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At least 1,045 records · Page 58

CD40L and TNF both activate the classical NF-κB pathway, which is not required for the CD40L induced alternative pathway in endothelial cells

Highlights: • In endothelial cells TNF induces a stronger response in gene expression as compared to CD40L. • There are no CD40L-specific genes expressed. • CD40L activates both the classical and the alternative pathway. • Activation of the alternative pathway is independent from the classical pathway. CD40L and TNF signal through engagement of their respective receptors, which are both members of the TNF receptor family. They use partially common signaling molecules leading, among others, to activation of the NF-κB pathway. However, whereas TNF activates the classical, CD40L has been reported to activate the alternative NF-κB pathway, leading to the anticipation that differences in the pattern of inflammatory gene expression would occur. Here, we have compared the gene expression repertoire of CD40L (CD154) and TNF stimulated HUVEC and report that unexpectedly, apart from a stronger response to TNF, no major qualitative differences could be observed. This applies for the period of up to 6 h, a time where the alternative pathway has already been activated. Analysis of the early events after receptor engagement revealed that both TNF and CD40L activate the classical NF-κB pathway, and confirm activation of the alternative by the latter. Furthermore, using genetic and pharmacological inhibition of the classical pathway we show that activation of the alternative occurs independently of the former. This reveals novel insights into NF-κB signaling by CD40L and TNF in endothelial cells.

60 APPLIED LIFE SCIENCES↗

Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation

Highlights: • Yoda1 induces activation of both Akt and ERK1/2 in endothelial cells (ECs). • Gadolinium and ruthenium red both block Yoda1-induced Akt phosphorylation. • GsMTx4 does not block Yoda1-induced Akt or ERK1/2 phosphorylation. • Yoda1-induced activation of Akt and ERK1/2 in ECs are Piezo1-independent. Piezo1 is a mechanosensitive cation channel that is activated by shear stress in endothelial cells (ECs). It has been shown to mediate shear-induced EC responses, including increased calcium influx, and vascular functions, such as vascular tone and blood pressure. Yoda1, a selective Piezo1 activator, has been shown to mimic shear-induced responses in ECs. Since shear-induced calcium influx causes Akt and ERK1/2 activation in ECs, we examined the effects of Yoda1 and the role of Piezo1 on their activation. Here, we show that Yoda1 robustly activates Akt and ERK1/2 in ECs. Additionally, the Piezo1 antagonists, gadolinium and ruthenium red, but not GsMTx4, effectively blocks Yoda1-induced Akt activation. Our results suggest that Yoda1-induced Akt and ERK1/2 activation is not dependent on Piezo1.

60 APPLIED LIFE SCIENCES↗

Differences in TLR7/8 activation between monocytes and macrophages

Highlights: • Only TLR8 agonists induced NF-κB and ISG activation in monocytes. • TLR8 could inhibit TLR7-induced NF-κB activation in monocytes. • Both TLR7 and TLR8 agonists only induced NF-κB but not ISG activation in macrophages. • Differences in expression levels of molecules involved in TLR signaling between monocytes and macrophages. • Comparison between monocytes and macrophages in expression levels of molecules after TLR7/8 activation. The recognition of single-stranded RNA by TLR7/8 leads to the production of NF-κB-mediated cytokines and type I IFNs. However, the role of TLR7/8 activation in monocytes and macrophages is still unclear. The aim of this study was to investigate the differences in the activation of TLR7/8 between these two cell types. Microarray analysis, qRT-PCR and flow cytometry were used to analyse TLR7/8 signalling pathways in monocytes and macrophages after stimulation with agonists. Our data indicated that TLR8 agonists activated the NF-κB- and IRF-mediated pathways in THP-1 cells, whereas TLR7 agonists did not. However, silent TLR8 and enhanced TLR7 expression could increase TLR7-induced NF-κB activation in monocytes. TLR7 and TLR8 agonists induced NF-κB activation but no ISG response in PMA-differentiated THP-1 cells. The mRNA levels of pro-inflammatory cytokine were elevated upon CL075 stimulation in macrophages compared to monocytes. Thus, TLR7 and TLR8 might modulate different immune responses in monocytes and macrophages.

