Nucleophilic Addition of Amides to Haloalkynes: Synthesis of ()-β-Halovinyl Amides as Dual Precursors of Alkylidene Carbenes and Allyl Halides.

Toward a regioselective method for the synthesis of β-halovinyl amides, we developed a transition-metal-free nucleophilic addition reaction of amides to haloalkynes. The regioselective nucleophilic addition was achieved under solvent-free conditions using phosphonates to protonate the intermediate alkylidene carbenoids, thus suppressing their decomposition. Furthermore, we demonstrate that β-halovinyl amides can serve as dual precursors of allyl halides and alkylidene carbenes to obtain functionalized indoles and pyrrolidones.

Invasion status of hatchery-origin pink salmon in an unstocked river at the Shiretoko World Natural Heritage Site in northern Japan.

Hatchery fish and their offspring (including hatchery-wild hybrids) have lower reproductive success than wild fish. Thus, the straying of hatchery fish may negatively impact wild populations, depending on the number of wild salmon returning and hatchery strays. We investigated the straying status of hatchery-origin pink salmon (Oncorhynchus gorbuscha), which have a higher straying rate than other salmonids, in an unstocked river at the Shiretoko World Natural Heritage Site, Japan.

Effects of pulsed electrical stimulation on α-smooth muscle actin and type I collagen expression in human dermal fibroblasts.

Pulsed electrical stimulation (PES) is known to affect cellular activities. We previously found PES to human dermal fibroblasts (HFs) promoted platelet-derived growth factor subunit A (PDGFA) gene expression, which enhanced proliferation. In this study, we investigated PES effects on fibroblast collagen production and differentiation into myofibroblasts.

Pulsed electrical stimulation and amino acid derivatives promote collagen gene expression in human dermal fibroblasts.

Several collagen types are important for maintaining skin structure and function. Previous reports show that l-hydroxyproline (Hyp), N-acetyl-l-hydroxyproline (AHyp), and l-alanyl-l-glutamine (Aln-Gln) are biological active substances with collagen synthesis-promoting effects. In this study, we combined the promotive effects of pulsed electrical stimulation (PES) with three amino acid derivatives in human dermal fibroblasts.

Normal Ventricular and Regional Blood Flow Volumes and Native T1 Values in Healthy Japanese Children Obtained from Comprehensive Cardiovascular Magnetic Resonance Imaging.

Age-related mean and reference ranges for ventricular volumes and mass, regional blood flow measurements, and T1 values using cardiovascular magnetic resonance (CMR) imaging are yet to be established for the pediatric population. Especially in infants and toddlers, no consistent flow volume sets or T1 values have been reported. The purpose of this study was to determine the relevant normal values.

Intentional release of native species undermines ecological stability.

The massive release of captive-bred native species ("intentional release") is a pervasive method to enhance wild populations of commercial and recreational species. However, such external inputs may disrupt the sensitive species interactions that allow competing species to coexist, potentially compromising long-term community stability. Here, we use theory and long-term data of stream fish communities to show that intentional release destabilizes community dynamics with limited demographic benefit to the enhanced species.

Novel double staining of the stratum corneum with fluorescent ε-poly-l-lysine and anionic dextran.

Objective: ε-Poly-l-lysine (PLL) is a cationic polymer consisting of 25-35 l-lysine residues. Our previous study revealed that fluorescently labelled PLL can stain the stratum corneum (SC) via ionic interactions between PLL and SC constituents. In this study, to further clarify the mechanisms underlying the interaction between PLL and the SC, the staining properties of fluorescent PLL were compared with that of fluorescently labelled anionic dextran (aDex), which has approximately the same molecular weight as PLL.

Staining of stratum corneum with fluorescent ε-poly-L-lysine and its application to evaluation of skin conditions.

Background: ε-Poly-L-lysine (PLL) is a cationic polymer consisting of 25 to 35 L-lysine residues that adheres to the surface of skin as well as hair. However, the properties of PLL regarding its adhesion to the skin remain to be elucidated. In this study, we examined the staining of stratum corneum (SC) with fluorescence-labeled PLL and explored its relationship with skin condition.

