Search results for: halo nucleus
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 186

Search results for: halo nucleus

186 Design and Analysis of Formula One Car Halo

Authors: Indira priyadarshini, B. Tulja Lal, K. Anusha, P. Sai Varun

Abstract:

Formula One cars are the fastest road course racing cars in the world, owing to very high cornering speeds achieved through the generation of large amounts of aerodynamic downforce. The main intentions and goals of this paper are to reduce the accidents and improving the safety without affecting the visibility of the driver by redesigning Halo that was developed by Mercedes in conjunction with the FIA to deflect flying debris, such as a loose wheel, away from a driver’s head while the hinged locking mechanism can quickly be removed for easy access. Halo design has been modified in order to reduce the weight without affecting the aerodynamics of the car. CFD simulation is carried out to observe the flow over the Halo. The velocity profile and pressure contours were analyzed. Halo is designed using SOLIDWORKS Furthermore, using the software ANSYS FLUENT 3D simulation of the airflow contour around the Halo in order to make changes in the geometry to improve the design by reducing air resistance and improving aerodynamics. According to our assumption, new 3D Halo model has better aerodynamic properties in order to analyse possible improvements compared to the initial design. Structural analysis is also done by using ANSYS by making an F1 tire colliding with Halo at 225 kmph in order to know the deflections in the structure.

Keywords: aerodynamics, Halo, safety, visibility

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185 Association of Geomagnetic Storms with Coronal Mass Ejections during 1997-2012

Authors: O. P. Tripathi, P. L. Verma

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Coronal Mass Ejections (CMEs) are mostly reached on Earth from 1 to 5 days from the Sun. As a consequence, slow CMEs are accelerated toward the speed of solar wind and fast CMEs are decelerated toward the speed of the solar wind. Coronal mass ejections (CMEs) are bursts of solar material i.e. clouds of plasma and magnetic fields that shoot off the sun’s surface. Other solar events include solar wind streams that come from the coronal holes on the Sun and solar energetic particles that are primarily released by CMEs. We have studied geomagnetic storms (DST ≤ - 80nT) during 1997-2012 with halo and partial halo coronal mass ejections and found that 73.28% CMEs (halo and partial halo coronal mass ejections) are associated with geomagnetic storms. The association rate of halo and partial halo coronal mass ejections are found 67.06% and 32.94% with geomagnetic storms respectively. We have also determined positive co-relation between magnitude of geomagnetic storms and speed of coronal mass ejection with correlation co-efficient 0.23.

Keywords: geomagnetic storms, coronal mass ejections (CMEs), disturbance storm time (Dst), interplanetary magnetic field (IMF)

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184 Effect of Halo Protection Device on the Aerodynamic Performance of Formula Racecar

Authors: Mark Lin, Periklis Papadopoulos

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This paper explores the aerodynamics of the formula racecar when a ‘halo’ driver-protection device is added to the chassis. The halo protection device was introduced at the start of the 2018 racing season as a safety measure against foreign object impacts that a driver may encounter when driving an open-wheel racecar. In the one-year since its introduction, the device has received wide acclaim for protecting the driver on two separate occasions. The benefit of such a safety device certainly cannot be disputed. However, by adding the halo device to a car, it changes the airflow around the vehicle, and most notably, to the engine air-intake and the rear wing. These negative effects in the air supply to the engine, and equally to the downforce created by the rear wing are studied in this paper using numerical technique, and the resulting CFD outputs are presented and discussed. Comparing racecar design prior to and after the introduction of the halo device, it is shown that the design of the air intake and the rear wing has not followed suit since the addition of the halo device. The reduction of engine intake mass flow due to the halo device is computed and presented for various speeds the car may be going. Because of the location of the halo device in relation to the air intake, airflow is directed away from the engine, making the engine perform less than optimal. The reduction is quantified in this paper to show the correspondence to reduce the engine output when compared to a similar car without the halo device. This paper shows that through aerodynamic arguments, the engine in a halo car will not receive unobstructed, clean airflow that a non-halo car does. Another negative effect is on the downforce created by the rear wing. Because the amount of downforce created by the rear wing is influenced by every component that comes before it, when a halo device is added upstream to the rear wing, airflow is obstructed, and less is available for making downforce. This reduction in downforce is especially dramatic as the speed is increased. This paper presents a graph of downforce over a range of speeds for a car with and without the halo device. Acknowledging that although driver safety is paramount, the negative effect of this safety device on the performance of the car should still be well understood so that any possible redesign to mitigate these negative effects can be taken into account in next year’s rules regulation.

Keywords: automotive aerodynamics, halo device, downforce. engine intake

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183 Subthalamic Nucleus in Adult Human Cadaveric Brain: A Morphometric Study

Authors: Mangala Kohli, P. A. Athira, Reeha Mahajan

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The subthalamic nucleus (STN) is a biconvex nucleus situated in the diencephalon. The knowledge of the morphometry of the subthalamic nucleus is essential for accurate targeting of the nucleus during Deep Brain Stimulation. The present study aims to note the morphometry of the subthalamic nucleus in both the cerebral hemispheres which will prove to be of great value to radiologists and neurosurgeons. A cross‐sectional observational study was conducted in the Departments of Anatomy and Forensic Medicine, Lady Hardinge Medical College & Associated Hospitals, New Delhi on thirty adult cadaveric brain specimens of unclaimed and donated corpses. The specimens were categorized into 3 age groups: 20-35, 35-50 and above 50 years. All samples were collected after following the standard protocol for ethical clearance. The morphometric study of 60 subthalamic nucleus was thus conducted. Transverse section of the brain was made at a plane 4mm ventral to the plane containing mid commissural point. The dimensions of the subthalamic nucleus were measured bilaterally with the aid of digital Vernier caliper and magnifying glass. In the present study, the mean length and width and AC-PC length of the subthalamic nucleus was recorded on the right and left side in Group A, B and C. On comparison of mean of subthalamic nucleus dimensions between the right and left side in Group C, no statistically significant difference was observed. The length and width of subthalamic nucleus measured in the 3 age groups were compared with each other and the p value calculated. There was no statistically significant difference between the dimensions of Group A and B, Group B and C as well as Group A and C. The present study reveals that there is no significant reduction in the size of the nucleus was noted with increasing age. Thus, the values obtained in the present study can be used as a reference for various invasive and non-invasive procedures on subthalamic nucleus.

