Search results for: drug diffusion
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 3028

Search results for: drug diffusion

1258 Evaluation of Anti-Inflammatory Activities in Wild Herb Urginea wightii

Authors: S. K. Hemalata, M. N. Shiva Kameshwari

Abstract:

The present work focusses on anti-inflammatory action of Urginea wightii in-vitro. Urginea wightii is a member of Hyacinthaceae and considered to be wonder plant because of its varied important medicinal properties. The plant is endemic to India, Africa, and Mediterranian regions. Presence of alkaloids, flavonoid-glycosides especially flavonone derivatives are responsible for the strong anti-inflammatory activity of Urginea wightii. In present research work, anti-inflammatory activity of methanol extract of the bulb powder was tested on Male Wistar Rats. In these test animals, inflammation was induced by injecting carrageenan as the irritant to induce paw edema in Wistar rats. Inflammation of Paw edema was treated with both plant extract and Pyrox gel a known synthetic anti-inflammatory drug through external application. The result indicated that anti-inflammatory activity of Urginea wightii extract was almost similar to the synthetic Pyrox gel. This disproves the modern world's scepticism towards the herbal medicines and encourages to rely on natural plant extracts.

Keywords: anti-inflammatory activity, flavonoid-glycosides, Pyrox gel, Urginia wightii

Procedia PDF Downloads 148
1257 Asymmetrically Contacted Tellurium Short-Wave Infrared Photodetector with Low Dark Current and High Sensitivity at Room Temperature

Authors: Huang Haoxin

Abstract:

Large dark current at room temperature has long been the major bottleneck that impedes the development of high-performance infrared photodetectors towards miniaturization and integration. Although infrared photodetectors based on layered 2D narrow bandgap semiconductors have shown admirable advantages compared with those based on conventional compounds, which typically suffer from expensive cryogenic operations, it is still urgent to develop a simple but effective strategy to further reduce the dark current. Herein, a tellurium (Te) based infrared photodetector is reported with a specifically designed asymmetric electrical contact area. The deliberately introduced asymmetric electrical contact raises the electric field intensity difference in the Te channel near the drain and the source electrodes, resulting in spontaneous asymmetric carrier diffusion under global infrared light illumination under zero bias. Specifically, the Te-based photodetector presents promising detector performance at room temperature, including a low dark current of≈1 nA, an ultrahigh photocurrent/dark current ratio of 1.57×10⁴, a high specific detectivity (D*) of 3.24×10⁹ Jones, and relatively fast response speed of ≈720 μs at zero bias. The results prove that the simple design of asymmetric electrical contact areas can provide a promising solution to high-performance 2D semiconductor-based infrared photodetectors working at room temperature.

Keywords: asymmetrical contact, tellurium, dark current, infrared photodetector, sensitivity

Procedia PDF Downloads 25
1256 Smart Energy Storage: W₁₈O₄₉ NW/Ti₃C₂Tₓ Composite-Enabled All Solid State Flexible Electrochromic Supercapacitors

Authors: Muhammad Hassan, Kemal Celebi

Abstract:

Developing a highly efficient electrochromic energy storage device with sufficient color fluctuation and significant electrochemical performance is highly desirable for practical energy-saving applications. Here, to achieve a highly stable material with a large electrochemical storage capacity, a W₁₈O₄₉ NW/Ti₃C₂Tₓ composite has been fabricated and deposited on a pre-assembled Ag and W₁₈O₄₉ NW conductive network by Langmuir-Blodgett technique. The resulting hybrid electrode composed of 15 layers of W₁₈O₄₉ NW/Ti₃C₂Tₓ exhibits an areal capacitance of 125 mF/cm², with a fast and reversible switching response. An optical modulation of 98.2% can be maintained at a current density of 5 mAcm⁻². Using this electrode, we fabricated a bifunctional symmetric electrochromic supercapacitor device having an energy density of 10.26 μWh/cm² and a power density of 0.605 mW/cm², with high capacity retention and full columbic efficiency over 4000 charge-discharge cycles. Meanwhile, the device displays remarkable electrochromic characteristics, including fast switching time (5 s for coloring and 7 s for bleaching) and a significant coloration efficiency of 116 cm²/C with good optical modulation stability. In addition, the device exhibits remarkable mechanical flexibility and fast switching while being stable over 100 bending cycles, which is promising for real-world applications.

Keywords: MXene, nanowires, supercapacitor, ion diffusion, electrochromic, coloration efficiency

Procedia PDF Downloads 45
1255 Development of Thermo-Regulating Fabric Using Microcapsules of Phase Change Material

Authors: D. Benmoussa, H. Hannache, O. Cherkaoui

Abstract:

In textiles, the major interest in microencapsulation is currently in the application of durable fragrances, skin softeners, phase-change materials, antimicrobial agents and drug delivery systems onto textile materials. In our research “Polyethylene Glycol” was applied as phase change material and it was encapsulated in polymethacrylic acid (PMA) by radical polymerization in suspension of methacrylic acid in presence of N,N'-methylenebisacrylamide (MBAM) as crosslinking agent. Thereafter the obtained microcapsule was modified by amidation with ethylenediamine as a spacer molecule. At the end of this spacer trichlorotriazine reactive group was fixed. Microcapsules were grafted onto cotton textile substrate. The surface morphologies of the microencapsulated phase change materials (micro PCMs) were studied by scanning electron microscopy (SEM). Thermal properties, thermal reliabilities and thermal stabilities of the as-prepared micro PCMs were investigated by differential scanning calorimetry (DSC) and thermogravmetric analysis (TGA). The results obtained show the obtaining microcapsules with a mean diameter of 10 µm and the resistance of the microcapsules is demonstrated by thermal analysis.

Keywords: energy storage, microencapsulation, phase-change materials, thermogravmetric analysis (TGA)

Procedia PDF Downloads 655
1254 The Pressure Losses in the Model of Human Lungs

Authors: Michaela Chovancova, Pavel Niedoba

Abstract:

For the treatment of acute and chronic lung diseases it is preferred to deliver medicaments by inhalation. The drug is delivered directly to tracheobronchial tree. This way allows the given medicament to get directly into the place of action and it makes rapid onset of action and maximum efficiency. The transport of aerosol particles in the particular part of the lung is influenced by their size, anatomy of the lungs, breathing pattern and airway resistance. This article deals with calculation of airway resistance in the lung model of Horsfield. It solves the problem of determination of the pressure losses in bifurcation and thus defines the pressure drop at a given location in the bronchial tree. The obtained data will be used as boundary conditions for transport of aerosol particles in a central part of bronchial tree realized by Computational Fluid Dynamics (CFD) approach. The results obtained from CFD simulation will allow us to provide information on the required particle size and optimal inhalation technique for particle transport into particular part of the lung.

