Search results for: mechanism of cytotoxicity
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 3321

Search results for: mechanism of cytotoxicity

3261 Evaluation of Anti-Cancer Activities of Formononetin in Lung Cancer by in vitro Methods

Authors: Vishnu Varthan Vaithiyalingam Jagannathan, Lakshmi Karunanidhi Santhanalakshmi, Srividya Ammayappan Rajam

Abstract:

Formononetin is the O-Methoxy Flavonol that has many pharmacological activities, which belongs to the flavonoid family. In the current study, activity of this molecule was evaluated in lung cancer cell lines. In general, flavonoids possess certain anticancer mechanism. Being a flavonoid subfamily, this molecule was subjected to evaluate cytotoxicity assay by MTT ((3-(4,5-Dimethylthiazol-2-yl)-2,5-Diphenyltetrazolium Bromide)) stain, mode of cell death assay stained by acridine orange and ethidium bromide and Evaluation of Apoptosis pathway (extrinsic or intrinsic) by Caspase 3/7 stain and Rhodamine-123 stain. From the results, we could able to confirm that the investigatory molecule formononetin has anticancer activity and in future, the study will propose to evaluate the formononetin action against genetic changes occurs during lung cancer progression.

Keywords: Caspase 3/7, formononetin, lung cancer, Rhodamine-123

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3260 Green Synthesis and Characterisation of Gold Nanoparticles from the Stem Bark and Leaves of Khaya Senegalensis and Its Cytotoxicity on MCF7 Cell Lines

Authors: Stephen Daniel Iduh, Evans Chidi Egwin, Oluwatosin Kudirat Shittu

Abstract:

The process for the development of reliable and eco-friendly metallic Nanoparticles is an important step in the field of Nanotechnology for biomedical application. To achieve this, use of natural sources like biological systems becomes essential. In the present work, extracellular biosynthesis of gold Nanoparticles using aqueous leave and stembark extracts of K. senegalensis has been attempted. The gold Nanoparticles produced were characterized using High Resolution scanning electron microscopy, Ultra Violet–Visible spectroscopy, zeta-sizer Nano, Energy-Dispersive X-ray (EDAX) Spectroscopy and Fourier Transmission Infrared (FTIR) Spectroscopy. The cytotoxicity of the synthesized gold nanoparticles on MCF-7 cell line was evaluated using MTT assay. The result showed a rapid development of Nano size and shaped particles within 5 minutes of reaction with Surface Plasmon Resonance at 520 and 525nm respectively. An average particle size of 20-90nm was confirmed. The amount of the extracts determines the core size of the AuNPs. The core size of the AuNPs decreases as the amount of extract increases and it causes the shift of Surface Plasmon Resonance band. The FTIR confirms the presence of biomolecules serving as reducing and capping agents on the synthesised gold nanoparticles. The MTT assay shows a significant effect of gold nanoparticles which is concentration dependent. This environment-friendly method of biological gold Nanoparticle synthesis has the potential and can be directly applied in cancer therapy.

Keywords: biosynthesis, gold nanoparticles, characterization, calotropis procera, cytotoxicity

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3259 Magnetic Properties and Cytotoxicity of Ga-Mn Magnetic Ferrites Synthesized by the Citrate Sol-Gel Method

Authors: Javier Sánchez, Laura Elena De León Prado, Dora Alicia Cortés Hernández

Abstract:

Magnetic spinel ferrites are materials that possess size, magnetic properties and heating ability adequate for their potential use in biomedical applications. The Mn0.5Ga0.5Fe2O4 magnetic nanoparticles (MNPs) were synthesized by sol-gel method using citric acid as chelating agent of metallic precursors. The synthesized samples were identified by X-Ray Diffraction (XRD) as an inverse spinel structure with no secondary phases. Saturation magnetization (Ms) of crystalline powders was 45.9 emu/g, which was higher than those corresponding to GaFe2O4 (14.2 emu/g) and MnFe2O4 (40.2 emu/g) synthesized under similar conditions, while the coercivity field (Hc) was 27.9 Oe. The average particle size was 18 ± 7 nm. The heating ability of the MNPs was enough to increase the surrounding temperature up to 43.5 °C in 7 min when a quantity of 4.5 mg of MNPs per mL of liquid medium was tested. Cytotoxic effect (hemolysis assay) of MNPs was determined and the results showed hemolytic values below 1% in all tested cases. According to the results obtained, these synthesized nanoparticles can be potentially used as thermoseeds for hyperthermia therapy.

Keywords: manganese-gallium ferrite, magnetic hyperthermia, heating ability, cytotoxicity

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3258 Analysis of Structure-Flow Interaction for Water Brake Mechanism

Authors: Murat Avci, Fatih Kosar, Ismail Yilmaz

Abstract:

In this study, structure-flow interaction for water brake mechanism is studied with Abaqus CEL approach. The water brake mechanism is used for dynamic systems such as sled system on rail. For the achievement of these system tests, structure-flow interaction should be investigated in detail. This study is about a sled test of an aircraft subsystem which rises to supersonic speeds thanks to rocket engines. To decrease or to stop the thrusting rocket sleds, water brake mechanisms are used. Water brake mechanism provides the deceleration of the structures that have supersonic speeds. Therefore, structure-flow interaction may cause damage to the water brake mechanism. To verify all design revisions with system tests are so costly so that some decisions are taken in accordance with numerical methods. In this study, structure-flow interaction that belongs to water brake mechanism is solved with Abaqus CEL approach. Fluid and deformation on the structure behaviors are modeled at the same time thanks to CEL approach. Provided analysis results are corrected with the dynamic tests. Deformation zones seen in numerical analysis are also observed in dynamic tests. Finally, Johnson-Cook material model parameters used for this analysis are proven, and it is understood that these parameters can be used for dynamic analysis like water brake mechanism.