Keywords: cerebral hemisphere, deep brain stimulation, morphometry, subthalamic nucleus

Procedia PDF Downloads 185
182 The Relationship of the Dentate Nucleus with the Pyramid of Vermis: A Microneurosurgical Anatomical Study

Authors: Santhosh K. S. Annayappa, Nupur Pruthi

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The region of dentate nucleus is a common site for various pathologies like hematomas, tumours, etc. We aimed to study in detail the relationship of this region with the vermis, especially the pyramid using microscopic fibre dissection technique. To achieve this aim, 20 cerebellar hemispheres were studied from the 11 cerebellums. Dissection was performed using wooden spatulas and micro dissectors under a microscope following Klingler’s preservation technique. The relationship between the pyramid of vermis and the dentate nucleus was studied in detail. A similar relationship was studied on the MRI of randomly selected trigeminal neuralgia patients and correlated with anatomical findings. Results show the mean distance of the lateral margin of the dentate nucleus from the midline on anatomic specimens was 21.4 ± 1.8 mm (19-25 mm) and 23.4 ± 3.4 mm (15-29 mm) on right and left side, respectively. Similar measurements made on the MRI were 22.97 ± 2.0 mm (20.03-26.15 mm) on the right side and 23.98 ± 2.1 mm (21.47-27.67 mm) on the left side. The amount of white matter dissection required to reach the dentate nucleus at the pyramidal attachment area was 7.3 ± 1.0 mm (6-9 mm) on the right side and 6.8 ± 1.4 mm (5-10 mm) on the left side. It was concluded that the pyramid of vermis has a constant relationship with the dentate nucleus and can be used as an excellent landmark during surgery to localise the dentate nucleus on the suboccipital surface.

Keywords: fiber dissection, micro neurosurgery, the dentate nucleus of cerebellum, the pyramid of vermis

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181 Pre-Administration of Thunbergia Laurifolia Linn. Prevent the Increase of Dopamine in the Nucleus Accumbens in Ethanol Addicted Rats

Authors: Watchareewan Thongsaard, Ratirat Sangpayap, Maneekarn Namsa-Aid

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Thunbergia laurifolia Linn. (TL) is a herbal medicine which has been used as an antidote for several poisonous agents including insecticides and as a component of a mixture of crude extracts to treat drug addicted patients. The aim of this study is to examine the level of dopamine in nucleus accumbens after chronic pre-administration of TL in ethanol addicted rats. Male Wistar rats weigh 200-250 g received TL methanol extract (200mg/kg, orally) 60 minutes before 20% ethanol (1 g/kg, i.p.) for 30 days. The nucleus accumbens was removed and tested for dopamine by HPLC-ECD. The level of dopamine was significantly increased by chronic ethanol administration, whereas the chronic TL extract administration did not cause a difference in dopamine level when compared to control. Moreover, the pre-treatment of TL extract before ethanol significantly reduced the dopamine level in nucleus accumbens to normal level when compared with chronic ethanol administration alone. These results suggested that the increase in dopamine level in the nucleus accumbens by chronic ethanol administration is the cause of ethanol addiction, and this effect is prevented by chronic TL pre-administration. Furthermore, chronic TL extract administration alone did not cause the changes in dopamine level in the nucleus accumbens, indicating that TL itself did not cause addiction.

Keywords: Thunbergia laurifolia Linn., alcohol addiction, dopamine, nucleus accumbens

Procedia PDF Downloads 143
180 Machine Learning Based Approach for Measuring Promotion Effectiveness in Multiple Parallel Promotions’ Scenarios

Authors: Revoti Prasad Bora, Nikita Katyal

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Promotion is a key element in the retail business. Thus, analysis of promotions to quantify their effectiveness in terms of Revenue and/or Margin is an essential activity in the retail industry. However, measuring the sales/revenue uplift is based on estimations, as the actual sales/revenue without the promotion is not present. Further, the presence of Halo and Cannibalization in a multiple parallel promotions’ scenario complicates the problem. Calculating Baseline by considering inter-brand/competitor items or using Halo and Cannibalization's impact on Revenue calculations by considering Baseline as an interpretation of items’ unit sales in neighboring nonpromotional weeks individually may not capture the overall Revenue uplift in the case of multiple parallel promotions. Hence, this paper proposes a Machine Learning based method for calculating the Revenue uplift by considering the Halo and Cannibalization impact on the Baseline and the Revenue. In the first section of the proposed methodology, Baseline of an item is calculated by incorporating the impact of the promotions on its related items. In the later section, the Revenue of an item is calculated by considering both Halo and Cannibalization impacts. Hence, this methodology enables correct calculation of the overall Revenue uplift due a given promotion.

Keywords: Halo, Cannibalization, promotion, Baseline, temporary price reduction, retail, elasticity, cross price elasticity, machine learning, random forest, linear regression

Procedia PDF Downloads 181
179 Visual Improvement Outcome of Pars Plana Vitrectomy Combined Endofragmentation and Secondary IOL Implantation for Dropped Nucleus After Cataract Surgery : A Case Report

Authors: Saut Samuel Simamora

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PURPOSE: Nucleus drop is one of the most feared and severe complications of modern cataract surgery. The lens material may drop through iatrogenic breaks of the posterior capsule. The incidence of the nucleus as the complication of phacoemulsification increases concomitant to the increased frequency of phacoemulsification. Pars plana vitrectomy (PPV) followed by endofragmentation and secondary intraocular lens (IOL) implantation is the choice of management procedure. This case report aims to present the outcome of PPV for the treatment dropped nucleus after cataract surgery METHODS: A 65 year old female patient came to Vitreoretina department with chief complaints blurry vision in her left eye after phacoemulsification one month before. Ophthalmological examination revealed visual acuity of the right eye (VA RE) was 6/15, and the left eye (VA LE) was hand movement. The intraocular pressure (IOP) on the right eye was 18 mmHg, and on the left eye was 59 mmHg. On her left eye, there were aphakic, dropped lens nucleus and secondary glaucoma.RESULTS: The patient got antiglaucoma agent until her IOP was decreased. She underwent pars plana vitrectomy to remove dropped nucleus and iris fixated IOL. One week post operative evaluation revealed VA LE was 6/7.5 and iris fixated IOL in proper position. CONCLUSIONS: Nucleus drop generally occurs in phacoemulsification cataract surgery techniques. Retained lens nucleus or fragments in the vitreous may cause severe intraocular inflammation leading to secondary glaucoma. The proper and good management for retained lens fragments in nucleus drop give excellent outcome to patient.

