Accumulation of Silicon and Changes in Water Balance under Drought Stress in Brassica napus var. napus L.

The aim of this study was to investigate the accumulation of silicon in oilseed rape and to characterize the changes in chosen water balance parameters in response to drought. The following parameters were estimated: water content, osmotic and water potential, evapotranspiration, stomatal conductance and abscisic acid level under optimal and drought conditions. It was shown that oilseed rape plants accumulate silicon after its supplementation to the soil, both in the case of silicon alone and silicon together with iron. It was revealed that silicon (without iron) helps maintain constant water content under optimal conditions. While no silicon influence on osmotic regulation was observed, a transpiration decrease was detected under optimal conditions after silicon application. Under drought, a reduction in stomatal conductance was observed, but it was similar for all plants. The decrease in leaf water content under drought was accompanied by a significant increase in abscisic acid content in leaves of control plants and those treated with silicon together with iron. To sum up, under certain conditions, silicon is accumulated even in non-accumulator species, such as oilseed rape, and presumably improves water uptake under drought stress.

Synthesis, Pharmacological Characterization, and Structure-Activity Relationships of Noncanonical Selective Agonists for α7 nAChRs.

A lack of selectivity of classical agonists for the nicotinic acetylcholine receptors (nAChR) has prompted us to identify and develop a distinct scaffold of α7 nAChR-selective ligands. Noncanonical 2,4,6-substituted pyrimidine analogues were framed around compound 40 for a structure-activity relationship study. The new lead compounds activate selectively the α7 nAChRs with EC50's between 30 and 140 nM in a PNU-120596-dependent, cell-based calcium influx assay. After characterizing the expanded lead landscape, we ranked the compounds for rapid activation using Xenopus oocytes expressing human α7 nAChR with a two-electrode voltage clamp. This approach enabled us to define the molecular determinants governing rapid activation, agonist potency, and desensitization of α7 nAChRs after exposure to pyrimidine analogues, thereby distinguishing this subclass of noncanonical agonists from previously defined types of agonists (agonists, partial agonists, silent agonists, and ago-PAMs). By NMR, we analyzed pKa values for ionization of lead candidates, demonstrating distinctive modes of interaction for this landscape of ligands.