Twin Boundary Superstructures Assembled by Periodic Segregation of Solute Atoms.

Twinning is a common deformation mechanism in metals, and twin boundary (TB) segregation of impurities/solutes plays an important role in the performances of alloys such as thermostability, mobility, and even strengthening. The occurrence of such segregation phenomena is generally believed as a one-layer coverage of solutes alternately distributed at extension/compression sites, in an orderly, continuous manner. However, in the Mn-free and Mn-containing Mg-Nd model systems, we reported unexpected three- and five-layered discontinuous segregation patterns of the coherent {101̅1} TBs, and not all the extension sites occupied by solutes larger in size than Mg, and even some larger sized solutes taking the compression sites. Nd/Mn solutes selectively segregate at substitutional sites and thus to generate two new types of ordered two-dimensional TB superstructures or complexions. These findings refresh the understanding of solute segregation in the perfect coherent TBs and provide a meaningful theoretical guidance for designing materials via targeted TB segregation.

Y-shaped bis-arylethenesulfonic acid esters: Potential potent and membrane permeable protein tyrosine phosphatase 1B inhibitors.

Known PTP1B inhibitors with bis-anionic moieties exhibit potent inhibitory activity, good selectivity, however, they are incapable of penetrating cellular membranes. Based upon our finding of a new pharmacophoric group in inhibition of PTP1B and the structural characteristics of the binding pocket of PTP1B, a series of bis-arylethenesulfonic acid ester derivatives were designed and synthesized. These novel molecules, particularly Y-shaped bis-arylethenesulfonic acid ester derivatives, exhibited high PTP1B inhibitory activity, moderate selectivity, and great potential in penetrating cellular membranes (compound 7p, CLogP=9.73, Papp=9.6×10-6cm/s; IC50=140, 1290 and 920nM on PTP1B, TCPTP and SHP2, respectively). Docking simulations suggested that these Y-shaped inhibitors might interact with multiple secondary binding sites in addition to the catalytic site of PTP1B.

Antiproliferative activity and SARs of caffeic acid esters with mono-substituted phenylethanols moiety.

A series of CAPE derivatives with mono-substituted phenylethanols moiety were synthesized and evaluated by MTT assay on growth of 4 human cancer cell lines (Hela, DU-145, MCF-7 and ECA-109). The substituent effects on the antiproliferative activity were systematically investigated for the first time. It was found that electron-donating and hydrophobic substituents at 2'-position of phenylethanol moiety could significantly enhance CAPE's antiproliferative activity. 2'-Propoxyl derivative, as a novel caffeic acid ester, exhibited exquisite potency (IC50=0.4±0.02 & 0.6±0.03µM against Hela and DU-145 respectively).

Characterization and Potential Antitumor Activity of Polysaccharide from Gracilariopsis lemaneiformis.

Substances with valuable antitumor properties have been identified in many marine algae, including an edible polysaccharide from the marine alga Gracilariopsis lemaneiformis (PGL). We previously reported transcriptome profiling data showing that PGL induced transcriptional alterations generate anti-lung cancer activity. To identify how PGL is detrimental to tumors, we purified PGL to characterize its chemical composition, molecular weight, and sugar and protein content and investigated its antitumor activity. We demonstrated that PGL exerted its antitumor activities by modulating cell viability, morphology, apoptosis, and the apoptosis-related Fas/FasL signaling pathway in the human lung cancer cell line A549, the gastric cancer cell line MKN28, and the mouse melanoma cell line B16. Our data provide the first evidence that PGL inhibits cell proliferation by inducing apoptosis, which is largely mediated by Fas/FasL in cancer cells, suggesting that PGL might be a novel therapeutic agent against cancer.

A Novel Robotic Bronchoscope System for Navigation and Biopsy of Pulmonary Lesions.

Transbronchial biopsy sampling, as a minimally invasive method with relatively low risk, has been proved to be a promising treatment in the field of respiratory surgery. Although several robotic bronchoscopes have been developed, it remains a great challenge to balance size and flexibility, while integrating multisensors to realize navigation during complex airway networks. This paper proposes a novel robotic bronchoscope system composed by end effector with relatively small size, relevant actuation unit, and navigation system with path planning and surgical guidance capability. The main part of the end effector is machined by bidirectional groove on a nickel-titanium tube, which can realize bending, rotation, and translation 3 degrees of freedom. A prototype of the proposed robotic bronchoscope system is designed and fabricated, and its performance is tested through several experiments to verify the stiffness, flexibility, and navigation performance. The results show that the proposed system is with good environment adaptiveness, and it can become a promising biopsy method through natural cavity of the human body.

Revealing the Molecular Weight Effect on Highly Efficient Polythiophene Solar Cells.

