Construction of Functionalized α-Imino Ketones via Pd-Catalyzed C-H Addition to Nitriles/Aerobic Oxidation Sequences.

Pd(II)-catalyzed addition of sp2 C-H to nitrile/aerobic oxidation sequences for the preparation of functionalized α-imino ketones is described in which readily available heteroarenes and O-acyl cyanohydrins were employed. Various functionalized targeted molecules can be prepared in good yields with high atom and step economy. Moreover, a broad substrate scope and the ready manipulation and availability of the reaction partners enable this protocol to be appealing to explore the chemical space of the construction of functionalized α-imino ketones with high efficiency.

Exercise combined with heat treatment improves insulin resistance in diet-induced obese rats.

Insulin resistance is a risk factor for various cardiovascular diseases, which seriously threaten human health. Thus, finding a safe, effective and economical strategy to treat insulin resistance is urgently needed. This study aimed to investigate the effects of exercise combined with heat treatment on the insulin sensitivity in skeletal muscle of diet-induced obese (DIO) rats. Obese rats were induced by a 10-week high-fat diet and were randomly divided into normal temperature + control (NC), normal temperature + exercise (NE), heat treatment + control (HC) and heat treatment + exercise (HE) groups for 7 weeks of incremental load endurance exercise and heat treatment (exposure to a high-temperature environment room). At the end of the 7-week intervention, we measured fasting blood glucose, serum fasting insulin, serum leptin, serum adiponectin, protein expression of HSF1/HSP27 and JAK2/STAT3 pathway in soleus (primarily composed of slow-twitch fibres) and extensor digitorum longus (primarily composed of fast-twitch fibres) muscles. The results showed that exercise combined with heat treatment can effectively improve insulin resistance by regulating HSF1/HSP27 and JAK2/STAT3 pathways in the slow-twitch muscle of DIO rats. Importantly, exercise combined with heat treatment is more effective in improving insulin resistance in DIO rats than exercise or heat treatment alone. Low-moderate intensity exercise that stimulates slow-twitch muscle, combined with heat treatment is an effective strategy to treat insulin resistance.

Hydration monitoring and rehydration guidance system for athletes based on urine color's L*a*b* parameters.

Maintaining proper hydration is essential for athletes to sustain optimal performance and preserve their physical health. Existing studies have confirmed that urine color is one of the effective indicators for the subjective evaluation of athletes' hydration through the urine color chart. However, the use of urine color charts to evaluate hydration is easily affected by the test environment, urine container and subjective feeling. At present, there are few hydration monitoring instruments based on quantitative analysis of urine color. In recent years, the L*a*b* color model has been widely used in the objective quantitative analysis of color. The L* value represents the luminance change from black to white, the a* value represents the chromaticity change from green to red, and the b* value represents the chromaticity change from blue to yellow. Our previous research has confirmed that the urine color b ∗ value is an effective new indicator to evaluate the hydration of athletes. The research team developed a urine hydration monitoring and rehydration guidance system based on the urine color's L*a*b* parameters via wireless network technology and digital image technology. The hardware structure of the system is composed of a cuvette, a standard light source, a camera, an image collector, a host system, and a touch screen system. The system software is composed of functional modules, such as user information, image acquisition, image processing, and image recognition. The system operation process includes starting the system, filling in basic information, putting the sample, testing the sample, local data review, local data upload, and cloud data review. The system exhibits stable performance, a friendly operation interface, and simple and fast testing. It can objectively and accurately evaluate the hydration of athletes and provide personalized rehydration guidance. The system offers a new method for solving practical problems in sports training, and it has broad application prospects.

Validation of urine colour L*a*b* for assessing hydration amongst athletes.

Objectives: Existing studies have confirmed that urine colour through a urine colour chart is one of the effective indicators for assessing hydration. In recent years, the L*a*b* colour space has been widely used in the objective quantitative analysis of colour. The L*, a* and b* values represent the luminance change from black to white, the chromaticity change from green to red and the chromaticity change from blue to yellow, respectively. This study aimed to examine the validity of the urine colour L*a*b* parameters for assessing the level of hydration amongst athletes. Methods: The study included a total of 474 young elite athletes (251 males and 223 females, age: 24.59 ± 4.86 years). A total of 803 urine samples were collected from the subjects in various stages of hydration, including morning urine and spot urine sample during rehydration. L*a*b* parameters were measured by spectrophotometer. Hydration status was assessed via urine osmolality and urine specific gravity. Results: Urine colour b* value has a high correlation with urine specific gravity and urine osmolality (r = 0.811, 0.741, both p < 0.01); L* value has a moderate correlation with urine specific gravity and urine osmolality (r = -0.508, -0.471, both p < 0.01); there was no significant correlation between a* value and urine specific gravity, urine osmolality (p > 0.05). Whether the diagnosis of hypohydration is based on Usg ≥ 1.020 or Uosm ≥ 700 mmol/kg: The AUC of b* values were all above 0.9 and the specificity and sensitivity of b* values were high (both greater than 80%). The AUC of both L* and a* values were less than 0.5. Whether the diagnosis of hyperhydration is based on Usg ≤ 1.010 or Uosm ≤ 500 mmol/kg: The AUC of b* values were all above 0.9 and the specificity and sensitivity of b* value were high (both greater than 90%). The AUC of both L* and a* values were less than 0.5. Conclusion: These results suggested that the validity of urine colour b* value for assessing hydration amongst athletes was high, however, the validity of urine colour L* and a* values were low.

Amelioration of Ambient Particulate Matter (PM2.5)-Induced Lung Injury in Rats by Aerobic Exercise Training.

