Search results for: Drug targets
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 408

Search results for: Drug targets

348 Analysis of Normal Penetration of Ogive -Nose Projectiles into Thin Metallic Plates

Authors: M. H. Pol, A. Bidi, A.V. Hoseini, G.H. Liaghat

Abstract:

In this note, a theoretical model for analyzing of normal penetration of the ogive – nose projectile into metallic targets is presented .The failure is assumed to be asymmetry petalling and the analysis is performed by using the energy balance and work done .The work done consist of the work required for plastic deformation Wp, the work for transferring the matter to new position Wd and the work for bending of the petals Wb. In several studies, it has been shown that we can neglect the loss of energy by temperature. In this present study, in first, by assuming the crater formation after perforation, the value of work done is calculated during the normal penetration of conical projectiles into thin metallic targets. Then the value of residual velocity and ballistic limit of the projectile is predicated by using the energy balance. In final, theoretical and experimental results is compared.

Keywords: Ogive Projectile, normal impact, penetration, thinmetallic target.

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347 Characterization of Inertial Confinement Fusion Targets Based on Transmission Holographic Mach-Zehnder Interferometer

Authors: B. Zare-Farsani, M. Valieghbal, M. Tarkashvand, A. H. Farahbod

Abstract:

To provide the conditions for nuclear fusion by high energy and powerful laser beams, it is required to have a high degree of symmetry and surface uniformity of the spherical capsules to reduce the Rayleigh-Taylor hydrodynamic instabilities. In this paper, we have used the digital microscopic holography based on Mach-Zehnder interferometer to study the quality of targets for inertial fusion. The interferometric pattern of the target has been registered by a CCD camera and analyzed by Holovision software. The uniformity of the surface and shell thickness are investigated and measured in reconstructed image. We measured shell thickness in different zone where obtained non uniformity 22.82 percent.  

Keywords: Inertial confinement fusion, Mach-Zehnder interferometer, Digital holographic microscopy.

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346 Phage Capsid for Efficient Delivery of Cytotoxic Drugs

Authors: Simona Dostalova, Ana Maria Jimenez Jimenez, Marketa Vaculovicova, Vojtech Adam, Rene Kizek

Abstract:

Various nanomaterials can be used as a drug delivery vehicles in nanomedicine, called nanocarriers. They can either be organic or inorganic, synthetic or natural-based. Although synthetic nanocarriers are easier to produce, they can often be toxic for the organism and thus not suitable for use in treatment. From naturalbased nanocarriers, the most commonly used are protein cages or viral capsids. In this work, virus bacteriophage λ was used for delivery of different cytotoxic drugs (cisplatin, carboplatin, oxaliplatin and doxorubicin). Large quantities of phage λ were obtained from phage λ-producing strain of E. coli cultivated in medium with 0.2% maltose. After killing of E. coli with chloroform and its removal by centrifugation, the phage was concentrated by ultracentrifugation at 130 000×g and 4°C for 3 h. The encapsulation of the drugs was performed by infusion method and four different concentrations of the drugs were encapsulated (200; 100; 50; 25 μg·mL-1). Free drug molecules were removed by filtration. The encapsulation was verified using the absorbance for doxorubicin and atomic absorption spectrometry for platinum cytostatics. The amount of encapsulated drug linearly increased with the increasing concentration of applied drug with the determination coefficient R2=0.989 for doxorubicin; R2=0.967 for cisplatin; R2=0.989 for carboplatin and R2=0.996 for oxaliplatin. The overall encapsulation efficiency was calculated as 50% for doxorubicin; 8% for cisplatin; 6% for carboplatin and 10% for oxaliplatin.

Keywords: Bacteriophage λ, doxorubicin, platinum cytostatics, protein-based nanocarrier, viral capsid.

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345 Intelligent Dynamic Decision-making Model Using in Robot's Movement

Authors: Yufang Cheng, Hsiu-Hua Yang

Abstract:

This work develops a novel intelligent “model of dynamic decision-making" usingcell assemblies network architecture in robot's movement. The “model of dynamic decision-making" simulates human decision-making, and follows commands to make the correct decisions. The cell assemblies approach consisting of fLIF neurons was used to implement tasks for finding targets and avoiding obstacles. Experimental results show that the cell assemblies approach of can be employed to efficiently complete finding targets and avoiding obstacles tasks and can simulate the human thinking and the mode of information transactions.

Keywords: Cell assemblies, fLIF, Hebbian learning rule.

