Design,Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders

Lysine demethylase 5 C (KDM5C) controls epigenetic gene expression and is attracting great interest in the field of chemical epigenetics. KDM5C has emerged as a therapeutic target for anti-prostate cancer agents, and recently we identified triazole 1 as an inhibitor of KDM5C. Compound 1 exhibited highly potent KDM5C-inhibitory activity in in vitro enzyme assays, but did not show strong anticancer effects. Therefore, a different approach is needed for the development of anticancer agents targeting KDM5C. Here, we attempted to identify KDM5C degraders by focusing on a protein-knockdown strategy. Compound 3 b , which was designed based on compound 1 , degraded KDM5C and inhibited the growth of prostate cancer PC-3 cells more strongly than compound 1 . These findings suggest that KDM5C degraders are more effective as anticancer agents than compounds that only inhibit the catalytic activity of KDM5C.     

Improving the shelf life stability of vacuum-packed fresh-cut peaches (Prunus persica L.) by radio frequency heating in water

The present study aimed to investigate the influence of radio frequency (RF) heating at 70 and 80 °C, in comparison with the traditional conventional heating. The RF heating technology was applied for maintaining the colour and textural quality as well as inactivating the enzymatic activity of polyphenol oxidase (PPO) and reducing the Escherichia coli growth in packaged fresh-cut peach samples. To evaluate this, 120 g of freshly cut peach fruit was placed in heat-resistant plastic bags, and 50 mL of sugar solution (12°Brix) was added to each bag and vacuum-packed for conventional heating and radio frequency (RF) heating. Our results demonstrated that the RF heating process could reduce the heating time by up to 83% at 70 and 80 °C as compared to conventional heating. Moreover, RF heating at 70 and 80 °C reduced the PPO enzymatic activity, which caused enzymatic browning, up to 85.46% and 93.5%, respectively, as compared to 40.86% reduction only for conventional heating. Furthermore, RF heating completely inhibited E. coli growth. Collectively, we demonstrated that RF heating is an emerging and promising technology for improving the quality of fresh-cut fruits such as peach during various storage conditions. The present study provides relatively novel information on the effectiveness of RF heating in maintaining the quality of fresh-cut peaches. In the future, we would like to investigate the effectiveness of RF heating on other agricultural products.     

Practical Continuous‐Flow Controlled/Living Anionic Polymerization

A continuous‐flow reaction system was developed, allowing flow conditions of the entire system to be maintained at a predetermined constant level, which is one of the most significant factors for successful industrial application. Controlled/living anionic polymerization was selected as a model reaction since the characteristics of its polymer products, molecular weights, and molecular weight distributions are highly susceptible to changes in the relative flow rates of a monomer and initiator solutions. In flow microreactors, controlled/living anionic polymerization of styrene in tetrahydrofuran (THF)/hexane initiated by THF‐diluted n‐butyllithium (n‐BuLi) was examined. Poly(styrenes) of larger molecule sizes such as Mn > 15 000 were successfully synthesized. After continuous operation for four hours, ca. 0.5 kg of the polymer was readily produced with narrow molecular weight distribution, demonstrating the applicability of this continuous‐flow system for controlled/living anionic polymerization on considerably large scale with a view to its industrial usage in the future.     

A Hydrogen Management Method in Residential Distributed Generation Systems with Photovoltaic Cells and Hydrogen‐Storage Type Fuel Cells

Recently, renewable energy has been attracting attention as a result of global warming and the depletion of fossil fuels. Photovoltaic (PV) systems have spread rapidly around the world because they generate electric power quietly and can be installed in many places. The output power generated in a PV system fluctuates with changes in solar irradiance and panel temperature. The reverse flow of surplus power in output spikes may have a negative effect on electric power quality, such as on the frequency and voltage in a power system. A residential distributed generation (DG) system composed of a fuel cell (FC) unit, an electrolyzer (EL) unit, and a PV system has been proposed in order to resolve these problems. In order to operate this system without interruption, the hydrogen storage volume must be managed. This paper proposes a novel hydrogen management method for a residential DG system with PV cells and hydrogen‐storage type FCs. The hydrogen storage volume is maintained at the preset frequency by operating the FC unit and the EL unit. Models of the PV, FC, and EL were constructed for a simulation. In the simulation, we showed that the proposed management method is viable for a residential DG system with PV cells and hydrogen‐storage FCs.     

Stimulation of THP-1 Macrophages with LPS Increased the Production of Osteopontin-Encapsulating Exosome

Osteopontin (OPN) mediates bone remodeling and tissue debridement. The OPN protein is cleaved, but it is unclear how full-length (FL)-OPN or its cleaved form perform their biological activities in target cells. We, therefore, performed the molecular characterization of OPN in exosomes (Exo). The Exo were isolated from lipopolysaccharide (LPS)-stimulated phorbol 12-myristate 13-acetate (PMA)-differentiated THP-1 macrophages. The Exo were also isolated from PMA-differentiated THP-1 macrophages. The Exo were identified using the qNano multiple analyzer (diameter 59–315 nm) and western blotting with a CD9 antibody. LPS-stimulated cells produced more particles than non-stimulated cells. The presence of the FL or the cleaved form of OPN was confirmed using western blot analysis. A mixture of FL and cleaved OPN was also measured using an ELISA system (Ud-OPN) and their presence in the Exo was confirmed. Ud/FL ratios became low after LPS stimulation, indicating the enhanced encapsulation of FL-OPN in the Exo by LPS. These findings suggest that LPS stimulation of human macrophages facilitates the synthesis of FL-OPN, which is cleaved in cells or the Exo after release. These findings indicate that Exo is a suitable vehicle to transfer OPN to the target cells.     

High-temperature corrosion of low Cr-Fe alloys in sulfur vapor

The sulfidation behavior of low Cr-Fe alloys was studied over the range of 700–900°C under 1 atm of pure sulfur vapor. Sulfidation of alloys with 3.7 and 7.4 wt.% Cr does not follow the parabolic rate law at 750–800° C, although for other alloy compositions and temperatures it obeys that law. Sulfide scales consisted of a three-layer structure. The outer layer was FeS, but the inner and intermediate layers contained FeS, FeCr₂S₄, and Cr₃S₄, their relative amounts and morphologies depending on the corrosion temperature and alloy composition. Increasing Cr contents resulted in a change in the morphology of FeCr₂S₄ from dispersed particles to a thick layer. Ultimately, FeCr₂S₄ was displaced by Cr₃S₄. The formation of FeCr₂S₄ and the scale growth mechanism are discussed also.     

Fast magneto-optical spectrometry by spectrometer

Time efficient measurement of the spectroscopic magneto-optical (MO) activity of materials has always been desirable. In conventional MO systems, the monochromator produces quasi-monochromatic light in a narrow wavelength window. Therefore, to measure the spectroscopic MO activity, a large number of measurements over the full spectra is required to obtain satisfactory wavelength resolution and thus is very time consuming. Here, we develop a novel system that is capable of fast measurement of the MO activity by only one white light source, two polarizers, one achromatic quarter-wave plate, and one spectrometer. This system is flexible from UV to IR region, only depending on the power spectra of light source and sensitivity of the detector at the corresponding wavelengths. As examples, we measured the intriguing optic and MO activity in glass, ferromagnetic thin film, and bulk GaAs in the visible to near infrared region. The results of glass demonstrated a minimum resolvable Faraday rotation angle of 0.004° by the currently equipped system.