Synthesis and Biological Evaluation of Novel Isonucleosides with 1,2,4‐Triazole‐3‐Carboxamide

Novel 1,2,4‐triazole isonucleosides (1 and 2) were efficiently synthesized starting from D‐ribose and D‐xylose, respectively. The key steps were condensation of cyclic sulfate 8 with methyl‐1,2,4‐triazole‐3‐carboxylate and nucleophilic displacement of the tosylate 15 with methyl‐1,2,4‐triazole‐3‐carboxylate, respectively.     

Synthesis of 3-Alkylidenecepham-4-carboxylic Acid derivatives by Samarium(II) Iodide Reduction

Samarium(II) iodide promoted reductive deacetoxylation of 7-aminocephalosporanic acid derivatives to synthesize 3-alkylidenecepham-4-carboxylates, which could be valuable intermediates for the synthesis of new cephalosporin antibiotics, was investigated.     

After‐Rinsing Hair Growth Promotions of Hinokitiol‐Containing Vesicles and Emulsions

Two kinds of topical dosage forms of hinokitiol (HKL), namely vesicles and oil‐in‐water (O/W) emulsions, were prepared. Behenyl trimethylammonium chloride (BTMAC) and fatty acids were used as bilayer‐forming materials of the vesicles, and oils were employed as oil phases of the emulsions. The substantivity of HKL in the preparations was evaluated in vitro using hairless mouse skins. After applying the preparations onto the skin and rinsing it, the amount of HKL left on the skin was determined using high performance liquid chromatography (HPLC). It was higher when HKL was encapsulated in cationic vesicles rather than in nonionic vehicles, emulsions. An ionic interaction between the cationic vehicle and negatively charged skin is likely to account for the high substantivity. Among the emulsion preparations, an emulsion having octyl salicylate as oil phase exhibited the highest substantivity of HKL. This is probably because that the oil is a good solvent for HKL and it is skin‐retentive. In vivo hair growth‐promotion effect of each dosage form was investigated, where the sample application onto the clipped backs of female mice (C57BL6) and the subsequent rinsing of the backs were done once a day for 30 days. Only HKL in the cationic vesicles had hair growth promotion effect, possibly due to the significant substantivity.     

Remediation of soil/concrete contaminated with uranium and radium by biological method

Biological method was studied for remediation of soil/concrete contaminated with uranium and radium. Optimum experiment conditions for mixing ratios of penatron and soil, and the pH of soil was obtained through several bioremediations with soil contaminated with uranium and radium. It was found that an optimum mixing ratio of penatron for bioremediation of uranium soil was 1 %. Also, the optimum pH condition for bioremediation of soil contaminated with uranium and radium was 7.5. The removal efficiencies of uranium and radium from higher concentration of soil were rather reduced in comparison with those from lower concentration of soil. Meanwhile, the removal of uranium and radium in concrete by bioremediation is possible but the removal rate from concrete was slower than that from soil. The removal efficiencies of uranium and radium from soil under injection of 1 % penatron at pH 7.5 for 120 days were 81.2 and 81.6 %, respectively, and the removal efficiencies of uranium and radium from concrete under the same condition were 63.0 and 45.2 %, respectively. Beyond 30 days, removal rates of uranium and radium from soil and concrete by bioremediation was very slow.     

Analysis of cell gap-dependent driving voltage in a fringe field-driven homogeneously aligned nematic liquid crystal display

We have studied cell gap-dependent driving voltage characteristics in a homogeneously aligned nematic liquid crystal (LC) cell driven by a fringe electric field, termed the fringe field switching (FFS) mode. The results show that for the FFS mode using a LC with positive dielectric anisotropy, the operating voltage decreases as the cell gap decreases, whereas it increases with a decreasing cell gap when using a LC with negative dielectric anisotropy. The difference between LCs is explained by simulation and experiment.     

Parallel synthesis of 2,4,5-trisubstituted thiophene-3-carbonitrile derivatives on traceless solid support

A parallel solid-phase synthesis of 2,4,5-trisubstituted thiophene-3-carbonitrile derivatives was developed. The polymer-supported synthetic route progressed using the sulfide linker via a traceless strategy. The initial synthesis utilized the Thorpe–Ziegler type cyclization of α-haloketone and polymer-supported 2,2-dicyanoethene-1,1-bis(thiolate), which was derived from the Merrifield resin. The resulting thiophene resin was introduced to one substitution by N-arylation. After oxidation of sulfides to sulfones in the thiophene resins for subsequent cleavage, nucleophilic desulfonative substitution with amines and thiols afforded the desired thiophene-3-carbonitrile derivatives in good overall yields.     