60 APPLIED LIFE SCIENCES↗

Sterol regulatory element binding protein 1 trans-activates 25-hydroxy vitamin D3 24-hydroxylase gene expression in renal proximal tubular cells

Highlights: • SREBP1 activates CYP24A1 transcription in a kidney proximal tubule cell line. • SREBP1 binds to a putative SRE in mouse Cyp24a1 to activate transcription. • Mice injected with thyroid hormone T{sub 3} had reduced renal Srebp1c and Cyp24a1 levels. • SREBP1 trans-activation of CYP24A1 expression could regulate vitamin D{sub 3} levels. The physiological activity of the steroid derived hormone vitamin D is regulated by several enzymatic steps. Both 25-hydroxy vitamin D{sub 3} 1α-hydroxylase (CYP27B1) and 25-hydroxyvitamin D{sub 3} 24-hydroxylase (CYP24A1) modulate blood levels of 1,25-dihydroxyvitamin D{sub 3}, an activated form of vitamin D. We previously demonstrated that CYP27B1 expression was trans-activated by sterol regulatory element binding protein 1 (SREBP1), although whether SREBP1 also regulates CYP24A1 transcription was unclear. Here we investigated the ability of SREBP1 to affect CYP24A1 transcription. In a luciferase reporter assay, mouse and human CYP24A1 promoter activity was strongly activated by SREBP1 in opossum kidney proximal tubular cells (OK-P). Three putative SREs (pSREs) were found in the mouse Cyp24a1 gene promoter and the SREBP1 protein showed specific binding to the pSRE1 element in EMSAs. Site-directed mutagenesis of the pSRE1 element strongly decreased SREBP1-mediated Cyp24a1 gene transcription. Moreover, siRNA-mediated SREBP1 knock-down repressed CYP24A1 expression in human renal proximal tubular epithelial cells (HKC-8). In animal studies, mice given various doses of thyroid hormone (T{sub 3}) showed dose-dependent reductions in renal Srebp1c and Cyp24a1 mRNA levels. Taken together, our results suggest that SREBP1 trans-activates CYP24A1 expression through SREBP binding elements present in the promoter.

60 APPLIED LIFE SCIENCES↗

Activation of TGR5 promotes mitochondrial biogenesis in human aortic endothelial cells

Highlights: • Activation of TGR5 increases the expression of PGC-1α, NRF1 and TFAM. • Activation of TGR5 promotes mitochondrial biogenesis. • Activation of TGR5 leads to a functional gain of mitochondria. • The effect of TGR5 on mitochondrial biogenesis is mediated by CREB. Impairment of mitochondrial biogenesis has been associated with vascular pathophysiology. The G-protein–coupled receptor (TGR5) is an important mediator of bile acid signaling and glucose metabolism. However, the effects of TGR5 on mitochondrial biogenesis in endothelial cells remain elusive. In this study, we found that activation of TGR5 using its specific agonist taurolithocholic acid (TLCA) promoted the expression of PGC-1α, a master regulator of mitochondrial biogenesis in human aortic endothelial cells (HAECs). Additionally, activation of TGR5 increased the expression of PGC-1α target genes, such as NRF1 and TFAM. Indeed, we found that TLCA treatment promoted mitochondrial biogenesis by increasing mitochondrial mass, mitochondrial-to-nuclear DNA (mtDNA/nDNA), COX-Ⅰ expression, and cytochrome c oxidase activity in HAECs. Notably, our results displayed that activation of TGR5 resulted in a functional gain in mitochondria by increasing the rate of respiration and ATP production. Mechanistically, we found that TLCA treatment activated the transcriptional factor CREB by inducing the phosphorylation of CREB at Ser133. Using the PKA/CREB inhibitor H89 abolished the effects of TLCA on PGC-1α, NRF1 and TFAM expression as well as the increase in mtDNA/nDNA and ATP production. These findings suggest that activation of TGR5 promoted mitochondrial biogenesis in endothelial cells, which is mediated by the CREB/PGC-1α signaling pathway.

