Search results for: Hira Jabbar

Authors: Zubair Khaliq, M. Bilal Qadir, Amir Shahzad, Zulfiqar Ali, Ahsan Nazir, Ali Afzal, Abdul Jabbar

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Carbon fibers are one of the most demanding materials on earth due to their potential application in energy, high strength materials, and conductive materials. The nanostructure of carbon fibers offers enhanced properties of conductivity due to the larger surface area. The next generation carbon nanofibers demand the porous structure as it offers more surface area. Multiple techniques are used to produce carbon fibers. However, electrospinning followed by carbonization of the polymeric materials is easy to carry process on a laboratory scale. Also, it offers multiple diversity of changing parameters to acquire the desired properties of carbon fibers. Polyacrylonitrile (PAN) is the most used material for the production of carbon fibers due to its promising processing parameters. Also, cellulose is one of the highest yield producers of carbon fibers. However, the electrospinning of cellulosic materials is difficult due to its rigid chain structure. The combination of PAN and cellulose can offer a suitable solution for the production of carbon fibers. Both materials are miscible in the mixed solvent of N, N, Dimethylacetamide and lithium chloride. This study focuses on the production of porous carbon fibers as a function of PAN/Cellulose blend ratio, solution properties, and electrospinning parameters. These single polymer and blend with different ratios were electrospun to give fine fibers. The higher amount of cellulose offered more difficulty in electrospinning of nanofibers. After carbonization, the carbon fibers were studied in terms of their blend ratio, surface area, and texture. Cellulose contents offered the porous structure of carbon fibers. Also, the presence of LiCl contributed to the porous structure of carbon fibers.

Keywords: cellulose, polyacrylonitrile, carbon nanofibers, electrospinning, blend

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Authors: Tahir Ali Akbar, Hirra Jabbar

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Land cover change analysis plays a significant role in understanding the trends of urban sprawl and land use transformation due to anthropogenic activities. In this study, the spatio-temporal dynamics of major land covers were analyzed in the last twenty years (1988-2016) for District Lahore located in the Punjab Province of Pakistan. The Landsat satellite imageries were downloaded from USGS Global Visualization Viewer of Earth Resources Observation and Science Center located in Sioux Falls, South Dakota USA. The imageries included: (i) Landsat TM-5 for 1988 and 2001; and (ii) Landsat-8 OLI for 2016. The raw digital numbers of Landsat-5 images were converted into spectral radiance and then planetary reflectance. The digital numbers of Landsat-8 image were directly converted into planetary reflectance. The normalized difference vegetation index (NDVI) was used to classify the processed images into six major classes of water, buit-up, barren land, shrub and grassland, sparse vegetation and dense vegetation. The NDVI output results were improved by visual interpretation using high-resolution satellite imageries. The results indicated that the built-up areas were increased to 21% in 2016 from 10% in 1988. The decrease in % areas was found in case of water, barren land and shrub & grassland. There were improvements in percentage of areas for the vegetation. The increasing trend of urban sprawl for Lahore requires implementation of GIS based spatial planning, monitoring and management system for its sustainable development.

Keywords: land cover changes, NDVI, remote sensing, urban sprawl

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Authors: Hira Lal Gope, Hidekazu Fukai

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The aim of this study is to develop a system which can identify and sort peaberries automatically at low cost for coffee producers in developing countries. In this paper, the focus is on the classification of peaberries and normal coffee beans using image processing and machine learning techniques. The peaberry is not bad and not a normal bean. The peaberry is born in an only single seed, relatively round seed from a coffee cherry instead of the usual flat-sided pair of beans. It has another value and flavor. To make the taste of the coffee better, it is necessary to separate the peaberry and normal bean before green coffee beans roasting. Otherwise, the taste of total beans will be mixed, and it will be bad. In roaster procedure time, all the beans shape, size, and weight must be unique; otherwise, the larger bean will take more time for roasting inside. The peaberry has a different size and different shape even though they have the same weight as normal beans. The peaberry roasts slower than other normal beans. Therefore, neither technique provides a good option to select the peaberries. Defect beans, e.g., sour, broken, black, and fade bean, are easy to check and pick up manually by hand. On the other hand, the peaberry pick up is very difficult even for trained specialists because the shape and color of the peaberry are similar to normal beans. In this study, we use image processing and machine learning techniques to discriminate the normal and peaberry bean as a part of the sorting system. As the first step, we applied Deep Convolutional Neural Networks (CNN) and Support Vector Machine (SVM) as machine learning techniques to discriminate the peaberry and normal bean. As a result, better performance was obtained with CNN than with SVM for the discrimination of the peaberry. The trained artificial neural network with high performance CPU and GPU in this work will be simply installed into the inexpensive and low in calculation Raspberry Pi system. We assume that this system will be used in under developed countries. The study evaluates and compares the feasibility of the methods in terms of accuracy of classification and processing speed.