Keywords: aircraft, rocket, structure-flow, supersonic

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3257 Physico‑chemical Behavior and Microstructural Manipulation of Nanocomposites Containing Hydroxyapatite, Alumina, and Graphene Oxide

Authors: Reim A. Almotiri, Manal M. Alkhamisi

Abstract:

Ternary nanocomposites based on hydroxyapatite (HAP) and alumina (Al2O3) were embedded through graphene oxide (GO) nanosheets to be investigated for medical applications. The composition of the preparations has been confirmed by X-ray photoelectron spectroscopy, energy-dispersive X-ray analysis, and Fourier-Transform infrared spectroscopy. Scanning and transmission electron microscopy have shown the typical morphologies of the components of the nanocomposites with hydroxyapatite nanorods reaching an average diameter of 22.26±2 nm and an average length of 69.56±19.25 nm in the ternary nanocomposites. The ternary nanocomposite has a microhardness of 5.8±0.1 GPa and a higher average roughness of 6.5 nm compared to pure HAP preparation with an average roughness of 2.7 nm. All preparations have shown an acceptable cytotoxicity profile with a percent osteoblasts cell viability of 98.6±1.3% after culturing with the ternary nanocomposite. The TNC has also shown the highest antibacterial activity compared to preparations of each of its constituents and their nanocomposites, with a zone of inhibition’s diameter of 14.1±0.8 mm and 13.6±0.6 mm against Staphylococcus aureus and Escherichia coli, respectively, compared to no zone of inhibition for the pure hydroxyapatite preparation.

Keywords: hydroxypatite, cytotoxicity, nanocomposites, X-ray analysis

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3256 Optimality of Shapley Value Mechanism under Sybil Strategies

Authors: Bruno Mazorra Roig

Abstract:

In the realm of cost-sharing mechanisms, the vulnerability to Sybil strategies, where agents can create fake identities to manipulate outcomes, has not yet been studied. In this paper, we delve into the intricacies of different cost-sharing mechanisms proposed in the literature, highlighting its non-Sybil-resistance nature. Furthermore, we prove that under mild conditions, a Sybil-proof cost-sharing mechanism for public excludable goods is at least (n/2 + 1)−approximate. This finding reveals an exponential increase in the worst-case social cost in environments where agents are restricted from using Sybil strategies. We introduce the concept of Sybil Welfare Invariant mechanisms, where a mechanism maintains its worst-case welfare under Sybil strategies for every set of prior beliefs with full support even when the mechanism is not Sybil-proof. Finally, we prove that the Shapley value mechanism for public excludable goods holds this property and so deduce that the worst-case social cost of this mechanism is the nth harmonic number Hn under the equilibrium of the game with Sybil strategies, matching the worst-case social cost bound for cost-sharing mechanisms. This finding carries important implications for decentralized autonomous organizations (DAOs), indicating that they are capable of funding public excludable goods efficiently, even when the total number of agents is unknown.

Keywords: game theory, mechanism design, cost sharing, false-name proofness

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3255 Design and Optimization for a Compliant Gripper with Force Regulation Mechanism

Authors: Nhat Linh Ho, Thanh-Phong Dao, Shyh-Chour Huang, Hieu Giang Le

Abstract:

This paper presents a design and optimization for a compliant gripper. The gripper is constructed based on the concept of compliant mechanism with flexure hinge. A passive force regulation mechanism is presented to control the grasping force a micro-sized object instead of using a sensor force. The force regulation mechanism is designed using the planar springs. The gripper is expected to obtain a large range of displacement to handle various sized objects. First of all, the statics and dynamics of the gripper are investigated by using the finite element analysis in ANSYS software. And then, the design parameters of the gripper are optimized via Taguchi method. An orthogonal array L9 is used to establish an experimental matrix. Subsequently, the signal to noise ratio is analyzed to find the optimal solution. Finally, the response surface methodology is employed to model the relationship between the design parameters and the output displacement of the gripper. The design of experiment method is then used to analyze the sensitivity so as to determine the effect of each parameter on the displacement. The results showed that the compliant gripper can move with a large displacement of 213.51 mm and the force regulation mechanism is expected to be used for high precision positioning systems.

Keywords: flexure hinge, compliant mechanism, compliant gripper, force regulation mechanism, Taguchi method, response surface methodology, design of experiment

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3254 Preparation, Characterisation, and Measurement of the in vitro Cytotoxicity of Mesoporous Silica Nanoparticles Loaded with Cytotoxic Pt(II) Oxadiazoline Complexes

Authors: G. Wagner, R. Herrmann

Abstract:

