Search results for: chemotherapeutic agents

Authors: Muhammad Rafi Ullah Khan, Yaodong Guo, Vanee Chonhenchob, Jinjin Pei, Chongxing Huang

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The effect of sodium alginate (1%) based edible coating incorporated natural essential oils; thymol, carvone and carvacrol as antimicrobial agents at different concentrations (0.1, 0.5 and 1.0 %) on the quality changes of fresh-cut pineapple were investigated. Pineapple dipped in distilled water was served as control. After coating, fruit were sealed in a modified atmosphere package (MAP) using high permeable film; and stored at 5 °C. Gas composition in package headspace, color values (L*, a*, b*, C*), TSS, pH, ethanol, browning, and microbial decay were monitored during storage. Oxygen concentration continuously decreased while carbon dioxide concentration inside all packages continuously increased over time. Color parameters (L*, b*, c*) decreased and a* values increased during storage. All essential oils significantly (p ≤ 0.05) prevented microbial growth than control. A significantly higher (p ≤ 0.05) ethanol content was found in the control than in all other treatments. Visible microbial growth, high ethanol, and low color values limited the shelf life to 6 days in control as compared to 9 days in all other treatments. Among all essential oils, thymol at all concentrations maintained the overall quality of the pineapple and could potentially be used commercially in fresh fruit industries for longer storage.

Keywords: essential oils, antibrowning agents, antimicrobial agents, modified atmosphere packaging, microbial decay, pineapple

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Authors: Patrick Santos, João Casal, João Santos Luis Varandas, Tiago Alves, Carlos Romeiro, Sérgio Lourenço

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Nowadays, technology makes it possible to, in one hand, communicate with various objects of the daily life through the Internet, and in the other, put these objects interacting with each other through this channel. Simultaneously, with the raise of smartphones as the most ubiquitous technology on persons lives, emerge new agents for these devices - Intelligent Personal Assistants. These agents have the goal of helping the user manage and organize his information as well as supporting the user in his/her day-to-day tasks. Moreover, other emergent concept is the Cloud Computing, which allows computation and storage to get out of the users devices, bringing benefits in terms of performance, security, interoperability and others. Connecting these three paradigms, in this work we propose an architecture for an intelligent system which provides an interface that assists the user on smart environments, informing, suggesting actions and allowing to manage the objects of his/her daily life.

Keywords: internet of things, cloud, intelligent personal assistant, architecture

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Authors: Nicole Merkle, Stefan Zander

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Ambient Assisted Living (AAL) describes a technological and methodological stack of (e.g. formal model-theoretic semantics, rule-based reasoning and machine learning), different aspects regarding the behavior, activities and characteristics of humans. Hence, a semantic representation of the user environment and its relevant elements are required in order to allow assistive agents to recognize situations and deduce appropriate actions. Furthermore, the user and his/her characteristics (e.g. physical, cognitive, preferences) need to be represented with a high degree of expressiveness in order to allow software agents a precise evaluation of the users’ context models. The correct interpretation of these context models highly depends on temporal, spatial circumstances as well as individual user preferences. In most AAL approaches, model representations of real world situations represent the current state of a universe of discourse at a given point in time by neglecting transitions between a set of states. However, the AAL domain currently lacks sufficient approaches that contemplate on the dynamic adaptions of context-related representations. Semantic representations of relevant real-world excerpts (e.g. user activities) help cognitive, rule-based agents to reason and make decisions in order to help users in appropriate tasks and situations. Furthermore, rules and reasoning on semantic models are not sufficient for handling uncertainty and fuzzy situations. A certain situation can require different (re-)actions in order to achieve the best results with respect to the user and his/her needs. But what is the best result? To answer this question, we need to consider that every smart agent requires to achieve an objective, but this objective is mostly defined by domain experts who can also fail in their estimation of what is desired by the user and what not. Hence, a smart agent has to be able to learn from context history data and estimate or predict what is most likely in certain contexts. Furthermore, different agents with contrary objectives can cause collisions as their actions influence the user’s context and constituting conditions in unintended or uncontrolled ways. We present an approach for dynamically updating a semantic model with respect to the current user context that allows flexibility of the software agents and enhances their conformance in order to improve the user experience. The presented approach adapts rules by learning sensor evidence and user actions using probabilistic reasoning approaches, based on given expert knowledge. The semantic domain model consists basically of device-, service- and user profile representations. In this paper, we present how this semantic domain model can be used in order to compute the probability of matching rules and actions. We apply this probability estimation to compare the current domain model representation with the computed one in order to adapt the formal semantic representation. Our approach aims at minimizing the likelihood of unintended interferences in order to eliminate conflicts and unpredictable side-effects by updating pre-defined expert knowledge according to the most probable context representation. This enables agents to adapt to dynamic changes in the environment which enhances the provision of adequate assistance and affects positively the user satisfaction.

Keywords: ambient intelligence, machine learning, semantic web, software agents

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Authors: Svetlana Guryeva, Inna Kornienko, Andrey Usanov, Dmitry Usanov, Elena Petersen

