivery. There are 4 field study location where interview took place as well as sites visit to some biofuel refining facilities. There are some major companies which involve on the production and distribution of biofuel and its relation with biofuel feedstock industry as the source of data. The research investigates how the government biofuel policies correlated with other policy issues such as land reclassification and carbon emission reduction which also influenced plantations expansion as well as its impact on the local people. The preliminary result shows tension of power between governing authorities caused the Indonesian biofuel policy being unfocused which led to failing to meet its mandatory blending target despite the abundance of its feedstock.

Keywords: biofuel, energy transition, renewable energy, political ecology

Procedia PDF Downloads 183
1067 Relationship Between In-Service Training and Employees’ Feeling of Psychological Ownership

Authors: Mahsa Kallhor Mohammadi, Hamideh Reshadatjoo

Abstract:

This study verified the relationship between in-service training and employees’ feeling of psychological ownership. This research applied a descriptive survey that investigated a correlation between variables. The target population was 140 employees of a Drilling Fluid and Waste Management Service Company, and the sample was 123 employees who were selected randomly and encouraged to complete an electronic questionnaire which was designed based on standard questionnaires for research variables covering 62 questions. The face validity of the questionnaire was supported by an experimental test, and its content validity was approved by the thesis supervisor and consulting advisor. For the descriptive statistics frequency tables and diagrams, measures of central tendency such as mode, median, and mean and measures of variability such as variance, standards deviation, and quartile deviation were used. In the inferential statistics section, the Pearson correlation coefficient was used to verify the relationship between the variables of the research. According to the results, all of the research hypotheses were supported. According to hypothesis 1, there was a positive and significant relationship between training policy-making and employees’ psychological ownership (r=0/408, α=0/05). According to hypothesis 2, there was a positive and significant relationship between training planning and employees’ psychological ownership (r=0/446, α=0/05). According to hypothesis 3, there was a positive and significant relationship between providing the training and employees’ psychological ownership (r=0/512, α=0/05). According to hypothesis 4, there was a positive and significant relationship between training performance management and employees’ psychological ownership (r=0/462, α=0/05). According to hypothesis 5, there was a positive and significant relationship between employees’ motivation and psychological ownership (r=0/694, α=0/05). Therefore, through systematic in-service training, which is in the same line with the strategic goals of an organization and is based on scientific needs analysis, design, implementation, and evaluation, it is possible to improve employees’ sense of psychological ownership toward an organization.

Keywords: in-service training, motivation, organizational behavior, psychological ownership

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1066 Impure CO₂ Solubility Trapping in Deep Saline Aquifers: Role of Operating Conditions

Authors: Seyed Mostafa Jafari Raad, Hassan Hassanzadeh

Abstract:

Injection of impurities along with CO₂ into saline aquifers provides an exceptional prospect for low-cost carbon capture and storage technologies and can potentially accelerate large-scale implementation of geological storage of CO₂. We have conducted linear stability analyses and numerical simulations to investigate the effects of permitted impurities in CO₂ streams on the onset of natural convection and dynamics of subsequent convective mixing. We have shown that the rate of dissolution of an impure CO₂ stream with H₂S highly depends on the operating conditions such as temperature, pressure, and composition of impurity. Contrary to findings of previous studies, our results show that an impurity such as H₂S can potentially reduce the onset time of natural convection and can accelerate the subsequent convective mixing. However, at the later times, the rate of convective dissolution is adversely affected by the impurities. Therefore, the injection of an impure CO₂ stream can be engineered to improve the rate of dissolution of CO₂, which leads to higher storage security and efficiency. Accordingly, we have identified the most favorable CO₂ stream compositions based on the geophysical properties of target aquifers. Information related to the onset of natural convection such as the scaling relations and the most favorable operating conditions for CO₂ storage developed in this study are important in proper design, site screening, characterization and safety of geological storage. This information can be used to either identify future geological candidates for acid gas disposal or reviewing the current operating conditions of licensed injection sites.