Keywords: human lungs, bronchial tree, pressure losses, airways resistance, flow, breathing

Procedia PDF Downloads 340
1253 miCoRe: Colorectal Cancer miRNAs Database

Authors: Rahul Agarwal, Ashutosh Singh

Abstract:

Colorectal cancer (CRC) also refers as bowel cancer or colon cancer. It involves the development of abnormal growth of cells in colon or rectum part of the body. This work leads to the development of a miRNA database in colorectal cancer. We named this database- miCoRe. This database comprises of all validated colon-rectal cancer miRNAs information from various published literature with an effectual knowledge based information retrieval system. miRNAs have been collected from various published literature reports. MySQL is used for main-framework of miCoRe while the front-end was developed in PHP script. The aim of developing miCoRe is to create a comprehensive central repository of colorectal carcinoma miRNAs with all germane information of miRNAs and their target genes. The current version of miCoRe consists of 238 miRNAs which are known to be implicated in malignancy of CRC. Alongside with miRNA information, miCoRe also contains the information related to the target genes of these miRNA. miCoRe furnishes the information about the mechanism of incidence and progression of the disease, which would further help the researchers to look for colorectal specific miRNAs therapies and CRC specific targeted drug designing. Moreover, it will also help in development of biomarkers for the better and early detection of CRC and will help in better clinical management of the disease.

Keywords: colorectal cancer, database, miCoRe, miRNAs

Procedia PDF Downloads 256
1252 Predicting and Obtaining New Solvates of Curcumin, Demethoxycurcumin and Bisdemethoxycurcumin Based on the Ccdc Statistical Tools and Hansen Solubility Parameters

Authors: J. Ticona Chambi, E. A. De Almeida, C. A. Andrade Raymundo Gaiotto, A. M. Do Espírito Santo, L. Infantes, S. L. Cuffini

Abstract:

The solubility of active pharmaceutical ingredients (APIs) is challenging for the pharmaceutical industry. The new multicomponent crystalline forms as cocrystal and solvates present an opportunity to improve the solubility of APIs. Commonly, the procedure to obtain multicomponent crystalline forms of a drug starts by screening the drug molecule with the different coformers/solvents. However, it is necessary to develop methods to obtain multicomponent forms in an efficient way and with the least possible environmental impact. The Hansen Solubility Parameters (HSPs) is considered a tool to obtain theoretical knowledge of the solubility of the target compound in the chosen solvent. H-Bond Propensity (HBP), Molecular Complementarity (MC), Coordination Values (CV) are tools used for statistical prediction of cocrystals developed by the Cambridge Crystallographic Data Center (CCDC). The HSPs and the CCDC tools are based on inter- and intra-molecular interactions. The curcumin (Cur), target molecule, is commonly used as an anti‐inflammatory. The demethoxycurcumin (Demcur) and bisdemethoxycurcumin (Bisdcur) are natural analogues of Cur from turmeric. Those target molecules have differences in their solubilities. In this way, the work aimed to analyze and compare different tools for multicomponent forms prediction (solvates) of Cur, Demcur and Biscur. The HSP values were calculated for Cur, Demcur, and Biscur using the chemical group contribution methods and the statistical optimization from experimental data. The HSPmol software was used. From the HSPs of the target molecules and fifty solvents (listed in the HSP books), the relative energy difference (RED) was determined. The probability of the target molecules would be interacting with the solvent molecule was determined using the CCDC tools. A dataset of fifty molecules of different organic solvents was ranked for each prediction method and by a consensus ranking of different combinations: HSP, CV, HBP and MC values. Based on the prediction, 15 solvents were selected as Dimethyl Sulfoxide (DMSO), Tetrahydrofuran (THF), Acetonitrile (ACN), 1,4-Dioxane (DOX) and others. In a starting analysis, the slow evaporation technique from 50°C at room temperature and 4°C was used to obtain solvates. The single crystals were collected by using a Bruker D8 Venture diffractometer, detector Photon100. The data processing and crystal structure determination were performed using APEX3 and Olex2-1.5 software. According to the results, the HSPs (theoretical and optimized) and the Hansen solubility sphere for Cur, Demcur and Biscur were obtained. With respect to prediction analyses, a way to evaluate the predicting method was through the ranking and the consensus ranking position of solvates already reported in the literature. It was observed that the combination of HSP-CV obtained the best results when compared to the other methods. Furthermore, as a result of solvent selected, six new solvates, Cur-DOX, Cur-DMSO, Bicur-DOX, Bircur-THF, Demcur-DOX, Demcur-ACN and a new Biscur hydrate, were obtained. Crystal structures were determined for Cur-DOX, Biscur-DOX, Demcur-DOX and Bicur-Water. Moreover, the unit-cell parameter information for Cur-DMSO, Biscur-THF and Demcur-ACN were obtained. The preliminary results showed that the prediction method is showing a promising strategy to evaluate the possibility of forming multicomponent. It is currently working on obtaining multicomponent single crystals.

Keywords: curcumin, HSPs, prediction, solvates, solubility

Procedia PDF Downloads 45
1251 Thermochemical Study of the Degradation of the Panels of Wings in a Space Shuttle by Utilization of HSC Chemistry Software and Its Database

Authors: Ahmed Ait Hou

Abstract:

The wing leading edge and nose cone of the space shuttle are fabricated from a reinforced carbon/carbon material. This material attains its durability from a diffusion coating of silicon carbide (SiC) and a glass sealant. During re-entry into the atmosphere, this material is subject to an oxidizing high-temperature environment. The use of thermochemical calculations resulting at the HSC CHEMISTRY software and its database allows us to interpret the phenomena of oxidation and chloridation observed on the wing leading edge and nose cone of the space shuttle during its mission in space. First study is the monitoring of the oxidation reaction of SiC. It has been demonstrated that thermal oxidation of the SiC gives the two compounds SiO₂(s) and CO(g). In the extreme conditions of very low oxygen partial pressures and high temperatures, there is a reaction between SiC and SiO₂, leading to SiO(g) and CO(g). We had represented the phase stability diagram of Si-C-O system calculated by the use of the HSC Chemistry at 1300°C. The principal characteristic of this diagram of predominance is the line of SiC + SiO₂ coexistence. Second study is the monitoring of the chloridation reaction of SiC. The other problem encountered in addition to oxidation is the phenomenon of chloridation due to the presence of NaCl. Indeed, after many missions, the leading edge wing surfaces have exhibited small pinholes. We have used the HSC Chemistry database to analyze these various reactions. Our calculations concorde with the phenomena we announced in research work resulting in NASA LEWIS Research center.