Polythiophenes (PTs) are promising electron donors in organic solar cells (OSCs) due to their simple structures and excellent synthetic scalability. Benefiting from the rational molecular design, the power conversion efficiency (PCE) of PT solar cells has been greatly improved. Herein, five batches of the champion PT (P5TCN-F25) with molecular weights ranging from 30 to 87 kg mol-1 were prepared, and the effect of the molecular weight on the blend film morphology and photovoltaic performance of PT solar cells was systematically investigated. The results showed that the PCEs of the devices improved first and then maintained a high value with the increase of molecular weight, and the highest PCE of 16.7% in binary PT solar cells was obtained. Further characterizations revealed that the promotion in photovoltaic performance mainly comes from finer phase separation structures and more compact molecular packing in the blend film. The best device stabilities were also achieved by polymers with high molecular weights. Overall, this study highlights the importance of optimizing the molecular weight for PTs and offers directions to further improve the PCE of PT solar cells.

Physiological Measurements and Transcriptome Survey Reveal How Semi-mangrove Clerodendrum inerme Tolerates Saline Adversity.

Salinity adversity has been a major environmental stressor for plant growth and reproduction worldwide. Semi-mangrove Clerodendrum inerme, a naturally salt-tolerant plant, can be studied as a successful example to understand the biological mechanism of saline resistance. Since it is a sophisticated and all-round scale process for plants to react to stress, our greenhouse study interpreted the response of C. inerme to salt challenge in the following aspects: morphology, osmotic protectants, ROS production and scavenging, ion homeostasis, photosynthetic efficiency, and transcriptome reprogramming. The results drew an overview picture to illustrate the tolerant performance of C. inerme from salt acclimatization (till medium NaCl level, 0.3 mol/L) to salinity stress (high NaCl level, 0.5 mol/L). The overall evaluation leads to a conclusion that the main survival strategy of C. inerme is globally reshaping metabolic and ion profiles to adapt to saline adversity. These findings uncover the defense mechanism by which C. inerme moderates its development rate to resist the short- and long-term salt adversity, along with rebalancing the energy allocation between growth and stress tolerance.

Purification Efficiency of Three Combinations of Native Aquatic Macrophytes in Artificial Wastewater in Autumn.

Water pollution caused by excessive nutrient and biological invasion is increasingly widespread in China, which can lead to problems with drinking water as well as serious damage to the ecosystem if not be properly treated. Aquatic plant restoration (phytoremediation) has become a promising and increasingly popular solution. In this study, eight native species of low-temperature-tolerant aquatic macrophytes were chosen to construct three combinations of aquatic macrophytes to study their purification efficiency on eutrophic water in large open tanks during autumn in Guangzhou City. The total nitrogen (TN) removal rates of group A (Vallisneria natans + Ludwigia adscendens + Monochoria vaginalis + Saururus chinensis), group B (V. natans + Ipomoea aquatica + Acorus calamus + Typha orientalis), and group C (V. natans + L. adscendens + Schoenoplectus juncoides + T. orientalis) were 79.10%, 46.39%, and 67.46%, respectively. The total phosphorus (TP) removal rates were 89.39%, 88.37%, and 91.96% in groups A, B, and C, respectively, while the chemical oxygen demand (COD) removal rates were 93.91%, 96.48%, and 92.78%, respectively. In the control group (CK), the removal rates of TN, TP, and COD were 70.42%, 86.59%, and 87.94%, respectively. The overall removal rates of TN, TP, and COD in the plant groups were only slightly higher than that in CK group, which did not show a significant advantage. This may be related to the leaf decay of some aquatic plants during the experiment, whereby the decay of V. natans was the most obvious. The results suggest that a proper amount of plant residue will not lead to a significant deterioration of water quality.

Assessment of the Nutrient Removal Potential of Floating Native and Exotic Aquatic Macrophytes Cultured in Swine Manure Wastewater.

Although eutrophication and biological invasion have caused serious harm to aquatic ecosystems, exotic and even invasive plants have been used extensively in phytoremediation water systems in China. To identify native aquatic plants with excellent water restoration potential, two representative native floating aquatic plants from Guangdong Province, namely Ludwigia adscendens (PL) and Trapa natans (PT), were selected, with Eichhornia crassipes as a control, to study their growth status, adaptability, and nutrient removal potentials in swine manure wastewater. The results demonstrated that the two native plants offered greater advantages than E. crassipes in water restoration. Within 60 days, PL and PT exhibited excellent growth statuses, and their net biomass growth rates were 539.8% and 385.9%, respectively, but the E. crassipes decayed and died with an increasing HRT (hydraulic retention time). The PL and PT could adjust the pH of the wastewater, improve the dissolved oxygen and oxidation-reduction potential, and reduce the electrical conductivity value. The removal rates of NH4+-N, NO3--N, NO2--N, total nitrogen, total phosphorus, chemical oxygen demand (COD), and Chl-a in the PL group reached 98.67%, 64.83%, 26.35%, 79.30%, 95.90%, 69.62%, and 92.23%, respectively; those in the PT group reached 99.47%, 95.83%, 85.17%, 83.73%, 88.72%, 75.06%, and 91.55%, respectively. The absorption contribution rates of total nitrogen (TN) and total phosphorus (TP) in the PL group were 40.6% and 43.5%, respectively, while those in the PT group were 36.9% and 34.5%, respectively. The results indicated that L. adscendens and T. natans are both promising aquatic plants for application to the restoration of swine manure wastewater in subtropical areas.