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Every day cells in our organism are exposed to various factors: chemical agents, reactive oxygen species, ionizing radiation, and others. These factors can cause damage to DNA, cellular membrane, intracellular compartments, and proteins. The fate of cells depends on the exposure intensity and duration. The prolonged and intense exposure causes the irreversible damage accumulation, which triggers the permanent cell cycle arrest (cellular senescence) or cell death programs. In the case of low dose of impacts, it can lead to cell renovation and to cell functional state improvement. Therefore, it is a pivotal question to investigate the factors and doses that result in described positive effects. In order to estimate the influence of different agents, the proliferation index and levels of cell death markers (annexin V/propidium iodide), senescence-associated β-galactosidase, and lipofuscin were measured. The experiments were conducted on primary human fibroblasts of the 8th passage. According to the levels of mentioned markers, these cells were defined as senescent cells. The effect of low-frequency magnetic field was investigated. Different modes of magnetic field exposure were tested. The physical agents were compared with chemical agents: metformin (10 mM) and taurine (0.8 mM and 1.6 mM). Cells were incubating with chemicals for 5 days. The highest decrease in the level of senescence-associated β-galactosidase (21%) and lipofuscin (17%) was observed in the primary senescent fibroblasts after 5 days after double treatments with 48 h intervals with low-frequency magnetic field. There were no significant changes in the proliferation index after magnetic field application. The cytotoxic effect of magnetic field was not observed. The chemical agent taurine (1.6 mM) decreased the level of senescence-associated β-galactosidase (23%) and lipofuscin (22%). Metformin improved the activity of senescence-associated β-galactosidase on 15% and the level of lipofuscin on 19% in this experiment. According to these results, the effect of double treatment with 48 h interval with low-frequency magnetic field and the effect of taurine (1.6 mM) were comparable to the effect of metformin, for which anti-aging properties are proved. In conclusion, this study can become the first step towards creation of the standardized system for the investigation of different effects on senescent cells.

Keywords: biomarkers, magnetic field, metformin, primary fibroblasts, senescence, taurine

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Authors: Recep Keşli, Cengiz Demir, Onur Türkyılmaz

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Objective: The aim of this study was to determine the prevalence of Mycoplasma hominis and Ureaplasma urealyticum as the causative agents in men with non-gonococcal urethtritis, and anti-bacterial resistance rates. Methods: The Study was carried out in the two Medical Microbiology Laboratories belonging to: Konya Education and Research Hospital and ANS Practice and Research Hospital, Afyon Kocatepe University, between January 2012 and December 2015. Urethral samples were obtained from patients by using a swab. Mycoplasma hominis and Ureaplasma urealyticum were detected by using Mycoplasma IST-2 kit (bio-Mérieux, Marcy l'Étoile, France). Neisseria gonorrhoea was excluded by Gram staining and culture methods. Results: Of all the one hundred and eighty-eight male patients with urethritis, forty M. hominis and forty two U. urealyticum were detected. Resistance rates of M. hominis strains against to doxycycline, ofloxacin, erythromycin, tetracycline, ciprofloxacin, azithromycin, clarithromycin, and pristinamycin were found as 5 %, 65 %, 25 %, 5 %, 80 %, 20 %, 20 %, 20 %, 5 %, respectively. Resistance rates of U. urealyticum strains against to doxycycline, ofloxacin, erythromycin, tetracycline, ciprofloxacin, azithromycin, clarithromycin, and pristinamycin were found as 4.7 %, 66.6 %, 23.8 %, 4.75 %, 81 %, 19 %, 19 %, 4.7 % respectively. No resistance was detected against to josamycin, for both the strains. Conclusions: It was concluded that; ciprofloxacin and ofloxacin had the weakest; josamycin, doxycycline, and tetracycline had the strongest in vitro anti-bacterial activity, for treatment of the NGU. So josamycin, doxycycline, and tetracycline should be preferred as the first choice of anti-bacterial agents, for treatment of the patients with non-gonococcal male urethritis.

Keywords: antimicrobial resistance, Mycoplasma hominis, non-gonococcal urethritis, Ureaplasma urealyticum

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Authors: Meral Tuncbilek, Duygu Sac, Irem Durmaz, Rengul Cetin Atalay

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Nucleoside analogs are a pharmacologically diverse family that includes cytotoxic compounds, antiviral agents, and immunosuppressive molecules. Purine nucleoside derivatives such as fludarabine, cladribine, and pentostatin are significant drugs used in chemotherapy for the treatment of solid tumors and hematological malignancies. In this study, we synthesized novel purine ribonucleoside analogs containing a 4-(4-substituted phenylsulfonyl) piperazine in the substituent at N6- and O-substituted sulfonyl group at 5’-position as putative cytotoxic agents. The newly obtained compounds were then characterized for their cytotoxicity in human cancer cell lines. The 5’, 6-disubstituted 9-(β-D-ribofuranosyl)purine derivatives (44-67) were readily obtained from commercially available inosine in seven steps in very cost effective synthesis approach. The newly synthesized compounds were first evaluated for their anti-tumor activities against human liver (Huh7), colon (HCT116) and breast (MCF7) carcinoma cell lines. The IC50 values were in micromolar concentrations with 5’, 6-disubstituted purine nucleoside derivatives. Time-dependent IC50 values for each molecule were also calculated in comparison with known cytotoxic agents Camptothecin (CPT), 5-Fluorouracil (5-FU), Cladribine, Pentostatine and Fludarabine. N6-(4-trifluoromethyl phenyl) / N6-(4-bromophenyl) and 5’-O-(4-methoxybenzene sulfonyl) / 5’-O-(benzenesulfonyl) derivatives 54, 64 displayed the best cytotoxic activity with IC50 values of 8.8, 7 µM against MCF7 cell line. The N6-(4-methylphenyl) analog 50 was also very active (IC50= 10.7 μM) against HCT116 cell line. Furthermore, compound 64 had a better cytotoxic activity than the known cell growth inhibitors 5-FU and Fludarabine on Huh7 (1.5 vs 30.7, 29.9 μM for 5-FU and Fludarabine).