Association between dietary hardness score and activities of daily living among individuals aged 90 years.

Objectives: With the rapidly aging world population, Japan has many older people with difficulties in maintaining oral health. This study aimed to investigate the relationship between dietary hardness score and performance of activities of daily living (ADL) of 90-year-old individuals in rural areas of Japan.

Material And Methods: A total of 236 individuals (64 men and 172 women) aged 90 years in Mitsugi town, Hiroshima, Japan, were included.

Diel migration pattern of pink salmon fry in small streams.

Downstream migration is a critical stage in the anadromous salmonid life cycle, but previous studies have shown different results between rivers or surveys for the diel downstream migration pattern of the fry of the pink salmon Oncorhynchus gorbuscha. We investigated the diel migration pattern of pink salmon fry in three small streams. Our results showed that pink salmon fry migrate mainly within a few hours after sunset; 89.

Temperature-Dependent Swimming Performance Differs by Species: Implications for Condition-Specific Competition between Stream Salmonids.

Condition-specific competition is a phenomenon by which inter-specific competitive dominance changes as a result of environment, and is an important factor determining species distribution. Congeneric charrs in Hokkaido, Japan, provide one of the best examples of condition-specific competition: Dolly Varden, , often dominate in cold streams (6-8°C), whereas white-spotted charr, , dominate in warmer streams (> 10°C). While past laboratory and field experiments have demonstrated the great advantage of white-spotted charr at higher water temperatures, the advantages of Dolly Varden at lower temperature have not always been clear.

Effects of pulsed electrical stimulation on growth factor gene expression and proliferation in human dermal fibroblasts.

Human dermal fibroblast proliferation plays an important role in skin wound healing, and electrical stimulation (ES) promotes skin wound healing. Although the use of ES for skin wound healing has been investigated, the mechanism underlying the effects of ES on cells is still unclear. This study examined the effects of pulsed electrical stimulation (PES) on human dermal fibroblasts.

Global health landscape challenges triggered by COVID-19.

The COVID-19 pandemic highlighted the vulnerability of every aspect of the globalized world, including R&D. Potentially critical R&D areas have been neglected because of the lack of market-driven incentives. However, new initiatives are emerging to address the present crisis of COVID-19 and possibly future similar incidents that will threaten humanity.

Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability.

We previously reported that MGS0008 is a selective group II metabotropic glutamate receptor (mGlu2/3 receptor) agonist that is effective in animal models of schizophrenia. MGS0008 is a highly hydrophilic glutamate analog and is therefore expected to show low oral bioavailability in humans. To improve the oral bioavailability of MGS0008, ester prodrugs of MGS0008 were synthesized and their usefulness was evaluated.

Hysteresis in the gas sorption isotherms of metal-organic cages accompanied by subtle changes in molecular packing.

Structural deformation in response to gas sorption is rarely observed for porous molecular solids, when compared to porous framework materials. Here, we describe the effect of chemical modification on the exterior of lantern-type metal-organic cages on the emergence and then disappearance of cooperative gas uptake. The results suggest that supramolecular design of ligands can be used to reveal this behaviour.

Phosphoproteomic and proteomic profiling of serine/threonine protein kinase PkaE of A3(2) and its role in secondary metabolism and morphogenesis.

This study aimed to investigate the role of serine/threonine kinase PkaE in A3(2). Liquid chromatography tandem mass spectrometry was performed for comparative phosphoproteome and proteome analyses of A3(2), followed by an phosphorylation assay. Actinorhodin production in the deletion mutant was lower than that in wild-type A3(2), and the spores of the deletion mutant were damaged.

Metapopulation stability in branching river networks.

