Novel α-glucosidase inhibitors from Macaranga tanarius leaves

One of the hyperglycaemic remedies is glucose absorption reduction by suppressing carbohydrate digestion due to utilisation of α-glucosidase inhibitors (AGIs). Determination of prospecting herbs done in vitro by using enzyme assay resulted in the finding of Macaranga tanarius, which showed a potent inhibitory activity. An EtOAc-soluble extract of M. tanarius leaves was chromatographed by a Diaion HP-20 column and the active fractions were further purified with high performance liquid chromatography (HPLC) to isolate active principles against α-glucosidase. Five ellagitannins were successfully isolated and identified. Structure determination revealed that these isolated compounds were mallotinic acid (IC₅₀ > 5.00 mM), corilagin (IC₅₀ = 2.63 mM), chebulagic acid (IC₅₀ = 1.00 mM), and two novel compounds named macatannins A (IC₅₀ = 0.80 mM) and B (IC₅₀ = 0.55 mM). AGIs play an important role for the treatment of diabetes, therefore this research results may suggest novel alternatives for diabetes treatment management.     

Dynamic characteristics and dual control of a ball screw drive with integrated piezoelectric actuator

This paper describes the precision continuous path tracking control by using a dual-actuated single stage. First, fine-drive mechanism and the dynamic model of the entire drive system are described. In the simulation model, the dynamic characteristic of the dual-actuated stage is investigated to see whether it can provide precise motion by using dual control. Second, the fine motion controller is designed. Adjusting the control parameters, a positioning resolution of 20 nm and a bandwidth of 260 Hz were obtained. Third, the frequency responses of coarse and fine drives are experimentally investigated. After that, the dual controller is designed based on the investigated dynamics. Finally, whether coarse motion and fine motion could work complimentarily by the dual servo is examined in the experiments. By using the simultaneous dual controller, tracking errors were reduced sufficiently compared to the single coarse control.     

Effect of re-oxidation on dielectric properties in Ni-MLCC

The effect of re-oxidation treatment on the solubility of dopants and the dielectric properties of rare-earths (La, Ho) and V-substituted BaTiO₃ solid solutions, assuming the shell phase of X7R dielectrics, was investigated. Ho-V-substituted samples showed larger increase of the lattice parameter and T _c by re-oxidation treatment compared with La-V-substituted samples. Electron spin resonance measurements revealed that the oxidation of V³⁺ to V⁴⁺ or V⁵⁺ appeared in the range in which the increase of lattice parameter by re-oxidation treatment was observed. This suggests that the increase of T _c is due to the change of preferential occupational site of Ho ion from A-site to B-site, being accompanied with the oxidation of V³⁺. We also investigated the effect of re-oxidation treatment on the electrical properties and microstructure in Ni-MLCC samples, using rare-earths (La, Ho, Yb) and acceptors (Mn, V) doped BaTiO₃ based X7R dielectrics. The change in temperature characteristic of the dielectric constant by re-oxidation treatment was observed for the MLCC samples containing V with smaller content. In the case of Ho-V- and Yb-V-doped samples showed larger increase of the dielectric constant at around 120 °C compared with La-V-doped samples. The relationship between the microstructure and electrical properties of the MLCC sample was investigated by impedance measurement at elevated temperature.     

A New Lead Identification Strategy: Screening an sp3-rich and Lead-like Compound Library Composed of 7-Azanorbornane Derivatives

Although the advantages of sp³-rich, sterically complicated molecules in drug development have been pointed out, modern screening libraries are filled with planar, sp²-rich components. Compounds that are sp³-rich are difficult to synthesize, and thus we aimed to invent an efficient method to construct sp³-rich libraries. By modifying sp³-rich 7-azanorbornane scaffolds through click chemistry, we efficiently prepared a small set of compounds. These compounds were not only sp³-rich, but also had sufficient “lead-like” properties in view of molecular weights and hydrophobicity. Screening assays of this library provided weak κ opioid receptor agonists and growth hormone secretagogue receptor agonists with high hit rates. These results indicate that the 7-azanorbornane scaffold may be a “privileged structure” for lead identification in drug discovery.     