Keywords: cytotoxic activity, Huh7, HCT116, MCF7, nucleoside, synthesis

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Authors: Benjamin Castillo, Luis Pastenes, Fernando Cerdova

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The contamination of food by microbial agents is a common problem in the industry, especially regarding the elaboration of animal source products. Incorrect manipulation of the machinery or on the raw materials can cause a decrease in production or an epidemiological outbreak due to intoxication. In order to improve food product quality, different methods have been used to reduce or, at least, to slow down the growth of the pathogens, especially deteriorated, infectious or toxigenic bacteria. These methods are usually carried out under low temperatures and short processing time (abiotic agents), along with the application of antibacterial substances, such as bacteriocins (biotic agents). This, in a controlled and efficient way that fulfills the purpose of bacterial control without damaging the final product. Therefore, the objective of the present study is to design a secondary mathematical model that allows the prediction of both the biotic and abiotic factor impact associated with animal source food processing. In order to accomplish this objective, the authors propose a three-dimensional differential equation model, whose components are: bacterial growth, release, production and artificial incorporation of bacteriocins and changes in pH levels of the medium. These three dimensions are constantly being influenced by the temperature of the medium. Secondly, this model adapts to an idealized situation of cross-contamination animal source food processing, with the study agents being both the animal product and the contact surface. Thirdly, the stochastic simulations and the parametric sensibility analysis are compared with referential data. The main results obtained from the analysis and simulations of the mathematical model were to discover that, although bacterial growth can be stopped in lower temperatures, even lower ones are needed to eradicate it. However, this can be not only expensive, but counterproductive as well in terms of the quality of the raw materials and, on the other hand, higher temperatures accelerate bacterial growth. In other aspects, the use and efficiency of bacteriocins are an effective alternative in the short and medium terms. Moreover, an indicator of bacterial growth is a low-level pH, since lots of deteriorating bacteria are lactic acids. Lastly, the processing times are a secondary agent of concern when the rest of the aforementioned agents are under control. Our main conclusion is that when acclimating a mathematical model within the context of the industrial process, it can generate new tools that predict bacterial contamination, the impact of bacterial inhibition, and processing method times. In addition, the mathematical modeling proposed logistic input of broad application, which can be replicated on non-meat food products, other pathogens or even on contamination by crossed contact of allergen foods.

Keywords: bacteriocins, cross-contamination, mathematical model, temperature

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Authors: Roy. H. A. Lindelauf

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Cyberattacks are complex processes consisting of multiple interwoven tasks conducted by a set of agents. Interdictions and defenses against such attacks often rely on cyber kill chain (CKC) models. A CKC is a framework that tries to capture the actions taken by a cyber attacker. There exists a growing body of literature on CKCs. Most of this work either a) describes the CKC with respect to one or more specific cyberattacks or b) discusses the tools and technologies used by the attacker at each stage of the CKC. Defenders, facing scarce resources, have to decide where to allocate their resources given the CKC and partial knowledge on the tools and techniques attackers use. In this presentation CKCs are analyzed through the lens of covert projects, i.e., interrelated tasks that have to be conducted by agents (human and/or computer) with the aim of going undetected. Various aspects of covert project models have been studied abundantly in the operations research and game theory domain, think of resource-limited interdiction actions that maximally delay completion times of a weapons project for instance. This presentation has investigated both cooperative and non-cooperative game theoretic covert project models and elucidated their relation to CKC modelling. To view a CKC as a covert project each step in the CKC is broken down into tasks and there are players of which each one is capable of executing a subset of the tasks. Additionally, task inter-dependencies are represented by a schedule. Using multi-glove cooperative games it is shown how a defender can optimize the allocation of his scarce resources (what, where and how to monitor) against an attacker scheduling a CKC. This study presents and compares several cooperative game theoretic solution concepts as metrics for assigning resources to the monitoring of agents.

Keywords: cyber defense, cyber kill chain, game theory, information warfare techniques

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Authors: Parastou Kharazmi

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Degradation of building materials particularly pipelines causes environmental damage during renovation or replacement and is a time consuming and costly process. Rehabilitation by polymer composites is a solution for renovation of degraded pipeline in heritage buildings and other structures which are less costly, faster and causes less damage to the environment; however, it is still not clear for how long these materials can perform as expected in the field and working condition. To study their service life, two types of composites based on Epoxy and Polyester resins have been evaluated by accelerated exposure and field exposure. The primary degradation agent used in accelerated exposure has been cycling temperature with half of the tests performed in presence of water. Thin films of materials used in accelerated testing were prepared in laboratory by using the same amount of material as well as technique of multi-layers application used in majority of the field installations. Extreme intensity levels of degradation agents have been used only to evaluate materials properties and as also mentioned in ISO 15686, are not directly correlated with degradation mechanisms that would be experienced in service. In the field exposure study, the focus has been to identify possible failure modes, causes, and effects. In field exposure, it has been observed that there are other degradation agents present which can be investigated further such as presence of contaminants and rust before application which prevents formation of a uniform layer of polymer or incompatibility between dissimilar materials. This part of the study also highlighted the importance of application’s quality of the materials in the field for providing the expected performance and service life. Results from extended accelerated exposure and field exposure can help in choosing inspection techniques, establishing the primary degradation agents and can be used for ageing exposure programs with clarifying relationship between different exposure periods and sites.

Keywords: building, renovation, service life, pipelines

Procedia PDF Downloads 187

Authors: W. P. Hu, J. V. Kumar, Jeffrey J. P. Tsai

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The inhibition of SH2 domain regulated protein-protein interactions is an attractive target for developing an effective chemotherapeutic approach in the treatment of disease. Molecular simulation is a useful tool for developing new drugs and for studying molecular recognition. In this study, we searched potential drug compounds for the inhibition of SH2 domain by performing structural similarity search in PubChem Compound Database. A total of 37 compounds were screened from the database, and then we used the LibDock docking program to evaluate the inhibition effect. The best three compounds (AP22408, CID 71463546 and CID 9917321) were chosen for MD simulations after the LibDock docking. Our results show that the compound CID 9917321 can produce a more stable protein-ligand complex compared to other two currently known inhibitors of Src SH2 domain. The compound CID 9917321 may be useful for the inhibition of SH2 domain based on these computational results. Subsequently experiments are needed to verify the effect of compound CID 9917321 on the SH2 domain in the future studies.

