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151.
Synthetic and Biological Studies of Sesquiterpene Polygodial: Activity of 9‐Epipolygodial against Drug‐Resistant Cancer Cells
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Dr. Ramesh Dasari Annelise De Carvalho Derek C. Medellin Kelsey N. Middleton Dr. Frédéric Hague Marie N. M. Volmar Prof. Liliya V. Frolova Dr. Mateus F. Rossato Jorge J. De La Chapa Nicholas F. Dybdal‐Hargreaves Akshita Pillai Prof. Véronique Mathieu Prof. Snezna Rogelj Prof. Cara B. Gonzales Prof. João B. Calixto Prof. Antonio Evidente Dr. Mathieu Gautier Dr. Gnanasekar Munirathinam Prof. Rainer Glass Prof. Patricia Burth Dr. Stephen C. Pelly Prof. Willem A. L. van Otterlo Prof. Robert Kiss Prof. Alexander Kornienko 《ChemMedChem》2015,10(12):2014-2026
Polygodial, a terpenoid dialdehyde isolated from Polygonum hydropiper L., is a known agonist of the transient receptor potential vanilloid 1 (TRPV1). In this investigation a series of polygodial analogues were prepared and investigated for TRPV1‐agonist and anticancer activities. These experiments led to the identification of 9‐epipolygodial, which has antiproliferative potency significantly exceeding that of polygodial. 9‐Epipolygodial was found to maintain potency against apoptosis‐resistant cancer cells as well as those displaying the multidrug‐resistant (MDR) phenotype. In addition, the chemical feasibility for the previously proposed mechanism of action of polygodial, involving the formation of a Paal–Knorr pyrrole with a lysine residue on the target protein, was demonstrated by the synthesis of a stable polygodial pyrrole derivative. These studies reveal rich chemical and biological properties associated with polygodial and its direct derivatives. These compounds should inspire further work in this area aimed at the development of new pharmacological agents, or the exploration of novel mechanisms of covalent modification of biological molecules with natural products. 相似文献
152.
Chou Yong Tan Ramesh Singh Yee Ching Teh Yoke Meng Tan Boon Kar Yap 《International Journal of Applied Ceramic Technology》2015,12(2):437-442
In this work, the sinterability of forsterite powder synthesized via solid‐state reaction was investigated. X‐ray diffraction (XRD) analyses indicate that the synthesized powder possessed peaks that correspond to stoichiometric forsterite. Scanning electron micrographs revealed that the powders were formed agglomerates, which were made up of loosely packed fine particles. Subsequently, the forsterite powders were cold isostatically pressed into a disk shape under 200 MPa and sintered in air at temperature ranging from 1200°C to 1500°C (interval of 50°C) with ramp rate of 10°C/min and dwelling time of 2 h. The sinterability of each sintered samples was examined in terms of phase stability, relative density, Vickers hardness, fracture toughness, and microstructural examination. XRD examination on all the sintered samples exhibited pure forsterite, in which the generated peaks were found to be in a good agreement with JCPDS card no. 34‐0189. The densification of forsterite progressed to reach a maximum relative density of ~91% at 1500°C. This study also revealed that high‐strength forsterite ceramic can be synthesized via solid‐state reaction as forsterite attained favorable mechanical properties, having fracture toughness of 4.88 MPam1/2 and hardness of 7.11 GPa at 1400°C. 相似文献
153.
Plasticized poly(vinyl chloride)/poly(ethyl methacrylate) PVC/PEMA-based blend polymer electrolyte films containing lithium perchlorate (LiClO4) as a salt were prepared by solvent casting technique. The effects of the plasticization on structural, thermal and electrical properties of the plasticized polymer blend electrolytes were investigated. The changes in the structural and complex formation properties of the materials were studied by XRD and FTIR techniques. Dielectric relaxation studies of the polymer electrolyte have been undertaken, and the results are discussed. TG/DTA technique is used to study the thermal stability. Complex impedance analysis is used to calculate the bulk resistance of the complexes. The effect of different plasticizer on the structural and physical properties of polymer blend electrolyte is well correlated. 相似文献
154.