Keywords: secondary glaucoma, complication of phacoemulsification, nucleus drop, pars plana vitrectomy

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178 Types of Neurons in the Spinal Trigeminal Nucleus of the Camel Brain: Golgi Study

Authors: Qasim A. El Dwairi, Saleh M. Banihani, Ayat S. Banihani, Ziad M. Bataineh

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Neurons in the spinal trigeminal nucleus of the camel were studied by Golgi impregnation. Neurons were classified based on differences in size and shape of their cell bodies, density of their dendritic trees, morphology and distribution of their appendages. In the spinal trigeminal nucleus of the camel, at least twelve types of neurons were identified. These neurons include, stalked, islets, octubus-like, lobulated, boat-like, pyramidal, multipolar, round, oval and elongated neurons. They have large number of different forms of appendages not only for their dendrites but also for their cell bodies. Neurons with unique large dilatations especially at their dendritic branching points were found. The morphological features of these neurons were described and compared with their counterparts in other species. Finding of large number of neuronal types with different size and shapes and large number of different forms of appendages for cell bodies and dendrites together with the presence of cells with unique features such as large dilated parts for dendrites may indicate to a very complex information processing for pain and temperature at the level of the spinal trigeminal nucleus in the camel that traditionally live in a very hard environment (the desert).

Keywords: camel, golgi, neurons , spinal trigeminal nucleus

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177 Non-Coplanar Nuclei in Heavy-Ion Reactions

Authors: Sahila Chopra, Hemdeep, Arshdeep Kaur, Raj K. Gupta

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In recent times, we noticed an interesting and important role of non-coplanar degree-of-freedom (Φ = 00) in heavy ion reactions. Using the dynamical cluster-decay model (DCM) with Φ degree-of-freedom included, we have studied three compound systems 246Bk∗, 164Yb∗ and 105Ag∗. Here, within the DCM with pocket formula for nuclear proximity potential, we look for the effects of including compact, non-coplanar configurations (Φc = 00) on the non-compound nucleus (nCN) contribution in total fusion cross section σfus. For 246Bk∗, formed in 11B+235U and 14N+232Th reaction channels, the DCM with coplanar nuclei (Φc = 00) shows an nCN contribution for 11B+235U channel, but none for 14N+232Th channel, which on including Φ gives both reaction channels as pure compound nucleus decays. In the case of 164Yb∗, formed in 64Ni+100Mo, the small nCN effects for Φ=00 are reduced to almost zero for Φ = 00. Interestingly, however, 105Ag∗ for Φ = 00 shows a small nCN contribution, which gets strongly enhanced for Φ = 00, such that the characteristic property of PCN presents a change of behaviour, like that of a strongly fissioning superheavy element to a weakly fissioning nucleus; note that 105Ag∗ is a weakly fissioning nucleus and Psurv behaves like one for a weakly fissioning nucleus for both Φ = 00 and Φ = 00. Apparently, Φ is presenting itself like a good degree-of-freedom in the DCM.

Keywords: dynamical cluster-decay model, fusion cross sections, non-compound nucleus effects, non-coplanarity

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176 Decay Analysis of 118Xe* Nucleus Formed in 28Si Induced Reaction

Authors: Manoj K. Sharma, Neha Grover

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Dynamical cluster decay model (DCM) is applied to study the decay mechanism of 118Xe* nucleus in reference to recent data on 28Si + 90Zr → 118Xe* reaction, as an extension of our previous work on the dynamics of 112Xe* nucleus. It is relevant to mention here that DCM is based on collective clusterization approach, where emission probability of different decay paths such as evaporation residue (ER), intermediate mass fragments (IMF) and fission etc. is worked out on parallel scale. Calculations have been done over a wide range of center of mass energies with Ec.m. = 65 - 92 MeV. The evaporation residue (ER) cross-sections of 118Xe* compound nucleus are fitted in reference to available data, using spherical and quadrupole (β2) deformed choice of decaying fragments within the optimum orientations approach. It may be noted that our calculated cross-sections find decent agreement with experimental data and hence provide an opportunity to analyze the exclusive role of deformations in view of fragmentation behavior of 118Xe* nucleus. The possible contribution of IMF fragments is worked out and an extensive effort is being made to analyze the role of excitation energy, angular momentum, diffuseness parameter and level density parameter to have better understanding of the decay patterns governed in the dynamics of 28Si + 90Zr → 118Xe* reaction.

Keywords: cross-sections, deformations, fragmentation, angular momentum

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175 Neuron Imaging in Lateral Geniculate Nucleus

Authors: Sandy Bao, Yankang Bao

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The understanding of information that is being processed in the brain, especially in the lateral geniculate nucleus (LGN), has been proven challenging for modern neuroscience and for researchers with a focus on how neurons process signals and images. In this paper, we are proposing a method to image process different colors within different layers of LGN, that is, green information in layers 4 & 6 and red & blue in layers 3 & 5 based on the surface dimension of layers. We take into consideration the images in LGN and visual cortex, and that the edge detected information from the visual cortex needs to be considered in order to return back to the layers of LGN, along with the image in LGN to form the new image, which will provide an improved image that is clearer, sharper, and making it easier to identify objects in the image. Matrix Laboratory (MATLAB) simulation is performed, and results show that the clarity of the output image has significant improvement.

Keywords: lateral geniculate nucleus, matrix laboratory, neuroscience, visual cortex

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174 Robustness Conditions for the Establishment of Stationary Patterns of Drosophila Segmentation Gene Expression

Authors: Ekaterina M. Myasnikova, Andrey A. Makashov, Alexander V. Spirov

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First manifestation of a segmentation pattern in the early Drosophila development is the formation of expression domains (along with the main embryo axis) of genes belonging to the trunk gene class. Highly variable expression of genes from gap family in early Drosophila embryo is strongly reduced by the start of gastrulation due to the gene cross-regulation. The dynamics of gene expression is described by a gene circuit model for a system of four gap genes. It is shown that for the formation of a steep and stationary border by the model it is necessary that there existed a nucleus (modeling point) in which the gene expression level is constant in time and hence is described by a stationary equation. All the rest genes expressed in this nucleus are in a dynamic equilibrium. The mechanism of border formation associated with the existence of a stationary nucleus is also confirmed by the experiment. An important advantage of this approach is that properties of the system in a stationary nucleus are described by algebraic equations and can be easily handled analytically. Thus we explicitly characterize the cross-regulation properties necessary for the robustness and formulate the conditions providing this effect through the properties of the initial input data. It is shown that our formally derived conditions are satisfied for the previously published model solutions.