60 APPLIED LIFE SCIENCES↗

Enhanced PKMT-substrate recognition through non active-site interactions

Protein lysine methyltransferases (PKMTs) catalyze the methylation of lysine residues on many different cellular proteins. Despite extensive biochemical and structural studies, focusing on PKMT active site-peptide interactions, little is known regarding how PKMTs recognize globular substrates. To examine whether these enzymes recognize protein substrates through interactions that take place outside of the active site, we have measured SETD6 and SETD7 activity with both protein and peptide RelA substrate. We have utilized the MTase-Glo™ methyltransferase assay to measure the activity of SETD6 and SETD7 with the different RelA substrates and calculated the Michaelis-Menten (MM) parameters. We found an up to ∼12-fold increase in K{sub M} of the PKMTs activity with RelA peptide relative to the respective full-length protein, emphasizing the significantly higher PKMT-protein interaction affinity. Examination of SETD6 and SETD7 activity toward the same RelA substrates highlight the similarity in substrate recognition for both PKMTs. Our results show that the interaction affinity of SETD6 and SETD7 with RelA is enhanced through interactions that occur outside of the active site leading to higher catalytic efficiency and specificity. These interactions can significantly vary depending on the PKMT and the specific methylation site on RelA. Overall, our results underline that PKMTs can recognize their substrates through docking interactions that occur out of the active site-peptide region for enhancing their activity and specificity in the cellular environment.

60 APPLIED LIFE SCIENCES↗

Calcium sensing receptor activates the NLRP3 inflammasome via a chaperone-assisted degradative pathway involving Hsp70 and LC3-II

Highlights: • CaSR activates the NLRP3-inflammasome via proteasome and lysosome. • CaSR signals via Gα{sub q} and Gβγ to activate the NLRP3 inflammasome. • CaSR stimulates Hsp70 expression leading to chaperone-assisted protein degradation. • CaSR promotes IL-1β processing via proteasome and lysosome-dependent pathways. • CaSR generates homeostasis-altering molecular processes. Calcium sensing receptor (CaSR) activates the NLRP3 inflammasome with consequences on homeostatic responses. However, little is known about how this process is orchestrated. Since proteolysis of critical regulators of NLRP3 inflammasome contribute to its activation, we aimed to understand how CaSR stimulates proteolytic pathways to activate the NLRP3 inflammasome. We found that proteasome and lysosome-dependent mechanisms are activated by CaSR to promote the degradation of important regulators of NLRP inflammasome. The pathway involves Gαq/PLC/PKC and Gβγ/PI3K signaling cascades and IRAK1 ubiquitination. In addition, CaSR stimulates Hsp70 expression activating a chaperone-assisted protein degradation that dictates the fate of ASC, NLRP3 (NOD-like receptor family protein 3), IRAK1 and TRAF6 proteins, turning on the NLRP3 inflammasome. In response to CaSR signaling, these proteins are degraded through the combination of CUPS (chaperone-assisted ubiquitin proteasome pathway) and CAEMI (chaperone-assisted endosomal microautophagy) systems being integrated by autophagosomes (chaperone-assisted macroautophagy, CAMA), as indicated by LC3-II, a classical marker for autophagy, that is induced in the process. Furthermore, CaSR triggers the proteolytic cleavage of pro-IL-1β (IL-1β, 31 kDa) into mature IL-1β (IL-1β, 17 kDa), via the proteasome. Taken together, our results indicate that CaSR promotes NLRP3 inflammasome activation and proteolytic maturation of IL-1β by inducing CUPS and CAEMI, chaperone-assisted degradation pathways. Overall, these results support the inclusion of CaSR as an activator of homeostasis-altering molecular processes.