Keywords: nonpeptide inhibitor, Src SH2 domain, LibDock, molecular dynamics simulation

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Authors: Raquel Camprubí

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Cultural tourism has been postulated as relevant motivation for tourist over the world during the last decades. In this context, museums are the main attraction for cultural tourists who are seeking to connect with the history and culture of the visited place. From the point of view of an urban destination, museums and other cultural resources are essential to have a strong tourist supply at the destination, in order to be capable of catching attention and interest of cultural tourists. In particular, museums’ challenge is to be prepared to offer the best experience to their visitors without to forget their mission-based mainly on protection of its collection and other social goals. Thus, museums individually want to be competitive and have good positioning to achieve their strategic goals. The life cycle of the destination and the level of maturity of its tourism product influence the need of tourism agents to cooperate and collaborate among them, in order to rejuvenate their product and become more competitive as a destination. Additionally, prior studies have considered an approach of different models of a public and private partnership, and collaborative and cooperative relations developed among the agents of a tourism destination. However, there are no studies that pay special attention to museums and the strategic alliances developed to obtain mutual benefits. Considering this background, the purpose of this study is to analyze in what extent museums of a given urban destination have established strategic links and relations among them, in order to improve their competitive position at both individual and destination level. In order to achieve the aim of this study, the city of Girona (Spain) and the museums located in this city are taken as a case study. Data collection was conducted using in-depth interviews, in order to collect all the qualitative data related to nature, strengthen and purpose of the relational ties established among the museums of the city or other relevant tourism agents of the city. To conduct data analysis, a Social Network Analysis (SNA) approach was taken using UCINET software. Position of the agents in the network and structure of the network was analyzed, and qualitative data from interviews were used to interpret SNA results. Finding reveals the existence of strong ties among some of the museums of the city, particularly to create and promote joint products. Nevertheless, there were detected outsiders who have an individual strategy, without collaboration and cooperation with other museums or agents of the city. Results also show that some relational ties have an institutional origin, while others are the result of a long process of cooperation with common projects. Conclusions put in evidence that collaboration and cooperation of museums had been positive to increase the attractiveness of the museum and the city as a cultural destination. Future research and managerial implications are also mentioned.

Keywords: cultural tourism, competitiveness, museums, Social Network analysis

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Authors: W. Mazari, K. Boucherit, Z. Boucherit-Otmani, M. N. Rahmoun, M. Benabdallah

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The hospital or any other establishment of care can be considered as an ecosystem where the patient comes into contact with a frightening microbial universe and a risk to contract infection that is referred to as nosocomial or health care-associated. In these last years, the incidence of these infections has risen sharply. Several microorganisms are the cause of these nosocomial infections and the emergence of resistance of the microbial strains against antibiotics creates a danger to public health. The search for new antimicrobial agents to overcome this problem has produced interesting compounds through chemical synthesis, which plays a very important role in the research and discovery of new drugs. It is in this framework that our study was conducted at our laboratory and it involves evaluating the antibacterial activity of thirteen 2-pyridone derivatives synthesized by two methods, the diffusion disc method and the dilution method against eight Gram negative bacterial strains. The results seem interesting especially for two products that have shown the best activities against Escherichia coli ATCC 25922 and Enterobacter cloacae ATCC 13047 with CMI of 512µg/ml.

Keywords: heterocyclic derivatives, chemical synthesis, antimicrobial activity, biotechnology

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Authors: A. Hol

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Even in the well developed countries like Australia, Small to Medium Farmers do not often have the power over the market prices as they are more often than not set by the farming agents. This in turn creates problems as farmers only get to know for how much their produce has been sold for by the agents three to four weeks after the sale has taken the place. To see and identify if and how peri-urban Sydney farmers could be assisted, carefully selected group of peri-urban Sydney farmers of the stone fruit has been interviewed. Following the case based interviews collected data was analyzed in detail using the Scenario Based Transformation principles. Analyzed data was then used to create a most common transformation case. The case identified that a mobile web based system could be develop so that framers can monitor agent earnings and in turn gain more power over the markets. It is expected that after the system has been in action for six months to a year, farmers will become empowered and they will gain means to monitor the market and negotiate agent prices.

Keywords: mobile applications, farming, scenario-based analysis, scenario-based transformation, user empowerment

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Authors: N. D. Iswarya, M. A. Maluk Mohamed, N. Vijaya

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Grid is infrastructure that allows the deployment of distributed data in large size from multiple locations to reach a common goal. Scheduling data intensive applications becomes challenging as the size of data sets are very huge in size. Only two solutions exist in order to tackle this challenging issue. First, computation which requires huge data sets to be processed can be transferred to the data site. Second, the required data sets can be transferred to the computation site. In the former scenario, the computation cannot be transferred since the servers are storage/data servers with little or no computational capability. Hence, the second scenario can be considered for further exploration. During scheduling, transferring huge data sets from one site to another site requires more network bandwidth. In order to mitigate this issue, this work focuses on incorporating cognitive science in scheduling. Cognitive Science is the study of human brain and its related activities. Current researches are mainly focused on to incorporate cognitive science in various computational modeling techniques. In this work, the problem solving approach of human brain is studied and incorporated during the data intensive scheduling in grid environments. Here, a cognitive engine is designed and deployed in various grid sites. The intelligent agents present in CE will help in analyzing the request and creating the knowledge base. Depending upon the link capacity, decision will be taken whether to transfer data sets or to partition the data sets. Prediction of next request is made by the agents to serve the requesting site with data sets in advance. This will reduce the data availability time and data transfer time. Replica catalog and Meta data catalog created by the agents assist in decision making process.

Keywords: data grid, grid workflow scheduling, cognitive artificial intelligence

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Authors: Edward W. Staley, Corban G. Rivera, Ashley J. Llorens

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Advances in reinforcement learning (RL) have resulted in recent breakthroughs in the application of artificial intelligence (AI) across many different domains. An emerging landscape of development environments is making powerful RL techniques more accessible for a growing community of researchers. However, most existing frameworks do not directly address the problem of learning in complex operating environments, such as dense urban settings or defense-related scenarios, that incorporate distributed, heterogeneous teams of agents. To help enable AI research for this important class of applications, we introduce the AI Arena: a scalable framework with flexible abstractions for distributed multi-agent reinforcement learning. The AI Arena extends the OpenAI Gym interface to allow greater flexibility in learning control policies across multiple agents with heterogeneous learning strategies and localized views of the environment. To illustrate the utility of our framework, we present experimental results that demonstrate performance gains due to a distributed multi-agent learning approach over commonly-used RL techniques in several different learning environments.