Keywords: drosophila, gap genes, reaction-diffusion model, robustness

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173 Perinatal Ethanol Exposure Modifies CART System in Rat Brain Anticipated for Development of Anxiety, Depression and Memory Deficits

Authors: M. P. Dandekar, A. P. Bharne, P. T. Borkar, D. M. Kokare, N. K. Subhedar

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Ethanol ingestion by the mother ensue adverse consequences for her offspring. Herein, we examine the behavioral phenotype and neural substrate of the offspring of the mother on ethanol. Female rats were fed with ethanol-containing liquid diet from 8 days prior of conception and continued till 25 days post-parturition to coincide with weaning. Behavioral changes associated with anxiety, depression and learning and memory were assessed in the offspring, after they attained adulthood (day 85), using elevated plus maze (EPM), forced swim (FST) and novel object recognition tests (NORT), respectively. The offspring of the alcoholic mother, compared to those of the pair-fed mother, spent significantly more time in closed arms of EPM and showed more immobility time in FST. Offspring at the age of 25 and 85 days failed to discriminate between novel versus familiar object in NORT, thus reflecting anxiogenic, depressive and amnesic phenotypes. Neuropeptide cocaine- and amphetamine-regulated transcript peptide (CART) is known to be involved in central effects of ethanol and hence selected for the current study. Twenty-five days old pups of the alcoholic mother showed significant augmentation in CART-immunoreactivity in the cells of Edinger-Westphal (EW) nucleus and lateral hypothalamus. However, a significant decrease in CART-immunoreactivity was seen in nucleus accumbens shell (AcbSh), lateral part of bed nucleus of the stria terminalis (BNSTl), locus coeruleus (LC), hippocampus (CA1, CA2 and CA3), and arcuate nucleus (ARC) of the pups and/or adults offspring. While no change in the CART-immunoreactive fibers of AcbSh and BNSTl, CA2 and CA3 was noticed in the 25 days old pups, the CART-immunoreactive cells in EW and paraventricular nucleus (PVN), and fibers in the central nucleus of amygdala of 85 days old offspring remained unaffected. We suggest that the endogenous CART system in these discrete areas, among other factors, may be a causal to the abnormalities in the next generation of an alcoholic mother.

Keywords: anxiety, depression, CART, ethanol, immunocytochemistry

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172 Study of Interplanetary Transfer Trajectories via Vicinity of Libration Points

Authors: Zhe Xu, Jian Li, Lvping Li, Zezheng Dong

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This work is to study an optimized transfer strategy of connecting Earth and Mars via the vicinity of libration points, which have been playing an increasingly important role in trajectory designing on a deep space mission, and can be used as an effective alternative solution for Earth-Mars direct transfer mission in some unusual cases. The use of vicinity of libration points of the sun-planet body system is becoming potential gateways for future interplanetary transfer missions. By adding fuel to cargo spaceships located in spaceports, the interplanetary round-trip exploration shuttle mission of such a system facility can also be a reusable transportation system. In addition, in some cases, when the S/C cruising through invariant manifolds, it can also save a large amount of fuel. Therefore, it is necessary to make an effort on looking for efficient transfer strategies using variant manifold about libration points. It was found that Earth L1/L2 Halo/Lyapunov orbits and Mars L2/L1 Halo/Lyapunov orbits could be connected with reasonable fuel consumption and flight duration with appropriate design. In the paper, the halo hopping method and coplanar circular method are briefly introduced. The former used differential corrections to systematically generate low ΔV transfer trajectories between interplanetary manifolds, while the latter discussed escape and capture trajectories to and from Halo orbits by using impulsive maneuvers at periapsis of the manifolds about libration points. In the following, designs of transfer strategies of the two methods are shown here. A comparative performance analysis of interplanetary transfer strategies of the two methods is carried out accordingly. Comparison of strategies is based on two main criteria: the total fuel consumption required to perform the transfer and the time of flight, as mentioned above. The numeric results showed that the coplanar circular method procedure has certain advantages in cost or duration. Finally, optimized transfer strategy with engineering constraints is searched out and examined to be an effective alternative solution for a given direct transfer mission. This paper investigated main methods and gave out an optimized solution in interplanetary transfer via the vicinity of libration points. Although most of Earth-Mars mission planners prefer to build up a direct transfer strategy for the mission due to its advantage in relatively short time of flight, the strategies given in the paper could still be regard as effective alternative solutions since the advantages mentioned above and longer departure window than direct transfer.

Keywords: circular restricted three-body problem, halo/Lyapunov orbit, invariant manifolds, libration points

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171 Study of Proton-9,11Li Elastic Scattering at 60~75 MeV/Nucleon

Authors: Arafa A. Alholaisi, Jamal H. Madani, M. A. Alvi

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The radial form of nuclear matter distribution, charge and the shape of nuclei are essential properties of nuclei, and hence, are of great attention for several areas of research in nuclear physics. More than last three decades have witnessed a range of experimental means employing leptonic probes (such as muons, electrons etc.) for exploring nuclear charge distributions, whereas the hadronic probes (for example alpha particles, protons, etc.) have been used to investigate the nuclear matter distributions. In this paper, p-9,11Li elastic scattering differential cross sections in the energy range  to  MeV have been studied by means of Coulomb modified Glauber scattering formalism. By applying the semi-phenomenological Bhagwat-Gambhir-Patil [BGP] nuclear density for loosely bound neutron rich 11Li nucleus, the estimated matter radius is found to be 3.446 fm which is quite large as compared to so known experimental value 3.12 fm. The results of microscopic optical model based calculation by applying Bethe-Brueckner–Hartree–Fock formalism (BHF) have also been compared. It should be noted that in most of phenomenological density model used to reproduce the p-11Li differential elastic scattering cross sections data, the calculated matter radius lies between 2.964 and 3.55 fm. The calculated results with phenomenological BGP model density and with nucleon density calculated in the relativistic mean-field (RMF) reproduces p-9Li and p-11Li experimental data quite nicely as compared to Gaussian- Gaussian or Gaussian-Oscillator densities at all energies under consideration. In the approach described here, no free/adjustable parameter has been employed to reproduce the elastic scattering data as against the well-known optical model based studies that involve at least four to six adjustable parameters to match the experimental data. Calculated reaction cross sections σR for p-11Li at these energies are quite large as compared to estimated values reported by earlier works though so far no experimental studies have been performed to measure it.