60 APPLIED LIFE SCIENCES↗

Syk and JNK signaling pathways are involved in inflammasome activation in macrophages infected with Streptococcus pneumoniae

Highlights: • Syk- and JNK-dependent ASC oligomerization is crucial for inflammasome assembling during S. pneumoniae infection. • PLY participates in phosphorylation and activation of Syk and JNK in S. pneumoniae-infected macrophages. • Syk may be involved in JNK phosphorylation in S. pneumoniae infection. Streptococcus pneumoniae is a pathogen of significant clinical importance worldwide that can cause severe invasive diseases, such as pneumonia, otitis media and meningitis. Inflammsomes has been reported to participate in host defense against S. pneumoniae infection. S. pneumoniae could induce the assembly of the nucleotide-binding oligomerization domain-like receptor family pyrin domain containing 3 (NLRP3)/absent in melanoma 2 (AIM2) inflammasome, which mediates the activation of caspase-1 and the subsequent maturation of Interleukin-1β (IL-1β). However, the precise signals that activate inflammasomes during pneumococcal infection remain to be fully elucidated. In the present study, primary mouse macrophages were selected as a cell model, and the effects of kinases on inflammasome activity induced by S. pneumoniae infection were examined by ELISA and western blotting after pretreatment with a kinase inhibitor. Here, we show that Syk and JNK signaling are required for S. pneumoniae-induced activation of the inflammasome. Inhibitors of Syk and JNK almost abolished the oligomerization of apoptosis-associated speck-like protein containing a caspase-activating and recruitment domain (ASC) and subsequent caspase-1 activation and IL-1β secretion. Moreover, pneumolysin (PLY) participated in this process and was critical for Syk/JNK activation. These results suggested that the Syk/JNK signaling pathway may play a vital role in the inflammasome activation and modulate host immune responses against S. pneumoniae.

60 APPLIED LIFE SCIENCES↗

Structural Basis of Smoothened Activation in Hedgehog Signaling

The seven-transmembrane-spanning protein Smoothened is the central transducer in Hedgehog signaling, a pathway fundamental in development and in cancer. Smoothened is activated by cholesterol binding to its extracellular cysteine-rich domain (CRD).How this interaction leads to changes in the transmembrane domain and Smoothened activation is unknown. Here, we report crystal structures of sterol-activated Smoothened. The CRD undergoes a dramatic reorientation, allosterically causing the transmembrane domain to adopt a conformation similar to active G-protein-coupled receptors. We show that Smoothened contains a unique inhibitory p-cation lock, which is broken on activation and is disrupted in constitutively active oncogenic mutants. Smoothened activation opens a hydrophobic tunnel, suggesting a pathway for cholesterol movement from the inner membrane leaflet to the CRD. All Smoothened antagonists bind the transmembrane domain and block tunnel opening, but cyclopamine also binds the CRD, inducing the active transmembrane conformation. Together, these results define the mechanisms of Smoothened activation and inhibition.

Huang, Pengxiang↗

Systematic identification of transcriptional activation domains from non-transcription factor proteins in plants and yeast

Transcription factors can promote gene expression through activation domains. Whole-genome screens have systematically mapped activation domains in transcription factors but not in non-transcription factor proteins (e.g., chromatin regulators and coactivators). To fill this knowledge gap, we employed the activation domain predictor PADDLE to analyze the proteomes of Arabidopsis thaliana and Saccharomyces cerevisiae. We screened 18,000 predicted activation domains from >800 non-transcription factor genes in both species, confirming that 89% of candidate proteins contain active fragments. Our work enables the annotation of hundreds of nuclear proteins as putative coactivators, many of which have never been ascribed any function in plants. Analysis of peptide sequence compositions reveals how the distribution of key amino acids dictates activity. Finally, we validated short, "universal" activation domains with comparable performance to state-of-the-art activation domains used for genome engineering. Our approach enables the genome-wide discovery and annotation of activation domains that can function across diverse eukaryotes.