Keywords: convolutional neural networks, coffee bean, peaberry, sorting, support vector machine

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Authors: A. Hira Masood, B. Umer Hameed, C. Ezza Nasir

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Contemporary studies support the strong co-relation between psychology and design. This study elaborates how different psychological personality test can help a fashion designer to judge the needs of their clients with respect to have products which will satisfy the client's request concerning costumised clothing. This study will also help the designer to improve the lacking in the personality and will enable him to put his effort in required areas for grooming the customer, control and direct organization regarding quality maintenance. The use of psychology test to support the choice of certain design strategies that how the right clothing can make client a better intellectual with enhanced self-esteem and confidence. Different projective personality test are being used to suggest to evaluate personality traits. The Rorschach Inkblot Test is projective mental comprising of 10 ink-blots synonymous with the clinical brain research. Lüsher Color Diagnostics measures a person’s psycho physical state, his or her ability to withstand stress to perform and communicate. HTP is a projective responsibility test measuring self-perception, attitudes. The TAT test intend to evaluate a person’s patterns of thoughts, attitudes, observation, capacity and emotional response to this ambiguous test materials. No doubt designers are already crucially redesigning the individuals by their attires, but to expose the behavioral mechanism of the customer, designers should be able to recognize the hidden complexity behind his client by using the above mentioned methods. The study positively finds the design and psychology need to become substantially contacted in order to create a new regime of norms to groom a personality under the concentration and services of a fashion designer in terms of clothing, This interactive activity altimately upgrade design team to help customers to find the suited way to satisfy their needs and wishes, offer client relible relationship and quality management services, and to become more disereable.

Keywords: projective personality tests, customized clothing, Rorschach Inkblot test, TAT, HTP, Lüsher color diagnostics, quality management services

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Authors: Safee Chaudhary, Mahnoor Naseer Gondal, Hira Anees Awan, Abdul Rehman, Ammar Arif, Risham Hussain, Huma Khawar, Zainab Arshad, Muhammad Faizyab Ali Chaudhary, Waleed Ahmed, Muhammad Umer Sultan, Bibi Amina, Salaar Khan, Muhammad Moaz Ahmad, Osama Shiraz Shah, Hadia Hameed, Muhammad Farooq Ahmad Butt, Muhammad Ahmad, Sameer Ahmed, Fayyaz Ahmed, Omer Ishaq, Waqar Nabi, Wim Vanderbauwhede, Bilal Wajid, Huma Shehwana, Muhammad Tariq, Amir Faisal

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Cancer is a manifestation of multifactorial deregulations in biomolecular pathways. These deregulations arise from the complex multi-scale interplay between cellular and extracellular factors. Such multifactorial aberrations at gene, protein, and extracellular scales need to be investigated systematically towards decoding the underlying mechanisms and orchestrating therapeutic interventions for patient treatment. In this work, we propose ‘TISON’, a next-generation web-based multiscale modeling platform for clinical systems oncology. TISON’s unique modeling abstraction allows a seamless coupling of information from biomolecular networks, cell decision circuits, extra-cellular environments, and tissue geometries. The platform can undertake multiscale sensitivity analysis towards in silico biomarker identification and drug evaluation on cellular phenotypes in user-defined tissue geometries. Furthermore, integration of cancer expression databases such as The Cancer Genome Atlas (TCGA) and Human Proteome Atlas (HPA) facilitates in the development of personalized therapeutics. TISON is the next-evolution of multiscale cancer modeling and simulation platforms and provides a ‘zero-code’ model development, simulation, and analysis environment for application in clinical settings.