Keywords: Bhagwat-Gambhir-Patil density, Coulomb modified Glauber model, halo nucleus, optical limit approximation

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170 Bioconversion of Antifungal Antibiotic Derived from Aspergillus Nidulans

Authors: Savitha Janakiraman, Shivakumar M. C

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Anidulafungin, an advanced class of antifungal agent used for the treatment of chronic fungal infections, is derived from Echinocandin B nucleus, an intermediate metabolite of Echinocandin B produced by Aspergillus nidulans. The enzyme acylase derived from the fermentation broth of Actinoplanes utahensis (NRRL 12052) plays a key role in the bioconversion of echinocandin B to echinocandin B nucleus. The membrane-bound nature of acylase and low levels of expression contributes to the rate-limiting process of enzymatic deacylation, hence low yields of ECB nucleus and anidulafungin. In the present study, this is addressed through novel genetic engineering approaches of overexpression and heterologous expression studies, immobilization of whole cells of Actinoplanes utahensis (NRRL 12052) and Co-cultivation studies. Overexpression of the acylase gene in Actinoplanes utahensis (NRRL 12052) was done by increasing the gene copy number to increase the echinocandin B nucleus production. Echinocandin B acylase gene, under the control of a PermE* promoter, was cloned in pSET152 vector and introduced into Actinoplanes utahensis (NRRL12052) by a ɸC31-directed site-specific recombination method. The resultant recombinant strain (C2-18) showed a 3-fold increase in acylase expression, which was confirmed by HPLC analysis. Pichia pastoris is one of the most effective and versatile host systems for the production of heterologous proteins. The ECB acylase gene was cloned into pPIC9K vector with AOX1 promoter and was transformed into Pichia pastoris (GS115). The acylase expression was confirmed by protein expression and bioconversion studies. The heterologous expression of acylase in Pichia pastoris, is a milestone in the development of antifungals. Actively growing cells of Actinoplanes utahensis (NRRL 12052) were immobilized and tested for bioconversion ability which showed >90% conversion in each cycle. The stability of immobilized cell beads retained the deacylation ability up to 60 days and reusability was confirmed up to 4 cycles. The significant findings from the study have revealed that immobilization of whole cells of Actinoplanes utahensis (NRRL 12052) could be an alternative option for bioconversion of echinocandin B to echinocandin B nucleus, which has not been reported to date. The concept of co-cultivation of Aspergillus nidulans and Actinoplanes utahensis strains for the production of the echinocandin B nucleus was also carried out in order to produce echinocandin B nucleus. The process completely reduced the ECB purification step and, therefore, could be recommended as an ingenious method to improve the yield of the ECB nucleus.

Keywords: acylase, anidulafungin, antifungals, Aspergillus nidulans

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169 Effect of Composition and Cooling Rate on the Solidification Structure of Al-Er Alloy

Authors: Jing Ning, Kunyuan Gao

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The microstructure and phase structure of Al-Er alloys with Er content of 10, 20, 30wt% at cooling rate of 60, 40 and 5℃/h were analyzed using scanning electron microscope (SEM) and X-ray diffraction (XRD). Experimental results showed that for solidification of the hypereutectic Al-Er alloys at different conditions, a halo of α-Al appeared around the primary Al₃Er phase. Analysis of the solidification process indicated that after the primary Al₃Er phase formed, the composition of supercooled liquid phase located outside the coupled zone of eutectic growth below the eutectic line, which leaded to the formation of Al halo. With the increase of Er content, the blocky primary Al₃Er phase expanded from 200μm to 1mm in size. With the decrease of cooling rate, the morphology and phase structure of alloy were different. At the cooling rate of 60℃/h, it was obtained the primary Al3Er phase with L1₂ structure, whose profile was straight. Meanwhile, the eutectic structure was flocculent. At the quite slow cooling rate of 5℃/h, it was obtained the primary Al₃Er phase with hR20 structure with irregular jagged profile, and the eutectic structure was approximately strip-shaped. These characteristics were closely related to the cooling rate of solidification. The XRD analysis showed that for Al₃Er phase, the lattice constant a of L1₂ structure was 4.2158Å, and a, c of hR20 structure were 6.0321Å and 35.6290Å, respectively.

Keywords: Al-Er alloy, composition, cooling rate, microstructure

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168 Human Lens Metabolome: A Combined LC-MS and NMR Study

Authors: Vadim V. Yanshole, Lyudmila V. Yanshole, Alexey S. Kiryutin, Timofey D. Verkhovod, Yuri P. Tsentalovich

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Cataract, or clouding of the eye lens, is the leading cause of vision impairment in the world. The lens tissue have very specific structure: It does not have vascular system, the lens proteins – crystallins – do not turnover throughout lifespan. The protection of lens proteins is provided by the metabolites which diffuse inside the lens from the aqueous humor or synthesized in the lens epithelial layer. Therefore, the study of changes in the metabolite composition of a cataractous lens as compared to a normal lens may elucidate the possible mechanisms of the cataract formation. Quantitative metabolomic profiles of normal and cataractous human lenses were obtained with the combined use of high-frequency nuclear magnetic resonance (NMR) and ion-pairing high-performance liquid chromatography with high-resolution mass-spectrometric detection (LC-MS) methods. The quantitative content of more than fifty metabolites has been determined in this work for normal aged and cataractous human lenses. The most abundant metabolites in the normal lens are myo-inositol, lactate, creatine, glutathione, glutamate, and glucose. For the majority of metabolites, their levels in the lens cortex and nucleus are similar, with the few exceptions including antioxidants and UV filters: The concentrations of glutathione, ascorbate and NAD in the lens nucleus decrease as compared to the cortex, while the levels of the secondary UV filters formed from primary UV filters in redox processes increase. That confirms that the lens core is metabolically inert, and the metabolic activity in the lens nucleus is mostly restricted by protection from the oxidative stress caused by UV irradiation, UV filter spontaneous decomposition, or other factors. It was found that the metabolomic composition of normal and age-matched cataractous human lenses differ significantly. The content of the most important metabolites – antioxidants, UV filters, and osmolytes – in the cataractous nucleus is at least ten fold lower than in the normal nucleus. One may suppose that the majority of these metabolites are synthesized in the lens epithelial layer, and that age-related cataractogenesis might originate from the dysfunction of the lens epithelial cells. Comprehensive quantitative metabolic profiles of the human eye lens have been acquired for the first time. The obtained data can be used for the analysis of changes in the lens chemical composition occurring with age and with the cataract development.