59 BASIC BIOLOGICAL SCIENCES↗

A one-pot, solid-state route for realizing highly visible light active Na-doped gC{sub 3}N{sub 4} photocatalysts

The visible light photocatalytic activity of graphitic carbon nitride (gC{sub 3}N{sub 4}), a promising metal-free photocatalytic material, is rather low, and is not as good as expected. Herein, to realize improved photocatalytic activity, sodium-doped gC{sub 3}N{sub 4} (Na-gC{sub 3}N{sub 4}) is prepared through a novel solid-state process based on the thermal polycondensation of urea in the presence of sodium chloride and ammonium chloride. The proposed solid-state process is simple, requires no solvent, and provides a general route for rapid and large-scale synthesis of metal-doped gC{sub 3}N{sub 4}. The Na species exist in + 1 oxidation state and bind N atoms in the nitride ring of gC{sub 3}N{sub 4}. The photocatalytic activity improvement of gC{sub 3}N{sub 4} for the mineralization of 17α-ethynylestradiol (EE2) under visible light is seen after the Na doping. The improved photocatalytic activity is due to increased absorption of light, increased separation of charge carriers, stronger oxidation ability of valance band holes, and increased specific surface area. The typical photocatalytic activity of 0.6 wt% Na-gC{sub 3}N{sub 4} for the EE2 mineralization with an initial EE2 concentration of 1 mg/L and a catalyst concentration of 1 g/L is 95.7% within 2 h of visible light irradiation. Under identical experimental conditions, the EE2 mineralization by pristine gC{sub 3}N{sub 4} is only 23.5%. - Graphical abstract: Highly visible light active Na-gC{sub 3}N{sub 4} photocatalysts were simply synthesized through a novel one-pot route based on the thermal polycondensation of urea. The doped Na species plays a critical role in improving the photocatalytic activity. Display Omitted - Highlights: • A new solid-state route is introduced to obtain visible light active Na-doped gC{sub 3}N{sub 4}. • The proposed synthesis route is fast, simple, and highly scalable. • Na doping leads to improved light absorption capability. • Na doping leads to improved separation of charge carriers. • Na doping leads to improved photocatalytic activity under visible light.

37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CH↗

TiO{sub 2}/Bi{sub 2}(BDC){sub 3}/BiOCl nanoparticles decorated ultrathin nanosheets with excellent photocatalytic reaction activity and selectivity

Graphical abstract: TiO{sub 2}/Bi{sub 2}(BDC){sub 3}/BiOCl nanoparticles decorated ultrathin nanosheets showed excellent photocatalytic reaction activity and selectivity. - Highlights: • TiO{sub 2}/Bi{sub 2}(BDC){sub 3}/BiOCl nanoparticles decorated ultrathin nanosheets were synthesized through a facile hydrothermal process. • The products showed excellent photocatalytic activities for the degradation of various dyes. • The photocatalytic activities of the composite materials could be easily adjusted through tuning the content of TiO{sub 2}. • TiO{sub 2}/Bi{sub 2}(BDC){sub 3}/BiOCl displayed obvious photocatalytic selectivity in mixed dyes systems of rhodamine B and eosin Y. - Abstract: Photocatalysts with excellent photocatalytic reaction activity and ideal selectivity are highly desirable for pollutants clearance and purification of targeted organics from a mixture. Continued efforts toward the goal, we here present a facile hydrothermal route to synthesize TiO{sub 2}/Bi-benzenedicarboxylate/BiOCl nanoparticles decorated ultrathin nanosheets with a thickness less than 5 nm on a large scale. The as-synthesized products showed excellent photocatalytic activities for the degradation of various dyes such as rhodamine B, eosin Y and methylene blue in aqueous solution under visible light irradiation. The photocatalytic activities of TiO{sub 2}/Bi-benzenedicarboxylate/BiOCl nanocomposites for the degradation of rhodamine B and eosin Y could be adjusted through tuning the content of TiO{sub 2}. With increasing the amount of TiO{sub 2}, the composites showed declining photocatalytic activities in decomposing of rhodamine B while on the contrary they displayed enhanced photocatalytic activities in decomposing of eosin Y. Interestingly, TiO{sub 2}/Bi-benzenedicarboxylate/BiOCl composite nanosheets showed obvious photocatalytic selectivity in a mixed dyes system. The photocatalytic reaction and selectivity mechanisms of the nanocomposites for the degradation of the dyes were discussed on the basis of experimental results. The current study not only develops a new methodology to synthesize ultrathin nanosheets but also provides a novel strategy to design composite photocatalysts with high reaction activity and good selectivity.