Keywords: CO₂ storage, solubility trapping, convective dissolution, storage efficiency

Procedia PDF Downloads 188
1065 Assessment of Isatin as Surface Recognition Group: Design, Synthesis and Anticancer Evaluation of Hydroxamates as Novel Histone Deacetylase Inhibitors

Authors: Harish Rajak, Kamlesh Raghuwanshi

Abstract:

Histone deacetylase (HDAC) are promising target for cancer treatment. The panobinostat (Farydak; Novartis; approved by USFDA in 2015) and chidamide (Epidaza; Chipscreen Biosciences; approved by China FDA in 2014) are the novel HDAC inhibitors ratified for the treatment of patients with multiple myeloma and peripheral T cell lymphoma, respectively. On the other hand, two other HDAC inhibitors, Vorinostat (SAHA; approved by USFDA in 2006) and Romidepsin (FK228; approved by USFDA in 2009) are already in market for the treatment of cutaneous T-cell lymphoma. Several hydroxamic acid based HDAC inhibitors i.e., belinostat, givinostat, PCI24781 and JNJ26481585 are in clinical trials. HDAC inhibitors consist of three pharmacophoric features - an aromatic cap group, zinc binding group (ZBG) and a linker chain connecting cap group to ZBG. Herein, we report synthesis, characterization and biological evaluation of HDAC inhibitors possessing substituted isatin moiety as cap group which recognize the surface of active enzyme pocket and thiosemicarbazide moiety incorporated as linker group responsible for connecting cap group to ZBG (hydroxamic acid). Several analogues were found to inhibit HDAC and cellular proliferation of Hela cervical cancer cells with GI50 values in the micro molar range. Some of the compounds exhibited promising results in vitro antiproliferative studies. Attempts were also made to establish the structure activity relationship among synthesized HDAC inhibitors.

Keywords: HDAC inhibitors, hydroxamic acid derivatives, isatin derivatives, antiproliferative activity, docking

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1064 Microwave Synthesis and Molecular Docking Studies of Azetidinone Analogous Bearing Diphenyl Ether Nucleus as a Potent Antimycobacterial and Antiprotozoal Agent

Authors: Vatsal M. Patel, Navin B. Patel

Abstract:

The present studies deal with the developing a series bearing a diphenyl ethers nucleus using structure-based drug design concept. A newer series of diphenyl ether based azetidinone namely N-(3-chloro-2-oxo-4-(3-phenoxyphenyl)azetidin-1-yl)-2-(substituted amino)acetamide (2a-j) have been synthesized by condensation of m-phenoxybenzaldehyde with 2-(substituted-phenylamino)acetohydrazide followed by the cyclisation of resulting Schiff base (1a-j) by conventional method as well as microwave heating approach as a part of an environmentally benign synthetic protocol. All the synthesized compounds were characterized by spectral analysis and were screened for in vitro antimicrobial, antitubercular and antiprotozoal activity. The compound 2f was found to be most active M. tuberculosis (6.25 µM) MIC value in the primary screening as well as this same derivative has been found potency against L. mexicana and T. cruzi with MIC value 2.09 and 6.69 µM comparable to the reference drug Miltefosina and Nifurtimox. To provide understandable evidence to predict binding mode and approximate binding energy of a compound to a target in the terms of ligand-protein interaction, all synthesized compounds were docked against an enoyl-[acyl-carrier-protein] reductase of M. tuberculosis (PDB ID: 4u0j). The computational studies revealed that azetidinone derivatives have a high affinity for the active site of enzyme which provides a strong platform for new structure-based design efforts. The Lipinski’s parameters showed good drug-like properties and can be developed as an oral drug candidate.

