Diethyl 6,9,17,20-tetra­bromo-2,13-di­oxo­hexa­cyclo­[10.10.2.03,24.05,10.014,23.016,21]tetra­cosa-5,7,9,16,18,20-hexa­ene-23,24-dicarboxyl­ate

In the title mol­ecule, C26H22Br4N4O6, the dihedral angle between the aromatic rings is 30.0 (1)°. One ethyl fragment is disordered between two positions in a 1:1 ratio. The crystal packing exhibits weak inter­molecular C—H⋯O hydrogen bonds and short Br⋯O contacts of 3.349 (6) Å

Diethyl 2-tert-butyl-4,11-dioxo-2,3-di­hydro-cis-1H,5H,10H-2,3a,4a,10a,11a-penta­azabenzo[f]indeno[2,1,7-ija]azulene-11b,11c-dicarboxyl­ate

In the title mol­ecule, C24H31N5O6, the two ethyl fragments are each disordered over two conformations [occupancy ratios 0.58 (13)/0.42 (13) and 0.56 (12)/0.44 (12)]. The crystal packing exhibits inter­molecular non-classical C—H⋯O hydrogen bonds and π–π inter­actions between benzene rings [centroid–centroid distances = 3.836 (5) Å]

Circ_0000284 facilitates the growth, metastasis and glycolysis of intrahepatic cholangiocarcinoma through miR-152-3p-mediated PDK1 expression

Background. Circular RNAs (circRNAs) are key molecules in the regulation of intrahepatic cholangiocarcinoma (ICC) progression. The purpose of this study was to analyze the function and underlying molecular mechanism of circ_0000284 in ICC. Methods. Quantitative real-time PCR was used to analyze the circ_0000284, microRNA (miR)-152-3p and pyruvate dehydrogenase kinase 1 (PDK1) expression. Cell proliferation, apoptosis, invasion and migration were executed by cell counting kit 8 assay, EdU assay, flow cytometry, transwell assay and wound healing assay, respectively. All protein expression levels were examined using western blot analysis. Cell glycolysis was analyzed by detecting glucose consumption, lactate production and ATP/ADP ratios. Target relationship was estimated by dual-luciferase reporter assay. The effect of circ_0000284 on ICC tumor growth in vivo was evaluated by constructing xenograft mice model. Results. We detected high expression of circ_0000284 in ICC tumor tissues and cells. Downregulated circ_0000284 inhibited ICC cell proliferation, invasion, migration, glycolysis, and accelerated apoptosis. MiR-152-3p was sponged by circ_0000284, and its inhibitor revoked the effect of circ_0000284 knockdown on ICC cell progression. PDK1 was a target of miR-152-3p, and its expression was suppressed by circ_0000284 knockdown. PDK1 overexpression reversed the inhibition effect of miR-152-3p on ICC cell growth, metastasis and glycolysis. In animal experiments, circ_0000284 downregulation also inhibited ICC tumor growth. Conclusion. Circ_0000284 promoted the growth, metastasis and glycolysis of ICC by miR-152-3p/PDK1 pathway, showing that circ_0000284 was a potential therapeutic target for ICC

A Novel Temperature Model of Regions Formed during the Preheating Stage of Belt Heating in Incremental Sheet Forming

The temperature of a forming region has a gradient distribution characteristic in the belt heating incremental sheet forming process, in which the relation between the heating power and the temperature distribution is ambiguous in the pre-heating stage. The setup of the heating power is therefore challenging, and the whole forming efficiency might decrease due to the above issue. Therefore, this paper proposes a belt heating method for electric conduction heating and presents a temperature calculation model for the forming region of the plate in the preheating state based on the heat conduction model. The calculated accuracy of the model is analysed through physical experiments, and the thermal transfer efficiency of heating tubes is analysed in detail. Based on the result, the thermal transfer efficiency value for heating tubes is determined to improve the accuracy of the suggested model. In addition, the effect of the model slope on the calculated result is further analysed, and the setting method of the slope value for the model is proposed according to different accuracy requirements

Over-expression of human cytomegalovirus miR-US25-2-3p downregulates eIF4A1 and inhibits HCMV replication

AbstractIt has been reported that human cytomegalovirus (HCMV) miR-US25-2 reduces DNA viral replication including HCMV. However, the mechanism remains unknown. In our study, eukaryotic translation initiation factor 4A1 (eIF4A1) was identified to be a direct target of miR-US25-2-3p. Small interfering RNA (siRNA) and miR-US25-2-3p mediated eIF4A1 knockdown experiments revealed that high level of miR-US25-2-3p in MRC-5 cells decreased HCMV and host genomic DNA synthesis, and inhibited cap-dependent translation and host cell proliferation. However, eIF4A1 up-regulation induced by miR-US25-2-3p inhibitor increased HCMV copy number. Therefore, the over-expression of miR-US25-2-3p and consequent lower expression of eIF4A1 may contribute to the inhibition of HCMV replication