36 MATERIALS SCIENCE↗

Preparation and catalytic activities for H{sub 2}O{sub 2} decomposition of Rh/Au bimetallic nanoparticles

Graphical abstract: PVP-protected Rh/Au bimetallic nanoparticles (BNPs) were prepared by using hydrogen sacrificial reduction method, the activity of Rh80Au20 BNPs were about 3.6 times higher than that of Rh NPs. - Highlights: • Rh/Au bimetallic nanoparticles (BNPs) of 3∼5 nm in diameter were prepared. • Activity for H{sub 2}O{sub 2} decomposition of BNPs is 3.6 times higher than that of Rh NPs. • The high activity of BNPs was caused by the existence of charged Rh atoms. • The apparent activation energy for H{sub 2}O{sub 2} decomposition over the BNPs was calculated. - Abstract: PVP-protected Rh/Au bimetallic nanoparticles (BNPs) were prepared by using hydrogen sacrificial reduction method and characterized by UV–vis, XRD, FT-IR, XPS, TEM, HR-TEM and DF-STEM, the effects of composition on their particle sizes and catalytic activities for H{sub 2}O{sub 2} decomposition were also studied. The as-prepared Rh/Au BNPs possessed a high catalytic activity for the H{sub 2}O{sub 2} decomposition, and the activity of the Rh{sub 80}Au{sub 20} BNPs with average size of 2.7 nm were about 3.6 times higher than that of Rh monometallic nanoparticles (MNPs) even the Rh MNPs possess a smaller particle size of 1.7 nm. In contrast, Au MNPs with size of 2.7 nm show no any activity. Density functional theory (DFT) calculation as well as XPS results showed that charged Rh and Au atoms formed via electronic charge transfer effects could be responsible for the high catalytic activity of the BNPs.

36 MATERIALS SCIENCE↗

Activated biomass carbon made from bamboo as electrode material for supercapacitors

Highlights: • Activated biomass carbon (ABC) produced from bamboo was prepared by carbonization and KOH activation. • The BET and morphology of the ABC have a strong dependence on the activation temperature. • High specific capacitance along with durability is achieved. • Activated biomass carbon can serve as efficient electrode material for energy storage. - Abstract: Activated biomass carbons (ABC) produced from bamboo by carbonization and activation have high specific surface areas and mesoporous structures. The specific surface area, total pore volume, and average pore size of the activated biomass carbon are controlled by adjusting the activation temperature from 700 to 1000 °C. The carbon materials activated at 900 °C have an optimal mesoporous structure with a high specific surface area (2221.1 m{sup 2} g{sup −1}), the highest capacitance (293 F g{sup −1} at 0.5 A g{sup −1} in 3 M KOH aqueous electrolyte) and excellent rate capability (193.8 F g{sup −1} at 20 A g{sup −1}). Symmetric supercapacitors made of the optimal electrodes exhibit a high energy density of 10.9 Wh kg{sup −1} (18.2 Wh L{sup −1}) at a power density of 63 W kg{sup −1} (105 W L{sup −1}) and outstanding capacitance retention of 91.8% over 10,000 cycles. The high electrochemical performance of the mesoporous ABCs show that they are highly promising for energy-storage applications with further optimization.

77 NANOSCIENCE AND NANOTECHNOLOGY↗

How “hot” are hotspots: Statistically localizing the high-activity areas on soil and rhizosphere images