Keywords: antimycobacterial, antiprotozoal, azetidinone, diphenylether, docking, microwave

Procedia PDF Downloads 145
1063 Performance Analysis of New Types of Reference Targets Based on Spaceborne and Airborne SAR Data

Authors: Y. S. Zhou, C. R. Li, L. L. Tang, C. X. Gao, D. J. Wang, Y. Y. Guo

Abstract:

Triangular trihedral corner reflector (CR) has been widely used as point target for synthetic aperture radar (SAR) calibration and image quality assessment. The additional “tip” of the triangular plate does not contribute to the reflector’s theoretical RCS and if it interacts with a perfectly reflecting ground plane, it will yield an increase of RCS at the radar bore-sight and decrease the accuracy of SAR calibration and image quality assessment. Regarding this problem, two types of CRs were manufactured. One was the hexagonal trihedral CR. It is a self-illuminating CR with relatively small plate edge length, while large edge length usually introduces unexpected edge diffraction error. The other was the triangular trihedral CR with extended bottom plate which considers the effect of ‘tip’ into the total RCS. In order to assess the performance of the two types of new CRs, flight campaign over the National Calibration and Validation Site for High Resolution Remote Sensors was carried out. Six hexagonal trihedral CRs and two bottom-extended trihedral CRs, as well as several traditional triangular trihedral CRs, were deployed. KOMPSAT-5 X-band SAR image was acquired for the performance analysis of the hexagonal trihedral CRs. C-band airborne SAR images were acquired for the performance analysis of the bottom-extended trihedral CRs. The analysis results showed that the impulse response function of both the hexagonal trihedral CRs and bottom-extended trihedral CRs were much closer to the ideal sinc-function than the traditional triangular trihedral CRs. The flight campaign results validated the advantages of new types of CRs and they might be useful in the future SAR calibration mission.

Keywords: synthetic aperture radar, calibration, corner reflector, KOMPSAT-5

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1062 Managing Data from One Hundred Thousand Internet of Things Devices Globally for Mining Insights

Authors: Julian Wise

Abstract:

Newcrest Mining is one of the world’s top five gold and rare earth mining organizations by production, reserves and market capitalization in the world. This paper elaborates on the data acquisition processes employed by Newcrest in collaboration with Fortune 500 listed organization, Insight Enterprises, to standardize machine learning solutions which process data from over a hundred thousand distributed Internet of Things (IoT) devices located at mine sites globally. Through the utilization of software architecture cloud technologies and edge computing, the technological developments enable for standardized processes of machine learning applications to influence the strategic optimization of mineral processing. Target objectives of the machine learning optimizations include time savings on mineral processing, production efficiencies, risk identification, and increased production throughput. The data acquired and utilized for predictive modelling is processed through edge computing by resources collectively stored within a data lake. Being involved in the digital transformation has necessitated the standardization software architecture to manage the machine learning models submitted by vendors, to ensure effective automation and continuous improvements to the mineral process models. Operating at scale, the system processes hundreds of gigabytes of data per day from distributed mine sites across the globe, for the purposes of increased improved worker safety, and production efficiency through big data applications.

Keywords: mineral technology, big data, machine learning operations, data lake

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1061 Analysis of the Cutting Force with Ultrasonic Assisted Manufacturing of Steel (S235JR)

Authors: Philipp Zopf, Franz Haas

Abstract:

Manufacturing of very hard and refractory materials like ceramics, glass or carbide poses particular challenges on tools and machines. The company Sauer GmbH developed especially for this application area ultrasonic tool holders working in a frequency range from 15 to 60 kHz and superimpose the common tool movement in the vertical axis. This technique causes a structural weakening in the contact area and facilitates the machining. The possibility of the force reduction for these special materials especially in drilling of carbide with diamond tools up to 30 percent made the authors try to expand the application range of this method. To make the results evaluable, the authors decide to start with existing processes in which the positive influence of the ultrasonic assistance is proven to understand the mechanism. The comparison of a grinding process the Institute use to machine materials mentioned in the beginning and steel could not be more different. In the first case, the authors use tools with geometrically undefined edges. In the second case, the edges are geometrically defined. To get valid results of the tests, the authors decide to investigate two manufacturing methods, drilling and milling. The main target of the investigation is to reduce the cutting force measured with a force measurement platform underneath the workpiece. Concerning to the direction of the ultrasonic assistance, the authors expect lower cutting forces and longer endurance of the tool in the drilling process. To verify the frequencies and the amplitudes an FFT-analysis is performed. It shows the increasing damping depending on the infeed rate of the tool. The reducing of amplitude of the cutting force comes along.