Keywords: thermochchemicals calculations, HSC software, oxidation and chloridation, wings in space

Procedia PDF Downloads 99
1250 Identification of Two Novel Carbapenemase Gene Variants from a Carbapenem-Resistant Aeromonas Veronii Environmental Isolate

Authors: Rafael Estrada, Cristian Ruiz Rueda

Abstract:

Carbapenems are last-resort antibiotics used in clinical settings to treat antibiotic-resistant bacterial infections. Thus, the emergence and spread of resistance to carbapenems is a major public health concern. Here, we have studied a carbapenem-resistant Aeromonas veronii strain previously isolated from a water sample from Sam Simeon Creek (Hearst San Simeon State Park, CA). Analysis of this isolate using disk-diffusion, CarbaNP, eCIM and mCIM assays revealed that it was resistant to amoxicillin-clavulanic acid and all carbapenems tested and that this isolate produced a potentially novel carbapenemase of the Metallo-β-lactamase family. Whole genome sequencing analysis revealed that this A. veronii isolate carries a novel variant of the blacₚₕₐ class β-carbapenemase gene that was closely related to the blacₚₕₐ₇ gene of Aeromonas jandaei. This isolate also carried a novel variant of the blaₒₓₐ class D carbapenemase gene that was most closely related to the blaₒₓₐ-₉₁₂ gene found in other Aeromonas veronii isolates. Finally, we also identified a novel class C β-lactamase gene moderately related to the blaFₒₓ-₁₇ gene of Providencia stuartii and other blaFₒₓ variants identified in Klebsiella pneumoniae, Escherichia coli and other Enterobacteriaceae. Overall, our findings reveal that environmental isolates are an important reservoir of multiple carbapenemases and other β-lactamases of clinical significance.

Keywords: β-lactamases, carbapenem, antibiotic-resistant, aeromonas veronii

Procedia PDF Downloads 72
1249 Arta (Calligonum Comosum, L'her.) Shoot Extract: Bio-mediator in Silver Nanoparticles Formation and Antimycotic Potential

Authors: Afrah E. Mohammed, Mudawi M. Nour

Abstract:

Environmentally friendly green synthesis of nanomaterial has a very significant part in nanotechnology. In the present research, the synthesis of silver nanoparticles (AgNPs) was established by treating silver ions with the aqueous extract of Calligonum comosum green shoots at room temperature. AgNPs formation was firstly detected by the colour change of mixed extract (plant extract and AgNO3). Further characterization was done by ultraviolet (UV)-Vis spectrophotometer, transmission electron microscopy (TEM), scanning electron microscopy (SEM), zeta potential and fourier transform infrared spectroscopy (FTIR). The peak values for UV-VIS- spectroscopy were in the range of 440 nm, TEM micrograph showed a spherical shape for the particles and zeta potential showed the formation of negative charged nanoparticles with an average size of about 105.8 nm. 1635.41 and 3249.83 cm−1 are the peaks detected from the FTIR analysis. In this study, biosynthesized silver nanoparticles mediated by C. comosum were tested for their antimycotic activity using a well diffusion method against fungal species; Aspergillus flavus, Penicillium sp, Fusarium oxysporum. Our findings indicated that biosynthesized AgNPs showed an efficient antimycotic activity against tested species. The antimycotic action of AgNPs varied according to different fungal species. Results confirmed the ability of C. comosum green shoot extract to act as an reducing and stabilizing agent during the synthesis of AgNPs.

Keywords: AGNPS, zeta potential, TEM, SEM

Procedia PDF Downloads 62
1248 Analgesic and Antipyretic Activity of Thunbergia laurifolia Lindl. Extract

Authors: Nantawan Soonklang, Linda Chularojanamontri, Urarat Nanna

Abstract:

Ethnopharmacological relevance: Thunbergia laurifolia Lindl. belongs to the family Acanthaceae commonly known as Rang jeud in Thailand. This plant is traditionally used in Thailand for centuries as an antidote for several poisons and drug overdose. Aim of the study: This research aimed to study the analgesic and antipyretic activities of T. laurifolia water extract by using animal models. Materials and Methods: The analgesic activity was studied using 2 methods of pain induction including acetic acid and heat induced pain. And the antipyretic activity study was performed by yeast-induced hyperthermia. Results: The results showed that the administration of T. laurifolia extract possessed analgesic activity by reducing acetic acid-induced writhing response and heat-induced pain as well as showed antipyretic activity by decreasing body temperature of hyperthermic rats induced by brewer’s yeast. Conclusion: The study indicates that the T. laurifolia extract possesses analgesic and antipyretic activities in animals.

Keywords: Thunbergia laurifolia extract, analgesic activity, antipyretic activity, hyperthermia

Procedia PDF Downloads 368
1247 Lessons Learned in Developing a Clinical Information System and Electronic Health Record (EHR) System That Meet the End User Needs and State of Qatar's Emerging Regulations

Authors: Darshani Premaratne, Afshin Kandampath Puthiyadath

Abstract:

The Government of Qatar is taking active steps in improving quality of health care industry in the state of Qatar. In this initiative development and market introduction of Clinical Information System and Electronic Health Record (EHR) system are proved to be a highly challenging process. Along with an organization specialized on EHR system development and with the blessing of Health Ministry of Qatar the process of introduction of EHR system in Qatar healthcare industry was undertaken. Initially a market survey was carried out to understand the requirements. Secondly, the available government regulations, needs and possible upcoming regulations were carefully studied before deployment of resources for software development. Sufficient flexibility was allowed to cater for both the changes in the market and the regulations. As the first initiative a system that enables integration of referral network where referral clinic and laboratory system for all single doctor (and small scale) clinics was developed. Setting of isolated single doctor clinics all over the state to bring in to an integrated referral network along with a referral hospital need a coherent steering force and a solid top down framework. This paper discusses about the lessons learned in developing, in obtaining approval of the health ministry and in introduction to the industry of the single doctor referral network along with an EHR system. It was concluded that development of this nature required continues balance between the market requirements and upcoming regulations. Further accelerating the development based on the emerging needs, implementation based on the end user needs while tallying with the regulations, diffusion, and uptake of demand-driven and evidence-based products, tools, strategies, and proper utilization of findings were equally found paramount in successful development of end product. Development of full scale Clinical Information System and EHR system are underway based on the lessons learned. The Government of Qatar is taking active steps in improving quality of health care industry in the state of Qatar. In this initiative development and market introduction of Clinical Information System and Electronic Health Record (EHR) system are proved to be a highly challenging process. Along with an organization specialized on EHR system development and with the blessing of Health Ministry of Qatar the process of introduction of EHR system in Qatar healthcare industry was undertaken. Initially a market survey was carried out to understand the requirements. Secondly the available government regulations, needs and possible upcoming regulations were carefully studied before deployment of resources for software development. Sufficient flexibility was allowed to cater for both the changes in the market and the regulations. As the first initiative a system that enables integration of referral network where referral clinic and laboratory system for all single doctor (and small scale) clinics was developed. Setting of isolated single doctor clinics all over the state to bring in to an integrated referral network along with a referral hospital need a coherent steering force and a solid top down framework. This paper discusses about the lessons learned in developing, in obtaining approval of the health ministry and in introduction to the industry of the single doctor referral network along with an EHR system. It was concluded that development of this nature required continues balance between the market requirements and upcoming regulations. Further accelerating the development based on the emerging needs, implementation based on the end user needs while tallying with the regulations, diffusion, and uptake of demand-driven and evidence-based products, tools, strategies, and proper utilization of findings were equally found paramount in successful development of end product. Development of full scale Clinical Information System and EHR system are underway based on the lessons learned.

