Development of Potent Adenosine Monophosphate Activated Protein Kinase (AMPK) Activators

Previously, we reported the identification of a thiazolidinedione‐based adenosine monophosphate activated protein kinase (AMPK) activator, compound 1 (N‐[4‐({3‐[(1‐methylcyclohexyl)methyl]‐2,4‐dioxothiazolidin‐5‐ylidene}methyl)phenyl]‐4‐nitro‐3‐(trifluoromethyl)benzenesulfonamide), which provided a proof of concept to delineate the intricate role of AMPK in regulating oncogenic signaling pathways associated with cell proliferation and epithelial–mesenchymal transition (EMT) in cancer cells. In this study, we used 1 as a scaffold to conduct lead optimization, which generated a series of derivatives. Analysis of the antiproliferative and AMPK‐activating activities of individual derivatives revealed a distinct structure–activity relationship and identified 59 (N‐(3‐nitrophenyl)‐N′‐{4‐[(3‐{[3,5‐bis(trifluoromethyl)phenyl]methyl}‐2,4‐dioxothiazolidin‐5‐ylidene)methyl]phenyl}urea) as the optimal agent. Relative to 1 , compound 59 exhibits multifold higher potency in upregulating AMPK phosphorylation in various cell lines irrespective of their liver kinase B1 (LKB1) functional status, accompanied by parallel changes in the phosphorylation/expression levels of p70S6K, Akt, Foxo3a, and EMT‐associated markers. Consistent with its predicted activity against tumors with activated Akt status, orally administered 59 was efficacious in suppressing the growth of phosphatase and tensin homologue (PTEN)‐null PC‐3 xenograft tumors in nude mice. Together, these findings suggest that 59 has clinical value in therapeutic strategies for PTEN‐negative cancer and warrants continued investigation in this regard.     

An intelligent skin‐color capture method based on fuzzy C‐means with applications

Consumer behavior is complicated. In the cosmetic market, personal intuition and fashion trends for color selection are guidelines for consumers. A systematic method for female facial skin‐color classification and an application in the makeup market are proposed in this study. In this article, face recognition with a large number of images is first discussed. Then, an innovative method to capture color at selected points is presented and complexion‐aggregated analysis is performed. This innovative method is an extension of face‐recognition theory. Images in RGB format are converted to CIELAB format during data collection and then Fuzzy C‐means theory is used to cluster and group the data. The results are classified and grouped in Lab value and RGB index. Two programs are created. The first program, “FaceRGB,” captures color automatically from images. The second program, “ColorFCM,” clusters and groups the skin‐color information. The results can be used to assist an expert system in the selection of customized colors during makeup and new‐product development.     

A consultation and simulation system for product color planning based on interactive genetic algorithms

In the early stage of a design process, it is important to create numerous and varied possible color plans for the target consumer group. These color plans help individual designers quickly find a few good color design schemes and give the design team ideas for brainstorming. The color plan of a product consists of the color combinations of its components and decorative patterns, which strongly influence the feelings of customers and thus their desire to purchase. However, very few studies have discussed these issues. In this study, a consultation and simulation system for product color planning that helps designers obtain the optimal color planning for components and decorative patterns of a product is proposed. This system includes two parts: one uses the interactive genetic algorithm to establish a creative evolutionary system that can interact with a designer to explore novel design schemes; the other extends the boundary extract algorithm to establish a color simulation system that can apply colors to the areas of product components and decorative patterns for color simulation. Finally, a case study of color planning for a motorcycle model is used to verify the feasibility of the proposed system. © 2012 Wiley Periodicals, Inc. Col Res Appl, 38, 375–390, 2013     

Experimental improvement of preparation of acrylic acid‐modified middle deacetylated chitosan and its application in absorbing paraquat

Chitosan with 45% deacetylation (CS45) grafted poly (acrylic acid) (CS45‐g‐PAA) was synthesized and characterized as an adsorbent of paraquat. CS45‐g‐PAA copolymers were prepared using H₂O_2(aq) as an initiator and NH₄OH_(aq) as a promoter. The highest grafting percentage of 44.2% was obtained using the traditional kinetic method. However, a maximum grafting percentage of 52.6% was calculated for the central composite design (CCD). Experimental results based on the reaction conditions that were predicted from the CCD are consistent with theoretical calculations. The grafted copolymer was characterized by FTIR, BET, and SEM. A representative CS45‐g‐PAA copolymer was hydrolyzed to a salt type (CS45‐g‐PANa) and used in the adsorption of paraquat. The adsorption equilibrium data correlate more closely with the Langmuir isotherm than with the Freundlich equation. The maximum adsorption capacity of CS45‐g‐PANa is 396.7 mg/g‐adsorbent. This value clearly exceeds that of Fuller's earth and the activated carbon which is the most commonly used binding agent for paraquat. POLYM. ENG. SCI., 2013. © 2012 Society of Plastics Engineers     

Thermophoresis of Liquid Airborne Particles in Gravity at Continuum Regime

An analytical study is presented for the thermophoretic motion of an aerosol droplet in a prescribed temperature gradient under the influence of gravity. The Peclet and Reynolds numbers are assumed small, so that the temperature distributions are governed by the Laplace equation and the flow fields are governed by the Stokes equation. The temperature discontinuity, thermal creep, and hydrodynamic slip features that occurred at the droplet surface are considered. The slow motion of a liquid aerosol sphere subject to the combination of thermophoresis and sedimentation is obtained by superposition of the individual solutions for pure thermophoresis and pure body-force-driven motion, since both the governing equations and boundary conditions in this problem are linear. The stream functions of the internal and external flows, which are displayed in both the laboratory frame and a reference frame moving with the droplet, as well as the migrating velocity of a droplet, are formulated generally. The flow structures manifest more remarkable topologies than do those of common intuition developed from sedimentation. Our results can be simplified to the corresponding motion for solid aerosol particles.     

