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The P2Y6 receptor (P2Y6R), a Gq-coupled receptor, is a potential drug discovery target for various inflammatory and degenerative conditions. Antagonists have been shown to attenuate colitis, acute lung injury, etc. In the search for competitive antagonists, we have investigated the SAR of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives, although high affinity is lacking. We now reveal that long-chain amino-functionalized congeners display greatly enhanced affinity in the antagonism of UDP-induced Ca2+ mobilization in human (h) P2Y6R-transfected 1321N1 astrocytoma cells. A 6-(Boc-amino-n-heptylethynyl) analogue 30 (MRS4940) had an IC50 of 162 nM, which was a 123-fold greater affinity than the corresponding unprotected primary alkylamine, 107-fold greater than the corresponding pivaloyl derivative 30, and 132-fold selective compared to the P2Y14R. However, similar Boc-amino chains attached at the 8-position produced weak µM affinity. Thus, the P2Y6R affinity depended on the chain length, attachment point, and terminal functionality. Off-target activities, at 45 sites, were tested for acylamino derivatives 20, 24, 26, 30, 31, and 37, which showed multiple interactions, particularly at the biogenic amine receptors. The more potent analogues may be suitable for evaluation in inflammation and cancer models, which will be performed in future studies. [ABSTRACT FROM AUTHOR]

Virtual reality (VR) exercise has been used as a strategy to promote physical health in older adults. Studies have revealed that the effects of exercise interventions vary across age groups. This study aimed to investigate the effects of a 12-week semi-immersion VR-based multicomponent exercise program on the functional fitness of young-old (65–73 years) and middle-old (74–85 years) adults. This study recruited two age groups (young-old adults, n = 49; middle-old adults, n = 37) and randomly assigned them to the experimental (EG) and control (CG) groups. EG participants performed a 75–90-min semi-immersion VR exercise routine twice weekly for 12 weeks, whereas CG participants maintained their original lifestyles without any alterations. The Senior Fitness Test was used to measure functional fitness by assessing upper- and lower-limb flexibility and muscle strength, cardiorespiratory fitness, and balance. EG participants exhibited greater improvements than their CG counterparts in certain functional fitness tests, specifically the Back Scratch, Arm Curl, 2-Minute Step, and 8-Foot Up-and-Go Tests. On comparing the age groups, a difference was exclusively noted in the effects of the Chair Sit-and-Reach Test. In the EG, the intervention significantly improved lower-body flexibility in young-old adults but elicited no such improvement in middle-old adults. Semi-immersion VR exercise improved the functional fitness of young-old and middle-old adults in the EG, with superior results in the former. Elucidating the impact of age-specific exercise interventions on functional capacity will help practitioners design age-specific exercise training content that enhances functional fitness in older adults of different ages. [ABSTRACT FROM AUTHOR]

The efficient dispersion of single-walled carbon nanotubes (SWCNTs) has been the subject of extensive research over the past decade. Despite these efforts, achieving individually dispersed SWCNTs at high concentrations remains challenging. In this study, we address the limitations associated with conventional methods, such as defect formation, excessive surfactant use, and the use of corrosive solvents. Our novel dispersion method utilizes the spontaneous charging of SWCNTs in a solvated electron system created by dissolving potassium in hexamethyl phosphoramide (HMPA). The resulting charged SWCNTs (c-SWCNTs) can be directly dispersed in the charging medium using only magnetic stirring, leading to defect-free c-SWCNT dispersions with high concentrations of up to 20 mg/mL. The successful dispersion of individual c-SWCNT strands is confirmed by their liquid-crystalline behavior. Importantly, the dispersion medium for c-SWCNTs exhibits no reactivity with metals, polymers, or other organic solvents. This versatility enables a wide range of applications, including electrically conductive free-standing films produced via conventional blade coating, wet-spun fibers, membrane electrodes, thermal composites, and core-shell hybrid microparticles. [ABSTRACT FROM AUTHOR]

The current research was the first to prove the existence of fluctuations in the metabolite constituents and antioxidant properties in different organs (leaves, stems, and roots) of the mountain-cultivated ginseng (MCG) plant during a two-month maturation period. Four metabolites, including fatty acids, amino acids, ginsenosides, and phenolic phytochemicals, exhibited considerable differences in organs and maturation times with the following order: leaves > stems > roots. The predominant metabolite contents were found in leaves, with fatty acid (1057.9 mg/100 g) on 31 May, amino acid (1989.2 mg/100 g) on 13 July, ginsenosides (88.7 mg/g) on 31 May, and phenolic phytochemical (638.3 μg/g) on 31 May. Interestingly, ginsenoside content in leaves were highest, with 84.8 → 88.7 → 82.2 → 78.3 mg/g. Specifically, ginsenosides Re, Rd, and F2 showed abundant content ranging from 19.1 to 16.9 mg/g, 8.5 to 14.8 mg/g, and 9.5 to 13.1 mg/g, respectively. Phenolic phytochemicals exhibited remarkable differences in organs compared to maturation periods, with the highest total phenolic content and total flavonoid content recorded at 9.48 GAE and 1.30 RE mg/g in leaves on 31 May. The antioxidant capacities on radical, FRAP, and DNA protection differed significantly, with leaves on 31 May exhibiting the highest values: 88.4% (DPPH), 89.5% (ABTS), 0.84 OD593 nm (FRAP) at 500 μg/mL, and 100% DNA protection at 50 μg/mL. Furthermore, principal cluster analysis revealed metabolite variability as follows: ginsenoside (83.3%) > amino acid (71.8%) > phenolic phytochemical (61.1%) > fatty acid (58.8%). A clustering heatmap highlighted significant changes in metabolite components under the maturation times for each organ. Our findings suggest that MCG leaves on 31 May may be a potential source for developing nutraceuticals, offering highly beneficial components and strong antioxidants. [ABSTRACT FROM AUTHOR]

Highly conducting nanomaterials have garnered significant attention owing to their potential application in Li‐ion batteries for stable electrodes. However, concerns persist regarding their dispersion and effective hybridization with active materials. This study reports a novel approach to enhance Si‐based anode materials using less defective graphene oxide (C‐GO) and highly oxidized single‐walled carbon nanotubes (C‐SWCNTs) fabricated using chlorate‐based oxidation. The method involves encapsulating Si alloy (SiA) particles with C‐GO and C‐SWCNTs, eliminating the need for additional additives. Composite structures with lithiophilic N‐doped SWCNTs and highly crystalline reduced C‐GO coatings on SiA surfaces are created through spray drying and subsequent chemical reduction. This unique combination yields high capacities, stable retention behaviors, and remarkable initial capacities (1224 mAh g−1) with excellent retention rates (82.3% at 100 cycles, 0.1 C). A LIB full‐cell with a SiA/nanocarbon anode exhibited a high energy density of 350 Wh kg−1, while maintaining 65% capacity retention after 200 cycles. The findings demonstrate the potential of this hybrid approach, which eliminates the need for other conducting additives while maintaining a minimal binder content (5 wt.%). This study presents a promising approach for enhancing Si‐based anode materials in lithium‐ion batteries, addressing the dispersion and hybridization challenges in nanomaterial‐enabled electrode design. [ABSTRACT FROM AUTHOR]