Regioselectivity of the Michael Addition of Nitromethane on α,β-Unsaturated Acid Esters

Triton B catalyzed Michael addition of nitromethane on esters of α,β-unsaturated acids 1 has been studied. The course and regioselectivity of the reaction is discussed in the view of structure of products 2a-g, 3a-g, 4g, f, 5g, f, assessed by GC/MS, NMR and IR spectroscopy and by MOPAC 6 (AM1) calculations, respectively.     

The Effect of Paraquat on the Radiosensitivity of Melanoma Cells: the Role of Superoxide Dismutase & CATALASE

The activities of reactive oxygen species scavenging enzymes, superoxide dismutases (SODs) and catalase (in cells of two melanomas (mouse B16 and human SK23) and in Chinese hamster ovary (CHO) cells were examined. Melanoma cells are relatively depleted in activities of superoxide dismutases and catalase as compared to CHO cells. Short equitoxic (500μM for CHO and B16 cells and 5 μM for SK23 cells) paraquat treatment (15 min before the X-irradiation, 45 min in postirradiation period - the total time of treatment was 1 h) caused an increase in radiation resistance, measured as colony forming ability, in two of the three lines examined.

It is proposed that PQ may exert its radioprotective effect by induction of antioxidant enzymes.     

Antioxidant and Enzyme Inhibitory Activities of Rhoifolin Flavonoid: In Vitro and in Silico Studies

Rhoifolin (apigenin-7-O-β-neohesperidoside) belongs to the class of flavonoids and was reported to exhibit anti-inflammatory, cytotoxic, antidiabetic, hepatoprotective, and cardioprotective activities. The current study presents the in-vitro evaluation of the antioxidative effects of rhoifolin by many assays, namely DPPH, CUPRAC, ABTS, phosphomolybdenum, and FRAP. Enzyme inhibitory potential was also evaluated for acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, amylase, and glucosidase enzymes. While results revealed weak antioxidant activities for rhoifolin, the compound demonstrated some promising enzyme inhibitory effects against BChE (4.03 mg GALAE/g) and tyrosinase (7.44 mg KAE/g) but was not active on AChE. Regarding anti-diabetic enzymes, the compound was active on amylase but did not show any inhibition effect on glucosidase. In-silico molecular docking study was performed for rhoifolin on the active site of NADPH oxidase, BChE, and amylase enzymes to verify the observed enzyme inhibitory effect. Good binding affinities were observed for rhoifolin on all the docked enzymes, revealing numerous hydrogen bonds, carbon-hydrogen, van der Waals interactions. This is the first study to evaluate the enzyme inhibition potential of rhoifolin. We concluded that the increase in the degree of glycosylation might decrease the antioxidant abilities of flavonoids and that rhoifolin had moderate enzyme inhibition abilities to be investigated in future studies.     

Improvement of Selected Morphological,Physiological, and Biochemical Parameters of Banana (<i>Musa acuminata</i> L.) Using Potassium Silicate under Drought Stress Condition Grown <i>in vitro</i>

Drought stress has become more common in recent years as a result of climate change impacts on the production of banana crops and other fruit trees. The growth and productivity of Musa spp are severely impacted by the gradual degradation of water resources and the erratic distribution pattern of annual precipitation amount. The aim of the work includes increased drought tolerance in light of water scarcity in the world as a result of the bananas’ being gluttonous for water needs. This investigation was carried out from 2019 to 2020 to study the effect of potassium silicate on morphological growth and biochemical parameters of Musa acuminata L under drought stress by PEG. As a result, drought stress reduced the morphological characteristics such as shoots number, shoot length, roots number, and survival percentage and biochemical characteristics such as chlorophyll a, b, carotenoids, stomatal status, and RWC. While proline content increased in the leaf of M. acuminata L. Media complemented with K₂SiO₃ (2 to 6 mM) either individually or in combination with PEG led to an improvement in all morphological and biochemical characteristics. The activities of CAT, POD, and PPO enzymes increased signifi- cantly compared to control. Furthermore, the lowest PPO, CAT, and POD activity were achieved. Additionally, K₂SiO₃ treatments under drought stress successfully enhanced the leaf stomatal behavior. Our results suggest that K₂SiO₃ can help to maintain plant integrity in the tested cultivar under drought stress.     

