VI-116, A Novel Potent Inhibitor of VRAC with Minimal Effect on ANO1

Volume-regulated anion channel (VRAC) is ubiquitously expressed and plays a pivotal role in vertebrate cell volume regulation. A heterologous complex of leucine-rich repeat containing 8A (LRRC8A) and LRRC8B-E constitutes the VRAC, which is involved in various processes such as cell proliferation, migration, differentiation, intercellular communication, and apoptosis. However, the lack of a potent and selective inhibitor of VRAC limits VRAC-related physiological and pathophysiological studies, and most previous VRAC inhibitors strongly blocked the calcium-activated chloride channel, anoctamin 1 (ANO1). In the present study, we performed a cell-based screening for the identification of potent and selective VRAC inhibitors. Screening of 55,000 drug-like small-molecules and subsequent chemical modification revealed 3,3′-((2-hydroxy-3-methoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) (VI-116), a novel potent inhibitor of VRAC. VI-116 fully inhibited VRAC-mediated I⁻ quenching with an IC₅₀ of 1.27 ± 0.18 μM in LN215 cells and potently blocked endogenous VRAC activity in PC3, HT29 and HeLa cells in a dose-dependent manner. Notably, VI-116 had no effect on intracellular calcium signaling up to 10 μM, which completely inhibited VRAC, and showed high selectivity for VRAC compared to ANO1 and ANO2. However, DCPIB, a VRAC inhibitor, significantly affected ATP-induced increases in intracellular calcium levels and Eact-induced ANO1 activation. In addition, VI-116 showed minimal effect on hERG K⁺ channel activity up to 10 μM. These results indicate that VI-116 is a potent and selective VRAC inhibitor and a useful research tool for pharmacological dissection of VRAC.     

Red bean extract reduces inflammation and increases survival in a murine sepsis model

This study used in vitro and in vivo experimental models to investigate the anti-inflammatory potential of the butanol fraction of red bean ethanol extract (BF-RBEE), which contains the biologically active molecule catechin-7-β-d-glucopyranoside. Treatment with BF-RBEE inhibited nitric oxide production in lipopolysaccharide (LPS)-stimulated macrophages through suppression of extracellular signalregulated kinase and IκBα activation. In an in vivo murine sepsis model, oral administration of BF-RBEE improved mouse survival. Specifically, the survival rate of mice injected with LPS was 0 and 40% in ICR and BALB/c mice, respectively, whereas the survival of mice co-treated with BF-RBEE was 100% in both mouse types. This increase in survival with the BF-RBEE administration was correlated with decreased tumor-necrosis factor-α and interferon-γ and increased interleukin-10. Oral administration of BF-RBEE also inhibited total and ovalbumin-specific IgE production in experimental mice. These results suggest the possible usefulness of red beans in the treatment of inflammatory diseases.     

Efficiency improvement of polymer light-emitting diodes using a quantum dot interlayer between a hole transport layer and an emitting layer

The current efficiency of polymer light-emitting diodes (PLEDs) were improved using a quantum dot interlayer between a hole transport layer and an emitting layer. The quantum dot interlayer played a role of controlling the hole transport in the PLEDs and enhanced the charge balance in the emitting layer. The current efficiency of the PLEDs was increased by more than 20% by the quantum dot interlayer. In particular, the efficiency improvement was significant at high luminance due to reduced efficiency roll-off in the quantum dot-embedded PLEDs.     

Enhanced transformation of triclosan by laccase in the presence of redox mediators

Triclosan (TCS), an antimicrobial agent, is an emerging and persistent environmental pollutant that is often found as a contaminant in surface waters and sediments; hence, knowledge of its degradability is important. In this study we investigated laccase-mediated TCS transformation and detoxification, using laccase (from the fungus Ganoderma lucidum) in the presence and absence of redox mediators. Transformation products were identified using HPLC, ESI-MS and GC-MS, and transformation mechanisms were proposed. In the absence of redox mediator, 56.5% TCS removal was observed within 24 h, concomitant with formation of new products with molecular weights greater than that of TCS. These products were dimers and trimers of TCS, as confirmed by ESI-MS analysis. Among the various mediators tested, 1-hydroxybenzotriazole (HBT) and syringaldehyde (SYD) significantly enhanced TCS transformation (∼90%). The presence of these mediators resulted in products with lower molecular weights than TCS, including 2,4-dichlorophenol (2,4-DCP; confirmed by GC-MS) and dechlorinated forms of 2,4-DCP. When SYD was used as the mediator, dechlorination resulted in 2-chlorohydroquinone (2-CHQ). Bacterial growth inhibition studies revealed that laccase-mediated transformation of TCS effectively decreased its toxicity, with ultimate conversion to less toxic or nontoxic products. Our results confirmed the involvement of two mechanisms of laccase-catalyzed TCS removal: (i) oligomerization in the absence of redox mediators, and (ii) ether bond cleavage followed by dechlorination in the presence of redox mediators. These results suggest that laccase in combination with natural redox mediator systems may be a useful strategy for the detoxification and elimination of TCS from aqueous systems.     