Investigation of stereoisomeric bisarylethenesulfonic acid esters for discovering potent and selective PTP1B inhibitors.

Protein tyrosine phosphatase 1B (PTP1B) has been considered as a promising therapeutic target for type 2 diabetes mellitus (T2DM) and obesity due to its key regulating effects in insulin signaling and leptin receptor pathways. In this work, a series of cis- and trans-pyrrolidine bisarylethenesulfonic acid esters were prepared and their PTP1B inhibitory potency, selectivity and membrane permeability were evaluated. These novel stereoisomeric molecules especially trans-isomers exhibited remarkable inhibitory activity, significant selectivity as well as good membrane permeability (e.g. compound 28a, IC50 = 120, 1940 and 2670 nM against PTP1B, TCPTP and SHP2 respectively, and Papp = 1.74 × 10-6 cm/s). Molecular simulations indicated that trans-pyrrolidine bisarylethenesulfonic acid esters yielded the stronger binding affinity than their cis-isomers by constructing more interactions with non-catalytic sites of PTP1B. Further biological activity studies revealed that compound 28a could enhance insulin-stimulated glucose uptake and insulin-mediated insulin receptor ß (IRß) phosphorylation with no significant cytotoxicity.

Robotic Versus Laparoscopic Roux-en-Y Gastric Bypass for Morbid Obesity: a Systematic Review and Meta-Analysis.

We aim to summarize the existing evidence to compare the surgical outcomes of robotic Roux-en-Y gastric bypass (RRYGB) and laparoscopic RYGB (LRYGB) and to determine if these two procedures are equivalent. Literature searches were conducted by a comprehensive search in PubMed, EMBASE, and the Cochrane Library. Nineteen articles met the inclusion criteria for this review. The robotic and laparoscopic procedures had no significant differences in hospitalization time, conversion, reoperation, readmission, and postoperative complications. However, RRYGB was associated with a longer mean operative time. RRYGB was not found to be superior to LRYGB. Future studies that would report detailed meaningful postoperative outcomes, such as complications and percentage of excess weight loss, are required to determine any further differences in the efficacy between RRYGB and LRYGB.

Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives.

The synthesis of (S)-2-(4-tert-butylphenoxy)-3-(benzoxazol-5-yl) propanoic acid derivatives (2a-k) were described and their in vitro antibacterial activities were determined against Gram-negative and -positive bacteria. These compounds were found to exert a broad spectrum of activity against the screened bacteria, but poor MIC values were found for Candida albicans fungi. Compound 2b bearing a hydrophobic aromatic tie was the most active derivative against all bacteria studied with MIC values ranging from 0.098 to 0.78 µg/mL. The activity of 2b against B. subtilis was 2-fold higher than Penicillin, and 8- to 510-fold higher than other control antibiotics.

Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent d-amino acid oxidase inhibitor.

A series of 5-azaquinoxaline-2,3-dione derivatives were synthesized and evaluated on d-amino acid oxidase (DAAO) inhibition as potential α-hydroxylactam-based inhibitors. The potent inhibitory activities in vitro suggested that 5-nitrogen could significantly enhance the binding affinity by strengthening relevant hydrogen bond interactions. The analgesic effects of intrathecal and systemic injection of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione, a representative molecule of 5-azaquinoxaline-2,3-dione, were investigated in rodents. This research not only confirmed the analgesic effect of the DAAO inhibitors but provided a new class of chemical entities with oral application potential for the treatment of chronic pain and morphine analgesic tolerance.

Synthesis of caffeic acid phenethyl ester derivatives, and their cytoprotective and neuritogenic activities in PC12 cells.

Twenty-one caffeic acid phenethyl ester (CAPE) derivatives were synthesized, and characterized by IR, HR-MS, (1)H and (13)C NMR analyses. All compounds were evaluated for their cytoprotective effects against H2O2-induced cytotoxicity and neuritogenic activities in the neurite outgrowth in PC12 cells. Compounds 1 and 20 exhibited stronger cytoprotective activities than their parent compound CAPE at 4 nM. Compounds 1, 4, 12 and 13 showed potential neuritogenic activities at 0.5 nM, while compounds 19 and 20 induced neurite outgrowth at 10 nM. The results from this study suggested that CAPE and its derivatives may be potential functional food ingredients for the prevention of neurodegenerative diseases.

Discovery of novel benzoxaborole-based potent antitrypanosomal agents.

We report the discovery of benzoxaborole antitrypanosomal agents and their structure-activity relationships on central linkage groups and different substitution patterns in the sulfur-linked series. The compounds showed in vitro growth inhibition IC50 values as low as 0.02 µg/mL and in vivo efficacy in acute murine infection models against Tryapnosoma brucei.