Raghavendra C. Mundargi Namdev B. Shelke V. Ramesh Babu Pradip Patel Vidhya Rangaswamy Tejraj M. Aminabhavi 《应用聚合物科学杂志》2010,116(3):1832-1841
Thermoresponsive microspheres of gellan gum‐poly(N‐isopropylacrylamide), i.e., GG‐P(NIPAAm) semi‐interpenetrating polymer networks (semi‐IPNs) have been prepared by ionic crosslinking and used to study the controlled release (CR) of atenolol (ATL), an antihypertensive drug. Interaction of the drug with polymers was studied by Fourier transform infrared (FTIR) spectroscopy. Differential scanning calorimetry (DSC) was used to confirm the polymorphism and molecular level dispersion of ATL. Scanning electron microscopy (SEM) indicated spherical nature and smooth surfaces of the microspheres with some debris attached on their surfaces. Mean particle size measured by laser light diffraction ranged between 34 and 76 μm. Equilibrium swelling performed at 25°C and 37°C in pH 7.4 phosphate buffer exhibited thermoresponsive nature of the polymers. In vitro drug release performed at 25°C and 37°C indicated temperature‐dependency of ATL release, which was extended up to 12 h. In vitro release profiles at both the temperatures confirmed thermoresponsive nature of the polymers giving pulsatile trends. The % cumulative release data have been fitted to an empirical equation to estimate transport parameters and to understand the nature of drug release. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010 相似文献
155.
Double gate FinFETs are shown to be better candidates for subthreshold logic design than equivalent bulk devices. However it is not so clear which configuration of DG FinFETs will be more optimal for subthreshold logic. In this paper, we compare the different device and circuit level performance metrics of DG FinFETs with symmetric, asymmetric, tied and independent gate options for subthreshold logic. We observe that energy delay product (EDP) shows a better subthreshold performance metric than power delay product (PDP) and it is observed that the tied gate symmetric option has ≈78% lower EDP value than that of independent gate option for subthreshold logic. The asymmetry in back gate oxide thickness adds to further reduction in EDP for tied gate and has no significant effect on independent gate option. The robustness (measured in terms of % variation in device/circuit performance metrics for a ±10% variation in design parameters) of DG FinFETs with various options has also been investigated in presence of different design parameter variations such as silicon body thickness, channel length, threshold voltage, supply voltage and temperature, etc. Independent gate option has been seen to be more robust (≈40% less) than that of tied gate option for subthreshold logic. Comparison of logic families for subthreshold regime with DG FinFET options shows that for tied gate option, sub-CMOS, sub-Domino and sub-DCVSL have almost similar and better energy consumption and robustness characteristics with respect to PVT variations than other families. 相似文献
156.
Prashant Singh Pradeep Kumar Anju Katyal Rashmi Kalra Sujata K. Dass Satya Prakash Ramesh Chandra 《Catalysis Letters》2010,134(3-4):303-308
In this present work, we report that phosphotungstic acid provides a simple, efficient and environmentally benign route is a two-component one-pot domino Knoevenagel-type condensation/Michael reaction between 4-coumarin derivative and an aldehyde in water as a solvent in shorter duration with high yields. 相似文献
157.
T. R. Vijaybabu T. Ramesh Suman Pandipati Sujit Mishra G Sridevi C Pradeep Raja Rhoda Afriyie Mensah Oisik Das Manjusri Misra Amar Mohanty Karthik Babu NB 《大分子材料与工程》2023,308(7):2300001
The lifespan and the performance of flexible electronic devices and components are affected by the large accumulation of heat, and this problem must be addressed by thermally conductive polymer composite films. Therefore, the need for the development of high thermal conductivity nanocomposites has a strong role in various applications. In this article, the effect of different particle reinforcements such as single and hybrid form, coated and uncoated particles, and chemically treated particles on the thermal conductivity of various polymers are reviewed and the mechanism behind the improvement of the required properties are discussed. Furthermore, the role of manufacturing processes such as injection molding, compression molding, and 3D printing techniques in the production of high thermal conductivity polymer composites is detailed. Finally, the potential for future research is discussed, which can help researchers to work on the thermal properties enhancement for polymeric materials. 相似文献
158.