Keywords: reinforcement learning, multi-agent, deep learning, artificial intelligence

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Authors: Mahsa Fathollahzadeh

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The various nanoparticles employed in drug delivery applications include micelles, liposomes, solid lipid nanoparticles, polymeric nanoparticles, functionalized nanoparticles, nanocrystals, cyclodextrins, dendrimers, and nanotubes. Micelles, composed of amphiphilic block copolymers, can encapsulate hydrophobic molecules, allowing for targeted delivery. Liposomes, vesicular structures made up of phospholipids, can encapsulate both hydrophobic and hydrophilic molecules, providing a flexible platform for delivering therapeutic agents. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are designed to improve the stability and bioavailability of lipophilic drugs. Polymeric nanoparticles, such as poly(lactic-co-glycolic acid) (PLGA), are biodegradable and can be engineered to release drugs in a controlled manner. Functionalized nanoparticles, coated with targeting ligands or antibodies, can specifically target diseased cells or tissues. Nanocrystals, engineered to have specific surface properties, can enhance the solubility and bioavailability of poorly soluble drugs. Cyclodextrins, doughnut-shaped molecules with hydrophobic cavities, can be complex with hydrophobic molecules, allowing for improved solubility and bioavailability. Dendrimers, branched polymers with a central core, can be designed to deliver multiple therapeutic agents simultaneously. Nanotubes and metallic nanoparticles, such as gold nanoparticles, offer real-time tracking capabilities and can be used to detect biomolecular interactions. The use of these nanoparticles has revolutionized the field of drug delivery, enabling targeted and controlled release of therapeutic agents, reduced toxicity, and improved patient outcomes.

Keywords: nanotechnology, nanopharmaceuticals, drug-delivery, proteins, ligands, nanoparticles, chemistry

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Authors: Milu T. Cherian, Sergio C. Chai, Morgan A. Casal, Taosheng Chen

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This study aims to use CINPA1, a recently discovered small-molecule inhibitor of the xenobiotic receptor CAR (constitutive androstane receptor) for understanding the binding modes of CAR and to guide CAR-mediated gene expression profiling studies in human primary hepatocytes. CAR and PXR are xenobiotic sensors that respond to drugs and endobiotics by modulating the expression of metabolic genes that enhance detoxification and elimination. Elevated levels of drug metabolizing enzymes and efflux transporters resulting from CAR activation promote the elimination of chemotherapeutic agents leading to reduced therapeutic effectiveness. Multidrug resistance in tumors after chemotherapy could be associated with errant CAR activity, as shown in the case of neuroblastoma. CAR inhibitors used in combination with existing chemotherapeutics could be utilized to attenuate multidrug resistance and resensitize chemo-resistant cancer cells. CAR and PXR have many overlapping modulating ligands as well as many overlapping target genes which confounded attempts to understand and regulate receptor-specific activity. Through a directed screening approach we previously identified a new CAR inhibitor, CINPA1, which is novel in its ability to inhibit CAR function without activating PXR. The cellular mechanisms by which CINPA1 inhibits CAR function were also extensively examined along with its pharmacokinetic properties. CINPA1 binding was shown to change CAR-coregulator interactions as well as modify CAR recruitment at DNA response elements of regulated genes. CINPA1 was shown to be broken down in the liver to form two, mostly inactive, metabolites. The structure-activity differences of CINPA1 and its metabolites were used to guide computational modeling using the CAR-LBD structure. To rationalize how ligand binding may lead to different CAR pharmacology, an analysis of the docked poses of human CAR bound to CITCO (a CAR activator) vs. CINPA1 or the metabolites was conducted. From our modeling, strong hydrogen bonding of CINPA1 with N165 and H203 in the CAR-LBD was predicted. These residues were validated to be important for CINPA1 binding using single amino-acid CAR mutants in a CAR-mediated functional reporter assay. Also predicted were residues making key hydrophobic interactions with CINPA1 but not the inactive metabolites. Some of these hydrophobic amino acids were also identified and additionally, the differential coregulator interactions of these mutants were determined in mammalian two-hybrid systems. CINPA1 represents an excellent starting point for future optimization into highly relevant probe molecules to study the function of the CAR receptor in normal- and pathophysiology, and possible development of therapeutics (for e.g. use for resensitizing chemoresistant neuroblastoma cells).

Keywords: antagonist, chemoresistance, constitutive androstane receptor (CAR), multi-drug resistance, structure activity relationship (SAR), xenobiotic resistance

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Authors: Tabassum Yasmin, Hamid Pahlevan

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HIV/Hepatitis C co-infection treatments have evolved substantially and they have similar sustained virologic response rates as those of Hepatitis C monoinfected population. There are a few studies on therapy of patients with dual genotypes, especially in HIV/Hepatic C coinfected group. Most studies portrayed case reports of dual genotype chronic Hepatitis C coinfection treatment with Sofosbuvir/Ledipasvir and Ribavirin. A 79-year-old male with a history of HIV on Truvada and Isentress had chronic Hepatitis C with 1a and 2 genotypes. The patient has a history of alcohol intake for 40 years but recently stopped drinking alcohol. He has a history of intravenous drug use in the past and currently is not using any recreational drugs. Patient has Fibro score of 0.7 with Metavir score F2 to F4. AFP is 3.2. The HCV RNA is 493,034 IU/ML. The HBV viral DNA is < 1.30 (not detected). The CD4 is 687CU/MM. The FIB 4 is 3.34 with APRI index 0.717. The HIV viral load is 101 copies/ML. MRI abdomen did not show any liver abnormality. Fixed dose Sofosbuvir/Ledipasvir was used for therapy without Ribavirin. He tolerated medication except for some minor gastrointestinal side effects like abdominal bloating. He demonstrated 100% adherence rate. Patient completed 12 weeks of therapy. HCV RNA was undetectable at 4 and 12 weeks. He achieved SVR at week 12 and subsequently had undetectable RNA for 2 years. Dual genotype prevalence in chronic hepatitis C population is rare, especially in HIV/hepatic coinfection. Our case demonstrates that dual genotypic cases can still be successfully treated with Direct Acting Antiviral agents. The newer agents for therapy for pan genotypes were not available at the time the patient was being treated. We demonstrated that dual agent therapy was still able to maintain SVR in our patient.