Cytotoxic platinum compounds play a major role in the chemotherapy of a large number of human cancers. However, due to the severe side effects for the patient and other problems associated with their use, there is a need for the development of more efficient drugs and new methods for their selective delivery to the tumours. One way to achieve the latter could be in the use of nanoparticular substrates that can adsorb or chemically bind the drug. In the cell, the drug is supposed to be slowly released, either by physical desorption or by dissolution of the particle framework. Ideally, the cytotoxic properties of the platinum drug unfold only then, in the cancer cell and over a longer period of time due to the gradual release. In this paper, we report on our first steps in this direction. The binding properties of a series of cytotoxic Pt(II) oxadiazoline compounds to mesoporous silica particles has been studied by NMR and UV/vis spectroscopy. High loadings were achieved when the Pt(II) compound was relatively polar, and has been dissolved in a relatively nonpolar solvent before the silica was added. Typically, 6-10 hours were required for complete equilibration, suggesting the adsorption did not only occur to the outer surface but also to the interior of the pores. The untreated and Pt(II) loaded particles were characterised by C, H, N combustion analysis, BET/BJH nitrogen sorption, electron microscopy (REM and TEM) and EDX. With the latter methods we were able to demonstrate the homogenous distribution of the Pt(II) compound on and in the silica particles, and no Pt(II) bulk precipitate had formed. The in vitro cytotoxicity in a human cancer cell line (HeLa) has been determined for one of the new platinum compounds adsorbed to mesoporous silica particles of different size, and compared with the corresponding compound in solution. The IC50 data are similar in all cases, suggesting that the release of the Pt(II) compound was relatively fast and possibly occurred before the particles reached the cells. Overall, the platinum drug is chemically stable on silica and retained its activity upon prolonged storage.

Keywords: cytotoxicity, mesoporous silica, nanoparticles, platinum compounds

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3253 Targeted Delivery of Novel Copper-Based Nanoparticles for Advance Cancer Therapeutics

Authors: Arindam Pramanik, Parimal Karmakar

Abstract:

We have explored the synergistic anti-cancer activity of copper ion and acetylacetone complex containing 1,3 diketone group (like curcumin) in metallorganic compound “Copper acetylacetonate” (CuAA). The cytotoxicity mechanism of CuAA complex was evaluated on various cancer cell lines in vitro. Among these, reactive oxygen species (ROS), glutathione level (GSH) in the cell was found to increase. Further mitochondrial membrane damage was observed. The fate of cell death was found to be induced by apoptosis. For application purpose, we have developed a novel biodegradable, non-toxic polymer-based nanoparticle which has hydrophobically modified core for loading of the CuAA. Folic acid is conjugated on the surface of the polymer (chitosan) nanoparticle for targeting to cancer cells for minimizing toxicity to normal cells in-vivo. Thus, this novel drug CuAA has an efficient anticancer activity which has been targeted specifically to cancer cells through polymer nanoparticle.

Keywords: anticancer, apoptosis, copper nanoparticle, targeted drug delivery

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3252 Cytotoxic Activity against Hepatocarcinoma and Cholangiocarcinoma Cells of Four Cathartic Herbal Medicines

Authors: Pranporn Kuropakornpong, Srisopa Ruangnoo, Arunporn Itharat

Abstract:

Liver cancer has the highest prevalence rate in the North and Northeast of Thailand. Four Thai medicinal plants such as resin of Ferula asafoetida Regel, latex of Aloe barbadensis Miller leaves, roots of Baliospermum manotanum, and latex of Garcinia hanburyi Hook are used in Thai traditional medicine as cathartic drug and detoxification in liver cancer patients. Thus, this research aimed to evaluate the cytotoxic activity of these plants against hepatocarcinoma (HepG2) and cholangiocarcinoma (KKU-M156) cells by SRB assay. These plants were macerated in 95% ethanol. The results showed that roots of Baliospermum manotanum and latex of Garcinia hanburyi Hook showed the strongest cytotoxicity against HepG2 (IC50 = 3.03+0.91 and 0.62+0.01µg/ml, respectively) and KKU-M156 (IC50 = 0.978+0.663 and 0.006+0.005 µg/ml, respectively). Latex of Garcinia hanburyi Hook also showed high cytotoxicity against normal cell line (IC50=8.86+0.31 µg/ml), and even though its selective values are high, dose of this herb should be limited.

Keywords: cholangiocarcinoma, cytotoxic activity, Garcinia hanburyi Hook, hepatocarcinoma

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3251 Preliminary Phytopharmacological Evaluation of Methanol and Petroleum Ether Extracts of Selected Vegetables of Bangladesh

Authors: A. Mohammad Abdul Motalib Momin, B. Sheikh Mohammad Adil Uddin, C. Md Mamunur Rashid, D. Sheikh Arman Mahbub, E. Mohammad Sazzad Rahman, F. Abdullah Faruque

Abstract:

The present study was designed to investigate the antioxidant and cytotoxicity potential of methanol and pet ether extracts of the Lagenaria siceraria (LM, LP), Cucumis sativus (CSM, CSP), Cucurbita maxima (CMM, CMP) plants. For the phytochemical screening, crude extract was tested for the presence of different chemical groups. In Lagenaria siceraria the following groups were identified: alkaloids, steroids, glycosides and saponins for methanol extract and alkaloids, steroids, glycosides, tannins and saponins are for pet ether extract. Glycosides, steroids, alkaloids, saponins and tannins are present in the methanol extract of Cucumis sativus; the pet ether extract has the alkaloids, steroids and saponins. Glycosides, steroids, alkaloids, saponins and tannins are present in both the methanolic and pet ether extract of Cucurbita maxima. In vitro antioxidant activity of the extracts were performed using DPPH radical scavenging, nitric oxide (NO) scavenging, total antioxidant capacity, total phenol content, total flavonoid content, and Cupric Reducing Antioxidant Capacity assays. The most prominent antioxidant activity was observed with the CSM in the DPPH free radical scavenging test with an IC50 value of 1667.23±11.00271 μg/ml as opposed to that of standard ascorbic acid (IC50 value of 15.707± 1.181 μg/ml.) In total antioxidant capacity method, CMP showed the highest activity (427.81±11.4 mg ascorbic acid/g). The total phenolic and flavonoids content were determined by Folin-Ciocalteu Reagent and aluminium chloride colorimetric method, respectively. The highest total phenols and total flavonoids content were found in CMM and LP with the value of 79.06±16.06 mg gallic acid/g & 119.0±1.41 mg quercetin/g, respectively. In nitric oxide (NO) scavenging the most prominent antioxidant activity was observed in CMM with an IC50 value of 8.119± 0.0036 μg/ml. The Cupric reducing capacity of the extracts was strong and dose dependent manner and CSM showed lowest reducing capacity. The cytotoxicity was determined by Brine shrimp lethality test and among these extracts most potent cytotoxicity was shown by CMM with LC50 value 16.98 µg/ml. The obtained results indicate that the investigated plants could be potential sources of natural antioxidants and can be used for various types of diseases.