Engineered features on pyrolytic carbon (PyC) have been demonstrated as an approach to improve the flow hemodynamics of the cardiovascular implants such as bileaflet mechanical heart valve. PyC also finds application in thermonuclear and missile components due to its unique directional thermal properties. However, very little work has been reported on modeling of machining/micromachining of PyC. Note that PyC is a brittle anisotropic material and its machining characteristics differ from plastically deformable isotropic materials. Consequently, this study is aimed at developing a finite element model to understand the mechanics of material removal in the plane of transverse isotropy (horizontally stacked laminae) of PyC. A damaged plasticity model has been used to capture the effect of material degradation under machining. Uniaxial tension/compression tests have been carried out to calibrate the damaged plasticity model. A cohesive element layer has been used between the chip layer and the bulk material to simulate the delamination/peeling effect. The model predicts cutting force and thrust forces at different set of process parameters. The orthogonal cutting model has been validated against the experimental data for different cutting conditions for cutting and thrust forces. In addition, the chip geometry has also been compared. The prediction error in the model lies between 9% and 27%. Parametric studies have also been performed to understand the effect of the machining parameters on the process response. It is found that use of the positive rake angle decreases the cutting forces up to 75%. 相似文献
159.
P. Srinivasa Revathy Baskaran M. Ramesh K. Harish Prashanth R. Tharanathan 《European Food Research and Technology》2002,215(6):504-508
The effect on the quality of mango fruits (Mangifera indica) during modified atmosphere packaging was investigated. The fruits were kept in carton boxes whose top surface was covered with either chitosan film or with low-density polyethylene (positive control) or kept as such (control) and stored at room temperature (27ǃ °C at 65% RH). The CO2 and O2 levels measured on day 3 were 23-26% and 3-6%, and at the end of the storage period they were 19-21% and 5-6%, respectively. Various quality parameters such as colour, chlorophyll, acidity, vitamin C, carotenoid and sugar contents were studied. The fruits stored as such had a shelf-life of 9ǃ days, whereas those stored in low-density polyethylene showed off-flavour due to fermentation and fungal growth on the stalk and around the fruits, and were partially spoiled. On the other hand, fruits stored in chitosan-covered boxes showed an extension of shelf-life of up to 18 days and without any microbial growth and off-flavour. Being biodegradable and ecofriendly, chitosan films are useful as an alternative to synthetic packaging films in the storage of freshly harvested mangoes. 相似文献
160.
The heat transfer effectiveness of nanofluids is adversely affected by the delay in convection onset. The lesser effectiveness, when compared to that of base fluid, is observed in a range of nanofluid layer thickness. The heat transfer coefficient of water–Al2O3 nanofluid can be enhanced by sustaining the equilibrium between Rayleigh number, temperature, particle volume fraction, and enclosure aspect ratio. In this paper, the specific correlation of fluid layer thickness and the onset of convection, which can significantly dominate the heat transfer characteristics of nanofluids are investigated using the concept of critical Rayleigh number. The water layer thickness for convection onset is first experimentally assessed for different real-life heat flux densities. It is then performed for Al2O3–water nanofluid for varying volume fractions. With the increase in volume fraction even though thermal conductivity increases, the overall heat transfer enhancement of the nanofluid is reduced. Temperature involved (heat flux density), the volume fraction of the nanofluid used, nanofluid layer thickness (space availability for the cooling system), and mass of the nanoparticle influence heat transfer enhancement. A higher volume fraction may not always result in enhancement of heat transfer as far as nanofluids are concerned. 相似文献