Keywords: systems oncology, cancer systems biology, cancer therapeutics, personalized therapeutics, cancer modelling

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Authors: Syeda Hira, Muhammad Gulfraz

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Background: Liver diseases cause serious health issues. Plants contain active compounds that significantly help in the treatment of various diseases. Ficus carica is traditionally used for the treatment of liver diseases. The purpose of the present study was the isolation and identification of active components from F.carica leaves which are responsible for hepatoprotective activity. Methods: The study was designed to identify the most active hepatoprotective sub-fraction from ethyl acetate fraction of Ficus carica by in vitro study and evaluation of its in vivo hepatoprotective effect in animal models. Ethyl acetate fraction was subjected to column, and a total of eight sub-fractions were obtained. In vitro, the hepatoprotective effect of all sub-fractions was determined on HepG2 cell lines. Toxicity was induced by CCl₄ (Carbon tetrachloride), and silymarin was used as a positive control. On the basis of the results, the most active sub-fraction was subjected to LC-MS and FT-IR analysis for the identification of bioactive compounds. In vivo, the hepatoprotective effect was determined in mice. Toxicity was induced by CCl₄; at the end of the experiment, biochemical parameters such as ALT, AST, ALP, bilirubin, and total protein were estimated in serum. Histopathology of liver tissues was also done. Results: Sub-fraction FVI exhibited significant (P<0.05) hepatoprotective activity as compared to other sub-fractions, which was almost similar to the standard drug silymarin. Six known bioactive compounds were identified from this sub-fraction after LC-MS analysis. In vivo, the hepatoprotective activity of sub-fraction FVI was evaluated in CCl₄-induced toxicated mice. Administration of CCl₄ significantly increased level of ALT (Alanine transaminase), AST (Aspartate aminotransferase), ALP (Alkaline phosphatase), and bilirubin and decreased the total protein. Treatment with sub-fraction FVI significantly (p<0.05) reversed the level of these biomarkers toward normal at both doses of 25 mg/kg and 50 mg/kg. Conclusion: Our findings confirmed the hepatoprotective effect of ethyl acetate fraction of F.carica. It could be a good candidate for the development of a natural hepatoprotective drug; pre-clinical investigation on ethyl acetate fraction is recommended.

Keywords: Ficus carica, hepatoprotective, CCl₄, bioactive compounds, liver markers

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Authors: Muhammad Arif Rahman, Gamma Abdul Jabbar, Enggar Handra Pangestu, Alfi Syahrin Qadri, Iryan Anugrah Putra, Rizqi Ramadhandi.

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Indonesia lies above three major tectonic plates, Indo-Australia plate, Eurasia plate, and Pacific plate. Interactions between those plates resulted in high tectonic and volcanic activities that corelates into high risk of geological hazards in adjacent areas, one of the areas is in North of Sulawesi’s Islands. This case raises a problem in terms of infrastructure in order to mitigate existing infrastructure and various future infrastructures plan. One of the infrastructures that is essentials to enhance telecommunication aspect is submarine fiber optic cable, that has risk to geological hazard. This cable is essential that act as backbone in telecommunication. Damaged fiber optic cables can pose serious problem that make existing signal to be loss and have negative impact to people’s social and economic factor with also decreasing various governmental services performance. Submarine cables are facing challenges in terms of geological hazards, for instance are seamounts activity. Previous studies show that until 2023, five seamounts are identified in North of Sulawesi. Seamounts itself can damage and trigger many activities that can risks submarine cables, one of the examples is submarine landslide. Main focuses of this study are to identify new possible seamounts and submarine landslide path in area North of Sulawesi Islands to help minimize risks pose by those hazards, either to existing or future plan submarine cables. Using bathymetry data, this study conduct slope analysis and use distinctive morphological features to interpret possible seamounts. Then we mapped out valleys in between seamounts and determine where sediments might flow in case of landslide, and to finally, know how it affect submarine cables in the area.