Full scale investigation of GCL damage mechanisms in small earth dam retrofit applications under earthquake loading

This paper reports results of full scale testing to further explore potential GCL damage mechanisms in earth dam retrofit applications in seismically active areas; in particular, to a) investigate whether shear displacements could reduce the magnitude of GCL panel overlap during earthquake shaking; b) explore the influence of gravel particles on GCL thickness at localised point of contact; and c) observe the consequences of an accidental exposure of an uncovered GCL to short duration rainfall in terms of moisture content and effects during subsequent compaction. The results of these experiments indicate that even under severe shaking no movements were detected at the GCL panel overlap. Whereas gravel particles were observed to locally reduce the thickness of the GCL to 2.2 mm, no plowing of the particle into the GCL occurred due to a lack of shear displacement at the interface, resulting in no localised internal erosion through the barrier. Furthermore, hydration of GCL panels during construction due to surface wetting was observed to result in a state of hydration less than its post-construction state. These results indicate that although each of the three GCL damage mechanisms cannot be ruled out to ever be relevant in practice, the performance of the GCL retrofitted earth dam tested was satisfactory under even severe Level 2 earthquake shaking, and suggests that the retrofitting of small earth dams with GCLs is a promising strategy to improve their static and seismic resistance.     

Development of Novel Inhibitors for Histone Methyltransferase SET7/9 based on Cyproheptadine

The histone methyltransferase SET7/9 methylates not only histone but also non‐histone proteins as substrates, and therefore, SET7/9 inhibitors are considered candidates for the treatment of diseases. Previously, our group identified cyproheptadine, used clinically as a serotonin receptor antagonist and histamine receptor (H1) antagonist, as a novel scaffold of the SET7/9 inhibitor. In this work, we focused on dibenzosuberene as a substructure of cyproheptadine and synthesized derivatives with various functional groups. Among them, the compound bearing a 2‐hydroxy group showed the most potent activity. On the other hand, a 3‐hydroxy group or another hydrophilic functional group such as acetamide decreased the activity. Structural analysis clarified a rationale for the improved potency only by tightly restricted location and type of the hydrophilic group. In addition, a SET7/9 loop, which was only partially visible in the complex with cyproheptadine, became more clearly visible in the complex with 2‐hydroxycyproheptadine. These results are expected to be helpful for further structure‐based development of SET7/9 inhibitors.     

Electron cyclotron resonance plasma production by using pulse mode microwaves and dependences of ion beam current and plasma parameters on the pulse condition

We measure the ion beam current and the plasma parameters by using the pulse mode microwave operation in the first stage of a tandem type ECRIS. The time averaged extracted ion beam current in the pulse mode operation is larger than that of the cw mode operation with the same averaged microwave power. The electron density n(e) in the pulse mode is higher and the electron temperature T(e) is lower than those of the cw mode operation. These plasma parameters are considered to cause in the increase of the ion beam current and are suitable to produce molecular or cluster ions.     

Manufacture of organic transistors on large‐area flexible substrate using direct imaging exposure system by wet process suitable for roll‐to‐roll production

Organic thin‐film transistors (OTFTs) can be fabricated via a wet process and have exceptionally high flexibility. Therefore, production using the roll‐to‐roll (RtoR) method is expected. We succeeded in developing a new OTFT wet fabrication process adaptable to the RtoR process. Utilizing the electroless plating method for wiring formation, all materials can be formed in a wet process and can be patterned using the photolithography process. In addition, we succeeded in fabricating OTFT on an A4‐type flexible substrate using RtoR direct imaging exposure system.     

Respirometer by a piezo device and its application to triage

In this paper, we present a novel respirometer using the effect of piezo devices and show its application to triage. We found that blowing on the piezo device generated several 100 mV voltage and also synchronizes with the respiration. Our detailed investigations of the phenomena showed that it was caused by the pyroelectric effect. In general, the piezo device when used as a sensing device generates output voltage in a batteryless manner and also functions as a buzzer, which can lead to a compact, simple and low-power respirometer. Here, the piezo device was used as a base of respirometer and not only as a respirometer, but also as an alarm sound generator. Thus, the proposed respirometer was realized only by one piezo device and a low-powered microprocessor driven by a small battery. We applied the respirometer to triage and realized a triage sensing system. In the system, we employed the triage priority determination procedure defined as an international standard. The triage sensing system set in a mask detects respiration and displays its condition by turning an LED on and off, synchronizing the respiration and also generating the alarm sound when the respiration falls into the pre-specified ill conditions.