Keywords: drilling, machining, milling, ultrasonic

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1060 African Swine Fewer Situation and Diagnostic Methods in Lithuania

Authors: Simona Pileviciene

Abstract:

On 24th January 2014, Lithuania notified two primary cases of African swine fever (ASF) in wild boars. The animals were tested positive for ASF virus (ASFV) genome by real-time PCR at the National Reference Laboratory for ASF in Lithuania (NRL), results were confirmed by the European Union Reference Laboratory for African swine fever (CISA-INIA). Intensive wild and domestic animal monitoring program was started. During the period of 2014-2017 ASF was confirmed in two large commercial pig holding with the highest biosecurity. Pigs were killed and destroyed. Since 2014 ASF outbreak territory from east and south has expanded to the middle of Lithuania. Diagnosis by PCR is one of the highly recommended diagnostic methods by World Organization for Animal Health (OIE) for diagnosis of ASF. The aim of the present study was to compare singleplex real-time PCR assays to a duplex assay allowing the identification of ASF and internal control in a single PCR tube and to compare primers, that target the p72 gene (ASF 250 bp and ASF 75 bp) effectivity. Multiplex real-time PCR assays prove to be less time consuming and cost-efficient and therefore have a high potential to be applied in the routine analysis. It is important to have effective and fast method that allows virus detection at the beginning of disease for wild boar population and in outbreaks for domestic pigs. For experiments, we used reference samples (INIA, Spain), and positive samples from infected animals in Lithuania. Results show 100% sensitivity and specificity.

Keywords: African swine fewer, real-time PCR, wild boar, domestic pig

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1059 Detection of Transgenes in Cotton (Gossypium hirsutum L.) by using Biotechnology/Molecular Biological Techniques

Authors: Ahmad Ali Shahid, M Shakil Shaukat

Abstract:

Agriculture is the backbone of economy of Pakistan and Cotton is the major agricultural export and supreme source of raw fiber for our textile industry. To combat against the developing resistance in the target insects and combating these challenges wholesomely, a novel combination of pyramided/stacked genes was conceptualized and later realized, through the means of biotechnology i.e., transformation of three genes namely, Cry1Ac, Cry2A, and EPSP synthase (glyphosate tolerant) genes in the locally cultivated cotton variety. The progenies of the transformed plants were successfully raised and screened under the tunnel conditions for two generations and the present study focused on the screening of plants which were confirmed for containing all of these three genes and their expressions. Initially, the screening was done through glyphosate spray assay and the plants which were healthy and showed no damage on leaves were selected after 07 days of spray. In the laboratory, the DNA of these plants were isolated and subjected to amplification of the three genes. Thus, seventeen out of twenty were confirmed positive for Cry1Ac gene and ten out of twenty were positive for Cry2A gene and all twenty were positive for presence of EPSP synthase gene. Then, the ten plant samples which were confirmed with presence of all three genes were subjected to expression analysis of these proteins through ELISA. The results showed that eight out of ten plants were actively expressing the three transgenes. Real-time PCR was also done to quantify the expression levels of the EPSP synthase gene. Finally, eight plants were confirmed for the presence and active expression of all three genes in T3 generation of the triple gene transformed cotton. These plants may be subjected to T4 generation to develop a new stable variety in due course of time.