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344 Development and Optimization of Colon Targeted Drug Delivery System of Ayurvedic Churna Formulation Using Eudragit L100 and Ethyl Cellulose as Coating Material

Authors: Anil Bhandari, Imran Khan Pathan, Peeyush K. Sharma, Rakesh K. Patel, Suresh Purohit

Abstract:

The purpose of this study was to prepare time and pH dependent release tablets of Ayurvedic Churna formulation and evaluate their advantages as colon targeted drug delivery system. The Vidangadi Churna was selected for this study which contains Embelin and Gallic acid. Embelin is used in Helminthiasis as therapeutic agent. Embelin is insoluble in water and unstable in gastric environment so it was formulated in time and pH dependent tablets coated with combination of two polymers Eudragit L100 and ethyl cellulose. The 150mg of core tablet of dried extract and lactose were prepared by wet granulation method. The compression coating was used in the polymer concentration of 150mg for both the layer as upper and lower coating tablet was investigated. The results showed that no release was found in 0.1 N HCl and pH 6.8 phosphate buffers for initial 5 hours and about 98.97% of the drug was released in pH 7.4 phosphate buffer in total 17 Hours. The in vitro release profiles of drug from the formulation could be best expressed first order kinetics as highest linearity (r2= 0.9943). The results of the present study have demonstrated that the time and pH dependent tablets system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of Embelin and Gallic acid for treatment of Helminthiasis.

Keywords: Embelin, Gallic acid, Vidangadi Churna, Colon targeted drug delivery.

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343 Determinants of Profitability in Indian Pharmaceutical Firms in the New Intellectual Property Rights Regime

Authors: Shilpi Tyagi, D. K. Nauriyal

Abstract:

This study investigates the firm level determinants of profitability of Indian drug and pharmaceutical industry. The study uses inflation adjusted panel data for a period 2000-2013 and applies OLS regression model with Driscoll-Kraay standard errors. It has been found that export intensity, A&M intensity, firm’s market power and stronger patent regime dummy have exercised positive influence on profitability. The negative and statistically significant influence of R&D intensity and raw material import intensity points to the need for firms to adopt suitable investment strategies. The study suggests that firms are required to pay far more attention to optimize their operating expenditures, advertisement and marketing expenditures and improve their export orientation, as part of the long term strategy.

Keywords: Indian drug and pharmaceutical industry, trade related intellectual property rights, research and development, food and drug administration.

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342 In vitro and in vivo Anticancer Activity of Nanosize Zinc Oxide Composites of Doxorubicin

Authors: E. R. Arakelova, S. G. Grigoryan, F. G. Arsenyan, N. S. Babayan, R. M. Grigoryan, N. K. Sarkisyan

Abstract:

The nanotechnology offers some exciting possibilities in cancer treatment, including the possibility of destroying tumors with minimal damage to healthy tissue and organs by targeted drug delivery systems. Considerable achievements in investigations aimed at the use of ZnO nanoparticles and nanocontainers in diagnostics and antitumor therapy were described. However, there are substantial obstacles to the purposes to be achieved by the use of zinc oxide nanosize materials in antitumor therapy. Among the serious problems are the techniques of obtaining ZnO nanosize materials. The article presents a new vector delivery system for the known antitumor drug, doxorubicin in the form of polymeric (PEO, starch-NaCMC) hydrogels, in which nanosize ZnO film of a certain thickness are deposited directly on the drug surface on glass substrate by DC-magnetron sputtering of a zinc target. Anticancer activity in vitro and in vivo of those nanosize zinc oxide composites is shown.

Keywords: Anticancer activity, cancer specificity, doxorubicin, zinc oxide.

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341 Determination of Cu and Mo Potential Targets in the Khatunabad Based on Analytical Hierarchy Process, West of Mianeh, Iran

Authors: R. Noori, F. Feizi, M.R. Jafari

Abstract:

Khatunabad area is situated geologically in Urmieh- Dokhtar magmatic belt in NW of Iran. In this research, studied area has been investigated in order to recognize the potential copper and molybdenum-bearing target areas. The survey layers include the lithologic units, alteration, geochemical result, tectonics and copper and molybdenum occurrence. As an accurate decision can have a considerable effect on exploration plans, so in this efforts have been made to make use of new combination method. For this purpose, the analytical hierarchy process was used and revealed highly potential copper and molybdenum mineralization areas. Based on achieved results, geological perspective in north of studied area is appropriate for advance stage, especially for subsurface exploration in future.

Keywords: Analytical hierarchy process, Potential targets, Khatunabad, Iran

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340 Vincristine-Dextran Complex Loaded Solid Lipid Nanoparticles for Drug Delivery to the Brain

Authors: E. Aboutaleb, R. Dinarvand

Abstract:

The purpose of this work was to inspect the potential of vincristine-dextran complex loaded solid lipid nanoparticles for drug delivery to the brain. The nanoparticles were stained with a fluorescence dye and their plasma pharmacokinetic and brain concentrations were investigated following injection to rats. The result revealed a significant improvement in the plasma concentration profile of the SLN injected animals as well as a sharp increased concentration in the brains.