Dewatering of cellulose nanofibrils using ultrasound

Although cellulose nanomaterials have promising properties and performance in a wide application space, one hinderance to their wide scale industrial application has been associated with their economics of dewatering and drying and the ability to redisperse them back into suspension without introducing agglomerates or lose of yield. The present work investigates the dewatering of aqueous suspensions of cellulose nanofibrils (CNFs) using ultrasound as a potentially low-cost, non-thermal, and scalable alternative to traditional heat-based drying methods such as spray drying. Specifically, we use vibrating mesh transducers to develop a direct-contact mode ultrasonic dewatering platform to remove water from CNF suspensions in a continuous manner. We demonstrate that the degree of dewatering is modulated by the number of transducers, their spatial configuration, and the flow rate of the CNF suspension. Water removal of up to 72 wt.% is achieved, corresponding to a final CNF concentration of 11 wt.% in 30 min using a two-transducer configuration. To evaluate the redispersibility of the dewatered CNF material, we use a microscopic analysis to quantify the morphology of the redispersed CNF suspension. By developing a custom software pipeline to automate image analysis, we compare the histograms of the dimensions of the redispersed dewatered fibrils with the original CNF samples and observe no significant difference, suggesting that no agglomeration is induced due to ultrasonic dewatering. We also perform SEM analysis to evaluate the nanoscale morphology of these fibrils showing a width range of 20 nm–4 um. We estimate that this ultrasound dewatering technique is also energy-efficient, consuming up to 36% less energy than the enthalpy of evaporation per kilogram of water. Together with the inexpensive cost of transducers (<?$1), the potential for scaling up in parallel flow configurations, and excellent redispersion of the dewatered CNFs, our work offers a proof-of-concept of a sustainable CNF dewatering system, that addresses the shortcomings of existing techniques.

     

Combinatorial Therapeutic Effect of Inhibitors of Aldehyde Dehydrogenase and Mitochondrial Complex I,and the Chemotherapeutic Drug,Temozolomide against Glioblastoma Tumorspheres

Resident cancer cells with stem cell-like features induce drug tolerance, facilitating survival of glioblastoma (GBM). We previously showed that strategies targeting tumor bioenergetics present a novel emerging avenue for treatment of GBM. The objective of this study was to enhance the therapeutic effects of dual inhibition of tumor bioenergetics by combination of gossypol, an aldehyde dehydrogenase inhibitor, and phenformin, a biguanide compound that depletes oxidative phosphorylation, with the chemotherapeutic drug, temozolomide (TMZ), to block proliferation, stemness, and invasiveness of GBM tumorspheres (TSs). Combination therapy with gossypol, phenformin, and TMZ induced a significant reduction in ATP levels, cell viability, stemness, and invasiveness compared to TMZ monotherapy and dual therapy with gossypol and phenformin. Analysis of differentially expressed genes revealed up-regulation of genes involved in programmed cell death, autophagy, and protein metabolism and down-regulation of those associated with cell metabolism, cycle, and adhesion. Combination of TMZ with dual inhibitors of tumor bioenergetics may, therefore, present an effective strategy against GBM by enhancing therapeutic effects through multiple mechanisms of action.     

Fabrication of a solution-processed thin-film transistor using zinc oxide nanoparticles and zinc acetate

We have fabricated a solution-processed ZnO thin-film transistor without vacuum deposition. ZnO nanoparticles were prepared by the polyol method from zinc acetate, polyvinyl pyrrolidone, and diethyleneglycol. The solution-processable semiconductor ink was prepared by dispersing the synthesized ZnO in a solvent. Inverted stagger type thin-film transistors were fabricated by spin casting the ZnO ink on the heavily doped Si wafer with 200 nm thick SiO₂, followed by evaporation of Cr/Au source and drain electrodes. After the drying and heat treatment at 600 C, a relatively dense ZnO film was obtained. The film characteristics were investigated by scanning electron microscopy (SEM) and X-ray diffraction (XRD). In order to obtain the electrical properties of the solution-derived transistor, the on–off ratio, threshold voltage, and mobility were measured.