Keywords: antioxidant, cytotoxicity, methanol, petroleum ether

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3250 Cationic Copolymer-Functionalized Nanodiamonds Stabilizes Silver Nanoparticles with Dual Antibacterial Activity and Lower Cytotoxicity

Authors: Weiwei Cao, Xiaodong Xing

Abstract:

In order to effectively resolve the microbial pollution and contamination, synthetic nano-antibacterial materials are widely used in daily life. Among them, nanodiamonds (NDs) have recently been demonstrated to hold promise as useful materials in biomedical applications due to their high specific surface area and biocompatibility. In this work, the copolymer, poly(4-vinylpyridine-co-2-hydroxyethyl methacrylate) was applied for the surface functionalization of NDs to produce the quaternized poly(4-vinylpyridine-co-2-hydroxyethyl methacrylate)-functionalized NDs (QNDs). Then, QNDs were used as a substrate for silver nanoparticles (AgNPs) to produce a QND@Ag hybrid. The composition and morphology of the resultant nanostructures were confirmed by Fourier transform infrared spectra (FT-IR), transmission electron microscope (TEM), X-ray diffraction (XRD), and thermogravimetric analysis (TGA). The mass fraction of AgNPs in the nanocomposites was about 35.7%. The antibacterial performances of the prepared nanocomposites were evaluated with Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus by minimum inhibitory concentration (MIC), inhibition zone testing and time-kill study. As a result, due to the synergistic antibacterial activity of QND and AgNPs, this hybrid showed substantially higher antibacterial activity than QND and polyvinyl pyrrolidone (PVP)-stabilized AgNPs, and the AgNPs on QND@Ag were more stable than the Ag NPs on PVP, resulting in long-term antibacterial effects. More importantly, this hybrid showed excellent water solubility and low cytotoxicity, suggesting the great potential application in biomedical applications. The present work provided a simple strategy that successfully turned NDs into nanosized antibiotics with simultaneous superior stability and biocompatibility, which would broaden the applications of NDs and advance the development of novel antibacterial agents.

Keywords: cationic copolymer, nanodiamonds, silver nanoparticles, dual antibacterial activity, lower cytotoxicity

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3249 Design and Analysis of Flexible Slider Crank Mechanism

Authors: Thanh-Phong Dao, Shyh-Chour Huang

Abstract:

This study presents the optimal design and formulation of a kinematic model of a flexible slider crank mechanism. The objective of the proposed innovative design is to take extra advantage of the compliant mechanism and maximize the fatigue life by applying the Taguchi method. A formulated kinematic model is developed using a Pseudo-Rigid-Body Model (PRBM). By means of mathematic models, the kinematic behaviors of the flexible slider crank mechanism are captured using MATLAB software. Finite Element Analysis (FEA) is used to show the stress distribution. The results show that the optimal shape of the flexible hinge includes a force of 8.5N, a width of 9mm and a thickness of 1.1mm. Analysis of variance shows that the thickness of the proposed hinge is the most significant parameter, with an F test of 15.5. Finally, a prototype is manufactured to prepare for testing the kinematic and dynamic behaviors.

Keywords: kinematic behavior, fatigue life, pseudo-rigid-body model, flexible slider crank mechanism

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3248 Anthocyanin Complex: Characterization and Cytotoxicity Studies

Authors: Sucharat Limsitthichaikoon, Kedsarin Saodaeng, Aroonsri Priprem, Teerasak Damrongrungruang

Abstract:

Complexation of anthocyanins to mimic natural copigmentation process was investigated. Cyanidin-rich extracts from Zea mays L. CeritinaKulesh. anddelphinidin-rich extracts from ClitoriaternateaL. were used to form 4 anthocyanin complexes, AC1, AC2, AC3, and AC4, in the presence of several polyphenols and a trace metal. Characterizations of the ACs were conducted by UV, FTIR, DSC/TGA and morphological observations. Bathochromic shifts of the UV spectra of 4 formulas of ACs were observed at peak wavelengths of about 510-620 nm by 10 nm suggesting complex formation.FTIR spectra of the ACs indicate shifts of peaks from 1,733 cm-1 to 1,696 cm-1 indicating interactions and a decrease in the peak areas within the wavenumber of 3,400-3,500 cm-1 indicating changes in hydrogen bonding.Thermal analysis of all of the ACs suggests increases in melting temperature after complexation. AC with the highest melting temperature was morphologically observed by SEM and TEM to be crystal-like particles within a range of 50 to 200 nm. Particle size analysis of the AC by laser diffraction gave a range of 50-600 nm, indicating aggregation. This AC was shown to have no cytotoxic effect on cultured HGEPp0.5 and HGF (all p> 0.05) by MTT. Therefore, complexation of anthocyanins was simple and self-assembly process, potentially resulting in nanosized particles of anthocyanin complex.

