Electrophilic aromatic substitution using fluorinated isoxazolines at the C5 position C-F bond cleavage.

Electrophilic aromatic substitution at the C5 position of isoxazolines and construction of a new quaternary carbon center were achieved in this paper. This is the first report of carbon-carbon (C-C) bond formation onto isoxazoline without compromising the ring structure. Various aromatics including heteroaromatics gave the desired products in good yields, especially aromatics bearing electron-donating groups.

Installation of superacidic carbon acid moieties into polymer materials post-polymerization modification.

In the fields of polymer and material chemistries, strong acid units have mainly included sulfonic acids, which has limited the extension of related material chemistries. Here, a unique carbon acid functionality, namely the bis[(trifluoromethyl)sulfonyl]methyl group, was integrated with polymers a simple postpolymerization modification with the outstandingly electrophilic 1,1-bis[(trifluoromethyl)sulfonyl]ethylene. The proposed synthesis protocol was verified as an efficient process even for solid-state reactions.

Effect of Royal Sun Medicinal Mushroom Agaricus brasiliensis KA21 (Agaricomycetes) Cultivated Outdoors on Wound Healing and Maintaining Skin Elasticity.

Royal sun medicinal mushroom Agaricus brasiliensis KA21 has various beneficial pharmacological effects; however, these effects are influenced by its cultivation conditions. A. brasiliensis KA21 is rich in β-glucan, which promotes wound healing.

Addition of Mucoadhesive Agent to Enzymatically Polymerized Caffeic Acid-Based Nasal Vaccine Formulation Attenuates Antigen-Specific Antibody Responses in Mice.

Mucosal vaccination is a promising strategy for combating infectious diseases caused by pathogenic microbes, as it can generate antigen-specific immune responses in both systemic and mucosal compartments. In our recent study, we developed a nasal vaccine system for Streptococcus pneumoniae infections in mice using enzymatically polymerized polyphenols such as caffeic acid. However, the efficacy of this mucosal vaccine system is approximately 70%, indicating a need for improvement.

Effects of Outdoor-Grown Royal Sun Medicinal Mushroom Agaricus brasiliensis KA21 (Agaricomycetes) Fruiting Body on Canine Malassezia Dermatitis.

Brazil-grown outdoor-cultivated Agaricus brasiliensis KA21 fruiting body (KA21) significantly increases the production of serum anti-beta-glucan antibody. Therefore, KA21 ingestion may be useful for the prevention and alleviation of fungal infections. This study aimed to determine the effects of KA21 in fungal infections in animals.

Prevention of amyloid β fibril deposition on the synaptic membrane in the precuneus by ganglioside nanocluster-targeting inhibitors.

Alzheimer's disease (AD), a progressive neurodegenerative condition, is one of the most common causes of dementia. Senile plaques, a hallmark of AD, are formed by the accumulation of amyloid β protein (Aβ), which starts to aggregate before the onset of the disease. Gangliosides, sialic acid-containing glycosphingolipids, play a key role in the formation of toxic Aβ aggregates.

Total syntheses of -hypocoprin A and -hypocoprin B.

This study reports the stereoselective total syntheses of the antipodes of the unique 3/10 bicyclic skeletal sesquiterpenoids, namely, hypocoprin A and hypocoprin B. The synthesis involved conjugate addition accelerated by trimethylsilyl chloride, construction of the ten-membered ring the intramolecular S2 reaction promoted by 1,8-diazabicyclo[5.4.

Synthesis of Spirocyclic Cyclobutenes through Desulfinative Spirocyclisation of gem-Bis(triflyl)cyclobutenes.

A two-step synthesis of less accessible spiro[cyclobutene-1,9'-fluorene] compounds from biaryl-alkynes and 2-(2-fluoropyridin-1-ium-1-yl)-1,1-bis((trifluoromethyl)sulfonyl)ethan-1-ide, which serves as a potent precursor for outstandingly electrophilic Tf C=CH , has been developed. This synthetic methodology includes selective formation of gem-bis(triflyl)cyclobutenes from biaryl-alkynes and Tf C=CH followed by desulfinative spirocyclisation mediated by 1,1,1,3,3,3-hexafluoroisopropyl alcohol (HFIP). Besides, on the basis of the chameleonic reactivity of sulfone functionality, several derivatisations of triflylated spiro[cyclobutene-1,9'-fluorene] products have been successfully achieved.

Systemic delivery of siRNA to the colon using peptide modified PEG-PCL polymer micelles for the treatment of ulcerative colitis.