Keywords: bathymetry, geological hazard, mitigation, seamount, submarine cable, submarine landslide, volcanic activity

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Authors: Komal Ghafoor, Tauqir Ahmad, Murtaza Hanif, Hira Zaheer

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Assistive technology has been developed to support visually impaired people in their social interactions. Conversation assistive technology is designed to enhance communication skills, facilitate social interaction, and improve the quality of life of visually impaired individuals. This technology includes speech recognition, text-to-speech features, and other communication devices that enable users to communicate with others in real time. The technology uses natural language processing and machine learning algorithms to analyze spoken language and provide appropriate responses. It also includes features such as voice commands and audio feedback to provide users with a more immersive experience. These technologies have been shown to increase the confidence and independence of visually impaired individuals in social situations and have the potential to improve their social skills and relationships with others. Overall, conversation-assistive technology is a promising tool for empowering visually impaired people and improving their social interactions. One of the key benefits of conversation-assistive technology is that it allows visually impaired individuals to overcome communication barriers that they may face in social situations. It can help them to communicate more effectively with friends, family, and colleagues, as well as strangers in public spaces. By providing a more seamless and natural way to communicate, this technology can help to reduce feelings of isolation and improve overall quality of life. The main objective of this research is to give blind users the capability to move around in unfamiliar environments through a user-friendly device by face, object, and activity recognition system. This model evaluates the accuracy of activity recognition. This device captures the front view of the blind, detects the objects, recognizes the activities, and answers the blind query. It is implemented using the front view of the camera. The local dataset is collected that includes different 1st-person human activities. The results obtained are the identification of the activities that the VGG-16 model was trained on, where Hugging, Shaking Hands, Talking, Walking, Waving video, etc.

Keywords: dataset, visually impaired person, natural language process, human activity recognition

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Authors: Wajiha Javed, Arsalan Jabbar, Nelofer Mehboob, Muhammad Tafseer, Zahid Memon

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Introduction: Researchers globally have strived to explore diverse factors that augment the continuation and uptake of family planning methods. Clients’ satisfaction is one of the core determinants facilitating continuation of family planning methods. There is a major debate yet scanty evidence to contrast public and private sectors with respect to client satisfaction. The objective of this study is to compare quality-of-care provided by public and private sectors of Pakistan through a client satisfaction lens. Methods: We used Pakistan Demographic Heath Survey 2012-13 dataset (Sindh province) on a total of 3133 Married Women of Reproductive Age (MWRA) aged 15-49 years. Source of family planning (public/private sector) was the main exposure variable. Outcome variable was client satisfaction judged by ten different dimensions of client satisfaction. Means and standard deviations were calculated for continuous variable while for categorical variable frequencies and percentages were computed. For univariate analysis, Chi-square/Fisher Exact test was used to find an association between clients’ satisfaction in public and private sectors. Ten different multivariate models were made. Variables were checked for multi-collinearity, confounding, and interaction, and then advanced logistic regression was used to explore the relationship between client satisfaction and dependent outcome after adjusting for all known confounding factors and results are presented as OR and AOR (95% CI). Results: Multivariate analyses showed that clients were less satisfied in contraceptive provision from private sector as compared to public sector (AOR 0.92,95% CI 0.63-1.68) even though the result was not statistically significant. Clients were more satisfied from private sector as compared to the public sector with respect to other determinants of quality-of-care (follow-up care (AOR 3.29, 95% CI 1.95-5.55), infection prevention (AOR 2.41, 95% CI 1.60-3.62), counseling services (AOR 2.01, 95% CI 1.27-3.18, timely treatment (AOR 3.37, 95% CI 2.20-5.15), attitude of staff (AOR 2.23, 95% CI 1.50-3.33), punctuality of staff (AOR 2.28, 95% CI 1.92-4.13), timely referring (AOR 2.34, 95% CI 1.63-3.35), staff cooperation (AOR 1.75, 95% CI 1.22-2.51) and complications handling (AOR 2.27, 95% CI 1.56-3.29).