Keywords: HIV/Hepatitis C, SVR (sustained virologic response), DAA (direct active antiviral agents, dual genotype

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Authors: Radka Obořilová, Hana Šimečková, Matěj Pastucha, Jan Přibyl, Petr Skládal, Ivana Mašlaňová, Zdeněk Farka

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Due to the spreading of antimicrobial resistance, alternative approaches to combat superinfections are being sought, both in the field of lysing agents and methods for studying bacterial lysis. A suitable alternative to antibiotics is phage therapy and enzybiotics, for which it is also necessary to study the mechanism of their action. Biosensor-based techniques allow rapid detection of pathogens in real time, verification of sensitivity to commonly used antimicrobial agents, and selection of suitable lysis agents. The detection of lysis takes place on the surface of the biosensor with immobilized bacteria, which has the potential to be used to study biofilms. An example of such a biosensor is surface plasmon resonance (SPR), which records the kinetics of bacterial lysis based on a change in the resonance angle. The bacteria are immobilized on the surface of the SPR chip, and the action of phage as the mass loss is monitored after a typical lytic cycle delay. Atomic force microscopy (AFM) is a technique for imaging of samples on the surface. In contrast to electron microscopy, it has the advantage of real-time imaging in the native conditions of the nutrient medium. In our case, Staphylococcus aureus was lysed using the enzyme lysostaphin and phage P68 from the familyPodoviridae at 37 ° C. In addition to visualization, AFM was used to study changes in mechanical properties during lysis, which resulted in a reduction of Young’s modulus (E) after disruption of the bacterial wall. Changes in E reflect the stiffness of the bacterium. These advanced methods provide deeper insight into bacterial lysis and can help to fight against bacterial diseases.

Keywords: biosensors, atomic force microscopy, surface plasmon resonance, bacterial lysis, staphylococcus aureus, phage P68

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Authors: Yingqi Cui, Changran Huang, Raymond Lee

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In this paper, we proposed an AI Tutor using ontology and natural language process techniques to generate a computer science domain knowledge graph and answer users’ questions based on the knowledge graph. We define eight types of relation to extract relationships between entities according to the computer science domain text. The AI tutor is separated into two agents: learning agent and Question-Answer (QA) agent and developed on JADE (a multi-agent system) platform. The learning agent is responsible for reading text to extract information and generate a corresponding knowledge graph by defined patterns. The QA agent can understand the users’ questions and answer humans’ questions based on the knowledge graph generated by the learning agent.

Keywords: artificial intelligence, natural Language processing, knowledge graph, intelligent agents, QA system

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Authors: Nneka Augustina Akwu, Yougasphree Naidoo

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Molecular advancement in technology has created a means whereby the atoms and molecules (solid forms) of certain materials such as plants, can now be reduced to a range of 1-100 nanometres. Green synthesis of silver nanoparticles (AgNPs) was carried out at room temperature (RT) 25 ± 2°C and 80°C, using the metabolites in the aqueous extracts of the leaves and stem bark of Grewia lasiocarpa as reductants and stabilizing agents. The biosynthesized AgNPs were characterized by UV-Vis spectrophotometry, attenuated total reflectance - Fourier transforms infrared (ATR-FTIR) spectroscopy, nanoparticle tracking analysis (NTA), Energy Dispersive X-ray fluorescence scanning electron microscope (SEM-EDXRF) and high-resolution transmission electron microscopy (HRTEM). The AgNPs were biologically evaluated for antioxidant, antibacterial and cytotoxicity activities. The phytochemical and FTIR analyses revealed the presence of metabolites that act as reducing and capping agents, while the UV-Vis spectroscopy of the biosynthesized NPs showed absorption between 380-460 nm, confirming AgNP synthesis. The Zeta potential values were between -9.1 and -20.6 mV with a hydrodynamics diameter ranging from 38.3 to 46.7 nm. SEM and HRTEM analyses revealed that AgNPs were predominately spherical with an average particle size of 2- 31 nm for the leaves and 5-27 nm for the stem bark. The cytotoxicity IC50 values of the AgNPs against HeLa, Caco-2 and MCF-7 were >1 mg/mL. The AgNPs were sensitive to all strains of bacteria used, with methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) being more sensitive to the AgNPs. Our findings propose that antibacterial and anticancer agents could be derived from these AgNPs of G. lasiocarpa, and warrant their further investigation.

Keywords: antioxidant, cytotoxicity, Grewia lasiocarpa, silver nanoparticles, Zeta potentials

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Authors: Vijaya Yuvaram Singh V M, Kameshwar Rao J V

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The challenge with development of neural network based methods for medical is the availability of data. Anatomical landmark detection in the medical domain is a process to find points on the x-ray scan report of the patient. Most of the time this task is done manually by trained professionals as it requires precision and domain knowledge. Traditionally object detection based methods are used for landmark detection. Here, we utilize reinforcement learning and query based method to train a single agent capable of detecting multiple landmarks. A deep Q network agent is trained to detect single and multiple landmarks present on hip and shoulder from x-ray scan of a patient. Here a single agent is trained to find multiple landmark making it superior to having individual agents per landmark. For the initial study, five images of different patients are used as the environment and tested the agents performance on two unseen images.