Keywords: anthocyanins, complexation, purple corn cops, butterfly pea, physicochemical characteristics, cytotoxicity

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3247 Synergistic Cytotoxicity of Cisplatin and Taxol in Overcoming Taxol Resistance through the Inhibition of LDHA in Oral Squamous Cell Carcinoma

Authors: Lin Feng, Ling-Ling E., Hong-Chen Liu

Abstract:

The development of chemoresistance in patients represents a major challenge in cancer treatment. Lactate dehydrogenase‑A (LDHA) is one of the principle isoforms of LDH that is expressed in breast tissue, controlling the conversion of pyruvate to lactate and also playing a significant role in the metabolism of glucose. The aim of this study was to identify whether LDHA was involved in oral cancer cell resistance to Taxol and whether the downregulation of LDHA, as a result of cisplatin treatment, may overcome Taxol resistance in human oral squamous cells. The OECM‑1 oral epidermal carcinoma cell line was used, which has been widely used as a model of oral cancer in previous studies. The role of LDHA in Taxol and cisplatin resistance was investigated and the synergistic cytotoxicity of cisplatin and/or Taxol in oral squamous cells was analyzed. Cell viability was analyzed by MTT assay, LDHA expression was analyzed by western blot analysis and siRNA transfection was performed to knock down LDHA expression. The present study results showed that decreased levels of LDHA were responsible for the resistance of oral cancer cells to cisplatin (CDDP). CDDP treatments downregulated LDHA expression and lower levels of LDHA were detected in the CDDP‑resistant oral cancer cells compared with the CDDP‑sensitive cells. By contrast, the Taxol‑resistant cancer cells showed elevated LDHA expression levels. In addition, small interfering RNA‑knockdown of LDHA sensitized the cells to Taxol but desensitized them to CDDP treatment while exogenous expression of LDHA sensitized the cells to CDDP, but desensitized them to Taxol. The present study also revealed the synergistic cytotoxicity of CDDP and Taxol for killing oral cancer cells through the inhibition of LDHA. This study highlights LDHA as a novel therapeutic target for overcoming Taxol resistance in oral cancer patients using the combined treatments of Taxol and CDDP.

Keywords: cisplatin, Taxol, carcinoma, oral squamous cells

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3246 Cytotoxicity of a Short Chain Fatty Acid Histone Deactylase Inhibitor on HCT116 Human Colorectal Carcinoma Cell Line

Authors: N. A. Kazemi Sefat, M. M. Mohammadi, J. Hadjati, S. Talebi, M. Ajami, H. Daneshvar

Abstract:

Colorectal cancer metastases result in a significant number of cancer related deaths. Histone deacetylase (HDAC) inhibitors induce growth arrest and apoptosis in a variety of human cancer cells. Sodium butyrate (SB) is a short chain fatty acid, belongs to HDAC inhibitors which is released in the colonic lumen as a consequence of fiber fermentation. In this study, we are about to assess the effect of sodium butyrate on HCT116 human colorectal carcinoma cell line. The viability of cells was measured by microscopic morphologic study and MTT assay. After 48 hours, treatments more than 10 mM lead to cell injury in HCT116 by increasing cell granulation and decreasing cell adhesion (p>0.05). After 72 hours, treatments at 10 mM and more lead to significant cell injury (p<0.05). Our results may suggest that the gene expression which is contributed in cell proliferation and apoptosis has been changed under pressure of HDAC inhibition.

Keywords: colorectal cancer, sodium butyrate, cytotoxicity, MTT

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3245 Rauvolfine B Isolated from the Bark of Rauvolfia reflexa (Apocynaceae) Induces Apoptosis through Activation of Caspase-9 Coupled with S Phase Cell Cycle Arrest

Authors: Mehran Fadaeinasab, Hamed Karimian, Najihah Mohd Hashim, Hapipah Mohd Ali

Abstract:

In this study, three indole alkaloids namely; rauvolfine B, macusine B, and isoreserpiline have been isolated from the dichloromethane crude extract of Rauvolfia reflexa bark (Apocynaceae). The structural elucidation of the isolated compounds has been performed using spectral methods such as UV, IR, MS, 1D, and 2D NMR. Rauvolfine B showed anti proliferation activity on HCT-116 cancer cell line, its cytotoxicity induction was observed using MTT assay in eight different cell lines. Annexin-V is serving as a marker for apoptotic cells and the Annexin-V-FITC assay was carried out to observe the detection of cell-surface Phosphatidylserine (PS). Apoptosis was confirmed by using caspase-8 and -9 assays. Cell cycle arrest was also investigated using flowcytometric analysis. rauvolfine B had exhibited significantly higher cytotoxicity against HCT-116 cell line. The treatment significantly arrested HCT-116 cells in the S phase. Together, the results presented in this study demonstrated that rauvolfine B inhibited the proliferation of HCT-116 cells and programmed cell death followed by cell cycle arrest.