Compression molding of biodegradable drug‐eluting implants for sustained release of metronidazole and doxycycline

The purpose of this report was to develop solvent‐free biodegradable drug‐eluting implants that provide sustained release of metronidazole and doxycycline. The drug‐eluting implants were prepared using the compression molding technique. To fabricate the implants, polylactide‐polyglycolide copolymers were premixed with metronidazole or doxycycline. The mixture was then compression molded and sintered to form implants of various sizes and geometries. An elution method and an HPLC assay were used to characterize the in vitro release rates of the antibiotics over a 28‐day period. A bacterial inhibition test was also carried out to determine the bioactivity of released antibiotics. The concentrations of both metronidazole and doxycycline were much greater than the minimum inhibitory concentration of Escherichia coli for up to 3 and 4 weeks, respectively, and the bioactivities of the antibiotics remained high after the fabrication process. Furthermore, the initial burst could be minimized and the release rate could be reduced by increasing the size of the implants and by adopting low drug to polymer ratios. By using this compression molding technique and appropriate processing parameters, we will be able to fabricate biodegradable implants of various types of antibacterial drugs for long‐term local deliveries. Eventually, biodegradable drug‐eluting implants may be used to treat various periodontal diseases. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2013     

Equilibrium and kinetic studies of the extraction of chelated copper(II) anions with Aliquat 336

The equilibrium and kinetics of solvent extraction of Cu²⁺ from aqueous solutions containing equimolar EDTA with Aliquat 336 in n‐decanol and kerosene at 298 K were investigated. The concentrations of Cu²⁺ (8–50 mol m^?3), Cl^? (5–60 mol m^?3), and Aliquat 336 (20–100 mol m^?3) were varied. A semi‐empirical model with three parameters was proposed to describe the equilibrium behavior, in which the non‐idealities in both aqueous and organic phases were considered. Over the ranges studied, the model agreed reasonably well with the experimental data (standard deviation, 15%). The forward and backward reaction rate constants were determined as (5.31 ± 0.16)×10^?6 m^9/4 mol^?3/4 s^?1 and (2.62 ± 0.09)×10^?7 s^?1, respectively, at 298 K. An interfacial reaction mechanism was proposed, which revealed that the reaction between the chelated anions and trimeric amine molecules at the interface was rate limiting. The derived rate laws were consistent with the experimental results. © 2002 Society of Chemical Industry     

Effects of molecular weight and molecular structure of low profile additives on the properties of bulk molding compound (BMC)

The effects of molecular weight and molecular structure of styrene(St)‐based and vinyl acetate(VAc)‐based low‐profile additive (LPA) on the curing kinetics and compatibility of unsaturated polyester (UP)/LPA system and linear shrinkage, water absorption rate, surface gloss and pigmentability of bulk molding compound (BMC) were investigated. Results show that the curing reaction rate decreases with an increase of the molecular weight of LPA due to the chain entanglement effect. The plasticizing effect of LPA on the (UP) network was reduced with an increase of the molecular weight of LPA. Water absorption of BMC increases as the molecular weight of LPA increases, implying that more microvoids were formed inside the BMC, resulting a lower linear shrinkage rate, and worse pigmentability. However, good shrinkage control LPA does not necessarily lead to a smoother surface and better surface gloss. Furthermore, modified LPAs possess better compatibility with UP, the final curing conversion of UP is elevated, and both better shrinkage control and surface properties are also observed.     

Water‐assisted injection molding of thermoplastic materials: Effects of processing parameters

The objective of this study was to experimentally investigate the effects of various processing parameters on the water‐assisted injection molding of thermoplastic materials. Experiments were carried out on a lab‐developed water‐assisted injection molding system, which included a water pump, a water injection pin, a water tank equipped with a temperature regulator, and a control circuit. Two types of water injection pins designs were proposed to mold the parts. After molding, the lengths of water penetration in molded parts were measured. The effects of different processing parameters on the lengths of water penetration were determined. It was found that the shrinkage rate and the viscosity of the polymeric materials, and the void shapes of the hollowed cores mainly determined the water‐penetration lengths in molded products. In addition, a comparison has been made between the parts molded by water assisted injection molding and gas‐assisted injection molding. It was found that water‐assisted injection molded parts exhibit less uniform void sizes along the water channel. The cycle time for water‐assisted injection molded parts was shorter than that of conventional injection molded parts and gas‐assisted injection molded parts.     

Short-range spin-phonon coupling in in-plane CuO nanowires: a low-temperature Raman investigation

We report an application of low-temperature Raman scattering on in-plane CuO nanowires, in which an overview of the characteristic parameter of spin-phonon coefficient, the interaction of incident light with the spin degrees of freedom, and size effects will be given. The appearance of spin-phonon coefficient decrease reflects the existence of finite size effect.