Ambient particulate matter (PM2.5), as an inflammation-inducing factor, increases the prevalence of lung injury. The aim of this study was to examine the protective effect and mechanism of aerobic exercise on PM2.5 exposure-induced lung injury. Forty Wistar rats were randomly divided into four groups: sedentary+PM2.5 exposure, exercise+PM2.5 exposure, sedentary, and exercise groups. All rats in the exercise-related groups underwent 8-week aerobic interval treadmill training (5daysweek-1, 1hday-1). PM-exposed rats were exposed to ambient PM2.5 (6h day-1) for 3weeks after the 8-week exercise intervention. Then, ventilation function, histopathological changes, and inflammation responses of pulmonary tissue were examined. Results showed that PM2.5 exposure induced lung injury as manifested by decreased pulmonary function, abnormal histopathological changes, and increased pro-inflammatory cytokine levels (tumor necrosis factor-α and Interleukin-1α). Aerobic exercise alleviated the airway obstruction, reduced respiratory muscle strength, bronchial mucosal exfoliation, ultrastructure damage, and inflammatory responses induced by PM2.5 in exercise-related groups. The benefits of exercise were related with the downregulation of p38-mitogen-activated protein kinase (MAPK), and the subsequent inhibition of the pathways of the cyclooxygenase 2 (COX-2) product, prostaglandin E2 (PGE2). Thus, pre-exercise training may be an effective way to protect against PM2.5-induced lung inflammatory injury in rats.

Aerobic exercise ameliorates particulate matter-induced lung injury in aging rats.

Particulate matter 2.5 (PM2.5) is an inflammatory-inducing factor that is considered to be related to many adverse respiratory problems, especially in the elderly. This study aimed to examine whether pre-exercise training could prevent pulmonary injury induced by urban PM2.5 in aging rats and investigate its relationship with inflammatory pathways. Male Wistar rats (aged 16 months) were randomly divided into four groups: sedentary, exercise, sedentary + PM2.5 exposure, and exercise + PM2.5 exposure. All rats in exercise-related groups were treadmill-trained for 8 weeks (65%-75% VO2max for 30 min every other day). Sedentary groups' rats lived freely in cages without exercise intervention. Rats in the PM-related groups were exposed to ambient PM2.5 (4 h day-1) for 2 weeks after an 8-week exercise intervention or sedentary treatment. Finally, all rats' pulmonary function, lung morphology, degree of inflammation, and relevant protein and mRNA transcript expression levels were examined. The results indicated that PM2.5 exposure induced lung injury in the sedentary + PM2.5 exposure group, as evidenced by the deterioration of pulmonary function, histopathological characteristics, and inflammatory changes. Aerobic exercise alleviated PM2.5-induced airway obstruction, deterioration of pulmonary function, bronchial mucosal exfoliation, and inflammatory responses in aging rats. These effects in exercise groups were associated with the increased expression of intracellular 70 kDa heat shock protein (iHSP70) and the suppression of nuclear transcription factor-κB (NF-κB) activation, as confirmed by increased expression of inhibitor of NF-κB (IκBα) and a reduction in phospho-IKBα (p-IκBα), which is regulated by inhibiting kappa B kinase beta (IKKß). Taken together, aerobic pre-exercise had protective effects on lung injury and reduced vulnerability to inflammation induced by PM2.5 exposure, possibly through the toll-like receptor 4 (TLR4)/NF-κB signaling pathways mediated by the extracellular-to-intracellular HSP70 ratio. Pre-exercise training may be an effective way to protect against PM2.5-induced lung toxicity in aging individuals.

α-Iminol Rearrangement Triggered by Pd-Catalyzed C-H Addition to Nitriles Sequences: Synthesis of Functionalized α-Amino Cyclopentanones.

A α-iminol rearrangement triggered by Pd-catalyzed C-H addition of electronic-rich heteroarenes to cyclobutanone-derived O-acyl cyanohydrins was described, which provided a practical and efficient protocol for the preparation of functionalized α-amino cyclopentanones in an atom- and step-economic fashion. In addition, further synthetic transformations of products have also been demonstrated.

Hot environments decrease exercise capacity and elevate multiple neurotransmitters.

AIMS: This study aimed to test the hypothesis that different neurotransmitters and hormones are presented at exercise fatigue in hot temperatures with differing relative humidities (RH). MAIN METHODS: Eight trained male athletes performed a graded maximum oxygen consumption (VO2max) test in five different environmental conditions, namely, 21°C/20% RH (Normal), 33°C/20% RH (Hot 20%), 33°C/40% RH (Hot 40%), 33°C/60% RH (Hot 60%), and 33°C/80% RH (Hot 80%). Blood samples were taken pre- and post-exercise and analyzed for noradrenaline (NA), adrenaline (ADR), dopamine (DA), serotonin (5-HT), 5-hydroxyindoleacetic acid (5-HIAA), and prolactin (PRL). Weight and oral and skin temperatures were recorded pre- and post-exercise. Heart rate was continuously monitored throughout the exercise. KEY FINDINGS: Hot 20%, Hot 40%, and Hot 80% had lower VO2max levels compared with Normal (P<0.05). The data pooled from all five conditions indicated that the NA (P<0.0001), PRL (P<0.0001), 5-HT (P=0.002), 5-HIAA (P=0.029), and DA (P=0.016) levels were affected by exercise. Accordingly, NA level was significantly associated with performance time. However, ADR did not show any significant effect between pre- and post-exercise (P=0.187). SIGNIFICANCE: The maximal aerobic capacity was impaired in high temperature and most humidity conditions. NA was strongly associated with exercise time, which suggested that exercise duration and intensity had an important influence on NA neurotransmitter level irrespective of the environmental conditions.