Toward Stable Co-Saliency Detection and Object Co-Segmentation.

In this paper, we present a novel model for simultaneous stable co-saliency detection (CoSOD) and object co-segmentation (CoSEG). To detect co-saliency (segmentation) accurately, the core problem is to well model inter-image relations between an image group. Some methods design sophisticated modules, such as recurrent neural network (RNN), to address this problem. However, order-sensitive problem is the major drawback of RNN, which heavily affects the stability of proposed CoSOD (CoSEG) model. In this paper, inspired by RNN-based model, we first propose a multi-path stable recurrent unit (MSRU), containing dummy orders mechanisms (DOM) and recurrent unit (RU). Our proposed MSRU not only helps CoSOD (CoSEG) model captures robust inter-image relations, but also reduces order-sensitivity, resulting in a more stable inference and training process. Moreover, we design a cross-order contrastive loss (COCL) that can further address order-sensitive problem by pulling close the feature embedding generated from different input orders. We validate our model on five widely used CoSOD datasets (CoCA, CoSOD3k, Cosal2015, iCoseg and MSRC), and three widely used datasets (Internet, iCoseg and PASCAL-VOC) for object co-segmentation, the performance demonstrates the superiority of the proposed approach as compared to the state-of-the-art (SOTA) methods.

Valorization of Chinese hickory shell as novel sources for the efficient production of xylooligosaccharides.

Chinese hickory shell, a by-product of the food industry, is still not utilized and urgent to develop sustainable technologies for its valorization. This research focuses on the systematical evaluation of degraded products and xylooligosaccharide production with high yield from the shell via hydrothermal process. The pretreatment was carried out in a bath pressurized reactor at 140-220 °C for 0.5-2 h. The results indicated that the pretreatment condition strongly affected the chemical structures and compositions of the liquid fraction. The maximum yield of XOS (55.3 wt%) with limitation of by-products formation was achieved at 160 °C for 2 h. High temperature (220 °C) and short time (0.5 h) contributed to hydrolysis of xylooligosaccharide with high DP to yield 37.5 wt% xylooligosaccharide with DP from 2 to 6. Xylooligosaccharide obtained mainly consisted of xylan with branches according to the HSQC NMR analysis. Overall, the production of XOS with a high yield from food waste will facilitate the valorization of food waste in the biorefinery industry.

Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin.

Mimicking different pharmacophoric units into one scaffold is a promising structural modification tool to design new drugs with enhanced biological properties. To continue our research on the tubulin inhibitors, the synthesis and biological evaluation of arylpyridine derivatives (9-29) are described herein. Among these compounds, 6-arylpyridines (13-23) bearing benzo[d]imidazole side chains at the 2-position of pyridine ring displayed selective antiproliferative activities against HT-29 cells. More interestingly, 2-trimethoxyphenylpyridines 25, 27, and 29 bearing benzo[d]imidazole and benzo[d]oxazole side chains displayed more broad-spectrum antitumor activities against all tested cancer cell lines. 29 bearing a 6-methoxybenzo[d]oxazole group exhibited comparable activities against A549 and U251 cells to combretastatin A-4 (CA-4) and lower cytotoxicities than CA-4 and 5-Fu. Further investigations revealed 29 displays strong tubulin polymerization inhibitory activity (IC50 = 2.1 µM) and effectively binds at the colchicine binding site and arrests the cell cycle of A549 in the G2/M phase by disrupting the microtubules network.

Novel recyclable deep eutectic solvent boost biomass pretreatment for enzymatic hydrolysis.

Deep eutectic solvent (DES) with protonic acid shows the great potential for biomass valorization. However, the acid corrosion and recycling are still severe challenges in biorefinery. Herein, a novel DES by coordinating FeCl3 in choline chloride/glycerol DES was designed for effective and recyclable pretreatment. As compared to DESs with FeCl2, ZnCl2, AlCl3 and CuCl2, DES with FeCl3 approvingly retained most of cellulose in pretreated Hybrid Pennisetum (95.2%). Meanwhile, the cellulose saccharification significantly increased to 99.5%, which was six-fold higher than that of raw biomass. The excellent pretreatment performance was mainly attributed to the high removal of lignin (78.88 wt%) and hemicelluloses (93.63 wt%) under the synergistic effect of Lewis acid and proper hydrogen-bond interaction of DES with FeCl3. Furthermore, almost all cellulose still can be converted into glucose after five recycling process. Overall, the process demonstrated designed pretreatment was great potential for the low-cost biorefinery and boost the biofuel development.