Keywords: Brain, Coumarin-6, Nanoparticles, SLN.

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339 Learners’ Violent Behaviour and Drug Abuse as Major Causes of Tobephobia in Schools

Authors: Prakash Singh

Abstract:

Many schools throughout the world are facing constant pressure to cope with the violence and drug abuse of learners who show little or no respect for acceptable and desirable social norms. These delinquent learners tend to harbour feelings of being beyond reproach because they strongly believe that it is well within their rights to engage in violent and destructive behaviour. Knives, guns, and other weapons appear to be more readily used by them on the school premises than before. It is known that learners smoke, drink alcohol, and use drugs during school hours, hence, their ability to concentrate, work, and learn, is affected. They become violent and display disruptive behaviour in their classrooms as well as on the school premises, and this atrocious behaviour makes it possible for drug dealers and gangsters to gain access onto the school premises. The primary purpose of this exploratory quantitative study was therefore to establish how tobephobia (TBP), caused by school violence and drug abuse, affects teaching and learning in schools. The findings of this study affirmed that poor discipline resulted in producing poor quality education. Most of the teachers in this study agreed that educating learners who consumed alcohol and other drugs on the school premises resulted in them suffering from TBP. These learners are frequently abusive and disrespectful, and resort to violence to seek attention. As a result, teachers feel extremely demotivated and suffer from high levels of anxiety and stress. The word TBP will surely be regarded as a blessing by many teachers throughout the world because finally, there is a word that will make people sit up and listen to their problems that cause real fear and anxiety in schools.

Keywords: Aims and objectives of quality education, Debilitating effects of tobephobia, Fear of failure associated with education, learners’ violent behaviour and drug abuse.

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338 Formulation and Evaluation of Niosomes Containing an Antihypertensive Drug

Authors: Sunil Kamboj, Suman Bala, Vipin Saini

Abstract:

Niosomes were formulated with an aim of enhancing the oral bioavailability of losartan potassium and formulated in different molar ratios of surfactant, cholesterol and dicetyl phosphate. The formulated niosomes were found in range of 54.98 µm to 107.85 µm in size. Formulations with 1:1 ratio of surfactant and cholesterol have shown maximum entrapment efficiencies. Niosomes with sorbitan monostearate showed maximum drug release and zero order release kinetics, at the end of 24 hours. The in vivo study has shown the significant enhancement in oral bioavailability of losartan potassium in rats, after a dose of 10 mg/kg. The average relative bioavailability in relation with pure drug solution was found 2.56, indicates more than two fold increase in oral bioavailability. A significant increment in MRT reflects the release retarding ability of the vesicles. In conclusion, niosomes could be a promising delivery of losartan potassium with improved oral bioavailability and prolonged release profiles.

Keywords: Non-ionic surfactant vesicles, losartan potassium, oral bioavailability, controlled release.

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337 Polymeric Sustained Biodegradable Patch Formulation for Wound Healing

Authors: Abhay Asthana, Gyati Shilakari Asthana

Abstract:

It is the patient compliance and stability in combination with controlled drug delivery and biocompatibility that forms the core feature in present research and development of sustained biodegradable patch formulation intended for wound healing. The aim was to impart sustained degradation, sterile formulation, significant folding endurance, elasticity, biodegradability, bio-acceptability and strength. The optimized formulation comprised of polymers including Hydroxypropyl methyl cellulose, Ethylcellulose, and Gelatin, and Citric Acid PEG Citric acid (CPEGC) triblock dendrimers and active Curcumin. Polymeric mixture dissolved in geometric order in suitable medium through continuous stirring under ambient conditions. With continued stirring Curcumin was added with aid of DCM and Methanol in optimized ratio to get homogenous dispersion. The dispersion was sonicated with optimum frequency and for given time and later casted to form a patch form. All steps were carried out under strict aseptic conditions. The formulations obtained in the acceptable working range were decided based on thickness, uniformity of drug content, smooth texture and flexibility and brittleness. The patch kept on stability using butter paper in sterile pack displayed folding endurance in range of 20 to 23 times without any evidence of crack in an optimized formulation at room temperature (RT) (24 ± 2°C). The patch displayed acceptable parameters after stability study conducted in refrigerated conditions (8±0.2°C) and at RT (24 ± 2°C) up to 90 days. Further, no significant changes were observed in critical parameters such as elasticity, biodegradability, drug release and drug content during stability study conducted at RT 24±2°C for 45 and 90 days. The drug content was in range 95 to 102%, moisture content didn’t exceeded 19.2% and patch passed the content uniformity test. Percentage cumulative drug release was found to be 80% in 12h and matched the biodegradation rate as drug release with correlation factor R2>0.9. The biodegradable patch based formulation developed shows promising results in terms of stability and release profiles.

