Involvement of GPR17 in Neuronal Fibre Outgrowth

Characterization of new pharmacological targets is a promising approach in research of neurorepair mechanisms. The G protein-coupled receptor 17 (GPR17) has recently been proposed as an interesting pharmacological target, e.g., in neuroregenerative processes. Using the well-established ex vivo model of organotypic slice co-cultures of the mesocortical dopaminergic system (prefrontal cortex (PFC) and substantia nigra/ventral tegmental area (SN/VTA) complex), the influence of GPR17 ligands on neurite outgrowth from SN/VTA to the PFC was investigated. The growth-promoting effects of Montelukast (MTK; GPR17- and cysteinyl-leukotriene receptor antagonist), the glial cell line-derived neurotrophic factor (GDNF) and of two potent, selective GPR17 agonists (PSB-16484 and PSB-16282) were characterized. Treatment with MTK resulted in a significant increase in mean neurite density, comparable with the effects of GDNF. The combination of MTK and GPR17 agonist PSB-16484 significantly inhibited neuronal growth. qPCR studies revealed an MTK-induced elevated mRNA-expression of genes relevant for neuronal growth. Immunofluorescence labelling showed a marked expression of GPR17 on NG2-positive glia. Western blot and RT-qPCR analysis of untreated cultures suggest a time-dependent, injury-induced stimulation of GPR17. In conclusion, MTK was identified as a stimulator of neurite fibre outgrowth, mediating its effects through GPR17, highlighting GPR17 as an interesting therapeutic target in neuronal regeneration.     

Discovery of Natural Products Possessing Selective Eukaryotic Readthrough Activity: 3‐epi‐Deoxynegamycin and Its Leucine Adduct

Herein we report the first discovery of natural readthrough products that do not display antimicrobial activity. Two natural negamycins, 3‐epi‐deoxynegamycin and its leucine adduct, isolated 37 years ago, were found to be potent readthrough agents against nonsense mutations of eukaryotes, but not prokaryotes, without displaying antimicrobial activity. These results suggest that the compounds are valuable leads for the development of readthrough drugs against nonsense‐mediated genetic diseases without the potential for contributing to the emergence of drug‐resistant bacteria.     

Cooking qualities of parboiled rices produced at low and high temperatures

The cooking characteristics of parboiled rice are related to (i) its hydration behaviour at temperatures above and below the gelatinisation point; (ii) to kernel elongation on cooking; and (iii) to the extent of amylose solubility. These properties differ among samples, depending on the parboiling conditions. Samples were prepared by parboiling paddy at 70, 80, 90, 100, 110 and 120°C. The kernel elongation on cooking and the amount of soluble amylose in the gruel were then determined. The water uptake values for raw and parboiled rice samples were determined by hydrating them at room temperature (25-30), 60 and 98°C (boiling temperature) for optimal cooking times. The rate of hydration at temperatures below the gelatinisation point increased on parboiling and, conversely, a reverse pattern above this point. Close correlations existed between the temperature of parboiling and the properties studied. The different properties studied also correlated well. The temperature of parboiling influenced the linear elongation of the kernel after cooking. The soluble amylose content was negatively correlated with the temperature of parboiling. Though the hydration properties of different parboiled samples differed among themselves, depending on the degree of parboiling, they fell into two distinct classes, viz. the samples parboiled at a temperature close to the gelatinisation point having cooking qualities similar to raw rice, and above this point qualities differing from raw rice. The water uptake values at room temperature and at 60°C, and the ratio of water uptake at 98°C and optimum cooking time to that at 60°C were found to be useful in differentiating the parboiled rices into the two classes.     

Quality changes in HTST processing of rice parboiling

Paddy soaked to saturation level, when treated at a high temperature for a short time in a mechanical sand roaster is parboiled and dried in a single pass of 47 s duration. The extent of drying depends on the sand temperature. The sand temperature is critical as it decides the associated quality changes in the milled rice. Even at a sand temperature of 125°C, paddy could fully be parboiled but with mild effect. The parboiling became severe at high temperatures. Roasting the soaked paddy at 250°C, reduced the cooking time of the resultant milled rice. A sand temperature of 125–150°C was considered suitable for producing normal parboiled rice by this technique.