Intraspecific population diversity (specifically, spatial asynchrony of population dynamics) is an essential component of metapopulation stability and persistence in nature. In 2D systems, theory predicts that metapopulation stability should increase with ecosystem size (or habitat network size): Larger ecosystems will harbor more diverse subpopulations with more stable aggregate dynamics. However, current theories developed in simplified landscapes may be inadequate to predict emergent properties of branching ecosystems, an overlooked but widespread habitat geometry.

Parasite infection induces size-dependent host dispersal: consequences for parasite persistence.

Host dispersal is now recognized as a key predictor of the landscape-level persistence and expansion of parasites. However, current theories treat post-infection dispersal propensities as a fixed trait, and the plastic nature of host's responses to parasite infection has long been underappreciated. Here, we present a mark-recapture experiment in a single host-parasite system (larval parasites of the freshwater mussel and its salmonid fish host ) and provide, to our knowledge, the first empirical evidence that parasite infection induces size-dependent host dispersal in the field.

The Regional Centralization of Electronic Fetal Heart Rate Monitoring and Its Impact on Neonatal Acidemia and the Cesarean Birth Rate.

Objective. The improvement of the accuracy of fetal heart rate (FHR) pattern interpretation to improve perinatal outcomes remains an elusive challenge. We examined the impact of an FHR centralization system on the incidence of neonatal acidemia and cesarean births.

Ablation of a small subpopulation of diabetes-specific bone marrow-derived cells in mice protects against diabetic neuropathy.

Diabetic peripheral neuropathy (DPN) is a major diabetic complication. Previously, we showed that hyperglycemia induces the appearance of proinsulin (PI)-producing bone marrow-derived cells (PI-BMDCs), which fuse with dorsal root ganglion neurons, causing apoptosis, nerve dysfunction, and DPN. In this study, we have devised a strategy to ablate PI-BMDCs in mice in vivo.

Rhodium-Catalyzed Intramolecular C-H Bond Activation with Triazoles: Preparation of Stereodefined Pyrrolidines and Other Related Cyclic Compounds.

On treatment of triazoles having an N-sulfonyl-protected benzylamine moiety with [Rh2 (C7 H15 CO2 )4 ], intramolecular C-H bond insertion takes place at the benzylic position to give cis-N-sulfonyl-2-aryl-3-[(sulfonylimino)methyl]pyrrolidines in good yields and with highly stereoselectivities. Analogously, the similar treatment of triazoles having an ether or even an alkyl moiety affords 2-alkyl- or 2-aryl-3-[(sulfonylimino)methyl]tetrahydrofurans or a 2-alkyl-3-[(sulfonylimino)methyl]cyclopentane in good yields.

Antipsychotic profiles of TASP0443294, a novel and orally active positive allosteric modulator of metabotropic glutamate 2 receptor.

Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. The stimulation of metabotropic glutamate (mGlu) 2 receptor has been shown to be effective in a number of animal models of schizophrenia. In this study, we investigated the antipsychotic profiles of (2S)-5-methyl-2-{[4-(1,1,1-trifluoro-2-methylpropan-2-yl)phenoxy]methyl}-2,3-dihydroimidazo[2,1-b][1,3]oxazole-6-carboxamide (TASP0443294), a newly synthesized positive allosteric modulator of the mGlu2 receptor.

Expression and characterization of Streptomyces coelicolor serine/threonine protein kinase PkaE.

We identified and characterized a new eukaryotic-type protein kinase (PkaE) from Streptomyces coelicolor A3 (2) M145. PkaE, consisting of 510 amino acid residues, is a cytoplasmic protein kinase and contains the catalytic domain of eukaryotic protein kinases in the N-terminal region. Recombinant PkaE was found to be autophosphorylated at threonine residues only.

Photoelectrochemical properties of SrNbO2N photoanodes for water oxidation fabricated by the particle transfer method.

SrNbO(2)N photoanodes, which have a band gap energy of 1.8 eV, were tested for photoelectrochemical water oxidation in water splitting. The photoanodes were fabricated either by a particle transfer method or an electrophoretic deposition method.