Keywords: client satisfaction, family planning, public private partnership, quality of care

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Authors: Rizwan Ahmed Bhutto, Noor ul ain Hira Bhutto, Mingwei Wang, Shahid Iqbal, Jiang Yi

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Curcumin, a natural polyphenolic compound, boasts numerous health benefits; however, its industrial applications are hindered by instabilities and poor solubility. Encapsulating curcumin in Pickering emulsion presents a promising strategy to enhance its bioavailability. Yet, the development of an efficient and straightforward method to fabricate a natural emulsifier for Pickering emulsion poses a significant challenge. Chitosan has garnered attention due to its non-toxicity and excellent emulsifying properties. This study aimed to prepare four distinct types of self-aggregated chitosan particles using a pH-responsive self-assembling approach. The properties of the aggregated particles were adjusted by pH, degree of deacetylation (DDA), and molecular weight (MW), thereby controlling surface charge, size (ranging from nano to micro and floc), and contact angle. Pickering emulsions were then formulated using these various aggregated particles. As MW and pH increased and DDA decreased, the networked structures of the aggregated particles formed, resulting in highly elastic gels that were more resistant to the breakdown of Pickering emulsion at ambient temperature. With elevated temperatures, the kinetic energy of the aggregated particles increased, disrupting hydrogen bonds and potentially transforming the systems from fluids to gels. The Pickering emulsion based on aggregated particles served as a carrier for curcumin encapsulation. It was observed that DDA and MW played crucial roles in regulating drug loading, encapsulation efficiency, and release profile. This research sheds light on selecting suitable chitosan for controlling the release of bioactive compounds in Pickering emulsions, considering factors such as adjustable rheological properties, microstructure, and macrostructure. Furthermore, this study introduces an environmentally friendly and cost-effective synthesis of pH-responsive aggregate particles without the need for high-pressure homogenizers. It underscores the potential of aggregate particles with various MWs and DDAs for encapsulating other bioactive compounds, offering valuable applications in industries including food, flavor/fragrance, cosmetics, and medicine.

Keywords: chitosan, molecular weight, rheological properties, curcumin encapsulation

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Authors: Iman Jabbar

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Within the scope of professionalism and in order to compete with the modern world, teachers, are expected to develop their teaching skills and activities in addition to their professional knowledge. At the college level, the teacher should be able to face classroom challenges through his engagement with the learning situation to understand the students and their needs. In our field of TESOL, the role of the English teacher is no longer restricted to teaching English texts, but rather he should endeavor to enhance the students’ skills such as communication and critical analysis. Within the literature of professionalism, there are certain strategies and tools that an English teacher should adopt to develop his competence and performance. Reflective practice, which is an exploratory process, is one of these strategies. Another strategy contributing to classroom development is motivation. It is crucial in students’ learning as it affects the quality of learning English in the classroom in addition to determining success or failure as well as language achievement. This is a qualitative study grounded on interpretive perspectives of teachers and students regarding the process of professional development. This study aims at (a) understanding how teachers at the college level conceptualize reflective practice and motivation inside EFL classroom, and (b) exploring the methods and strategies that they implement to practice reflection and motivation. This study and is based on two questions: 1. How do EFL teachers perceive and view reflection and motivation in relation to their teaching and professional development? 2. How can reflective practice and motivation be developed into practical strategies and actions in EFL teachers’ professional context? The study is organized into two parts, theoretical and practical. The theoretical part reviews the literature on the concept of reflective practice and motivation in relation to professional development through providing certain definitions, theoretical models, and strategies. The practical part draws on the theoretical one, however; it is the core of the study since it deals with two issues. It involves the research design, methodology, and methods of data collection, sampling, and data analysis. It ends up with an overall discussion of findings and the researcher's reflections on the investigated topic. In terms of significance, the study is intended to contribute to the field of TESOL at the academic level through the selection of the topic and investigating it from theoretical and practical perspectives. Professional development is the path that leads to enhancing the quality of teaching English as a foreign or second language in a way that suits the modern trends of globalization and advanced technology.

Keywords: professional development, motivation, reflection, learning

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Authors: Arsalan Jabbar, Wajiha Javed, Nelofer Mehboob, Zahid Memon