Keywords: apocynacea, indole alkaloid, apoptosis, cell cycle arrest

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3244 Effects of Manufacture and Assembly Errors on the Output Error of Globoidal Cam Mechanisms

Authors: Shuting Ji, Yueming Zhang, Jing Zhao

Abstract:

The output error of the globoidal cam mechanism can be considered as a relevant indicator of mechanism performance, because it determines kinematic and dynamical behavior of mechanical transmission. Based on the differential geometry and the rigid body transformations, the mathematical model of surface geometry of the globoidal cam is established. Then we present the analytical expression of the output error (including the transmission error and the displacement error along the output axis) by considering different manufacture and assembly errors. The effects of the center distance error, the perpendicular error between input and output axes and the rotational angle error of the globoidal cam on the output error are systematically analyzed. A globoidal cam mechanism which is widely used in automatic tool changer of CNC machines is applied for illustration. Our results show that the perpendicular error and the rotational angle error have little effects on the transmission error but have great effects on the displacement error along the output axis. This study plays an important role in the design, manufacture and assembly of the globoidal cam mechanism.

Keywords: globoidal cam mechanism, manufacture error, transmission error, automatic tool changer

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3243 Development of a Harvest Mechanism for the Kahramanmaraş Chili Pepper

Authors: O. E. Akay, E. Güzel, M. T. Özcan

Abstract:

The pepper has quite a rich variety. The development of a single harvesting machine for all kinds of peppers is a difficult research topic. By development of harvesting mechanisms, we could be able to facilitate the pepper harvesting problems. In this study, an experimental harvesting machine was designed for chili pepper. Four-bar mechanism was used for the design of the prototype harvesting machine. At the result of harvest trials, 80% of peppers were harvested and 8% foreign materials were collected. These results have provided some tips on how to apply to large-scale pepper Four-bar mechanism of the harvest machine.

Keywords: kinematic simulation, four bar linkage, harvest mechanization, pepper harvest

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3242 Mechanism of Changing a Product Concept

Authors: Kiyohiro Yamazaki

Abstract:

The purpose of this paper is to examine the hypothesis explaining the mechanism in the case, where the product is deleted or reduced the fundamental function of the product through the product concept changes in the digital camera industry. This paper points out not owning the fundamental technology might cause the change of the product concept. Casio could create new competitive factor so that this paper discusses a possibility of the mechanism of changing the product concept.

Keywords: firm without fundamental technology, product development, product concept, digital camera industry, Casio

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3241 Explicable Enzymatic Mechanism of H-Ido to Oxidise Tryptophan by Employing Various Substrates

Authors: Ali Bahri Lubis

Abstract:

The study of dioxygenase enzymatic mechanism on tryptophan oxidation has been a wide interest since the reaction is rate-limiting step of kynurenine pathway. In this research, observation of tryptophan oxidation through h-IDO enzyme along with synthesis of enzyme products was conducted in order to comprehend how the enzyme works on distinct substrates. UV-vis spectrophotometry, LC-MS, H-NMR and HSQC measurement were carried out to characterise enzyme product. It is found that while tryptophan was oxidised to form Nformylkynurenine (NFK) as a major product and hydroxypyrroloindole amine carboxylic acid (HPIC) in cis and trans confirmed in HSQC, N-methyl tryptophan substrate was converted to NFK and trans HPIC only. Other intriguing results showed that 5-hydroxy- tryptophan and Stryptophan was degraded to become NFK and epoxide cyclic respectively. The formation of NFK was considered through dioxygenation pathway, however HPIC was formed via monooxygenation. The epoxide cyclic—considered as intermediate compound in the mechanism— from S-tryptophan was not able to cleave the epoxide ring since bond energy of epoxide was probably much stronger. This validates the enzymatic mechanism where the intermediate compound in the enzymatic mechanism is epoxide cyclic.

Keywords: tryptophan oxidation, heme-dioxygenases, N-formylkynurenine, hydroxypyrrroloindoleamine, monooxidation

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3240 A Workable Mechanism to Support Students Who Are at Risk

Authors: Mohamed Chabi

Abstract:

The project of helping students at risk started at the Math department in the new foundation program at Qatar University in the fall 2012 semester. The purpose was to find ways to help students who were struggling with their math courses Elementary algebra or Precalculus course due to many factors. Department had formed the Committee “students at Risk” at the start of 12-13 to assist struggling students in our math courses to get their studies on track. A mechanism was developed to support students who are at risk using a developed E-Monitoring system. E-Monitoring system was developed to manage automatically all transactions relevant to the students’ attendance, Students ‘‘warning Students’’ grading, etc. E-Monitoring System produce various statistics such as, Overall course statistics, Performance, Students at Risk… to help department to develop a higher quality of education in the Foundation Program at Math department. The mechanism was studies and evaluated. Whatever the cause, the sooner we identify students who are not performing well academically, the sooner we can provide, or direct them to the resources that are available to them. In this paper, we outline the mechanism and its effect on students’ performance. The collected data from various exams shows that students had benefited from the mechanism.