The topic of microbial hotspots in soil requires not only visualizing their spatial distribution and biochemical analyses, but also statistical approaches to identify these hotspots and separate them from the surrounding activities (background). We hypothesized that each hotspot type (e.g. enzyme activities in the rhizosphere, root exudation, localization of herbicide accumulation) is a result of local process driven by biotic and/or abiotic factors, and the process rates in the hotspots are much faster than those in the soil background. We further hypothesized that the background and hotspot activities in soil belong to different statistical distributions. Consequently, hotspot determination should be based on statistical separation of activities significantly higher than the background. We analyzed for the statistical distributions of grey values on three groups of published images: 1) 14 C images of carbon input by roots into the rhizosphere, 2) 14 C glyphosate accumulation in the plant, and 3) zymogram of leucine aminopeptidase activity in rooted soil. The two Gaussian distributions were fit (the first representing the background, the second the hotspots) to the distribution of grey values in the images, the parameters (means and standard deviations, SD) of the fitted distributions were calculated, and the background was removed. Thus, we identified hotspots as areas outside of the Mean+2SD image intensity (corresponding to the upper ~ 2.5% of activity, being over 97.5% of background values) and finally, visualized images of solely hotspot locations. Finally, these results were compared with previously used decisions on hotspot intensity thresholding (i.e. Top-25% and 17 standard thresholding approaches in ImageJ) and discussed the advantages of the Mean+2SD as well as Mean+3SD approaches. These advantages include: i) simple unification of the thresholding approach for several imaging methods with various principles of activity distribution, ii) identification of hotspots with various activity levels, iii) analysis of “time-specific” hotspots in temporal sequences of images. Compared with 17 standard thresholding methods, we concluded that objectively elucidating and separating the hotspots should be based on statistical distribution analysis, e.g. using the Mean+2SD or Mean+3SD approaches. Furthermore, this simple Mean+2SD approach delivered suitable results for three groups of images and so, helps to understand the processes responsible for the highest activities and elucidate hotspots.

59 BASIC BIOLOGICAL SCIENCES↗

Totarol prevents neuronal injury in vitro and ameliorates brain ischemic stroke: Potential roles of Akt activation and HO-1 induction

The natural product totarol, a phenolic diterpenoid and a major constituent isolated from the sap of Podocarpus totara, has been reported to have a potent antimicrobial activity. In this study, we determined whether totarol possessed an additional neuroprotective activity in vitro and in vivo. We found that totarol prevented glutamate- and oxygen and glucose deprivation-induced neuronal death in primary rat cerebellar granule neuronal cells and cerebral cortical neurons. Totarol increased Akt and GSK-3β phosphorylation, Nrf2 and heme oxygenase-1 (HO-1) protein expressions and suppressed oxidative stress by increasing GSH and SOD activities. The PI3K/Akt inhibitor LY294002 prevented totarol neuroprotective effect by suppressing the totarol-induced changes in HO-1 expression and the activities of GSH and SOD. The HO-1 inhibitor ZnPPIX also prevented totarol-increased GSH and SOD activities. In a model of acute cerebral ischemic injury in Sprague–Dawley rats, produced by occlusion of the middle cerebral artery for 2 h followed by 22 h or 46 h of reperfusion, totarol significantly reduced infarct volume and improved the neurological deficit. In this model, totarol increased HO-1 expression and the activities of GSH and SOD. These observations suggest that totarol may be a novel activator of the Akt/HO-1 pathway protecting against ischemic stroke through reduction of oxidative stress. - Graphical abstract: It is unknown whether the natural product totarol has neuroprotective effects in vitro and in vivo. This study underscores that totarol prevents neuronal injury in vitro, not only by activating PI3K/Akt pathway, but also via induction of Nrf2, HO-1, GSH and SOD expressions. Totarol also ameliorated acute cerebral ischemic injury in a rat ischemic stroke model. The findings highlight that totarol may be exploited for protecting against ischemic stroke through Akt/HO-1 pathway. - Highlights: • Totarol protects glutamate- and OGD-induced neuronal injury in vitro. • Totarol activates PI3K/Akt pathway in neurons. • Totarol induces HO-1, GSH and SOD expression in vitro and in vivo. • Totarol exhibits neuroprotective effects in rat brain ischemic stroke model.