Keywords: clinical information system, electronic health record, state regulations, integrated referral network of clinics

Procedia PDF Downloads 348
1246 Analysis of Patient No-Shows According to Health Conditions

Authors: Sangbok Lee

Abstract:

There has been much effort on process improvement for outpatient clinics to provide quality and acute care to patients. One of the efforts is no-show analysis or prediction. This work analyzes patient no-shows along with patient health conditions. The health conditions refer to clinical symptoms that each patient has, out of the followings; hyperlipidemia, diabetes, metastatic solid tumor, dementia, chronic obstructive pulmonary disease, hypertension, coronary artery disease, myocardial infraction, congestive heart failure, atrial fibrillation, stroke, drug dependence abuse, schizophrenia, major depression, and pain. A dataset from a regional hospital is used to find the relationship between the number of the symptoms and no-show probabilities. Additional analysis reveals how each symptom or combination of symptoms affects no-shows. In the above analyses, cross-classification of patients by age and gender is carried out. The findings from the analysis will be used to take extra care to patients with particular health conditions. They will be forced to visit clinics by being informed about their health conditions and possible consequences more clearly. Moreover, this work will be used in the preparation of making institutional guidelines for patient reminder systems.

Keywords: healthcare system, no show analysis, process improvment, statistical data analysis

Procedia PDF Downloads 216
1245 Environmental Risk of Pharmaceuticals, Drugs of Abuse and Stimulant Caffeine in Marine Water: A Case Study in the North-Western of Spain

Authors: Raquel Dafouz Neus Cáceres, Javier Fernandez-Rubio, Belinda Huerta José Luis Rodríguez-Gil, Nicola Mastroianni, Miren López de Alda, Damià Barceló, Yolanda Valcárcel

Abstract:

The region of Galicia, found in north-western (NW) Spain, is a national and world leader in shellfish, especially mussel production, and recognized for its fishing industry. Few studies have evaluated the presence of emerging contaminants in NW Spain, with those published mainly concerning the continental aquatic environment. The objective of this study was to identify the environmental risk posed by the presence of pharmaceuticals and drugs of abuse in this important coastal region. The presence of sixteen pharmaceuticals (benzodiazepines, anxiolytics, and caffeine), and 19 drugs of abuse (cocainics, amphetamine-like compounds, opiates and opioids, lysergic compounds, and cannabinoids) was assessed in 23 sites located in the Rías (Coastal inlets) of Muros, Arousa, and Pontevedra (NW Spain). Twenty-two of these locations were affected by waste-water treatment plant (WWTP) effluents, and one represented the effluent of one of these WWTPs. Venlafaxine was the pharmaceutical compound detected at higher concentration in the three Rías, with a maximum value of 291 ng/L at the site Porto do Son (Ría de Muros). Total concentration in the three Rías was 819,26 ng/L. Next, citalopram and lorazepam were the most prevalent compounds detected. Metabolite of cocaine benzoylecgonine was the drug of abuse with the highest concentration, measured at 972 ng/L in the Ría of Noia WWTP (no dilution). This compound was also detected at 142 ng/L in the site La Isla de Aros, Ría of Pontevedra. Total concentration for the three Rías was 1210 ng/L. Ephedrine was also detected at high level in the three Rías, with a total concentration of 579,28 ng/L. The results obtained for caffeine show maximum and average concentrations of 857 ng/L Isla de Arosa, Ría de Pontevedra the highest measured in seawater in Spain. A preliminary hazard assessment was carried out by comparing these measured environmental concentrations (MEC) to predicted no-effect concentrations (PNECs) for aquatic organisms. Six out of the 22 seawater samples resulted in a Hazard Quotient (HQ) from chronic exposure higher than 1 with the highest being 17.14, indicating a high probability of adverse effects in the aquatic environment. In addition, the risk was assessed on the basis of persistence, bioaccumulation, and toxicity (PBT). This work was financially supported by the Spanish Ministry of Economy and Competitiveness through the Carlos III Health Institute and the program 'Proyectos de Investigacion en Salud 2015-2017' FIS (PI14/00516), the European Regional Development Fund (ERDF), the Catalan Government (Consolidated Research Groups '2014 SGR 418 - Water and Soil Quality Unit' and 2014 SGR 291 - ICRA), and the European Union’s Seventh Framework Programme for research, technological development and demonstration under grant agreement no. 603437. The poster entitled 'Environmental Risk of Pharmaceuticals, Drugs of Abuse and Stimulant Caffeine in Marine Water: A Case Study in the North-Western of Spain'.

Keywords: drug of abuse, pharmaceuticals, caffeine, environmental risk, seawater

Procedia PDF Downloads 204
1244 The Effects of Xiang Sha Liu Jun Zi Tang to Diarrhea and Growth Performance of Piglets

Authors: Siao-Wei Jiang, Boy-Young Hsieh, Ching-Liang Hsieh, Cheng-Yung Lin

Abstract:

The problems of multiple drug resistance in the pig farming industry have been emphasized in recent years. Diarrhea syndrome is common in weaning piglets and often treated with antibiotics as a feed additive, leading to the rapid spread of antibiotic resistance and posing high health risks to humans. The study aimed to alleviate diarrhea syndrome with traditional herbal medicine, Xiang Sha Liu Jun Zi Tang, whose effects enhanced digestive function. Piglets at 4 weeks old with stool classified to Bristol stool classification type 6 or type 7 were randomly divided into the control group, group A (1% of Xiang Sha Liu Jun Zi Tang) and group B (0.1% Colistin). The piglets were administrated for 7 days, and their weight, feed intake, and stool score were recorded daily before and after the trial. The results showed that the diarrhea index score in group A and group B improved significantly compared to the control group, indicating that Xiang Sha Liu Jun Zi Tang may have the same effect on alleviating diarrhea syndrome as Colistin, and it may be another replacement for antibiotics.