Keywords: students at risk, e-monitoring system, warning students, performance

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3239 Synthesis, Characterization, and Biological Evaluation of 1,3,4-Mercaptooxadiazole Ether Derivatives Analogs as Antioxidant, Cytotoxic, and Molecular Docking Studies

Authors: Desta Gebretekle Shiferaw, Balakrishna Kalluraya

Abstract:

Oxadiazoles and their derivatives with thioether functionalities represent a new and exciting class of physiologically active heterocyclic compounds. Several molecules with these moieties play a vital role in pharmaceuticals because of their diverse biological activities. This paper describes a new class of 1,3,4- oxadiazole-2-thioethers with acetophenone, coumarin, and N-phenyl acetamide residues (S-alkylation), with the hope that the addition of various biologically active molecules will have a synergistic effect on anticancer activity. The structure of the synthesized title compounds was determined by the combined methods of IR, proton-NMR, carbon-13-NMR, and mass spectrometry. Further, all the newly prepared molecules were assessed against their antioxidant activity. Furthermore, four compounds were assessed for their molecular docking interactions and cytotoxicity activity. The synthesized derivatives have shown moderate antioxidant activity compared to the standard BHA. The IC50 of the tilted molecules (11b, 11c, 13b, and 14b) observed for in vitro anti-cancer activities were 11.20, 15.73, 59.61, and 27.66 g/ml at 72-hour treatment time against the A549 cell lines, respectively. The tested compounds' biological evaluation showed that 11b is the most effective molecule in the series.

Keywords: antioxidant activity, cytotoxicity activity, molecular docking, 1, 3, 4-Oxadiazole-2 thioether derivatives

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3238 In vitro Cytotoxic and Genotoxic Effects of Arsenic Trioxide on Human Keratinocytes

Authors: H. Bouaziz, M. Sefi, J. de Lapuente, M. Borras, N. Zeghal

Abstract:

Although arsenic trioxide has been the subject of toxicological research, in vitro cytotoxicity and genotoxicity studies using relevant cell models and uniform methodology are not well elucidated. Hence, the aim of the present study was to evaluate the cytotoxicity and genotoxicity induced by arsenic trioxide in human keratinocytes (HaCaT) using the MTT [3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] and alkaline single cell gel electrophoresis (Comet) assays, respectively. Human keratinocytes were treated with different doses of arsenic trioxide for 4 h prior to cytogenetic assessment. Data obtained from the MTT assay indicated that arsenic trioxide significantly reduced the viability of HaCaT cells in a dose-dependent manner, showing a IC50 value of 34.18 ± 0.6 µM. Data generated from the comet assay also indicated a significant dose-dependent increase in DNA damage in HaCaT cells associated with arsenic trioxide exposure. We observed a significant increase in comet tail length and tail moment, showing an evidence of arsenic trioxide -induced genotoxic damage in HaCaT cells. This study confirms that the comet assay is a sensitive and effective method to detect DNA damage caused by arsenic.

Keywords: arsenic trioxide, cytotoxixity, genotoxicity, HaCaT

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3237 Antibacterial and Cytotoxicity Activity of Cinchona Alkaloids

Authors: Alma Ramić, Mirjana Skočibušić, Renata Odžak, Tomica Hrenar, Ines Primožič

Abstract:

In an attempt to identify a new class of antimicrobial agents, the antimicrobial potential of Cinchona alkaloid derivatives was evaluated. The bark of the Cinchona trees is the source of a variety of alkaloids, among which the best known are quinine, quinidine, cinchonine and cinchonidine. They are very useful as organocatalysts in stereoselective synthesis. On the other hand, quinine is traditionally used in the treatment of malaria. Furthermore, Cinchona alkaloids possess various analgesic, anti-inflammatory and anti–arrhythmic properties as well. In this work we present the synthesis of twenty quaternary derivatives of pseudo−enantiomeric Cinchona alkaloid derivatives to evaluate their antibacterial activity. Quaternization of quinuclidine moiety was carried out with groups diverse in their size. The structures of compounds were systematically modified to obtain drug-like properties with proper physical and chemical properties and avoiding toxophore. All compounds were prepared in good yields and were characterized by standard analytical spectroscopy methods (1D and 2D NMR, IR, MS). The antibacterial activities of all compounds were evaluated against series of recent clinical isolates of antibiotic susceptible Gram-positive and resistant Gram-negative pathogens by determining their zone of inhibition and minimum inhibitory concentrations. All compounds showed good to strong broad-spectrum activity, equivalent or better in comparison with standard antibiotics used. Furthermore, seven compounds exhibited significant antibacterial efficiency against Gram-negative isolates. To visualize the results, principal component analysis was used as an additional classification tool. Cytotoxicity of compounds with different cell lines in human cell culture was determined. Based on these results, substituted quaternary Cinchona scaffold can be considered as promising new class of antimicrobials and further investigations should be performed. Supported by Croatian Science Foundation, Project No 3775 ADESIRE.

Keywords: antibacterial efficiency, cinchona alkaloids, cytotoxicity, pseudo‐enantiomers

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3236 Structured Access Control Mechanism for Mesh-based P2P Live Streaming Systems

Authors: Chuan-Ching Sue, Kai-Chun Chuang

Abstract:

Peer-to-Peer (P2P) live streaming systems still suffer a challenge when thousands of new peers want to join into the system in a short time, called flash crowd, and most of new peers suffer long start-up delay. Recent studies have proposed a slot-based user access control mechanism, which periodically determines a certain number of new peers to enter the system, and a user batch join mechanism, which divides new peers into several tree structures with fixed tree size. However, the slot-based user access control mechanism is difficult for accurately determining the optimal time slot length, and the user batch join mechanism is hard for determining the optimal tree size. In this paper, we propose a structured access control (SAC) mechanism, which constructs new peers to a multi-layer mesh structure. The SAC mechanism constructs new peer connections layer by layer to replace periodical access control, and determines the number of peers in each layer according to the system’s remaining upload bandwidth and average video rate. Furthermore, we propose an analytical model to represent the behavior of the system growth if the system can utilize the upload bandwidth efficiently. The analytical result has shown the similar trend in system growth as the SAC mechanism. Additionally, the extensive simulation is conducted to show the SAC mechanism outperforms two previously proposed methods in terms of system growth and start-up delay.