Keywords: agriculture, cotton, transformation, cry genes, ELISA, PCR

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1058 Network Conditioning and Transfer Learning for Peripheral Nerve Segmentation in Ultrasound Images

Authors: Harold Mauricio Díaz-Vargas, Cristian Alfonso Jimenez-Castaño, David Augusto Cárdenas-Peña, Guillermo Alberto Ortiz-Gómez, Alvaro Angel Orozco-Gutierrez

Abstract:

Precise identification of the nerves is a crucial task performed by anesthesiologists for an effective Peripheral Nerve Blocking (PNB). Now, anesthesiologists use ultrasound imaging equipment to guide the PNB and detect nervous structures. However, visual identification of the nerves from ultrasound images is difficult, even for trained specialists, due to artifacts and low contrast. The recent advances in deep learning make neural networks a potential tool for accurate nerve segmentation systems, so addressing the above issues from raw data. The most widely spread U-Net network yields pixel-by-pixel segmentation by encoding the input image and decoding the attained feature vector into a semantic image. This work proposes a conditioning approach and encoder pre-training to enhance the nerve segmentation of traditional U-Nets. Conditioning is achieved by the one-hot encoding of the kind of target nerve a the network input, while the pre-training considers five well-known deep networks for image classification. The proposed approach is tested in a collection of 619 US images, where the best C-UNet architecture yields an 81% Dice coefficient, outperforming the 74% of the best traditional U-Net. Results prove that pre-trained models with the conditional approach outperform their equivalent baseline by supporting learning new features and enriching the discriminant capability of the tested networks.

Keywords: nerve segmentation, U-Net, deep learning, ultrasound imaging, peripheral nerve blocking

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1057 Cannabidiol (CBD) Resistant Salmonella Strains Are Susceptible to Epsilon 34 Phage Tailspike Protein

Authors: Ibrahim Iddrisu, Joseph Ayariga, Junhuan Xu, Ayomide Adebanjo, Boakai K. Robertson, Michelle Samuel-Foo, Olufemi Ajayi

Abstract:

The rise of antimicrobial resistance is a global public health crisis that threatens the effective control and prevention of infections. Due to the emergence of pan drug-resistant bacteria, most antibiotics have lost their efficacy. Bacteriophages or their components are known to target bacterial cell walls, cell membranes, and lipopolysaccharides (LPS) and hydrolyze them. Bacteriophages, being the natural predators of pathogenic bacteria, are inevitably categorized as ‘human friends’, thus fulfilling the adage that ‘the enemy of my enemy is my friend’. Leveraging on their lethal capabilities against pathogenic bacteria, researchers are searching for more ways to overcome the current antibiotic resistance challenge. In this study, we expressed and purified epsilon 34 phage tail spike protein (E34 TSP) from the E34 TSP gene, then assessed the ability of this bacteriophage protein in the killing of two CBD-resistant strains of Salmonella spp. We also assessed the ability of the tail spike protein to cause bacteria membrane disruption and dehydrogenase depletion. We observed that the combined treatment of CBD-resistant strains of Salmonella with CBD and E34 TSP showed poor killing ability, whereas the mono treatment with E34 TSP showed considerably higher killing efficiency. This study demonstrates that the inhibition of the bacteria by E34 TSP was due in part to membrane disruption and dehydrogenase inactivation by the protein. The results of this work provide an interesting background to highlight the crucial role phage proteins such as E34 TSP could play in pathogenic bacterial control.

Keywords: cannabidiol, resistance, Salmonella, antimicrobials, phages

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1056 Colorimetric Measurement of Dipeptidyl Peptidase IV (DPP IV) Activity via Peptide Capped Gold Nanoparticles

Authors: H. Aldewachi, M. Hines, M. McCulloch, N. Woodroofe, P. Gardiner

Abstract:

DPP-IV is an enzyme whose expression is affected in a variety of diseases, therefore, has been identified as possible diagnostic or prognostic marker for various tumours, immunological, inflammatory, neuroendocrine, and viral diseases. Recently, DPP-IV enzyme has been identified as a novel target for type II diabetes treatment where the enzyme is involved. There is, therefore, a need to develop sensitive and specific methods that can be easily deployed for the screening of the enzyme either as a tool for drug screening or disease marker in biological samples. A variety of assays have been introduced for the determination of DPP-IV enzyme activity using chromogenic and fluorogenic substrates, nevertheless these assays either lack the required sensitivity especially in inhibited enzyme samples or displays low water solubility implying difficulty for use in vivo samples in addition to labour and time-consuming sample preparation. In this study, novel strategies based on exploiting the high extinction coefficient of gold nanoparticles (GNPs) are investigated in order to develop fast, specific and reliable enzymatic assay by investigating synthetic peptide sequences containing a DPP IV cleavage site and coupling them to GNPs. The DPP IV could be detected by colorimetric response of peptide capped GNPs (P-GNPS) that could be monitored by a UV-visible spectrophotometer or even naked eyes, and the detection limit could reach 0.01 unit/ml. The P-GNPs, when subjected to DPP IV, showed excellent selectivity compared to other proteins (thrombin and human serum albumin) , which led to prominent colour change. This provided a simple and effective colorimetric sensor for on-site and real-time detection of DPP IV.

Keywords: gold nanoparticles, synthetic peptides, colorimetric detection, DPP-IV enzyme

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1055 Study of Demographic, Hematological Profile and Risk Stratification in Chronic Myeloid Leukemia Patients

Authors: Rajandeep Kaur, Rajeev Gupta

Abstract:

Background: Chronic myeloid leukemia (CML) is the most common leukaemia in India. The annual incidence of chronic myeloid leukemia in India was originally reported to be 0.8 to 2.2 per 1,00,000 population. CML is a clonal disorder that is usually easily diagnosed because the leukemic cells of more than 95% of patients have a distinctive cytogenetic abnormality, the Philadelphia chromosome (Ph1). The approval of tyrosine kinase inhibitors (TKIs), which target BCR-ABL1 kinase activity, has significantly reduced the mortality rate associated with chronic myeloid leukemia (CML) and revolutionized treatment. Material and Methods: 80 diagnosed cases of CML were taken. Investigations were done. Bone marrow and molecular studies were also done and with EUTOS, patients were stratified into low and high-risk groups and then treatment with Imatinib was given to all patients and the molecular response was evaluated at 6 months and 12 months follow up with BCR-ABL by RT-PCR quantitative assay. Results: In the study population, out of 80 patients in the study population, 40 were females and 40 were males, with M: F is 1:1. Out of total 80 patients’ maximum patients (54) were in 31-60 years age group. Our study showed a most common symptom of presentation is abdominal discomfort followed by fever. Out of the total 80 patients, 25 (31.3%) patients had high EUTOS scores and 55 (68.8%) patients had low EUTOS scores. On 6 months follow up 36.3% of patients had Complete Molecular Response, 16.3% of patients had Major Molecular Response and 47.5% of patients had No Molecular Response but on 12 months follow up 71.3% of patients had Complete Molecular Response, 16.25% of patients had Major Molecular Response and 12.5% patients had No Molecular Response. Conclusion: In this study, we found a significant correlation between EUTOS score and Molecular response at 6 months and 12 months follow up after Imatinib therapy.

Keywords: chronic myeloid leukemia, European treatment and outcome study score, hematological response, molecular response, tyrosine kinase inhibitor

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1054 Impact of Adolescent Smoking on the Behaviour, Academic and Health Aspects in Qatar

Authors: Abdelsalam Gomaa, Mahjabeen Ramzan, Tooba Ali Akbar, Huma Nadeem

Abstract:

The use of tobacco and the health risks linked to it are well known in this day and age due to the presence of easily available information through the internet. The media is a powerful platform that is used by many anti-smoking awareness campaigns to reach their target audience; yet, it has been found that adolescents are taking up smoking every passing day. Half of this smoking population of youngsters resides in Asia alone, which includes Qatar, the focus country of this study. As smoking happens to be one of the largest avoidable causes of serious diseases like cancers and heart problems, children are taking up smoking at an alarming rate everywhere including Qatar. Importance of the health of the citizens of Qatar is one of the pillars of the Qatar vision 2030, which is to ensure a healthy population, both physically and mentally. Since the youth makes up a significant percentage of the population and in order to achieve the health objectives of the Qatar vision 2030, it is essential to ensure the health and well-being of this part of the population of the country as they are the future of Qatar. Children, especially boys who tend to be more aggressive by nature, are highly likely to develop behavioral and health issues due to smoking at an early age. Research conducted around the world has also emphasized on this association between the smokers developing a bad behaviour as well as poor social communication skills. However, due to lack of research into this association, very little is known about the extent to which smoking impacts the children’s academics, health and behaviour. Moreover, a study of this nature has not yet been conducted in Qatar previously as most of the studies focus on adult smokers and ways to minimize the number of smoking habits in universities and workplaces. This study solely focuses on identifying a relationship between smoking and its impacts on the adolescents by conducting a research on different schools across Qatar.

Keywords: adolescents, modelling techniques, Qatar, smoking

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1053 Genome Editing in Sorghum: Advancements and Future Possibilities: A Review

Authors: Micheale Yifter Weldemichael, Hailay Mehari Gebremedhn, Teklehaimanot Hailesslasie

Abstract:

The advancement of target-specific genome editing tools, including clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR-associated protein9 (Cas9), mega-nucleases, base editing (BE), prime editing (PE), transcription activator-like endonucleases (TALENs), and zinc-finger nucleases (ZFNs), have paved the way for a modern era of gene editing. CRISPR/Cas9, as a versatile, simple, cost-effective and robust system for genome editing, has dominated the genome manipulation field over the last few years. The application of CRISPR/Cas9 in sorghum improvement is particularly vital in the context of ecological, environmental and agricultural challenges, as well as global climate change. In this context, gene editing using CRISPR/Cas9 can improve nutritional value, yield, resistance to pests and disease and tolerance to different abiotic stress. Moreover, CRISPR/Cas9 can potentially perform complex editing to reshape already available elite varieties and new genetic variations. However, existing research is targeted at improving even further the effectiveness of the CRISPR/Cas9 genome editing techniques to fruitfully edit endogenous sorghum genes. These findings suggest that genome editing is a feasible and successful venture in sorghum. Newer improvements and developments of CRISPR/Cas9 techniques have further qualified researchers to modify extra genes in sorghum with improved efficiency. The fruitful application and development of CRISPR techniques for genome editing in sorghum will not only help in gene discovery, creating new, improved traits in sorghum regulating gene expression sorghum functional genomics, but also in making site-specific integration events.

Keywords: CRISPR/Cas9, genome editing, quality, sorghum, stress, yield

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1052 The Associations between Self-Determined Motivation and Physical Activity in Patients with Coronary Heart Disease

Authors: I. Hua Chu, Hsiang-Chi Yu, Hsuan Su

Abstract:

Purpose: To examine the associations between self-determined motivation and physical activity in patients with coronary heart disease (CHD) in a longitudinal study. Methods: Patients with CHD were recruited for this study. Their motivations for exercise were measured by the Behavioral Regulation in Exercise Questionnaire-2 (BREQ-2). Physical activity was assessed using the 7-day physical activity recall questionnaire. Duration and energy expenditure of moderate to vigorous physical activity (MVPA) were used in data analysis. All outcome measures were assessed at baseline and 12 months follow up. Data were analyzed using Pearson correlation analysis and regression analysis. Results: The results of the 45 participants (mean age 60.24 yr; 90.2% male) revealed that there were significant negative correlations between amotivation at baseline and duration (r=-.295, p=.049) and energy expenditure (r=-.300, p=.045) of MVPA at 12 months. In contrast, there were significant positive correlations between calculated relative autonomy index (RAI) at baseline and duration (r=.377, p=.011) and energy expenditure (r=.382, p=.010) of MVPA at 12 months. There was no significant correlation between other subscales of the BREQ-2 and duration or energy expenditure of MVPA. Regression analyses revealed that RAI was a significant predictor of duration (p=.011) and energy expenditure (p=.010) of MVPA at 12 months follow-up. Conclusions: These results suggest that the relative degree of self-determined motivation could predict long-term MVPA behaviors in CHD patients. Physical activity interventions are recommended to target enhancing one’s identified and intrinsic motivation to increase the likelihood of physical activity participation in this population.