Keywords: pig, diarrhea, herbal medicine, Xiang Sha Liu Jun Zi Tang

Procedia PDF Downloads 34
1243 LncRNA-miRNA-mRNA Networks Associated with BCR-ABL T315I Mutation in Chronic Myeloid Leukemia

Authors: Adenike Adesanya, Nonthaphat Wong, Xiang-Yun Lan, Shea Ping Yip, Chien-Ling Huang

Abstract:

Background: The most challenging mutation of the oncokinase BCR-ABL protein T315I, which is commonly known as the “gatekeeper” mutation and is notorious for its strong resistance to almost all tyrosine kinase inhibitors (TKIs), especially imatinib. Therefore, this study aims to identify T315I-dependent downstream microRNA (miRNA) pathways associated with drug resistance in chronic myeloid leukemia (CML) for prognostic and therapeutic purposes. Methods: T315I-carrying K562 cell clones (K562-T315I) were generated by the CRISPR-Cas9 system. Imatinib-treated K562-T315I cells were subjected to small RNA library preparation and next-generation sequencing. Putative lncRNA-miRNA-mRNA networks were analyzed with (i) DESeq2 to extract differentially expressed miRNAs, using Padj value of 0.05 as cut-off, (ii) STarMir to obtain potential miRNA response element (MRE) binding sites of selected miRNAs on lncRNA H19, (iii) miRDB, miRTarbase, and TargetScan to predict mRNA targets of selected miRNAs, (iv) IntaRNA to obtain putative interactions between H19 and the predicted mRNAs, (v) Cytoscape to visualize putative networks, and (vi) several pathway analysis platforms – Enrichr, PANTHER and ShinyGO for pathway enrichment analysis. Moreover, mitochondria isolation and transcript quantification were adopted to determine the new mechanism involved in T315I-mediated resistance of CML treatment. Results: Verification of the CRISPR-mediated mutagenesis with digital droplet PCR detected the mutation abundance of ≥80%. Further validation showed the viability of ≥90% by cell viability assay, and intense phosphorylated CRKL protein band being detected with no observable change for BCR-ABL and c-ABL protein expressions by Western blot. As reported by several investigations into hematological malignancies, we determined a 7-fold increase of H19 expression in K562-T315I cells. After imatinib treatment, a 9-fold increment was observed. DESeq2 revealed 171 miRNAs were differentially expressed K562-T315I, 112 out of these miRNAs were identified to have MRE binding regions on H19, and 26 out of the 112 miRNAs were significantly downregulated. Adopting the seed-sequence analysis of these identified miRNAs, we obtained 167 mRNAs. 6 hub miRNAs (hsa-let-7b-5p, hsa-let-7e-5p, hsa-miR-125a-5p, hsa-miR-129-5p, and hsa-miR-372-3p) and 25 predicted genes were identified after constructing hub miRNA-target gene network. These targets demonstrated putative interactions with H19 lncRNA and were mostly enriched in pathways related to cell proliferation, senescence, gene silencing, and pluripotency of stem cells. Further experimental findings have also shown the up-regulation of mitochondrial transcript and lncRNA MALAT1 contributing to the lncRNA-miRNA-mRNA networks induced by BCR-ABL T315I mutation. Conclusions: Our results have indicated that lncRNA-miRNA regulators play a crucial role not only in leukemogenesis but also in drug resistance, considering the significant dysregulation and interactions in the K562-T315I cell model generated by CRISPR-Cas9. In silico analysis has further shown that lncRNAs H19 and MALAT1 bear several complementary miRNA sites. This implies that they could serve as a sponge, hence sequestering the activity of the target miRNAs.

Keywords: chronic myeloid leukemia, imatinib resistance, lncRNA-miRNA-mRNA, T315I mutation

Procedia PDF Downloads 139
1242 Mathematical Modelling of Ultrasound Pre-Treatment in Microwave Dried Strawberry (Fragaria L.) Slices

Authors: Hilal Uslu, Salih Eroglu, Betul Ozkan, Ozcan Bulantekin, Alper Kuscu

Abstract:

In this study, the strawberry (Fragaria L.) fruits, which were pretreated with ultrasound (US), were worked on in the microwave by using 90W power. Then mathematical modelling was applied to dried fruits by using different experimental thin layer models. The sliced fruits were subjected to ultrasound treatment at a frequency of 40 kHz for 10, 20, and 30 minutes, in an ultrasonic water bath, with a ratio of 1:4 to fruit/water. They are then dried in the microwave (90W). The drying process continued until the product moisture was below 10%. By analyzing the moisture change of the products at a certain time, eight different thin-layer drying models, (Newton, page, modified page, Midilli, Henderson and Pabis, logarithmic, two-term, Wang and Singh) were tested for verification of experimental data. MATLAB R2015a statistical program was used for the modelling, and the best suitable model was determined with R²adj (coefficient of determination of compatibility), and root mean square error (RMSE) values. According to analysis, the drying model that best describes the drying behavior for both drying conditions was determined as the Midilli model by high R²adj and low RMSE values. Control, 10, 20, and 30 min US for groups R²adj and RMSE values was established as respectively; 0,9997- 0,005298; 0,9998- 0,004735; 0,9995- 0,007031; 0,9917-0,02773. In addition, effective diffusion coefficients were calculated for each group and were determined as 3,80x 10⁻⁸, 3,71 x 10⁻⁸, 3,26 x10⁻⁸ ve 3,5 x 10⁻⁸ m/s, respectively.

Keywords: mathematical modelling, microwave drying, strawberry, ultrasound

Procedia PDF Downloads 139
1241 Development of Starch Nanoparticles as Vehicles for Curcumin Delivery

Authors: Fernando G. Torres, Omar P. Troncoso

Abstract:

Starch is a highly biocompatible, non-toxic, and biodegradable polymer. It is widely used in biomedical applications, including drug delivery systems and tissue engineering scaffolds. Curcumin, a phenolic compound found in the dried root of Curcuma longa, has been used as a nutritional supplement due to its antimicrobial, anti-inflammatory, and antioxidant effects. However, the major problem with ingesting curcumin by itself is its poor bioavailability due to its poor absorption and rapid metabolism. In this study, we report a novel methodology to prepare starch nanoparticles loaded with curcumin. The nanoparticles were synthesized via nanoprecipitation of starch granules extracted from native Andean potatoes (Solanum tuberosum ssp. and Andigena var Huamantanga varieties). The nanoparticles were crosslinked and stabilized by using sodium tripolyphosphate and Tween®80, respectively. The characterization of the nanoparticles loaded with curcumin was assessed by Fourier Transform Infrared Spectroscopy, Dynamic Light Scattering, Zeta potential, and Differential scanning calorimetry. UV-vis spectrophotometry was used to evaluate the loading efficiency and capacity of the samples. The results showed that native starch nanoparticles could be used to prepare promising nanocarriers for the controlled release of curcumin.

Keywords: starch nanoparticle, nanoprecipitation, curcumin, biomedical applications

Procedia PDF Downloads 104
1240 Evaluation of Anticancer and Antioxidant Activity of Purified Lovastatin from Aspergillus terreus (KM017963)

Authors: Bhargavi Santebennur Dwarakanath, Praveen Vadakke Kamath, Savitha Janakiraman

Abstract:

Cervical cancer is one of the leading causes of mortality in women and is the second most common malignancy worldwide. Lovastatin, a non polar, anticholesterol drug which also exerts antitumour activity in vitro. In the present study, lovastatin from Aspergillus terreus (KM017963) was purified by adsoprtion chromatography and evaluated for its anticancer and anti-oxidant properties in human cervical cancer cell lines (HeLa). The growth inhibitory and proapoptotic effects of purified lovastatin on HeLa cell lines were investigated by determining its influence on cytotoxicity, Mitochondrial Membrane Potential (MMP), DNA fragmentation and antioxidant property (Hydroxy radical scavenging effect and the levels of total reduced glutathione). Flow cytometry analysis by propidium iodide staining confirmed the induction of apoptotic cell death and revealed cell cycle arrest at G0/G1 phase. Results of the study give leads for anticancer effects of lovastatin and its potential efficacy in the chemotherapy of cervical cancer.