Keywords: peer-to-peer, live video streaming system, flash crowd, start-up delay, access control

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3235 Inhibition and Breaking of Advanced Glycation End Products with Nuts and Polyphenols

Authors: Moon Ho Do, Sin-Hee Park, Jae Hyuk Lee, Kyo Hee Cho, Jae Kyung Chae, Sun Yeou Kim

Abstract:

Long-term hyperglycemic conditions associated with diabetes lead to the formation of advanced glycation end-products (AGEs). Highly reactive glucose metabolites, methylglyoxal (MGO) and glyoxal (GO), induced carbonyl stress and it may induce cellular damage, cross-linking of proteins, and glycation, playing an important role in the impairment of kidney function. Small molecules that have the ability to inhibit AGE formation, and even break preformed AGEs have a beneficial impact on metabolic syndrome, diabetes, and cancer. We quantified contents of polyphenols in nuts and investigated the protective effect of nuts and polyphenols on MGO-induced cytotoxicity in porcine kidney epithelial cells (LLC-PK1). Moreover, we evaluated the inhibitory effect of AGEs formation in the presence of MGO or GO and possess the ability to break preformed AGEs. In this study, we confirmed twenty polyphenols in diverse nuts using LC-MS/MS system. Nuts and polyphenols play a protective role in LLC-PK1 cells by reducing MGO-induced cytotoxicity. They could also prevent the formation of MGO or GO-mediated AGEs and Break AGEs crosslink. It can be surmised that increased consumption of nuts would be an effective means of preventing diabetic diseases.

Keywords: advanced glycation end products, LLC-PK1, methylglyoxal, nut, polyphenol

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3234 Configuration Design and Optimization of the Movable Leg-Foot Lunar Soft-Landing Device

Authors: Shan Jia, Jinbao Chen, Jinhua Zhou, Jiacheng Qian

Abstract:

Lunar exploration is a necessary foundation for deep-space exploration. For the functional limitations of the fixed landers which are widely used currently and are to expand the detection range by the use of wheeled rovers with unavoidable path-repeatability, a movable lunar soft-landing device based on cantilever type buffer mechanism and leg-foot type walking mechanism is presented. Firstly, a 20 DoFs quadruped configuration based on pushrod is proposed. The configuration is of the bionic characteristics such as hip, knee and ankle joints, and can make the kinematics of the whole mechanism unchanged before and after buffering. Secondly, the multi-function main/auxiliary buffers based on crumple-energy absorption and screw-nut mechanism, as well as the telescopic device which could be used to protect the plantar force sensors during the buffer process are designed. Finally, the kinematic model of the whole mechanism is established, and the configuration optimization of the whole mechanism is completed based on the performance requirements of slope adaptation and obstacle crossing. This research can provide a technical solution integrating soft-landing, large-scale inspection and material-transfer for future lunar exploration and even mars exploration, and can also serve as the technical basis for developing the reusable landers.

Keywords: configuration design, lunar soft-landing device, movable, optimization

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3233 Idea Expropriation, Incentives, and Governance within Organizations

Authors: Gulseren Mutlu, Gurupdesh Pandher

Abstract:

This paper studies the strategic interplay between innovation, incentives, expropriation threat and disputes arising from expropriation from an intra-organization perspective. We present a simple principal-agent model with hidden actions and hidden information in which two employees can choose how much (innovative) effort to exert, whether to expropriate the innovation of the other employee and whether to dispute if innovation is expropriated. The organization maximizes its expected payoff by choosing the optimal reward scheme for both employees as well as whether to encourage or discourage disputes. We analyze two mechanisms under which innovative ideas are not expropriated. First, we show that under a non-contestable mechanism (in which the organization discourages disputes among employees), the organization has to offer a “rent” to the potential expropriator. However, under a contestable mechanism (in which the organization encourages disputes), there is no need for such rent. If the cost of resolving the dispute is negligible, the organization’s expected payoff is higher under a contestable mechanism. Second, we develop a comparable team mechanism in which innovation takes place as a result of the joint efforts of employees and innovation payments are made based on the team outcome. We show that if the innovation value is low and employees have similar productivity, then the organization is better off under a contestable mechanism. On the other hand, if the innovation value is high, the organization is better off under a team mechanism. Our results have important practical implications for the design of innovation reward system for employees, hiring policy and governance for different companies.

Keywords: innovation, incentives, expropriation threat, dispute resolution

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3232 Soot Formation in the Field of Combustion

Authors: Nacira Mecheri, N. Boussid

Abstract:

A new chemical mechanism designed to study the process of forming the first aromatic ring (benzene) and polycyclic aromatic hydrocarbons (PAH) from a flame of acetylene (C2H2) has been developed. The mechanism developed, contains 50 chemical species involved in 268 reversible elementary reactions. The comparison between the results from modelling and experimental measurements allowed us to test the validity of the postulated mechanism in specific experimental conditions. Kinetic analysis of the flame by calculating the maximum rates for each elementary reaction, allowed us to identify key reactions pathways of consumption and formation of main precursors of soot.

Keywords: benzene, PAH, acetylene, modeling, flame, soot

Procedia PDF Downloads 310