Keywords: Sustained biodegradation, wound healing, polymeric patch, stability.

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336 Molecular Dynamics Study on Laninamivir Inhibiting Neuraminidases of H5N1 and pH1N1 Influenza a Viruses

Authors: A. Meeprasert, W. Khuntawee, S. Hannongbua, T. Rungrotmongkol

Abstract:

Viral influenza A subtypes H5N1 and pandemic H1N1 (pH1N1) have worldwide emerged and transmitted. The most common anti-influenza drug for treatment of both seasonal and pandemic influenza viruses is oseltamivir that nowadays becomes resistance to influenza neuraminidase. The novel long-acting drug, laninamivir, was discovered for treatment of the patients infected with influenza B and influenza A viruses. In the present study, laninamivir complexed with wild-type strain of both H5N1 and pH1N1 viruses were comparatively determined the structures and drug-target interactions by means of molecular dynamics (MD) simulations. The results show that the hydrogen bonding interactions formed between laninamivir and its binding residues are likely similar for the two systems. Additionally, the presence of intermolecular interactions from laninamivir to the residues in the binding pocket is established through their side chains in accordance with hydrogen bond interactions.

Keywords: Laninamivir, neuraminidase, H5N1, pandemic H1N1, wild-type, MD simulation

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335 Computational Identification of MicroRNAs and their Targets in two Species of Evergreen Spruce Tree (Picea)

Authors: Muhammad Y.K. Barozai, Ifthikhar A. Baloch, M. Din

Abstract:

MicroRNAs (miRNAs) are small, non-coding and regulatory RNAs about 20 to 24 nucleotides long. Their conserved nature among the various organisms makes them a good source of new miRNAs discovery by comparative genomics approach. The study resulted in 21 miRNAs of 20 pre-miRNAs belonging to 16 families (miR156, 157, 158, 164, 165, 168, 169, 172, 319, 390, 393, 394, 395, 400, 472 and 861) in evergreen spruce tree (Picea). The miRNA families; miR 157, 158, 164, 165, 168, 169, 319, 390, 393, 394, 400, 472 and 861 are reported for the first time in the Picea. All 20 miRNA precursors form stable minimum free energy stem-loop structure as their orthologues form in Arabidopsis and the mature miRNA reside in the stem portion of the stem loop structure. Sixteen (16) miRNAs are from Picea glauca and five (5) belong to Picea sitchensis. Their targets consist of transcription factors, growth related, stressed related and hypothetical proteins.

Keywords: BLAST, Comparative Genomics, Micro-RNAs, Spruce

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334 Distributed Coverage Control by Robot Networks in Unknown Environments Using a Modified EM Algorithm

Authors: Mohammadhosein Hasanbeig, Lacra Pavel

Abstract:

In this paper, we study a distributed control algorithm for the problem of unknown area coverage by a network of robots. The coverage objective is to locate a set of targets in the area and to minimize the robots’ energy consumption. The robots have no prior knowledge about the location and also about the number of the targets in the area. One efficient approach that can be used to relax the robots’ lack of knowledge is to incorporate an auxiliary learning algorithm into the control scheme. A learning algorithm actually allows the robots to explore and study the unknown environment and to eventually overcome their lack of knowledge. The control algorithm itself is modeled based on game theory where the network of the robots use their collective information to play a non-cooperative potential game. The algorithm is tested via simulations to verify its performance and adaptability.

Keywords: Distributed control, game theory, multi-agent learning, reinforcement learning.

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333 Detection of Temporal Change of Fishery and Island Activities by DNB and SAR on the South China Sea

Authors: I. Asanuma, T. Yamaguchi, J. Park, K. J. Mackin

Abstract:

Fishery lights on the surface could be detected by the Day and Night Band (DNB) of the Visible Infrared Imaging Radiometer Suite (VIIRS) on the Suomi National Polar-orbiting Partnership (Suomi-NPP). The DNB covers the spectral range of 500 to 900 nm and realized a higher sensitivity. The DNB has a difficulty of identification of fishing lights from lunar lights reflected by clouds, which affects observations for the half of the month. Fishery lights and lights of the surface are identified from lunar lights reflected by clouds by a method using the DNB and the infrared band, where the detection limits are defined as a function of the brightness temperature with a difference from the maximum temperature for each level of DNB radiance and with the contrast of DNB radiance against the background radiance. Fishery boats or structures on islands could be detected by the Synthetic Aperture Radar (SAR) on the polar orbit satellites using the reflected microwave by the surface reflecting targets. The SAR has a difficulty of tradeoff between spatial resolution and coverage while detecting the small targets like fishery boats. A distribution of fishery boats and island activities were detected by the scan-SAR narrow mode of Radarsat-2, which covers 300 km by 300 km with various combinations of polarizations. The fishing boats were detected as a single pixel of highly scattering targets with the scan-SAR narrow mode of which spatial resolution is 30 m. As the look angle dependent scattering signals exhibits the significant differences, the standard deviations of scattered signals for each look angles were taken into account as a threshold to identify the signal from fishing boats and structures on the island from background noise. It was difficult to validate the detected targets by DNB with SAR data because of time lag of observations for 6 hours between midnight by DNB and morning or evening by SAR. The temporal changes of island activities were detected as a change of mean intensity of DNB for circular area for a certain scale of activities. The increase of DNB mean intensity was corresponding to the beginning of dredging and the change of intensity indicated the ending of reclamation and following constructions of facilities.

Keywords: Day night band, fishery, SAR, South China Sea.

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332 Design and Development of Graphene Oxide Modified by Chitosan Nanosheets Showing pH-Sensitive Surface as a Smart Drug Delivery System for Controlled Release of Doxorubicin

Authors: Parisa Shirzadeh

Abstract:

Drug delivery systems in which drugs are traditionally used, multi-stage and at specified intervals by patients, do not meet the needs of the world's up-to-date drug delivery. In today's world, we are dealing with a huge number of recombinant peptide and protean drugs and analogues of hormones in the body, most of which are made with genetic engineering techniques. Most of these drugs are used to treat critical diseases such as cancer. Due to the limitations of the traditional method, researchers sought to find ways to solve the problems of the traditional method to a large extent. Following these efforts, controlled drug release systems were introduced, which have many advantages. Using controlled release of the drug in the body, the concentration of the drug is kept at a certain level, and in a short time, it is done at a higher rate. Graphene is a natural material that is biodegradable, non-toxic, natural and wide surfaces of graphene plates makes it more effective to modify graphene than carbon nanotubes. Graphene oxide is often synthesized using concentrated oxidizers such as sulfuric acid, nitric acid, and potassium permanganate based on Hummer method. graphene oxide is very hydrophilic and easily dissolves in water and creates a stable solution. Graphene oxide (GO) has been modified by chitosan (CS) covalently, developed for control release of doxorubicin (DOX). In this study, GO is produced by the hummer method under acidic conditions. Then, it is chlorinated by oxalyl chloride to increase its reactivity against amine. After that, in the presence of CS, the amino reaction was performed to form amide transplantation, and the DOX was connected to the carrier surface by π-π interaction in buffer phosphate. GO, GO-CS, and GO-CS-DOX were characterized by FT-IR and TGA to recognize new functional groups which show the new bonding of CS to GO, RAMA and SEM to recognize size of layers that show changing in size and number of layers. The ability to load and release is determined by UV-Visible spectroscopy. The loading result showed a high capacity of DOX absorption (99%) and pH dependence identified as a result of DOX release from GO-CS nanosheet at pH 5.3 and 7.4, which show a fast release rate in acidic conditions.

Keywords: Graphene oxide, chitosan, nanosheet, controlled drug release, doxorubicin.

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331 The Citizen Participation in Preventing Illegal Drugs Program in Bangkok, Thailand

Authors: Ratthapong Bunyanuwat

Abstract:

The purposes of this research were to study the citizen participation in preventing illegal drugs in one of a poor and small community of Bangkok, Thailand and to compare the level of participation and concern of illegal drugs problem by using demographic variables. This paper drew upon data collected from a local citizens survey conducted in Bangkok, Thailand during summer of 2012. A total of 200 respondents were elicited as data input for, and one way ANOVA test. The findings revealed that the overall citizen participation was in the level of medium. The mean score showed that benefit from the program was ranked as the highest and the decision to participate was ranked as second while the follow-up of the program was ranked as the lowest. In terms of the difference in demographic such as gender, age, level of education, income, and year of residency, the hypothesis testing’s result disclosed that there were no difference in their level of participation. However, difference in occupation showed a difference in their level of participation and concern which was significant at the 0.05 confidence level.

Keywords: Citizen Participation, Illegal drug, Preventing drug problem, Resolving drug problem

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330 Impact of Revenue Gap on Budget Deficit, Debt Burden and Economic Growth: An Evidence from Pakistan

Authors: M. W. Siddiqi, M. Ilyas

Abstract:

Availability and mobilization of revenue is the main essential with which an economy is managed and run. While planning or while making the budgets nations set revenue targets to be achieved. But later when the accounts are closed the actual collections of revenue through taxes or even the non-tax revenue collection would invariably be different as compared to the initial estimates and targets set to be achieved. This revenue-gap distorts the whole system and the economy disturbing all the major macroeconomic indicators. This study is aimed to find out short and long term impact of revenue gap on budget deficit, debt burden and economic growth on the economy of Pakistan. For this purpose the study uses autoregressive distributed lag approach to cointegration and error correction mechanism on three different models for the period 1980 to 2009. The empirical results show that revenue gap has a short and long run relationship with economic growth and budget deficit. However, revenue gap has no impact on debt burden.