Keywords: apoptosis, Aspergillus terreus, cervical cancer, lovastatin

Procedia PDF Downloads 292
1239 Determination of the Effect of Kaolin on the Antimicrobial Activity of Metronidazole-Kaolin Interaction

Authors: Omaimah Algohary

Abstract:

Kaolin is one of the principle intestinal adsorbents, has traditionally been used internally in the treatment of various enteric disorders, colitis, enteritis, dysentery, and diarrhea associated with food and alkaloidal poisoning and in traveler’s diarrhea. It binds to and traps bacteria and its toxins and gases in the gut. It also binds to water in the gut, which helps to make the stools firmer, hence giving symptomatic relief. Metronidazole is a synthetic antibacterial agent that is used primarily in the treatment of various anaerobic infections such as intra-abdominal infections, antiprotozoal, and as amebicidal. The need for safe, therapeutically effective antidiarrheal combination continuously lead to effective treatment. Metronidazol used for treatment of anaerobic bacteria and kaolin , when administered simultaneously, Metronidazole–Kaolin interactions have been reported by FDA but not studied. This project is the first to study the effect of Metronidazole–Kaolin interactions on the antimicrobial activity of metronidazole. Agar diffusion method performed to test the antimicrobial activity of metronidazole–kaolin antidiarrheal combination from aqueous solutions at an in-vivo simulated pHs conditions that obtained at 37+0.5 °C on Helicobacter pylori as anaerobic bacteria and E.coli as aerobic bacteria and used as a control for the technique. The antimicrobial activity of metronidazole combination as 1:1 and 1:2 with kaolin was abolished in acidic media as no zones of inhibition shown compared to only metronidazole that used as a control. In alkaline media metronidazole combination as 1:1 and 1:2 with kaolin showed diminutive activity compared to the control. These results proved that the kaolin adsorb metronidazole and abolish its antimicrobial activity and such combination should be avoided.

Keywords: kaolin, metronidazole, interaction, Helicobacter pylori. E. coli, antimicrobial activity

Procedia PDF Downloads 370
1238 In Vitro Antibacterial Effect of Hydroalcoholic Extract of Lawsonia Inermis, Malva Sylvestris and Boswellia Serrata on Aggregatibacter Actinomycetemcomitans

Authors: Surena V.

Abstract:

Background and Aim: Periodontal diseases are among the most common infectious diseases all around the world, even in developed countries. Considering the increased rate of microbial resistance to antibiotics and the chemical side effects of antibiotics and antiseptics used for the treatment of periodontal disease, there is a need for an alternative antimicrobial agent with fewer complications. Medicinal herbs have recently become popular as antimicrobial and preventive agents. This study aimed to assess the antibacterial effects of hydroalcoholic extracts of Lawsonia inermis, Malva sylvestris and Boswellia serrata on Aggregatibacter actinomycetemcomitans (A. actinomycetemcomitans). Materials and Methods: Hydroalcoholic extracts of the three medicinal plants were obtained by the maceration technique and A. actinomycetemcomitans was cultured. The antimicrobial efficacy of the three medicinal plants was compared with that of 0.2% chlorhexidine (CHX) according to the CLSI protocol using agar disc diffusion and broth microdilution techniques. All tests were repeated three times. Results: Hydroalcoholic extracts of all three plants had antimicrobial activity against A. actinomycetemcomitans. The minimum inhibitory concentration (MIC) of Lawsonia inermis, Malva sylvestris, and Boswellia serrata was 78.1, 156.2, and 1666 µg/mL with no significant difference between them. The MIC of CHX was 3.33 µg/mL, which was significantly higher than that of Boswellia serrata extract. Conclusion: Given that, further in vivo studies confirm other properties of these extracts and their safety in terms of cytotoxicity and mutagenicity, hydroalcoholic extracts of Lawsonia inermis and Malva sylvestris may be used in mouthwashes or local delivery systems to affect periodontal biofilm.

Keywords: actinobacilus actinomycetem commitans, lawsonia inermis, malva sylvestris, boswellia serrata

Procedia PDF Downloads 40
1237 An Application of Vector Error Correction Model to Assess Financial Innovation Impact on Economic Growth of Bangladesh

Authors: Md. Qamruzzaman, Wei Jianguo

Abstract:

Over the decade, it is observed that financial development, through financial innovation, not only accelerated development of efficient and effective financial system but also act as a catalyst in the economic development process. In this study, we try to explore insight about how financial innovation causes economic growth in Bangladesh by using Vector Error Correction Model (VECM) for the period of 1990-2014. Test of Cointegration confirms the existence of a long-run association between financial innovation and economic growth. For investigating directional causality, we apply Granger causality test and estimation explore that long-run growth will be affected by capital flow from non-bank financial institutions and inflation in the economy but changes of growth rate do not have any impact on Capital flow in the economy and level of inflation in long-run. Whereas, growth and Market capitalization, as well as market capitalization and capital flow, confirm feedback hypothesis. Variance decomposition suggests that any innovation in the financial sector can cause GDP variation fluctuation in both long run and short run. Financial innovation promotes efficiency and cost in financial transactions in the financial system, can boost economic development process. The study proposed two policy recommendations for further development. First, innovation friendly financial policy should formulate to encourage adaption and diffusion of financial innovation in the financial system. Second, operation of financial market and capital market should be regulated with implementation of rules and regulation to create conducive environment.

Keywords: financial innovation, economic growth, GDP, financial institution, VECM

Procedia PDF Downloads 245
1236 Chemical Composition and Antibacterial Activity of the Essential Oils from Bunium alpinum and Bunium incrassatum

Authors: Hayet El Kolli, Hocine Laouer

Abstract:

Bunium in the world comprises about 50 to 100 species, mostly distributed in: Algeria, Italy, Pakistan, Iran, and South Africa. Bunium species have several uses like: Bunium persicum which is commonly used as antispasmodic, carminative, anti-obesity and lactogage. This plant have been widely used as an additive in food stuff such as in bread cooking, rice and yoghurt for its carminative, anti-dyspepsia and antispasmodic effect. The B. paucifolium oil has a wide spectrum of action against moulds, yeast and bacteria. The chemical compositions of Bunium incrassatum and Bunium alpinum essential oils were carry out by GC and GC/MS. Therefore, antibacterial activity of two oils was investigated by disk diffusion method against Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922, Salmonella typhimurium ATCC 1331, Staphylococcus aureus ATCC 25923, Klebsiella pneumoniae ATCC 700603, Bacillus cereus ATCC 10876, Enterococcus faecalis ATCC 49452, Lysteria monocytogenes ATCC 15313, Citrobacter freundii ATCC 8090, Proteus mirabilis ATCC 35659. A moderate antibacterial activity was found. In conclusion, it is found that essential oils of the two species are rich in sesquiterpens and other oxygenated compounds. These compounds have been reported to show bactericidal activity and the presence of phenolic compounds makes them useful antioxidants so that results confirm some ethnopharmacologique applications of these two oils of Bunium.