Stretchable,Transparent Zinc Oxide Thin Film Transistors

Stretchable and transparent thin film transistors (TFTs) with intrisically brittle oxide semiconductors are built using a wavy structural configuration that can provide high flexibility and stretchability. After device fabrication procedures including high temperature annealing, the oxide semiconductor‐based TFT arrays can be transferred directly to plastic or rubber substrates, without an additional device process, using transfer printing methods. This procedure can avoid some of the thermal degradation problems associated with plastic or rubber substrates by separating them from the annealing procedure needed to improve the device performance. These design and fabrication methods offer the possibility of developing a new format of stretchable electronics.     

Photonic Crystal Palette of Binary Block Copolymer Blends for Full Visible Structural Color Encryption

Structural color (SC) arising from a periodically ordered self-assembled block copolymer (BCP) photonic crystal (PC) is useful for reflective-mode sensing displays owing to its capability of stimuli-responsive structure alteration. However, a set of PC inks, each providing a precisely addressable SC in the full visible range, has rarely been demonstrated. Here, a strategy for developing BCP PC inks with tunable structures is presented. This involves solution-blending of two lamellar-forming BCPs with different molecular weights. By controlling the mixing ratio of the two BCPs, a thin 1D BCP PC film is developed with alternating in-plane lamellae whose periodicity varies linearly from ≈46 to ≈91 nm. Subsequent preferential swelling of one-type lamellae with either solvent or non-volatile ionic liquid causes the photonic band gap of the films to red-shift, giving rise to full-visible-range SC correlated with the pristine nanostructures of the blended films in both liquid and solid states. The BCP PC palette of solution-blended binary solutions is conveniently employed in various coating processes, allowing facile development of BCP SC on the targeted surface. Furthermore, full-color SC paintings are realized with their transparent PC inks, facilitating low-power pattern encryption.     

A 10-bit 205-MS/s 1.0- mm2 90-nm CMOS Pipeline ADC for Flat Panel Display Applications

This paper describes a 10-bit 205-MS/s pipeline analog-to-digital converter (ADC) for flat panel display applications with the techniques to alleviate the design limitations in the deep-submicron CMOS process. The switched source follower combined with a resistor-switch ladder eliminates the sampling switches and achieves high linearity for a large single-ended input signal. Multistage amplifiers adopting the complementary common-source topology increase the output swing range with lower transconductance variation and reduce the power consumption. The supply voltage for the analog blocks is provided by the low drop-out regulator for a high power-supply rejection ratio (PSRR) under the noisy operation environment. The pipeline stages of the ADC are optimized in the aspect of power consumption through the iterated calculation of the sampling capacitance and transconductance. The ADC occupies an active area of 1.0 mm² in a 90-nm CMOS process and achieves a 53-dB PSRR for a 100-MHz noise tone with the regulator and a 55.2-dB signal-to-noise-and-distortion ratio for a 30-MHz 1.0-V_PP single-ended input at 205 MS/s. The ADC core dissipates 40 mW from a 1.0-V nonregulated supply voltage.     

Holography and plasma oxidation for uniform nanoscale two dimensional channel formation of vertical organic field-effect transistors with suppressed gate leakage current

Vertical organic field-effect transistors (VOFETs) with nanoscale channel openings have been fabricated using pentacene as an active layer material. To achieve uniform nanoscale two-dimensional channel openings, a laser holography lithography has been introduced. Uniformly distributed and well-aligned holes with 250 nm diameter were successfully obtained with the laser holography lithography. VOFET devices with these channel openings have shown high on/off ratio of about 10³ without any further treatment. Gate leakage current was also decreased with an additional insulating layer generated on the gate electrode sidewall via plasma oxidation.     

Thermal buffer materials for enhancement of device performance of organic light emitting diodes fabricated by laser imaging process

Laser Induced Thermal Imaging (LITI) is a laser addressed thermal patterning technology with unique advantages such as an excellent uniformity of transfer film thickness, a capability of multilayer stack transfer and a possibility to fabricate high resolution as well as large-area display. Nevertheless, it has been an obstacle to use such a laser imaging process as a commercial technology so far because of serious deterioration of the device performances plausibly due to a re-orientation of the molecular stacking especially in the emitting layer during thermal transfer process. To improve device performances, we devised a new concept to suppress the thermal degradation during such kind of thermal imaging process by using a high molecular weight small molecular species with large steric hindrance as well as high thermostability as a thermal buffer layer to realize highly efficient LITI devices. As a result, we obtained very high relative efficiency (by EQE) up to 91.5% at 1000 cd/m² from the LITI devices when we utilize 10-(naphthalene-2-yl)-3-(phenanthren-9-yl)spiro[benzo[ij]tetraphene-7,9′-fluorene] as a thermal buffer material.     

Variable length signal detection framework for cognitive radio systems

The cognitive radio (CR) system opportunistically utilizes the frequency bands temporally unoccupied by the primary user. In the CR system, the energy or cyclostationary detector is used to detect the primary user signal. For protecting the primary user tightly, the signal detection time can be very long, which leads to inefficiency in the CR system. Thus, we propose a novel signal detector that greatly reduces the average detection time. The proposed detector periodically decides whether it terminates the detection process or receives more input signal for more information. Therefore, the proposed detector has variable detection time. We will call the proposed detector the variable length signal detector (VLSD). The VLSD is designed by using a partially observable Markov decision process framework for optimal performance. We present the numerical results showing that the VLSD requires much smaller average detection time compared with the traditional fixed length signal detector to achieve a given detection error probability. Copyright © 2012 John Wiley & Sons, Ltd.