Pharmacological activation of PPARbeta promotes rapid and calcineurin-dependent fiber remodeling and angiogenesis in mouse skeletal muscle

Recent studies have shown that administration of peroxisome proliferator-activated receptor-beta (PPARbeta) agonists enhances fatty acid oxidation in rodent and human skeletal muscle and that muscle-restricted PPARbeta overexpression affects muscle metabolic profile by increasing oxidative myofiber number, which raises the possibility that PPARbeta agonists alter muscle morphology in adult animals. This possibility was examined in this study in which adult mice were treated with a PPARbeta agonist, and the resulting changes in myofiber metabolic phenotype and angiogenesis were quantified in tibialis anterior muscles. The findings indicate a muscle remodeling that is completed within 2 days and is characterized by a 1.63-fold increase in oxidative fiber number and by a 1.55-fold increase in capillary number. These changes were associated with a quick and transient upregulation of myogenic and angiogenic markers. Both myogenic and angiogenic responses were dependent on the calcineurin pathway, as they were blunted by cyclosporine A administration. In conclusion, the data indicate that PPARbeta activation is associated with a calcineurin-dependent effect on muscle morphology that enhances the oxidative phenotype.     

Ablation of Csk in neural crest lineages causes corneal anomaly by deregulating collagen fibril organization and cell motility

Src family kinases (SFKs) have been implicated in the regulation of cell motility. To verify their in vivo roles during development, we generated mutant mice in which Csk, a negative regulator of SFKs, was inactivated in neural crest lineages using the Protein zero promoter in a Cre-loxP system. Inactivation of Csk caused deformities in various tissues of neural crest origins, including facial dysplasia and corneal opacity. In the cornea, the stromal collagen fibril was disorganized and there was an overproduction of collagen 1a1 and several metalloproteases. The corneal endothelium failed to overlie the central region of the eye and the peripheral endothelium displayed a disorganized cytoskeleton. Corneal mesenchymal cells cultured from mutant mice showed attenuated cell motility. In these cells, p130 Crk-associated substrate (Cas) was hyperphosphorylated and markedly downregulated. The expression of a dominant negative Cas (CasΔSD) could suppress the cell motility defects. Fluorescence resonance energy transfer analysis revealed that activation of Rac1 and Cdc42 was depolarized in Csk-inactivated cells, which was restored by the expression of either Csk or CasΔSD. These results demonstrate that the SFKs/Csk circuit plays crucial roles in corneal development by controlling stromal organization and by ensuring cell motility via the Cas-Rac/Cdc42 pathways.     

The C-terminal transmembrane domain of Bcl-xL mediates changes in mitochondrial morphology

We investigate the effect of mitochondrial localization and the Bcl-x_L C-terminal transmembrane (TM) domain on mitochondrial morphology and subcellular light scattering. CSM 14.1 cell lines stably expressed yellow fluorescent protein (YFP), YFP-Bcl-x_L, YFP-Bcl-x_L-ΔTM, containing the remainder of Bcl-x_L after deletion of the last 21 amino acids corresponding to the TM domain, or YFP-TM, consisting of YFP fused at its C-terminal to the last 21 amino acids of Bcl-x_L. YFP-Bcl-x_L and YFP-TM localized to the mitochondria. Their expression decreased the intensity ratio of wide-to-narrow angle forward scatter by subcellular organelles, and correlated with an increase in the proportion of mitochondria with an expanded matrix having greatly reduced intracristal spaces as observed by electron microscopy. Cells expressing YFP-TM also exhibited significant autophagy. In contrast, YFP-Bcl-x_L-ΔTM was diffusely distributed in the cells, and its expression did not alter light scattering or mitochondrial morphology compared with parental cells. Expression of YFP-Bcl-x_L or YFP-Bcl-x_L-ΔTM provided significant resistance to staurosporine-induced apoptosis. Surprisingly however, YFP-TM expression also conferred a moderate level of cell death resistance in response to staurosporine. Taken together, our results suggest the existence of a secondary Bcl-x_L function that is mediated by the transmembrane domain, alters mitochondrial morphology, and is distinct from BH3 domain sequestration.     

Prevalence of metabolic syndrome in the interior of Croatia: the Baranja region

Metabolic syndrome (MS), a constellation of metabolic risk factors associated with development of cardiovascular diseases and Type 2 diabetes (T2D), has emerged as a public health problem of enormous proportions in developed and developing countries. We have reported previously its prevalence in several island populations of the Eastern Adriatic coast of Croatia. In spite of leading a relatively traditional life style pattern including adherence to a Mediterranean diet, the prevalence of MS in these populations is high and comparable to that in developed nations. However, data on prevalence of MS among the mainland Croatian populations is limited. Therefore, we conducted a study in an outbred population comprising of Croats, Hungarians and Serbs from the Baranja region of mainland Croatia. Although this is an ethnically heterogeneous population, the constituent groups exchange mates and therefore, are not reproductively isolated. The life style patterns are also similar. Overall prevalence of MS, assessed by the National Cholesterol Education Program (NCEP) criteria, is 40% (35% in males and 42% in females) with Body Mass Index (BMI) as the predictor of obesity and 42% (52% in males and 39% in females) with Waist Hip Ratio (WHR) as the predictor of obesity. It is likely that, in addition to genetic risk factors, a host of environmental factors that include dietary habits and relatively urban life style in a modernized society have influenced the levels of the constituent metabolic traits leading to an increased prevalence of MS.