Ulcerative colitis (UC) is a refractory inflammatory bowel disease that causes inflammation and ulcers in the digestive tract, and significantly reduces the patient's quality of life. While existing UC treatments have many challenges, nanotechnology, and small interfering RNA (siRNA) based formulations are novel and promising for UC treatment. We previously reported that intravenous administration of MPEG-PCL-CH2R4H2C nanomicelles had high inflammatory site accumulation and remarkable therapeutic effects on rheumatoid arthritis by a phenomenon similar to enhanced permeability and retention effect.

Molecular crystalline capsules that release their contents by light.

Here, we present single crystalline capsules of a photoresponsive molecule produced by simple recrystallization from organic solutions without direct human processing. During the crystal growth process, a movie was taken of the capsule taking in the organic solution. The capsules responded rapidly (<1 s) to the UV light stimuli and released the captured solution or solute.

Binding Specificity of a New Artificial β-Glucan Recognition Protein and Its Application to β-Glucan Detection in Mushroom Extracts.

β-1,3-D-glucan (BG) activates innate immunity and enhances immune responses. Fungi, such as mushrooms, produce a relatively large amount of BG, the structure and molecular weight of which varies depending on the species of fungi. This study was conducted to develop a detection probe for quantifying or detecting BG from fungi using BG-binding proteins.

Open-Label Study of the Influence of Food Containing the Royal Sun Mushroom, Agaricus brasiliensis KA21 (Agaricomycetes), on β-Glucan-Specific Antibody Production in Healthy Human Volunteers.

The edible mushroom Agaricus brasiliensis contains a large amount β-glucan, which is mainly composed of a β-1,6-glucan structure. In this study, we investigated the effect of A. brasiliensis strain KA21 on the anti-β-glucan antibody titer in healthy humans and the role of antibodies as an immunomodulator.

Development of a Liquid Crystal Formulation that Can Penetrate the Stratum Corneum for Intradermal Delivery of Small Interfering RNA.

Topical delivery of small interfering RNA (siRNA) can be an attractive method for the treatment of skin diseases and improving the quality of life of patients. However, it is difficult for siRNA to pass through the two major barriers of the skin: the stratum corneum (SC) and tight junctions. We have previously reported that atopic dermatitis of skin without the SC can be efficiently treated by the intradermal administration of trans-activator of transcription (Tat) peptide and AT1002 (tight junction opening peptide).

Quantification of Mushroom-Derived Soluble β-1,6-Glucan Using the Function-Modified Recombinant β-1,6-Glucanase.

Mushroom is one of the major sources of β-glucan used in medical applications and traditional therapies. Thus, structure analysis and quantification of β-glucan content is crucial to evaluate medicinal mushrooms. Most studies concerning mushroom-derived β-glucan have been focused on β-1,3-glucans.

Zn(ii)2,9-dimethyl-1,10-phenanthroline stimulates cultured bovine aortic endothelial cell proliferation.

Vascular endothelial cells cover the luminal surface of blood vessels in a monolayer. Proliferation of these cells is crucial for the repair of damaged endothelial monolayers. In the present study, we identified a zinc complex, Zn(ii)2,9-dimethyl-1,10-phenanthroline (Zn-12), that stimulates the proliferation of bovine aortic endothelial cells in a culture system.

Development of an on-chip sample injection system with a 6-port valve incorporated in a microchip.

Micro-flow-injection analysis (μFIA) is amenable to high-throughput systems with lower consumption of sample and reagent volumes. On-chip sample injection methods are important to prevent reduced analytical performance associated with dead volumes and diffusion of sample solutions. In this study, we have developed an on-chip sample injection system with a small-sized 6-port valve incorporated on a microchip.

Total synthesis of squafosacin F: stereodivergent approach to mono-tetrahydrofuran acetogenins.

Annonaceous acetogenins have a wide range of potential biological activities. The development of simple and diversity-oriented approaches to their synthesis is therefore important. We have achieved the first total synthesis of squafosacin F and assigned its absolute configuration.

Cascade Reaction in Human Live Tissue Allows Clinically Applicable Diagnosis of Breast Cancer Morphology.

Clean operating margins in breast cancer surgery are important for preventing recurrence. However, the current methods for determining margins such as intraoperative frozen section analysis or imprint cytology are not satisfactory since they are time-consuming and cause a burden on the patient and on hospitals with a limited accuracy. A "click-to-sense" probe is developed based on the detection of acrolein, which is a substance released by oxidatively stressed cancer cells and can be visualized under fluorescence microscopy.

Intravenous injection of neural progenitor cells facilitates angiogenesis after cerebral ischemia.

Earlier we demonstrated that the injection of neural progenitor cells (NPCs) has therapeutic potential for the improvement of learning dysfunction after cerebral ischemia. However, it remained to be clarified how transplantation of NPCs can improve ischemia-induced dysfunction. In this study, we examined whether intravenous injection of NPCs after cerebral ischemia could enhance angiogenesis by affecting the expression of angiogenic factors.