Keywords: reinforcement learning, medical landmark detection, multi target detection, deep neural network

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Authors: Ravi J. Shah

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The present study deals with the synthesis of novel spiro[azetidine-2, 3’-indole]-2’, 4(1’H)-dione derivative from the reactions of 3-(phenylimino)-1,3-dihydro-2H-indol-2-one derivatives with chloracetyl chloride in presence of triethyl amine (TEA). All the compounds were characterized using IR, 1H NMR, MS and elemental analysis. They were screened for their antibacterial and antifungal activities. Results revealed that, compounds (7a), (7b), (7c), (7d) and (7e) showed very good activity with MIC value of 6.25-12.5 μg/ml against three evaluated bacterial strains and the remaining compounds showed good to moderate activity comparable to standard drugs as antibacterial agents. Compounds (7c) and (7h) displayed equipotent antifungal activity in comparison to standard drugs. Structure-activity relationship study of the compounds showed that the presence of electron withdrawing group substitution at 5’ and 7’ positions of indoline ring and on ortho or para position of phenyl ring increases both antibacterial and antifungal activity of the compound. Henceforth, our findings will have a good impact on chemists and biochemists for further investigations in search of bromine containing spiro fused antimicrobial agents.

Keywords: antibacterial activity, antifungal activity, 2-Azetidinone, indoline

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Authors: Lorena G. Calvo, Marta Lores, Trinidad de Miguel

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Natural extracts containing high polyphenolic concentration possess antibacterial and antifungal activity. The present research characterizes a hydro-organic extract with a high polyphenolic content as an antimicrobial candidate. As a result of this composition, the extract showed pronounced bioactivities with potential uses in agricultural, veterinary, pharmaceutical, and cosmetic industries. Polyphenol compounds were extracted by using hydro-organic solvent mixtures from the shrub Cytisus scoparius. The in vitro antimicrobial activity of this extract was evaluated on Gram-positive and Gram-negative bacteria and the fungus Candida albicans. Microbial species investigated, Bacillus cereus, Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa, are causing agents of several human and animal diseases. The extract showed activity against all tested species. So, it could be used for the development of biocides to control a wide range of pathogenic agents and contribute to the creation of economic and eco-friendly alternatives to antibiotics.

Keywords: antimicrobial properties, antioxidant properties, Cytisus scoparius, polyphenolic extract

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Authors: Felix Golla

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In an era where technology increasingly intersects with education, the potential of chatbots and ChatGPT agents in enhancing student learning experiences in higher education is both significant and timely. This study explores the integration of these AI-driven tools in educational settings, emphasizing their design and functionality to meet the specific needs of students. Recognizing the gap in literature concerning student-centered AI applications in education, this research offers valuable insights into the role and efficacy of chatbots and ChatGPT agents as educational tools. Employing qualitative research methodologies, the study involved conducting semi-structured interviews with university students. These interviews were designed to gather in-depth insights into the students' experiences and expectations regarding the use of AI in learning environments. The High-Performance Cycle Model, renowned for its focus on goal setting and motivation, served as the theoretical framework guiding the analysis. This model helped in systematically categorizing and interpreting the data, revealing the nuanced perceptions and preferences of students regarding AI tools in education. The major findings of the study indicate a strong preference among students for chatbots and ChatGPT agents that offer personalized interaction, adaptive learning support, and regular, constructive feedback. These features were deemed essential for enhancing student engagement, motivation, and overall learning outcomes. Furthermore, the study revealed that students perceive these AI tools not just as passive sources of information but as active facilitators in the learning process, capable of adapting to individual learning styles and needs. In conclusion, this study underscores the transformative potential of chatbots and ChatGPT agents in higher education. It highlights the need for these AI tools to be designed with a student-centered approach, ensuring their alignment with educational objectives and student preferences. The findings contribute to the evolving discourse on AI in education, suggesting a paradigm shift towards more interactive, responsive, and personalized learning experiences. This research not only informs educators and technologists about the desirable features of educational chatbots but also opens avenues for future studies to explore the long-term impact of AI integration in academic curricula.

Keywords: chatbot design in education, high-performance cycle model application, qualitative research in AI, student-centered learning technologies

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Authors: Adnan Bekhit, Eskedar Lodebo, Ariaya Hymete, Hanan Ragab, Alaa El-Din Bekhit

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Malaria and leishmaniasis have emerged as serious universal health problems throughout history of mankind. According to the WHO 2008 malarial report, half of the world population is at risk of malarial infection with an estimate of 1 million deaths occurring annually mainly in the African region. Furthermore, 12-15 million people are infected with Leishmaniasis worldwide. Despite the continuous introduction of a large number of agents for the treatment of malaria, there is still unmet medical needs due to the emergence of resistance. Resistance has occurred for almost all therapeutic agents approved for the treatment of malaria. Accordingly, it was the aim of this work to design and synthesis a group of antimalarial-antileshmanial agents that would show inhibitory activity against chloroquine-resistant strain of Plasmodium falciparum. The synthesized compounds were designed to contain a pyrazolylpyrazoline moiety having an aromatic group (p-tolyl or p-chlorophenyl) at N1-position of one pyrazoline ring due to the reports of promising activities of such compounds. A formyl or acyl substituent was introduced at the N1-position of the other pyrazoline ring, to investigate the effect of bulkiness of acyl substituents at this position. The synthesized compounds were evaluated for their in-vivo antimalarial activity against Plasmodium berghei infected mice at dose levels of 20 and 30 mg/Kg. the two most active compounds were evaluated for their antimalarial activity against chloroquin-resistant strain (RKL9) of Plasmodium falciparum. In addition, the synthesized compounds were tested for their in-vitro antileshmanial activity against Leishmania aethiopica promastigotes and amastigotes. For both antimalarial and antileishmanial activities, compounds having an N1-p-tolyl group at the first pyrazoline ring did not require bulkiness at the second pyrazoline ring nitrogen where the compound bearing an acetyl group proved to be the most active of the whole series. On the other hand, bulkiness at the N1-position of the second pyazoline ring was necessary in case of compounds carrying the p-chlorophenyl group, where the two derivatives having an N1-butanoyl and an N1-benzoyl moieties at the second pyrazoline showed the best activity. Furthermore, the toxicity of the active compounds were tested and were proved to be non-toxic at 125, 250 and 500 mg/Kg. In addition, docking of the most active compound (having a p-tolyl group at the first pyrazoline-N and an acetyl moiety on the other pyrazoline-N) was performed against dihydrofolate reductase enzyme.