Keywords: cataract, lens, NMR, LC-MS, metabolome

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167 Breeding for Hygienic Behavior in Honey Bees

Authors: Michael Eickermann, Juergen Junk

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The Western honey (Apis mellifera) is threatened by a number of parasites, especially the devastating Varroa mite (Varroa destructor) is responsible for a high level of mortality over winter, e.g., in Europe and USA. While the use of synthetic pesticides or organic acids has been preferred so far to control this parasite, breeding strategies for less susceptible honey bees are in early stages. Hygienic behavior can be an important tool for controlling Varroa destructor. Worker bees with a high level of this behavior are able to detect infested brood in the cells under the wax lid during pupation and remove them out of the hive. The underlying processes of this behavior are only partly investigated, but it is for sure that hygienic behavior is heritable and therefore, can be integrated into commercial breeding lines. In a first step, breeding lines with a high level of phenotypic hygienic behavior have been identified by using a bioassay for accurate assessment of this trait in a long-term national breeding program in Luxembourg since 2015. Based on the artificial infestation of nucleus colonies with 150 phoretic Varroa destructor mites, the level of phenotypic hygienic behavior was detected by counting the number of mites in all stages, twelve days after infestation. A nucleus with a high level of hygienic behavior was overwintered and used for breeding activities in the following years. Artificial insemination was used to combine different breeding lines. Buckfast lines, as well as Carnica lines, were used. While Carnica lines offered only a low increase of hygienic behavior up to maximum 62.5%, Buckfast lines performed much better with mean levels of more than 87.5%. Some mating ends up with a level of 100%. But even with a level of 82.5% Varroa mites are not able to reproduce in the colony anymore. In a final step, a nucleus with a high level of hygienic behavior were build up to full colonies and located at two places in Luxembourg to build up a drone congregation area. Local beekeepers can bring their nucleus to this location for mating the queens with drones offering a high level of hygienic behavior.

Keywords: agiculture, artificial insemination, honey bee, varroa destructor

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166 Limbic Involvement in Visual Processing

Authors: Deborah Zelinsky

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The retina filters millions of incoming signals into a smaller amount of exiting optic nerve fibers that travel to different portions of the brain. Most of the signals are for eyesight (called "image-forming" signals). However, there are other faster signals that travel "elsewhere" and are not directly involved with eyesight (called "non-image-forming" signals). This article centers on the neurons of the optic nerve connecting to parts of the limbic system. Eye care providers are currently looking at parvocellular and magnocellular processing pathways without realizing that those are part of an enormous "galaxy" of all the body systems. Lenses are modifying both non-image and image-forming pathways, taking A.M. Skeffington's seminal work one step further. Almost 100 years ago, he described the Where am I (orientation), Where is It (localization), and What is It (identification) pathways. Now, among others, there is a How am I (animation) and a Who am I (inclination, motivation, imagination) pathway. Classic eye testing considers pupils and often assesses posture and motion awareness, but classical prescriptions often overlook limbic involvement in visual processing. The limbic system is composed of the hippocampus, amygdala, hypothalamus, and anterior nuclei of the thalamus. The optic nerve's limbic connections arise from the intrinsically photosensitive retinal ganglion cells (ipRGC) through the "retinohypothalamic tract" (RHT). There are two main hypothalamic nuclei with direct photic inputs. These are the suprachiasmatic nucleus and the paraventricular nucleus. Other hypothalamic nuclei connected with retinal function, including mood regulation, appetite, and glucose regulation, are the supraoptic nucleus and the arcuate nucleus. The retino-hypothalamic tract is often overlooked when we prescribe eyeglasses. Each person is different, but the lenses we choose are influencing this fast processing, which affects each patient's aiming and focusing abilities. These signals arise from the ipRGC cells that were only discovered 20+ years ago and do not address the campana retinal interneurons that were only discovered 2 years ago. As eyecare providers, we are unknowingly altering such factors as lymph flow, glucose metabolism, appetite, and sleep cycles in our patients. It is important to know what we are prescribing as the visual processing evaluations expand past the 20/20 central eyesight.

Keywords: neuromodulation, retinal processing, retinohypothalamic tract, limbic system, visual processing

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165 Periodical System of Isotopes

Authors: Andriy Magula

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With the help of a special algorithm being the principle of multilevel periodicity, the periodic change of properties at the nuclear level of chemical elements was discovered and the variant for the periodic system of isotopes was presented. The periodic change in the properties of isotopes, as well as the vertical symmetry of subgroups, was checked for consistency in accordance with the following ten types of experimental data: mass ratio of fission fragments; quadrupole moment values; magnetic moment; lifetime of radioactive isotopes; neutron scattering; thermal neutron radiative capture cross-sections (n, γ); α-particle yield cross-sections (n, α); isotope abundance on Earth, in the Solar system and other stellar systems; features of ore formation and stellar evolution. For all ten cases, the correspondences for the proposed periodic structure of the nucleus were obtained. The system was formed in the usual 2D table, similar to the periodic system of elements, and the mass series of isotopes was divided into 8 periods and 4 types of ‘nuclear’ orbitals: sn, dn, pn, fn. The origin of ‘magic’ numbers as a set of filled charge shells of the nucleus was explained. Due to the isotope system, the periodic structure is shown at a new level of the universe, and the prospects of its practical use are opened up.

Keywords: periodic system, isotope, period, subgroup, “nuclear” orbital, nuclear reaction

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164 Applying the Crystal Model Approach on Light Nuclei for Calculating Radii and Density Distribution

Authors: A. Amar

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A new model, namely the crystal model, has been modified to calculate the radius and density distribution of light nuclei up to ⁸Be. The crystal model has been modified according to solid-state physics, which uses the analogy between nucleon distribution and atoms distribution in the crystal. The model has analytical analysis to calculate the radius where the density distribution of light nuclei has obtained from analogy of crystal lattice. The distribution of nucleons over crystal has been discussed in a general form. The equation that has been used to calculate binding energy was taken from the solid-state model of repulsive and attractive force. The numbers of the protons were taken to control repulsive force, where the atomic number was responsible for the attractive force. The parameter has been calculated from the crystal model was found to be proportional to the radius of the nucleus. The density distribution of light nuclei was taken as a summation of two clusters distribution as in ⁶Li=alpha+deuteron configuration. A test has been done on the data obtained for radius and density distribution using double folding for d+⁶,⁷Li with M3Y nucleon-nucleon interaction. Good agreement has been obtained for both the radius and density distribution of light nuclei. The model failed to calculate the radius of ⁹Be, so modifications should be done to overcome discrepancy.