Keywords: self-determined motivation, physical activity, coronary heart disease, relative autonomy index (RAI)

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1051 Measuring the Influence of Functional Proximity on Environmental Urban Performance via IMM: Four Study Cases in Milan

Authors: Massimo Tadi, M. Hadi Mohammad Zadeh, Ozge Ogut

Abstract:

Although how cities’ forms are structured is studied, more efforts are needed on systemic comprehensions and evaluations of the urban morphology through quantitative metrics that are able to describe the performance of a city in relation to its formal properties. More research is required in this direction in order to better describe the urban form characteristics and their impact on the environmental performance of cities and to increase their sustainability stewardship. With the aim of developing a better understanding of the built environment’s systemic structure, the intention of this paper is to present a holistic methodology for studying the behavior of the built environment and investigate the methods for measuring the effect of urban structure to the environmental performance. This goal will be pursued through an inquiry into the morphological components of the urban systems and the complex relationships between them. Particularly, this paper focuses on proximity, referring to the proximity of different land-uses, is a concept with which Integrated Modification Methodology (IMM) explains how land-use allocation might affect the choice of mobility in neighborhoods, and especially, encourage or discourage non-motived mobility. This paper uses proximity to demonstrate that the structure attributes can quantifiably relate to the performing behavior in the city. The target is to devise a mathematical pattern from the structural elements and correlate it directly with urban performance indicators concerned with environmental sustainability. The paper presents some results of this rigorous investigation of urban proximity and its correlation with performance indicators in four different areas in the city of Milan, each of them characterized by different morphological features.

Keywords: built environment, ecology, sustainable indicators, sustainability, urban morphology

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1050 Synergistic Effect of Doxorubicin-Loaded Silver Nanoparticles – Polymeric Conjugates on Breast Cancer Cells

Authors: Nancy M. El-Baz, Laila Ziko, Rania Siam, Wael Mamdouh

Abstract:

Cancer is one of the most devastating diseases, and has over than 10 million new cases annually worldwide. Despite the effectiveness of chemotherapeutic agents, their systemic toxicity and non-selective anticancer actions represent the main obstacles facing cancer curability. Due to the effective enhanced permeability and retention (EPR) effect of nanomaterials, nanoparticles (NPs) have been used as drug nanocarriers providing targeted cancer drug delivery systems. In addition, several inorganic nanoparticles such as silver (AgNPs) nanoparticles demonstrated a potent anticancer activity against different cancers. The present study aimed at formulating core-shell inorganic NPs-based combinatorial therapy based on combining the anticancer activity of AgNPs along with doxorubicin (DOX) and evaluating their cytotoxicity on MCF-7 breast cancer cells. These inorganic NPs-based combinatorial therapies were designed to (i) Target and kill cancer cells with high selectivity, (ii) Have an improved efficacy/toxicity balance, and (iii) Have an enhanced therapeutic index when compared to the original non-modified DOX with much lower dosage The in-vitro cytotoxicity studies demonstrated that the NPs-based combinatorial therapy achieved the same efficacy of non-modified DOX on breast cancer cell line, but with 96% reduced dose. Such reduction in DOX dose revealed that the combination between DOX and NPs possess a synergic anticancer activity against breast cancer. We believe that this is the first report on a synergic anticancer effect at very low dose of DOX against MCF-7 cells. Future studies on NPs-based combinatorial therapy may aid in formulating novel and significantly more effective cancer therapeutics.

Keywords: nanoparticles-based combinatorial therapy, silver nanoparticles, doxorubicin, breast cancer

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