Keywords: pyrazoline derivatives, in-vivo antimalarial activity, docking, dihydrofolate reductase

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Authors: Amna J. Ghith, Khaled Abu Zid, Khairia Youssef, Nasser Saad

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Backgrounds: The multikinase and vascular endothelial growth factor (VEGF) receptor inhibitors interrupt the pathway by which angiogenesis becomes established and promulgated, resulting in the inadequate nourishment of metastatic disease. VEGFR-2 has been the principal target of anti-angiogenic therapies. We disclose the new thieno pyrimidines as inhibitors of VEGFR-2 designed by a molecular modeling approach with increased synergistic activity and decreased side effects. Purpose: 2-substituted thieno pyrimidines are designed and synthesized with anticipated anticancer activity based on its in silico molecular docking study that supports the initial pharmacophoric hypothesis with a same binding mode of interaction at the ATP-binding site of VEGFR-2 (PDB 2QU5) with high docking score. Methods: A series of compounds were designed using discovery studio 4.1/CDOCKER with a rational that mimic the pharmacophoric features present in the reported active compounds that targeted VEGFR-2. An in silico ADMET study was also performed to validate the bioavailability of the newly designed compounds. Results: The Compounds to be synthesized showed interaction energy comparable to or within the range of the benzimidazole inhibitor ligand when docked with VEGFR-2. ADMET study showed comparable results most of the compounds showed absorption within (95-99) zone varying according to different substitutions attached to thieno pyrimidine ring system. Conclusions: A series of 2-subsituted thienopyrimidines are to be synthesized with anticipated anticancer activity and according to docking study structure requirement for the design of VEGFR-2 inhibitors which can act as powerful anticancer agents.

Keywords: docking, discovery studio 4.1/CDOCKER, heterocycles based anticancer agents, 2-subsituted thienopyrimidines

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Authors: Mahmoud H. Abu Elella, Riham R. Mohamed, Magdy W. Sabaa

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Introduction: Microbial pollution is global problem threatening the human health. It is resulted by pathogenic microorganisms such as Escherichia coli (E. coli), Staphylococcus aureus (S. aureus) and other pathogenic strains. They cause a dangerous effect on human health, so great efforts have been exerted to produce new and effective antimicrobial agents. Nowadays, natural polysaccharides, such as chitosan and its derivatives are used as antimicrobial agents. The aim of our work is to synthesize of a biodegradable polymer such as N-quaternized chitosan (NQC) then Characterization of NQC by using different analysis techniques such as Fourier transform infrared (FTIR) and Scanning electron microscopy (SEM) and using it as an antibacterial agent against different pathogenic bacteria. Methods: Synthesis of NQC using dimethylsulphate. Results: FTIR technique exhibited absorption peaks of NQC, SEM images illustrated that surface of NQC was smooth and antibacterial results showed that NQC had a high antibacterial effect. Discussion: NQC was prepared and it was proved by FTIR technique and SEM images antibacterial results exhibited that NQC was an antibacterial agent.

Keywords: antimicrobial agent, N-quaternized chitosan chloride, silver nanocomposites, sodium polyacrylate

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Authors: Rasha A.Ibrahim El-Ghazawy, Ashraf M. El-Saeed, Heusin El-Shafey, M. Abdel-Raheim, Maher A. El-Sockary

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Two thermotropic liquid crystalline curing agents based on abietic acid with different mesogens (LCC1 and LCC2) were synthesized for producing thermally stable liquid crystal networks suitable for high performance epoxy coatings. Differential scanning calorimetry (DSC) and polarized optical microscope (POM) was used to identify the liquid crystal phase transformation temperatures and texture, respectively. POM micro graphs for both LCCs revealing cholesteric texture. A multifunctional epoxy resin with two abietic acid moieties was also synthesized. Dynamic mechanical (DMA) and thermogravimetric (TGA) analyses show that the fully bio-based cured epoxies by either LCCs possess high glass transition temperature (Tg), high modulus (G`) and improved thermal stability. The chemical structure of the synthesized LCCs and epoxy resin was investigated through FTIR and 1HNMR spectroscopic techniques.

Keywords: abietic acid, dynamic mechanical analysis, epoxy resin, liquid crystal, thermo gravimetric analysis

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Authors: Zerrin Erginkaya, Gözde Konuray

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Microbial degradation of foods is defined as a decrease of food safety due to microorganism activity. Organic acids, sulfur dioxide, sulfide, nitrate, nitrite, dimethyl dicarbonate and several preservative gases have been used as chemical preservatives in foods as well as natural preservatives which are indigenous in foods. It is determined that usage of herbal preservatives such as blueberry, dried grape, prune, garlic, mustard, spices inhibited several microorganisms. Moreover, it is determined that animal origin preservatives such as whey, honey, lysosomes of duck egg and chicken egg, chitosan have antimicrobial effect. Other than indigenous antimicrobials in foods, antimicrobial agents produced by microorganisms could be used as natural preservatives. The antimicrobial feature of preservatives depends on the antimicrobial spectrum, chemical and physical features of material, concentration, mode of action, components of food, process conditions, and pH and storage temperature. In this review, studies about antimicrobial components which are indigenous in food (such as herbal and animal origin antimicrobial agents), antimicrobial materials synthesized by microorganisms, and their usage as an antimicrobial agent to preserve foods are discussed.

Keywords: animal origin preservatives, antimicrobial, chemical preservatives, herbal preservatives

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