Discovery of arylbenzylamines as PDE4 inhibitors with potential neuroprotective effect.

Growing evidence confirms the potential of PDE4 inhibitors for the treatment of Parkinson's disease. Our reported PDE4 inhibitors FCPR16 and FCPR03 have displayed neuroprotective effects in SH-SY5Y cells, but have very low oral bioavailability. To access analogues with improved bioavailability, a new series of arylbenzylamine derivatives were designed and synthesized. Preliminary screening results of the series showed that arylbenzylamine derivatives bearing a pyridin-3-amine side chain displayed good inhibitory activities against human PDE4B1 and PDE4D7 isoforms. Moreover, kinetic studies revealed that the most potent compounds 11r and 11s with mid-nanomolar IC50 values partially bind to PDE4B1 (Imax = 93% and 90% respectively). Molecular docking results revealed the possible interactions of compounds 11r and 11s with upstream conserved region 2 (UCR2) of PDE4B1, which illuminate possible reasons for their partial inhibition against PDE4. Using a cell-based model of PD, compounds 11r and 11s were found to alleviate cellular apoptosis in SH-SY5Y cells induced by MPP+ (1-methyl-4-phenylpyridinium), with this neuroprotective effect being greater than PDE4 inhibitor rolipram. Furthermore, compound 11r displayed nearly sevenfold oral bioavailability (8.20%) than FCPR03 (1.23%).

Discovery of 2-(3,4-dialkoxyphenyl)-2-(substituted pyridazin-3-yl)acetonitriles as phosphodiesterase 4 inhibitors with anti-neuroinflammation potential based on three-dimensional quantitative structure-activity relationship study.

Phosphodiesterase 4 (PDE4) inhibitors with potential activities for CNS disorders provide a new therapeutic strategy for depression. To discover PDE4 inhibitors with anti-neuroinflammation activities, reliable three-dimensional quantitative structure-activity relationship (3D-QSAR) models on our previous reported catecholic PDE4 inhibitors was built with a statistically significant cross-validated coefficient (q2 ), conventional coefficient (r2 ), and good predictive capabilities based on the molecular docking results, using comparative molecular field analysis (CoMFA) and comparative molecular similarity index analysis (CoMSIA) methods. Based on the analysis of CoMFA and CoMSIA contour maps, a series of 2-(3,4-dialkoxyphenyl)-2-(substituted pyridazin-3-yl) acetonitriles 16a-i was designed and synthesized. Among these compounds, compound 16a exhibited good inhibitory activities toward PDE4B1 and PDE4D7 with mid-nanomolar IC50 values and potential anti-neuroinflammation activity in BV-2 cells. Docking simulation of compound 16a in the PDE4 catalytic domain activity pocket revealed that compound 16a maybe assumed a "V-shaped" conformation, extending the side chain to S-pocket.

Study on changes of blood electrolyte levels and assessment of mortality rate in patients with different degrees of craniocerebral injury / 国际检验医学杂志

Objective To investigate the relationship between electrolyte level change with prognosis in the patients with craniocerebral injury.Methods A total of 360 patients with craniocerebral injury in this hospital during 2012-2015 were selected as the research subjects and divided into the mild craniocerebral injury group (171 cases),moderate craniocerebral injury group(104 cases)and severe craniocerebral injury group(85 cases) according to the Glasgow coma scale.The severe craniocerebral injury group was further divided into the high level blood sodium subgroup(73 cases)and stable level blood sodium subgroup(12 cases)according to the lev-el of blood sodium,meanwhile 70 persons undergoing healthy physical examination were selected as the control group.The plasma electrolyte levels(blood sodium,potassium,chloride)in each group were detected within 5 d after admission.Then the results were statistically analyzed.Results Compared with the control group,the blood sodium,potassium and chloride levels had no statistical difference between the mild and moderate craniocerebral injury groups(P>0.05).The blood sodium and chloride levels in the severe craniocerebral inju-ry group were higher than those in the mild and moderate craniocerebral injury groups,the difference was sta-tistically significant(P<0.01).The blood potassium level had no statistical difference between the mild,mod-erate and severe craniocerebral injury groups with control group(P>0.05).In the severe craniocerebral injury group,there were 58 cases(79.45%)of death in the high level blood sodium subgroup and 4 cases(33.33%) of death in the stable level blood sodium subgroup,the difference was statistically significant(P<0.01).Con-clusion Clinically monitoring the blood sodium level change in the patients with craniocerebral injury,espe-cially severe craniocerebral injury,is conducive to the disease recovery.