Keywords: Revenue Gap, Economic Growth, Budget Deficit, Debt Burden

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329 Beam Coding with Orthogonal Complementary Golay Codes for Signal to Noise Ratio Improvement in Ultrasound Mammography

Authors: Y. Kumru, K. Enhos, H. Köymen

Abstract:

In this paper, we report the experimental results on using complementary Golay coded signals at 7.5 MHz to detect breast microcalcifications of 50 µm size. Simulations using complementary Golay coded signals show perfect consistence with the experimental results, confirming the improved signal to noise ratio for complementary Golay coded signals. For improving the success on detecting the microcalcifications, orthogonal complementary Golay sequences having cross-correlation for minimum interference are used as coded signals and compared to tone burst pulse of equal energy in terms of resolution under weak signal conditions. The measurements are conducted using an experimental ultrasound research scanner, Digital Phased Array System (DiPhAS) having 256 channels, a phased array transducer with 7.5 MHz center frequency and the results obtained through experiments are validated by Field-II simulation software. In addition, to investigate the superiority of coded signals in terms of resolution, multipurpose tissue equivalent phantom containing series of monofilament nylon targets, 240 µm in diameter, and cyst-like objects with attenuation of 0.5 dB/[MHz x cm] is used in the experiments. We obtained ultrasound images of monofilament nylon targets for the evaluation of resolution. Simulation and experimental results show that it is possible to differentiate closely positioned small targets with increased success by using coded excitation in very weak signal conditions.

Keywords: Coded excitation, complementary Golay codes, DiPhAS, medical ultrasound.

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328 Stereoselective Reduction of Amino Ketone with Sodium Borohydride in the Presence of Metal Chloride. A Simple Pathway to S-Propranolol

Authors: R. Inkum, A. Teerawutgulrag, P. Puangsombat, N. Rakariyatham

Abstract:

Propranolol is worldwide hypertension drug that is active in S-isomer. Patients must use this drug throughout their lives, and this action employsa significant level of expenditure. A simpler synthesis and lower cost can reduce the price for the patient. A sis pathway of S-propranolol starting from protection of (R,S)-propranolol with di-t-butyldicarbonate and then the product is oxidized with pyridiniumchlorochromate. The selective reduction of ketone occurrs with sodiumborohydride in the presence of metal chloride provided S-propranolol.

Keywords: S-propranolol, selective reduction, sodium borohydride, metal chloride

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327 Controlled Release of Glucosamine from Pluronic-Based Hydrogels for the Treatment of Osteoarthritis

Authors: Papon Thamvasupong, Kwanchanok Viravaidya-Pasuwat

Abstract:

Osteoarthritis affects a lot of people worldwide. Local injection of glucosamine is one of the alternative treatment methods to replenish the natural lubrication of cartilage. However, multiple injections can potentially lead to possible bacterial infection. Therefore, a drug delivery system is desired to reduce the frequencies of injections. A hydrogel is one of the delivery systems that can control the release of drugs. Thermo-reversible hydrogels can be beneficial to the drug delivery system especially in the local injection route because this formulation can change from liquid to gel after getting into human body. Once the gel is in the body, it will slowly release the drug in a controlled manner. In this study, various formulations of Pluronic-based hydrogels were synthesized for the controlled release of glucosamine. One of the challenges of the Pluronic controlled release system is its fast dissolution rate. To overcome this problem, alginate and calcium sulfate (CaSO4) were added to the polymer solution. The characteristics of the hydrogels were investigated including the gelation temperature, gelation time, hydrogel dissolution and glucosamine release mechanism. Finally, a mathematical model of glucosamine release from Pluronic-alginate-hyaluronic acid hydrogel was developed. Our results have shown that crosslinking Pluronic gel with alginate did not significantly extend the dissolution rate of the gel. Moreover, the gel dissolution profiles and the glucosamine release mechanisms were best described using the zeroth-order kinetic model, indicating that the release of glucosamine was primarily governed by the gel dissolution.

Keywords: Controlled release, drug delivery system, glucosamine, Pluronic® F-127, thermoreversible hydrogel.