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Introduction: There are multiple social, individual and cultural factors that influence an individual’s decision to adopt family planning methods especially among non-users in patriarchal societies like Pakistan.Non-users, if targeted efficiently, can contribute significantly to country’s CPR. A research study showed that non-users if convinced to adopt lactational amenorrhea method can shift to long-term methods in future. Research shows that if non-users are targeted efficiently a 59% reduction in unintended pregnancies in Saharan Africa and South-Central and South-East Asia is anticipated. Methods: We did secondary data analysis on Pakistan Demographic Heath Survey (2012-13) dataset. Use of contraception (never-use/ever-use) was the outcome variable. At univariate level Chi-square/Fisher Exact test was used to assess relationship of baseline covariates with contraception use. Then variables to be incorporated in the model were checked for multi-collinearity, confounding, and interaction. Then binary logistic regression (with an urban-rural stratification) was done to find the relationship between contraception use and baseline demographic and social variables. Results: The multivariate analyses of the study showed that younger women (≤ 29 years) were more prone to be never users as compared to those who were > 30 years and this trend was seen in urban areas (AOR 1.92, CI 1.453-2.536) as well as rural areas (AOR 1.809, CI 1.421-2.303). While looking at regional variation, women from urban Sindh (AOR 1.548, CI 1.142-2.099) and urban Balochistan (AOR 2.403, CI 1.504-3.839) had more never users as compared to other urban regions. Women in the rich wealth quintile were more never users and this was seen both in urban and rural localities (urban (AOR 1.106 CI .753-1.624); rural areas (AOR 1.162, CI .887-1.524)) even though these were not statistically significant. Women idealizing more children(> 4) are more never users as compared to those idealizing less children in both urban (AOR 1.854, CI 1.275-2.697) and rural areas (AOR 2.101, CI 1.514-2.916). Women who never lost a pregnancy were more inclined to be non-users in rural areas (AOR 1.394, CI 1.127-1.723) .Women familiar with only traditional or no method had more never users in rural areas (AOR 1.717, CI 1.127-1.723) but in urban areas it wasn’t significant. Women unaware of Lady Health Worker’s presence in their area were more never users especially in rural areas (AOR 1.276, CI 1.014-1.607). Women who did not visit any care provider were more never users (urban (AOR 11.738, CI 9.112-15.121) rural areas (AOR 7.832, CI 6.243-9.826)). Discussion/Conclusion: This study concluded that government, policy makers and private sector family planning programs should focus on the untapped pool of never users (younger women from underserved provinces, in higher wealth quintiles, who desire more children.). We need to make sure to cover catchment areas where there are less LHWs and less providers as ignorance to modern methods and never been visited by an LHW are important determinants of never use. This all is in sync with previous literate from similar developing countries.

Keywords: contraception, demographic and health survey, family planning, never users

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Authors: Kirti Hira, A. Sajeli Begum, S. Mahibalan, Poorna Chandra Rao

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Introduction: Cancer is one of the leading causes of death worldwide. Although existing therapy effectively kills cancer cells, they do affect normal growing cells leading to many undesirable side effects. Hence there is need to develop effective as well as safe drug molecules to combat cancer, which is possible through phyto-research. The currently available plant-derived blockbuster drugs are the example for this. In view of this, an investigation was done to identify cytotoxic lead molecules from Hedyotis umbellata (Family Rubiaceae), a widely distributed weed in India. Materials and Methods: The methanolic extract of the whole plant of H. umbellata (MHU), prepared through Soxhlet extraction method was further fractionated with diethyl ether and n-butanol, successively. MHU, ether fraction (EMHU) and butanol fraction (BMHU) were lyophilized and were tested for the cytotoxic effect using 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay against non-small cell lung cancer (NSCLC) A549 cell lines. The potentially active EMHU was subjected to chromatographic purification using normal-phase silica columns, in order to isolate the responsible bioactive compounds. The isolated pure compounds were tested for their cytotoxic effect by MTT assay against A549 cells. Compound-3, which was found to be most active, was characterized using IR, 1H- and 13C-NMR and MS analysis. The study was further extended to decipher the mechanism of action of cytotoxicity of compound-3 against A549 cells through various in vitro cellular models. Cell cycle analysis was done using flow cytometry following PI (Propidium Iodide) staining. Protein analysis was done using Western blot technique. Results: Among MHU, EMHU, and BMHU, the non-polar fraction EMHU demonstrated a significant dose-dependent cytotoxic effect with IC50 of 67.7μg/ml. Chromatography of EMHU yielded seven compounds. MTT assay of isolated compounds explored compound-3 as potentially active one, which inhibited the growth of A549 cells with IC50value of 14.2μM. Further, compound-3 was identified as cedrelopsin, a coumarin derivative having molecular weight of 260. Results of in vitro mechanistic studies explained that cedrelopsin induced cell cycle arrest at G2/M phase and down-regulated the expression of G2/M regulatory proteins such as cyclin B1, cdc2, and cdc25C, dose dependently. This is the first report that explores the cytotoxic mechanism of cedrelopsin. Conclusion: Thus a potential small lead molecule, cedrelopsin isolated from H. umbellata, showing antiproliferative effect mediated by G2/M arrest in A549 cells was discovered. The effect of cedrelopsin against other cancer cell lines followed by in vivo studies can be performed in future to develop a new drug candidate.