60 APPLIED LIFE SCIENCES↗

2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) increases necroinflammation and hepatic stellate cell activation but does not exacerbate experimental liver fibrosis in mice

2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is a persistent environmental contaminant and high-affinity ligand for the aryl hydrocarbon receptor (AhR). Increasing evidence indicates that AhR signaling contributes to wound healing, which involves the coordinated deposition and remodeling of the extracellular matrix. In the liver, wound healing is attributed to the activation of hepatic stellate cells (HSCs), which mediate fibrogenesis through the production of soluble mediators and collagen type I. We recently reported that TCDD treatment increases the activation of human HSCs in vitro. The goal of this study was to determine how TCDD impacts HSC activation in vivo using a mouse model of experimental liver fibrosis. To elicit fibrosis, C57BL6/male mice were treated twice weekly for 8 weeks with 0.5 ml/kg carbon tetrachloride (CCl{sub 4}). TCDD (20 μg/kg) or peanut oil (vehicle) was administered once a week during the last 2 weeks. Results indicate that TCDD increased liver-body-weight ratios, serum alanine aminotransferase activity, and hepatic necroinflammation in CCl{sub 4}-treated mice. Likewise, TCDD treatment increased mRNA expression of HSC activation and fibrogenesis genes, namely α-smooth muscle actin, desmin, delta-like homolog-1, TGF-β1, and collagen type I. However, TCDD treatment did not exacerbate fibrosis, nor did it increase the collagen content of the liver. Instead, TCDD increased hepatic collagenase activity and increased expression of matrix metalloproteinase (MMP)-13 and the matrix regulatory proteins, TIMP-1 and PAI-1. These results support the conclusion that TCDD increases CCl{sub 4}-induced liver damage and exacerbates HSC activation, yet collagen deposition and the development of fibrosis may be limited by TCDD-mediated changes in extracellular matrix remodeling. - Highlights: • TCDD increased liver damage and inflammation in mice treated with CCl{sub 4}. • TCDD treatment enhanced markers of hepatic stellate cell activation and fibrogenesis. • TCDD did not increase the deposition of collagen type I or the severity of liver fibrosis. • TCDD increased hepatic collagenase activity and expression of matrix metalloproteinase-13.

60 APPLIED LIFE SCIENCES↗

Locomotor activity and tissue levels following acute administration of lambda- and gamma-cyhalothrin in rats

Pyrethroids produce neurotoxicity that depends, in part, on the chemical structure. Common behavioral effects include locomotor activity changes and specific toxic syndromes (types I and II). In general these neurobehavioral effects correlate well with peak internal dose metrics. Products of cyhalothrin, a type II pyrethroid, include mixtures of isomers (e.g., λ-cyhalothrin) as well as enriched active isomers (e.g., γ-cyhalothrin). We measured acute changes in locomotor activity in adult male rats and directly correlated these changes to peak brain and plasma concentrations of λ- and γ-cyhalothrin using a within-subject design. One-hour locomotor activity studies were conducted 1.5 h after oral gavage dosing, and immediately thereafter plasma and brains were collected for analyzing tissue levels using LC/MS/MS methods. Both isomers produced dose-related decreases in activity counts, and the effective dose range for γ-cyhalothrin was lower than for λ-cyhalothrin. Doses calculated to decrease activity by 50% were 2-fold lower for the γ-isomer (1.29 mg/kg) compared to λ-cyhalothrin (2.65 mg/kg). Salivation, typical of type II pyrethroids, was also observed at lower doses of γ-cyhalothrin. Administered dose correlated well with brain and plasma concentrations, which furthermore showed good correlations with activity changes. Brain and plasma levels were tightly correlated across doses. While γ-cyhalothrin was 2-fold more potent based on administered dose, the differences based on internal concentrations were less, with γ-cyhalothrin being 1.3- to 1.6-fold more potent than λ-cyhalothrin. These potency differences are consistent with the purity of the λ-isomer (approximately 43%) compared to the enriched isomer γ-cyhalothrin (approximately 98%). Thus, administered dose as well as differences in cyhalothrin isomers is a good predictor of behavioral effects. - Highlights: • Acute changes in locomotor activity were produced by λ- and γ-cyhalothrin. • γ-Cyhalothrin was about 2-fold more potent than λ-cyhalothrin. • Brain and plasma levels were tightly correlated across doses. • Activity changes correlated well with brain and plasma concentrations.

60 APPLIED LIFE SCIENCES↗