Keywords: Bunium alpinum, Bunium incrassatum, apiaceae, essential oil, sesquiterpens, phenols, antibacterial, antioxidant activities

Procedia PDF Downloads 357
1235 Estimation of Human Absorbed Dose Using Compartmental Model

Authors: M. Mousavi-Daramoroudi, H. Yousefnia, F. Abbasi-Davani, S. Zolghadri

Abstract:

Dosimetry is an indispensable and precious factor in patient treatment planning to minimize the absorbed dose in vital tissues. In this study, compartmental model was used in order to estimate the human absorbed dose of 177Lu-DOTATOC from the biodistribution data in wild type rats. For this purpose, 177Lu-DOTATOC was prepared under optimized conditions and its biodistribution was studied in male Syrian rats up to 168 h. Compartmental model was applied to mathematical description of the drug behaviour in tissue at different times. Dosimetric estimation of the complex was performed using radiation absorbed dose assessment resource (RADAR). The biodistribution data showed high accumulation in the adrenal and pancreas as the major expression sites for somatostatin receptor (SSTR). While kidneys as the major route of excretion receive 0.037 mSv/MBq, pancreas and adrenal also obtain 0.039 and 0.028 mSv/MBq. Due to the usage of this method, the points of accumulated activity data were enhanced, and further information of tissues uptake was collected that it will be followed by high (or improved) precision in dosimetric calculations.

Keywords: compartmental modeling, human absorbed dose, ¹⁷⁷Lu-DOTATOC, Syrian rats

Procedia PDF Downloads 179
1234 A Comparative Study on the Synthesis, Characterizations and Biological (Antibacterial and Antifungal) Activities of Zinc Doped Silica Oxide Nanoparticles Based on Various Solvents

Authors: Muhammad Arshad, Ghulam Hussain Bhatti, Abdul Qayyum

Abstract:

Zinc-doped silica oxide nanoparticles having size 7.93nm were synthesized by the deposition precipitation method by using different solvents (acetonitrile, n-hexane, isoamylalchol). Biological potential such as antibacterial activities against Bacillussubtilusand Escherichia coli, and antifungal activities against Candida parapsilosis and Aspergilusniger were also investigated by Disc diffusion method. Different characterizations techniques including Fournier Transmission Infrared Spectroscopy (FT-IR), X-ray diffraction (XRD), Scanning Electron Microscope (SEM), Transmission Electron Microscope (TEM), Thermo-gravimeteric Analysis (TGA), Atomic forced microscopy (AFM), and Dynamic Light Scattering (DLS) were used. FT-IR characterization confirmed the presence of metal oxide bond (SiO2) while XRD showed the hexagonal structure. SEM and TEM characterization showed the morphology of nanoparticles. AFM study showed good particle size distribution as depicted by a histogram. DLS study showed the gradual decease in the size of nanoparticles from 24.86nm to 13.24 nm. Highest antibacterial activities revealed by acetonitrile solvents (6%and 4.5%) followed by isoamylalchol (3% and 2.4%) while n-hexane solvent showed the lowest activity (2%and 1%) respectively. Higher antifungal activities exhibited by n-hexane (0.34 % and 0.43%) followed by isoamylalchol (0.27% and 0.19%) solvent while acetonitrile (0.21% and 0.17%) showed least activity respectively. Statistical analysis by using one-way ANOVA also indicated the significant results of both biological activities.

Keywords: nanoparticles, precipitation methods, antibacterial, antifungal, characterizations

Procedia PDF Downloads 187
1233 “SockGEL/PLUG” Injectable Smart/Intelligent and Bio-Inspired Sol-Gel Nanomaterials for Simple and Complex Oro-Dental and Cranio-Maxillo-Facial Interventional Applications

Authors: Ziyad S. Haidar

Abstract:

Millions of teeth are removed annually, and dental extraction is one of the most commonly performed surgical procedures globally. Whether due to caries, periodontal disease or trauma, exodontia and the ensuing wound healing and bone remodeling processes of the resultant socket (hole in the jaw bone) usually result in serious deformities of the residual alveolar osseous ridge and surrounding soft tissues (reduced height/width). Such voluminous changes render the placement of a proper conventional bridge, denture or even an implant-supported prosthesis extremely challenging. Further, most extractions continue to be performed with no regard for preventing the onset of alveolar osteitis (also known as dry socket, a painful and difficult-to-treat/-manage condition post-exodontia). Hence, such serious resorptive morphological changes often result in significant facial deformities and a negative impact on the overall Quality of Life (QoL) of patients (and oral health-related QoL), alarming, particularly for the geriatric with compromised healing and in light of the thriving longevity statistics. Opportunity: Despite advances in tissue/wound grafting, serious limitations continue to exist, including efficacy and clinical outcome predictability, cost, treatment time, expertise and risk of immune reactions. For cases of dry sockets, specifically, the commercially-available and often-prescribed home remedies are highly lacking. Indeed, most are not recommended for use anymore. Alveogyl is a fine example. Hence, there is a great market demand and need for alternative solutions. Solution: Herein, SockGEL/PLUG (patent pending), an all-natural, drug-free and injectable stimuli-responsive hydrogel, was designed, formulated, characterized and evaluated as an osteogenic, angiogenic, anti-microbial and pain-soothing suture-free intra-alveolar dressing, safe and efficacious for use in several oro-dental and cranio-maxillo-facial interventional applications; for example: in fresh dental extraction sockets, immediately post-exodontia. It is composed of FDA-approved, biocompatible and biodegradable polymers, self-assembled electro-statically to formulate a scaffolding matrix to (a) prevent the onset of alveolar osteitis via securing the fibrin-clot in situ and protecting/sealing the socket from contamination/infection; and (b) endogenously promote/accelerate wound healing and bone remodeling to preserve the volume of the alveolus. Findings: The intrinsic properties of the SockGEL/PLUG hydrogel were evaluated physico-chemico-mechanically for safety (cell viability), viscosity, rheology, bio-distribution and essentially, capacity to induce wound healing and osteogenesis (small defect, in vivo) without any signaling cues from exogenous cells, growth factors or drugs. The performed animal model of cranial critical-sized and non-vascularized bone defects shall provide vitally critical insights into the role and mechanism of the employed natural bio-polymer blend and gel product in endogenous reparative regeneration of soft tissues and bone morphogenesis. Alongside, the fine-tuning of our modified formulation method will further tackle appropriateness, reproducibility, scalability, ease and speed in producing stable, biodegradable and sterilizable stimuli (thermo-sensitive and photo-responsive) matrices (3-dimensional interpenetrating yet porous polymeric network) suitable for an intra-socket application, and beyond. Conclusions and Perspective: Findings are anticipated to provide sufficient evidence to translate into pilot clinical trials and validate the bionanomaterial before engaging the market for feasibility, acceptance and cost-effectiveness studies. The SockGEL/PLUG platform is patent pending: SockGEL is a bio-inspired drug-free hydrogel; SockPLUG is a drug-loaded hydrogel designed for complex indications.