Keywords: A549, cedrelopsin, G2/M phase, Hedyotis umbellata

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Authors: Sajeli A. Begum, Ameer Basha, Kirti Hira, Rukaiyya Khan

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Cyclic dipeptides are simple diketopiperazine derivatives being investigated by several scientists for their biological effects which include anticancer, antimicrobial, haematological, anticonvulsant, immunomodulatory effect, etc. They are potentially active microbial metabolites having been synthesized too, for developing into drug candidates. Cultures of Pseudomonas species have earlier been reported to produce cyclic dipeptides, helping in quorum sensing signals and bacterial–host colonization phenomena during infections, causing cell anti-proliferation and immunosuppression. Fluorescing Pseudomonas species have been identified to secrete lipid derivatives, peptides, pyrroles, phenazines, indoles, aminoacids, pterines, pseudomonic acids and some antibiotics. In the present work, results of investigation on the cyclic dipeptide metabolites secreted by the culture broth of Pseudomonas species as potent pro-inflammatory cytokine inhibitors are discussed. The bacterial strain was isolated from the rhizospheric soil of groundnut crop and identified as Pseudomonas aeruginosa by 16S rDNA sequence (GenBank Accession No. KT625586). Culture broth of this strain was prepared by inoculating into King’s B broth and incubating at 30 ºC for 7 days. The ethyl acetate extract of culture broth was prepared and lyophilized to get a dry residue (EEPA). Lipopolysaccharide (LPS)-induced ELISA assay proved the inhibition of tumor necrosis factor-alpha (TNF-α) secretion in culture supernatant of RAW 264.7 cells by EEPA (IC50 38.8 μg/mL). The effect of oral administration of EEPA on plasma TNF-α level in rats was tested by ELISA kit. The LPS mediated plasma TNF-α level was reduced to 45% with 125 mg/kg dose of EEPA. Isolation of the chemical constituents of EEPA through column chromatography yielded ten cyclic dipeptides, which were characterized using nuclear magnetic resonance and mass spectroscopic techniques. These cyclic dipeptides are biosynthesized in microorganisms by multifunctional assembly of non-ribosomal peptide synthases and cyclic dipeptide synthase. Cyclo (Gly-L-Pro) was found to be more potentially (IC50 value 4.5 μg/mL) inhibiting TNF-α production followed by cyclo (trans-4-hydroxy-L-Pro-L-Phe) (IC50 value 14.2 μg/mL) and the effect was equal to that of standard immunosuppressant drug, prednisolone. Further, the effect was analyzed by determining mRNA expression of TNF-α in LPS-stimulated RAW 264.7 macrophages using quantitative real-time reverse transcription polymerase chain reaction. EEPA and isolated cyclic dipeptides demonstrated diminution of TNF-α mRNA expression levels in a dose-dependent manner under the tested conditions. Also, they were found to control the expression of other pro-inflammatory cytokines like IL-1β and IL-6, when tested through their mRNA expression levels in LPS-stimulated RAW 264.7 macrophages under LPS-stimulated conditions. In addition, significant inhibition effect was found on Nitric oxide production. Further all the compounds exhibited weak toxicity to LPS-induced RAW 264.7 cells. Thus the outcome of the study disclosed the effectiveness of EEPA and the isolated cyclic dipeptides in down-regulating key cytokines involved in pathophysiology of autoimmune diseases.In another study led by the investigators, microbial cyclic dipeptides were found to exhibit excellent antimicrobial effect against Fusarium moniliforme which is an important causative agent of Sorghum grain mold disease. Thus, cyclic dipeptides are emerging small molecular drug candidates for various autoimmune diseases.

Keywords: cyclic dipeptides, cytokines, Fusarium moniliforme, Pseudomonas, TNF-alpha

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