Preparation of N-2-Nitrophenylsulfenyl Imino Peptides and Their Catalyst-Controlled Diastereoselective Indolylation.

N-2-Nitrophenylsulfenyl imino dipeptides bearing various functional groups were successfully prepared by MnO2 -mediated oxidation and then subjected to diastereoselective indolylation. Each diastereomer of the adduct was selectively obtained from the same substrates using the appropriate chiral phosphoric acid catalysts. These transformations would be useful for synthesizing non-canonical amino acid-containing peptides as novel drug candidates.

Thermoregulatory responses of lower limb amputees during exercise in a hot environment.

Lower limb amputees (LLAs) have less skin surface required for sweating; thus, the ability to dissipate heat from the body may decrease and the risk of heat illness may increase during exercise in a hot environment. However, no study has compared the thermoregulatory responses during exercise between LLAs and able-body (AB) individuals with different body surface areas. This study aimed to compare the thermoregulatory responses of LLAs with those of AB individuals during exercise in a hot environment. Seven LLAs (LLA group) and 7 able-body individuals (AB group) participated in the study. A 60% peak power output of arm crank upper-body exercise was performed for 60 min in a hot environment (32 °C, 50% relative humidity). There was no difference in the increase in rectal temperature (LLA: 0.8 ± 0.2 °C, AB: 0.8  ± 0.2 °C) and mean skin temperature between the groups during the 60-min exercise. In the LLA group, the accumulated local sweat rate of the thigh during exercise was significantly higher on the non-cut side than on the cut side (64.6 ± 43.0 mg/h vs. 37.0 ± 27.2 mg/h, p < 0.05). The total sweat rate was significantly higher in the LLA group than in the AB group (1.18 ± 0.37 kg/h vs. 0.84 ± 0.10 kg/h, p < 0.05). Thermal sensation and comfort were lower in the LLA group than in the AB group. Different heat loss responses were observed in the AB and LLA groups during exercise in the heat. The LLA group compensates for sweating on the cut side due to an increase in sweat loss on the intact limb, thereby preserving appropriate thermoregulation during exercise.

Stimulated neuronal expression of brain-derived neurotrophic factor by Neurotropin.

Expression of brain-derived neurotrophic factor (BDNF) was stimulated in human neuroblastoma SH-SY5Y cells by a nonprotein extract of inflamed rabbit skin inoculated with vaccinia virus (Neurotropin), an analgesic widely used in Japan for treatment of disorders associated with chronic pain, with the optimal dosage at 10mNU/mL. This stimulation was accompanied by activations of p42/44 MAP kinase, CREB and c-Fos expression. Inhibitors of MAP kinases or PI 3-kinase prevented the stimulatory action of Neurotropin, indicating that neuronal TrkB/CREB pathway mediates the action. Repetitive oral administration of Neurotropin (200NU/kg/day, 3months) prevented the age-dependent decline in hippocampal BDNF expression in Ts65Dn mice, a model of Down's syndrome. This effect was associated with the improvement of spatial cognition of the mice. These results open an intriguing new strategy in which Neurotropin may prove beneficial treatment for neurodegenerative disorders.

The relevance of whole or segmental body bioelectrical impedance phase angle and physical performance in adolescent athletes.

Objective. The physical condition of athletes can be assessed easily and quantitatively using objective indicators. Bioelectrical impedance measures the phase angle (PA), representing hydration and cell function, and is a potential clinical indicator of physical condition. This study aimed to investigate the association between PA and physical performance in adolescent athletes.Approach. Overall, 170 adolescent athletes underwent a sports medical check-up, including body composition measurements and physical performance tests. Whole-body and segmental PAs (arm and leg) were determined based on body composition values. Isometric grip power and knee isokinetic muscle strength were measured as parameters of muscle strength. Counter movement jump height and squat jump height were measured as jump parameters. Associations between PA and each muscle strength or jump parameters were analysed using Pearson product-moment correlation coefficient or Spearman's rank correlation coefficient.Main results. Whole-body and upper limb PAs were highly correlated with grip power (r= 0.70-0.80). Whole-body and lower limb PAs were correlated with knee isokinetic muscle strength (r= 0.43-0.59). Whole and all segmental PAs were correlated with counter movement jump height (r= 0.46-0.57) and squat jump height (r= 0.42-0.52).Significance. PA can be used to monitor physical condition and sports performance in adolescent athletes. Segmental PAs can help assess the condition of the corresponding body part.

Neurotropin promotes NGF signaling through interaction of GM1 ganglioside with Trk neurotrophin receptor in PC12 cells.

Activation of the high-affinity nerve growth factor (NGF) receptor Trk occurs through multiple processes consisted of translocation and clustering within the plasma membrane lipid rafts, dimerization and autophosphorylation. Here we found that a nonprotein extract of inflamed rabbit skin inoculated with vaccinia virus (Neurotropin(®)) enhanced efficiency of NGF signaling. In rat pheochromocytoma PC12 cells overexpressing Trk (PCtrk cells), Neurotropin augmented insufficient neurite outgrowth observed at suboptimal concentration of NGF (2ng/mL) in a manner depending on Trk kinase activity. Cellular exposure to Neurotropin resulted in an accumulation of Trk-GM1 complexes without affecting dimerization or phosphorylation states of Trk. Following NGF stimulation, Neurotropin significantly facilitated the time course of NGF-induced Trk autophosphorylation. These observations provide a unique mechanism controlling efficiency of NGF signaling, and raise the therapeutic potential of Neurotropin for various neurological conditions associated with neurotrophin dysfunction.