Keywords: hydrogel, injectable, dentistry, craniomaxillofacial complex, bioinspired, nanobiotechnology, biopolymer, sol-gel, stimuli-responsive, matrix, tissue engineering, regenerative medicine

Procedia PDF Downloads 53
1232 Nanoscale Metal-Organic Framework Coated Carbon Nitride Nanosheet for Combination Cancer Therapy

Authors: Rui Chen, Jinfeng Zhang, Chun-Sing Lee

Abstract:

In the past couple of decades, nanoscale metal-organic frameworks (NMOFs) have been highlighted as promising delivery platforms for biomedical applications, which combine many potent features such as high loading capacity, progressive biodegradability and low cytotoxicity. While NMOF has been extensively used as carriers for drugs of different modalities, so far there is no report on exploiting the advantages of NMOF for combination therapy. Herein, we prepared core-shell nanoparticles, where each nanoparticle contains a single graphitic-phase carbon nitride (g-C3N4) nanosheet encapsulated by a zeolitic-imidazolate frameworks-8 (ZIF-8) shell. The g-C3N4 nanosheets are effective visible-light photosensitizer for photodynamic therapy (PDT). When hosting DOX (doxorubicin), the as-synthesized core-shell nanoparticles could realize combinational photo-chemo therapy and provide dual-color fluorescence imaging. Therefore, we expect NMOFs-based core-shell nanoparticles could provide a new way to achieve much-enhanced cancer therapy.

Keywords: carbon nitride, combination therapy, drug delivery, nanoscale metal-organic frameworks

Procedia PDF Downloads 404
1231 Design, Synthesis, and Evaluation of Small Peptides for Managing Inflammation: Inhibition to Substrate Approach

Authors: Palwinder Singh, Baljit Kaur, Sukhmeet Kaur

Abstract:

Amongst a library of rationally designed small peptides, (H)Gly-Gly-Phe-Leu(OMe) was identified, reducing prostaglandin production of COX-2 with IC50 60 nM vs. 6000 nM for COX-1. The 5 mg Kg-1 dose of this compound rescued albino mice by 80% from capsaicin-induced paw licking and recovered it by 60% from carrageenan-induced inflammation. The mode of action of the compound for targeting COX-2, iNOS, and VGSC was investigated by using substances P, L-arginine, and veratrine, respectively, as the biomarkers. The interactions of the potent compound with COX-2 were supported by the isothermal calorimetry experiments showing Ka 6.10±1.10x104 mol-1 and ΔG -100.3 k J mol-1 in comparison to Ka 0.41x103 ±0.09 mol-1 and ΔG -19.2±0.06 k J mol-1 for COX-1. This compound did not show toxicity up to 2000 mg Kg-1 dose. Furthermore, beyond the conventional mode of working with anti-inflammatory agents through enzyme inhibition, COX-2 was provided with a peptide-based alternate substrate. Proline-centered pentapeptide iso-conformational to arachidonic acid exhibited appreciable selectivity for COX-2 overcoming acetic acid and formalin-induced pain in rats to almost 80% and was treated as a substrate by the enzyme. Hence, we suggest small peptides as highly potent and promising candidates for their further development into an anti-inflammatory drug.

Keywords: small peptides, cyclooxygenase, inflammation, substrate

Procedia PDF Downloads 67
1230 Polymer-Nanographite Nanocomposites for Biosensor Applications

Authors: Payal Mazumdar, Sunita Rattan, Monalisa Mukherjee

Abstract:

Polymer nanocomposites are a special class of materials having unique properties and wide application in diverse areas such as EMI shielding, sensors, photovoltaic cells, membrane separation properties, drug delivery etc. Recently the nanocomposites are being investigated for their use in biomedical fields as biosensors. Though nanocomposites with carbon nanoparticles have received worldwide attention in the past few years, comparatively less work has been done on nanographite although it has in-plane electrical, thermal and mechanical properties comparable to that of carbon nanotubes. The main challenge in the fabrication of these nanocomposites lies in the establishment of homogeneous dispersion of nanographite in polymer matrix. In the present work, attempts have been made to synthesize the nanocomposites of polystyrene and nanographite using click chemistry. The polymer and the nanographite are functionalized prior to the formation of nanocomposites. The polymer, polystyrene, was functionalized with alkyne moeity and nanographite with azide moiety. The fabricating of the nanocomposites was accomplished through click chemistry using Cu (I)-catalyzed Huisgen dipolar cycloaddition. The functionalization of filler and polymer was confirmed by NMR and FTIR. The nanocomposites formed by the click chemistry exhibit better electrical properties and the sensors are evaluated for their application as biosensors.

Keywords: nanocomposites, click chemistry, nanographite, biosensor

Procedia PDF Downloads 289
1229 Synthesis, Characterization and Antibacterial Activity of Metalloporphyrins: Role of Central Metal Ion

Authors: Belete B. Beyene, Ayenew M. Mihirteu, Misganaw T. Ayana, Amogne W. Yibeltal

Abstract:

Modification of synthetic porphyrins is one of the promising strategies in an attempt to get molecules with desired properties and applications. Here in, we report synthesis, photophysical characterization and antibacterial activity of 5, 10, 15, 20-tetrakis-(4- methoxy carbonyl phenyl) porphyrin M(II); where M = Co, Fe, Ni, Zn. Metallation of the ligand was confirmed by using UV–Vis spectroscopy and ESI-Ms measurement, in which the number of Q bands in absorption spectra of the ligand decreased from four to one or two as a result of metal insertion to the porphyrin core. The antibacterial activity study of the complexes toward two Gram-positive (Staphylococcus aureus (S. aureus) and Streptococcus pyogenes (s. pyogenes)) and two Gram-negative (Escherichia coli (E. coli) and Klebsiella pneumoniae (K. pneumoniae)) bacteria by disc diffusion method showed a promising inhibitory activity. The complexes exhibited highest activities at highest concentration and were better than the activity of free base ligand, the salts, and blank solution. This could be explained on the basis of Overton's concept of cell permeability and Tweed's Chelation theory. An increased lipo-solubility enhances the penetration of the complexes into the lipid membrane and interferes with the normal activities of the bacteria. Our study, therefore, showed that the growth inhibitory effect of these metalloporphyrins is generally in order of ZnTPPCOOMe > NiTPPCOOMe > CoTPPCOOMe> FeTPPCOOMe, which may be attributed to the better lipophilicity and binding of the complex with the cellular components.

Keywords: porphyrins, metalloporphyrins, spectral property, antibacterial activity, synthesis

Procedia PDF Downloads 49