Keywords: nuclear physics, nuclear lattice, study nucleus as crystal, light nuclei till to ⁸Be

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163 Structural and Histochemical Alterations in the Development of the Stigma in Vibirnum tinus

Authors: Aslihan Cetinbas Genc, Meral Unal

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This study presents the structural and cytochemical alterations of stigma at the stages of pre-anthesis, anthesis and post-anthesis in Vibirnum tinus. Capitate stigma continues with a closed style. The receptive surface of stigma is composed of unicellular papillae which are short and flattened at pre-anthesis stage. The papillae in this stage have dense cytoplasm with small vacuoles and a centrally located nucleus. With the start of anthesis, the stigma widens, papillae lengthen and become cylindrical. At anthesis stage, vacuoles enlarge, and nucleus moves to the base of the cell. At post-anthesis stage, the boundaries of the papillae become less noticeable. As proved by Periodic Acid Schiff procedure, the cytoplasm of papillae is rich in insoluble polysaccharides at all stages of development but it becomes remarkable at post-anthesis, particularly at the sub-papillar area. Although there is no significant difference in the content of protein in all stages of the development, it is more abundant at post-anthesis stage, as in Coomassie Brillant Blue stained sections. The surface of papillae is covered by a cuticle which becomes thicker at post-anthesis, and it gives positive reaction with Sudan Black B and Auramine O. The cuticle is covered by a pellicle stained by Coomassie Brillant Blue, indicating dry type of stigma.

Keywords: develeopmental features, histochemistry, stigma, Vibirnum tinus

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162 Levels of Family Empowerment and Parenting Skills of Parents with Children with Developmental Disabilities Who Are Users of Early Intervention Services

Authors: S. Bagur, S. Verger, B. Mut

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Early childhood intervention (ECI) is understood as the set of interventions aimed at the child population with developmental disorders or disabilities from 0 to 6 years of age, the family, and the environment. Under the principles of family-centred practices, the members of the family nucleus are direct agents of intervention. Thus, the multidisciplinary team of professionals should work to improve family empowerment and the level of parenting skills. The aim of the present study is to analyse descriptively and differentially the level of parenting skills and family empowerment of parents using ECI services during the foster care phase. There were 135 families participating in the study. Three questionnaires were completed. The results show that the employment situation, the age of the child receiving an intervention, and the number of children in the family nucleus or the professional carrying out the intervention are variables that have a differential impact on different items of empowerment and parenting skills. The results are discussed and future lines of research are proposed, with the understanding that the initial analysis of the variables of empowerment and parenting skills may be predictors for the improvement of child development and family well-being. In addition, it is proposed to identify and analyse professional training in order to be able to adapt early care practices without depending on the discipline of the professional of reference.

Keywords: developmental disabilities, early childhood intervention, family empowerment, parenting skills

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161 Hypothalamic Para-Ventricular and Supra-Optic Nucleus Histo-Morphological Alterations in the Streptozotocin-Diabetic Gerbils (Gerbillus Gerbillus)

Authors: Soumia Hammadi, Imane Nouacer, Lamine Hamida, Younes A. Hammadi, Rachid Chaibi

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Aims and objective: In the present work, we investigate the impact of both acute and chronic diabetes mellitus induced by streptozotocin (STZ) on the hypothalamus of the small gerbil (Gerbillus gerbillus). In this purpose, we aimed to study the histologic structure of the gerbil’s hypothalamic supraoptic (NSO) and paraventricular nucleus (NPV) at two distinct time points: two days and 30 days after diabetes onset. Methods: We conducted our investigation using 19 adult male gerbils weighing 25 to 28 g, divided into three groups as follow: Group I: Control gerbils (n=6) received an intraperitoneal injection of citrate buffer. Group II: STZ-diabetic gerbils (n=8) received a single intraperitoneal injection of STZ at a dose of 165 mg/kg of body weight. Diabetes onset (D0) is considered with the first hyperglycemia level exceeding 2,5 g/L. This group was further divided into two subgroups: Group II-1: Experimental Gerbils, at acute state of diabetes (n=8) sacrificed after 02 days of diabetes onset, Group II-2: Experimental Gerbils at chronic state of diabetes (n=7) sacrificed after 30 days of diabetes onset. Two and 30 days after diabetes onset, gerbils had blood drawn from the retro-orbital sinus into EDTA tubes. After centrifugation at -4°C, plasma was frozen at -80°C for later measurement of Cortisol, ACTH, and insulin. Afterward, animals were decapitated; their brain was removed, weighed, fixed in aqueous bouin, and processed and stained with Toluidine Bleu stain for histo-stereological analysis. A comparison was done with control gerbils treated with citrate buffer. Results: Compared to control gerbils, at 02 Days post diabetes onset, the neuronal somata of the paraventricular (NPV) and supraoptic nuclei (NSO) expressed numerous vacuoles of various sizes, we distinct also a neuronal juxtaposition and several unidentifiable vacuolated profiles were also seen in the neuropile. At the same time, we revealed the presence of à shrunken and condensed nuclei, which seem to touch the parvocellular neurons ( NPV); this leads us to suggest the presence of an apoptotic process in the early stage of diabetes. At 30 days of diabetes mellitus, the NPV manifests a few neurons with a distant appearance, in addition the magnocellular neurons in both NPV and NSO were hypertrophied with a rich euchromatin nucleus, a well-defined nucleolus, and a granular cytoplasm. Despite the neuronal degeneration at this stage, unexpectedly, ACTH registers a continuous significant high level compared to the early stage of diabetes mellitus and to control gerbils. Conclusion: The results suggest that the induction of diabetes mellitus using STZ in the small gerbils lead to alterations in the structure and morphology of the hypothalamus and hyper-secretion of ACTH and cortisol, possibly indicating hyperactivity of the hypothalamo-pituitary adrenal axis (HPA) during both the early and later stages of the disease. The subsequent quantitative evaluation of CRH, immunehistochemical evaluation of apoptosis, and oxidative stress assessment could corroborate our results.