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326 A DNA-Based Nanobiosensor for the Rapid Detection of the Dengue Virus in Mosquito

Authors: Lilia M. Fernando, Matthew K. Vasher, Evangelyn C. Alocilja

Abstract:

This paper describes the development of a DNA-based nanobiosensor to detect the dengue virus in mosquito using electrically active magnetic (EAM) nanoparticles as concentrator and electrochemical transducer. The biosensor detection encompasses two sets of oligonucleotide probes that are specific to the dengue virus: the detector probe labeled with the EAM nanoparticles and the biotinylated capture probe. The DNA targets are double hybridized to the detector and the capture probes and concentrated from nonspecific DNA fragments by applying a magnetic field. Subsequently, the DNA sandwiched targets (EAM-detector probe– DNA target–capture probe-biotin) are captured on streptavidin modified screen printed carbon electrodes through the biotinylated capture probes. Detection is achieved electrochemically by measuring the oxidation–reduction signal of the EAM nanoparticles. Results indicate that the biosensor is able to detect the redox signal of the EAM nanoparticles at dengue DNA concentrations as low as 10 ng/μl.

Keywords: Dengue, magnetic nanoparticles, mosquito, nanobiosensor.

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325 Titanium Dioxide Modified with Glutathione as Potential Drug Carrier with Reduced Toxic Properties

Authors: Olga Długosz, Jolanta Pulit-Prociak, Marcin Banach

Abstract:

The paper presents a process to obtain glutathione-modified titanium oxide nanoparticles. The processes were carried out in a microwave radiation field. The influence of the molar ratio of glutathione to titanium oxide and the effect of the fold of NaOH vs. stoichiometric amount on the size of the formed TiO2 nanoparticles was determined. The physicochemical properties of the obtained products were evaluated using dynamic light scattering (DLS), transmission electron microscope- energy-dispersive X-ray spectroscopy (TEM-EDS), low-temperature nitrogen adsorption method (BET), X-Ray Diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR) microscopy methods. The size of TiO2 nanoparticles was characterized from 30 nm to 336 nm. The release of titanium ions from the prepared products was evaluated. These studies were carried out using different media in which the powders were incubated for a specific time. These were: water, SBF and Ringer's solution. The release of titanium ions from modified products is weaker compared to unmodified titanium oxide nanoparticles. The reduced release of titanium ions may allow the use of such modified materials as substances in drug delivery systems.

Keywords: titanium dioxide, nanoparticles, drug carrier, glutathione

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324 User Satisfaction and Acceptability of Dialogue Systems for Detecting Counterfeit Drugs

Authors: Oyelami M. Olufemi

Abstract:

The menace of counterfeiting pharmaceuticals/drugs has become a major threat to consumers, healthcare providers, drug manufacturers and governments. It is a source of public health concern both in the developed and developing nations. Several solutions for detecting and authenticating counterfeit drugs have been adopted by different nations of the world. In this article, a dialogue system-based drug counterfeiting detection system was developed and the results of the user satisfaction and acceptability of the system are presented. The results show that the users were satisfied with the system and the system was widely accepted as a means of fighting counterfeited drugs.

Keywords: Counterfeiting, dialogue system, drugs, voice application.

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323 Assessing Efficiency Trends in the Indian Sugar Industry

Authors: S. P. Singh

Abstract:

This paper measures technical and scale efficiencies of 40 Indian sugar companies for the period from 2004-05 to 2013-14. The efficiencies are estimated through input-oriented DEA models using one output variable—value of output (VOP) and five input variables—capital cost (CA), employee cost (EMP), raw material (RW), energy & fuel (E&F) and other manufacturing expenses (OME). The sugar companies are classified into integrated and non-integrated categories to know which one achieves higher level of efficiency. Sources of inefficiency in the industry are identified through decomposing the overall technical efficiency (TE) into pure technical efficiency (PTE) and scale efficiency (SE). The paper also estimates input-reduction targets for relatively inefficient companies and suggests measures to improve their efficiency level. The findings reveal that the TE does not evince any trend rather it shows fluctuations across years, largely due to erratic and cyclical pattern of sugar production. Further, technical inefficiency in the industry seems to be driven more by the managerial inefficiency than the scale inefficiency, which implies that TE can be improved through better conversion of inputs into output.

Keywords: Sugar industry, companies, technical efficiency, data envelopment analysis, targets.