Inhibicija lipidne peroksidacije pomoću enzimskih hidrolizata izoliranih iz pšeničnih mekinja

Wheat bran, an important by-product of the cereal industry, is rich in potentially health-promoting phenolic compounds. The phenolics are mainly esterified to the cell wall polysaccharides. In our previous paper, wheat bran was destarched and deproteinated by α-amylase, protease and amyloglucosidase successively and further hydrolyzed using Bacillus subtilis xylanases, and the enzymatic hydrolysates from wheat bran (EHWB) showed good scavenging activity in vitro. The aim of this study is to further characterize the antioxidant potential of EHWB against various systems, both ex vivo and in vivo, namely, rat liver microsomal lipid peroxidation systems induced by Fe2+/H2O2 and Fe3+-adenosine diphosphate (ADP)/dihydronicotinamide adenine dinucleotide phosphate (NADPH), copper- and 2,2’-azo-bis(2-amidinopropane) dihydrochloride (AAPH)-induced human low-density lipoprotein (LDL) oxidation systems, and alloxan-induced in vivo lipid peroxidation in mice. EHWB inhibited lipid peroxidation in rat liver microsomes induced by Fe2+/H2O2 and Fe3+-ADP/NADPH in a concentration-dependent manner with 90.3 and 87 % inhibition of lipid peroxidation at 50 mg/L, respectively, which were similar to that of butylated hydroxytoluene (BHT) at 20 mg/L. The antioxidant potential of EHWB at a concentration ranging from 10 to 20 mg/L in the nonenzymatic system was more effective than in the enzymatic system. EHWB strongly inhibited in vitro copper- and AAPH-mediated oxidation of LDL in a concentration- and time-dependent manner with 52.41 and 63.03 % inhibition at 20 mg/L, respectively, which were similar to that of ascorbate at 10 mg/L. EHWB significantly decreased the level of thiobarbituric acid reactive substances (TBARS) and increased the activities of glutathione peroxidase (GSH-Px), catalase (CAT) and superoxide dismutase (SOD) in serum and liver of alloxan-treated mice compared with the control. These results demonstrated that EHWB might be efficient in the protection of food products and humans against free radical-induced oxidative damage.Pšenične su mekinje važan nusproizvod u proizvodnji žitarica, jer su bogate fenolnim spojevima što pozitivno utječu na zdravlje. Fenoli se uglavnom vežu esterskom vezom na staničnu stijenku polisaharida. U prijašnjem su istraživanju pomoću α-amilaze, proteaze i amiloglukozidaze iz pšeničnih mekinja uklonjeni škrob i proteini, te su enzimskom hidrolizom pomoću ksilanaza iz bakterije Bacillus subtilis dobiveni hidrolizati, koji su učinkovito uklanjali slobodne radikale in vitro. Svrha je ovoga rada bila iscrpnije opisati antioksidativni učinak tih hidrolizata ex vivo i in vivo u različitim sustavima, i to: sustavima lipidne peroksidacije mikrosoma u jetri štakora induciranih pomoću Fe2+/H2O2 i Fe3+-adenozin difosfata (ADP)/dihidronikotinamid adenin dinukleotid fosfata (NADPH), sustavima oksidacije humanoga lipoproteina male gustoće (LDL) induciranih pomoću bakra i 2,2\u27-azo-bis(2-amidinopropan) dihidroklorida (AAPH), te in vivo lipidnoj peroksidaciji u miševa induciranoj pomoću aloksana. Enzimski su hidrolizati iz pšeničnih mekinja u koncentraciji od 50 mg/L inhibirali lipidnu peroksidaciju u mikrosomima jetre štakora induciranu pomoću Fe2+/H2O2 za 90,3 %, a onu induciranu pomoću Fe3+-ADP/NADPH za 87 %. Taj je učinak sličan učinku butiliranog hidroksitoluena (BHT) u koncentraciji od 20 mg/L. Antioksidativni je učinak enzimskih hidrolizata iz pšeničnih mekinja u koncentracijama od 10 do 20 mg/L bio veći u neenzimskim nego u enzimskim sustavima. Hidrolizati su, ovisno o njihovoj koncentraciji (20 mg/L) i vremenu reakcije, znatno inhibirali in vitro oksidaciju LDL, i to onu induciranu bakrom za 52,41 %, a oksidaciju induciranu pomoću AAPH za 63,03 %, što je slično učinku askorbata pri koncentraciji od 10 mg/L. Također su bitno smanjili količinu reaktivnih spojeva tiobarbiturne kiseline i povećali aktivnost glutation-peroksidaze, katalaze i superoksid dismutaze u serumu i jetri miševa tretiranih aloksanom, u usporedbi s kontrolnim uzorkom. Rezultati pokazuju da enzimski hidrolizati iz pšeničnih mekinja mogu biti korisni u zaštiti prehrambenih proizvoda i zdravlja ljudi od oksidacijskih oštećenja uzrokovanih slobodnim radikalima