Keywords: diabetes type 1., streptozotocin., small gerbil., hypothalamus., paraventricular nucleus., supraoptic nucleus.

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160 Synthesis of Deformed Nuclei 260Rf, 261Rf and 262Rf in the Decay of 266Rf*Formed via Different Fusion Reactions: Entrance Channel Effects

Authors: Niyti, Aman Deep, Rajesh Kharab, Sahila Chopra, Raj. K. Gupta

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Relatively long-lived transactinide elements (i.e., elements with atomic number Z≥104) up to Z = 108 have been produced in nuclear reactions between low Z projectiles (C to Al) and actinide targets. Cross sections have been observed to decrease steeply with increasing Z. Recently, production cross sections of several picobarns have been reported for comparatively neutron-rich nuclides of 112 through 118 produced via hot fusion reactions with 48Ca and actinide targets. Some of those heavy nuclides are reported to have lifetimes on the order of seconds or longer. The relatively high cross sections in these hot fusion reactions are not fully understood and this has renewed interest in systematic studies of heavy-ion reactions with actinide targets. The main aim of this work is to understand the dynamics hot fusion reactions 18O+ 248Cm and 22Ne+244Pu (carried out at RIKEN and TASCA respectively) using the collective clusterization technique, carried out by undertaking the decay of the compound nucleus 266Rf∗ into 4n, 5n and 6n neutron evaporation channels. Here we extend our earlier study of the excitation functions (EFs) of 266Rf∗, formed in fusion reaction 18O+248Cm, based on Dynamical Cluster-decay Model (DCM) using the pocket formula for nuclear proximity potential, to the use of other nuclear interaction potentials derived from Skyrme energy density formalism (SEDF) based on semiclassical extended Thomas Fermi (ETF) approach and also study entrance channel effects by considering the synthesis of 266Rf* in 22Ne+244Pu reaction. The Skyrme forces used are the old force SIII, and new forces GSkI and KDE0(v1). Here, the EFs for the production of 260Rf, 261Rf and 262Rf isotope via 6n, 5n and 4n decay channel from the 266Rf∗ compound nucleus are studied at Elab = 88.2 to 125 MeV, including quadrupole deformations β2i and ‘hot-optimum’ orientations θi. The calculations are made within the DCM where the neck-length ∆R is the only parameter representing the relative separation distance between two fragments and/or clusters Ai which assimilates the neck formation effects.

Keywords: entrance channel effects, fusion reactions, skyrme force, superheavy nucleus

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159 Effect of Toxic Metals Exposure on Rat Behavior and Brain Morphology: Arsenic, Manganese

Authors: Tamar Bikashvili, Tamar Lordkipanidze, Ilia Lazrishvili

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Heavy metals remain one of serious environmental problems due to their toxic effects. The effect of arsenic and manganese compounds on rat behavior and neuromorphology was studied. Wistar rats were assigned to four groups: rats in control group were given regular water, while rats in other groups drank water with final manganese concentration of 10 mg/L (group A), 20 mg/L (group B) and final arsenic concentration 68 mg/L (group C), respectively, for a month. To study exploratory and anxiety behavior and also to evaluate aggressive performance in “home cage” rats were tested in “Open Field” and to estimate learning and memory status multi-branched maze was used. Statistically significant increase of motor and oriental-searching activity in experimental groups was revealed by an open field test, which was expressed in increase of number of lines crossed, rearing and hole reflexes. Obtained results indicated the suppression of fear in rats exposed to manganese. Specifically, this was estimated by the frequency of getting to the central part of the open field. Experiments revealed that 30-day exposure to 10 mg/ml manganese did not stimulate aggressive behavior in rats, while exposure to the higher dose (20 mg/ml), 37% of initially non-aggressive animals manifested aggressive behavior. Furthermore, 25% of rats were extremely aggressive. Obtained data support the hypothesis that excess manganese in the body is one of the immediate causes of enhancement of interspecific predatory aggressive and violent behavior in rats. It was also discovered that manganese intoxication produces non-reversible severe learning disability and insignificant, reversible memory disturbances. Studies of rodents exposed to arsenic also revealed changes in the learning process. As it is known, the distribution of metal ions differs in various brain regions. The principle manganese accumulation was observed in the hippocampus and in the neocortex, while arsenic was predominantly accumulated in nucleus accumbens, striatum, and cortex. These brain regions play an important role in the regulation of emotional state and motor activity. Histopathological analyzes of brain sections illustrated two morphologically distinct altered phenotypes of neurons: (1) shrunk cells with indications of apoptosis - nucleus and cytoplasm were very difficult to be distinguished, the integrity of neuronal cytoplasm was not disturbed; and (2) swollen cells - with indications of necrosis. Pyknotic nucleus, plasma membrane disruption and cytoplasmic vacuoles were observed in swollen neurons and they were surrounded by activated gliocytes. It’s worth to mention that in the cortex the majority of damaged neurons were apoptotic while in subcortical nuclei –neurons were mainly necrotic. Ultrastructural analyses demonstrated that all cell types in the cortex and the nucleus caudatus represent destructed mitochondria, widened neurons’ vacuolar system profiles, increased number of lysosomes and degeneration of axonal endings.

Keywords: arsenic, manganese, behavior, learning, neuron

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158 Microwave-Assisted Synthesis of a Class of Pyridine and Purine Thioglycoside Analogs

Authors: Mamdouh Abu-Zaied, K. Mohamed, Galal A. Nawwar

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Microwave-assisted synthesis of a new class of pyridine or purine thioglycoside analogs from readily available starting materials has been described. The key step of this protocol is the formation of sodium pyridine 4-thiolate 4 and pyrazolo[1,5-a]pyrimidine-7-thiolate 5 derivatives via condensation of 1 with cyanoacetanilide derivative 2 or 5-aminopyrazole derivative 3 respectively under microwave irradiation, followed by coupling with halo sugars to give the corresponding pyridine and purine thioglycoside analogs. The obtained compounds were evaluated in vitro against lung (A549), colon (HCT116), liver (HEPG2), and MCF-7(breast) cancer cell lines. Some of them recorded promising activities.

Keywords: antitumor, cyclic sugars, pyrazoles, pyridines, pyrimidines, purines, thioglycosides

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

Authors: Vatsal M. Patel, Navin B. Patel

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

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

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