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322 Virulent-GO: Prediction of Virulent Proteins in Bacterial Pathogens Utilizing Gene Ontology Terms

Authors: Chia-Ta Tsai, Wen-Lin Huang, Shinn-Jang Ho, Li-Sun Shu, Shinn-Ying Ho

Abstract:

Prediction of bacterial virulent protein sequences can give assistance to identification and characterization of novel virulence-associated factors and discover drug/vaccine targets against proteins indispensable to pathogenicity. Gene Ontology (GO) annotation which describes functions of genes and gene products as a controlled vocabulary of terms has been shown effectively for a variety of tasks such as gene expression study, GO annotation prediction, protein subcellular localization, etc. In this study, we propose a sequence-based method Virulent-GO by mining informative GO terms as features for predicting bacterial virulent proteins. Each protein in the datasets used by the existing method VirulentPred is annotated by using BLAST to obtain its homologies with known accession numbers for retrieving GO terms. After investigating various popular classifiers using the same five-fold cross-validation scheme, Virulent-GO using the single kind of GO term features with an accuracy of 82.5% is slightly better than VirulentPred with 81.8% using five kinds of sequence-based features. For the evaluation of independent test, Virulent-GO also yields better results (82.0%) than VirulentPred (80.7%). When evaluating single kind of feature with SVM, the GO term feature performs much well, compared with each of the five kinds of features.

Keywords: Bacterial virulence factors, GO terms, prediction, protein sequence.

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321 Anticancer Effect of Doxorubicin Loaded Heparin based Super-paramagnetic Iron oxide Nanoparticles against the Human Ovarian Cancer Cells

Authors: Amaneh Javid, Shahin Ahmadian, Ali A. Saboury, Saeed Rezaei-Zarchi

Abstract:

This study determines the effect of naked and heparinbased super-paramagnetic iron oxide nanoparticles on the human cancer cell lines of A2780. Doxorubicin was used as the anticancer drug, entrapped in the SPIO-NPs. This study aimed to decorate nanoparticles with heparin, a molecular ligand for 'active' targeting of cancerous cells and the application of modified-nanoparticles in cancer treatment. The nanoparticles containing the anticancer drug DOX were prepared by a solvent evaporation and emulsification cross-linking method. The physicochemical properties of the nanoparticles were characterized by various techniques, and uniform nanoparticles with an average particle size of 110±15 nm with high encapsulation efficiencies (EE) were obtained. Additionally, a sustained release of DOX from the SPIO-NPs was successful. Cytotoxicity tests showed that the SPIO-DOX-HP had higher cell toxicity than the individual HP and confocal microscopy analysis confirmed excellent cellular uptake efficiency. These results indicate that HP based SPIO-NPs have potential uses as anticancer drug carriers and also have an enhanced anticancer effect.

Keywords: Heparin, A2780 cells, ovarian cancer, nanoparticles, doxorubicin.

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320 Exploiting Non Circularity for Angle Estimation in Bistatic MIMO Radar Systems

Authors: Ebregbe David, Deng Weibo

Abstract:

The traditional second order statistics approach of using only the hermitian covariance for non circular signals, does not take advantage of the information contained in the complementary covariance of these signals. Radar systems often use non circular signals such as Binary Phase Shift Keying (BPSK) signals. Their noncicular property can be exploited together with the dual centrosymmetry of the bistatic MIMO radar system to improve angle estimation performance. We construct an augmented matrix from the received data vectors using both the positive definite hermitian covariance matrix and the complementary covariance matrix. The Unitary ESPRIT technique is then applied to the signal subspace of the augmented covariance matrix for automatically paired Direction-of-arrival (DOA) and Direction-of-Departure (DOD) angle estimates. The number of targets that can be detected is twice that obtainable with the conventional ESPRIT approach. Simulation results show the effectiveness of this method in terms of increase in resolution and the number of targets that can be detected.

Keywords: Bistatic MIMO Radar, Unitary Esprit, Non circular signals.

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319 Discovery of Human HMG-Coa Reductase Inhibitors Using Structure-Based Pharmacophore Modeling Combined with Molecular Dynamics Simulation Methodologies

Authors: Minky Son, Chanin Park, Ayoung Baek, Shalini John, Keun Woo Lee

Abstract:

3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) catalyzes the conversion of HMG-CoA to mevalonate using NADPH and the enzyme is involved in rate-controlling step of mevalonate. Inhibition of HMGR is considered as effective way to lower cholesterol levels so it is drug target to treat hypercholesterolemia, major risk factor of cardiovascular disease. To discover novel HMGR inhibitor, we performed structure-based pharmacophore modeling combined with molecular dynamics (MD) simulation. Four HMGR inhibitors were used for MD simulation and representative structure of each simulation were selected by clustering analysis. Four structure-based pharmacophore models were generated using the representative structure. The generated models were validated used in virtual screening to find novel scaffolds for inhibiting HMGR. The screened compounds were filtered by applying drug-like properties and used in molecular docking. Finally, four hit compounds were obtained and these complexes were refined using energy minimization. These compounds might be potential leads to design novel HMGR inhibitor.

Keywords: Anti-hypercholesterolemia drug, HMGR inhibitor, Molecular dynamics simulation, Structure-based pharmacophore modeling.

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