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We present a novel, eco-friendly and one-pot approach for synthesizing unsymmetrical oxalamides with the aid of dichloroacetamide and amine/amides in the presence of CBr4 in a basic medium. The use of water as a potent supplement for the oxygen atom source and the detailed mechanism have been disclosed. Moreover, the protocol involves triple cleavage of CCl2Br and the formation of new C–O/C–N bonds, with the advantage of achieving selective bromination using CBr4 with good to excellent yield under mild conditions. The method also demonstrates promise for industrial use, as proven by its effective implementation in gram-scale synthesis conducted in a batch process, along with its utilization in a continuous-flow system. [ABSTRACT FROM AUTHOR]

Anionic redox activity can trigger structural instability in Li‐rich Mn‐based cathodes. Lattice oxygen activity can be tuned through liquid acid‐induced spinel phases and oxygen vacancies. However, the liquid‐acid‐modified surface is still attacked by the electrolyte. Besides, the underlying mechanism of spinel phase suppression of lattice oxygen activity is controversial. Here, a solid acid strategy for modification is proposed and the underlying mechanism is investigated in detail. Unique solid acid can in situ generate an interface protection layer and remarkably stabilize the structure. Theoretical calculations and experimental characterizations reveal that the spinel phase suppresses the irreversible loss of lattice oxygen by decreasing the O 2p non‐bonding energy level and enriching electrons at the layered/spinel phase interface. The inert layer on the surface prevents highly active On− from being attacked by electrolytes. The obtained material exhibits significantly reduced irreversible lattice oxygen release and improved electrochemical performance. After 300 cycles, a slow capacity fading of 0.177 mAh g−1 per cycle and suppressed voltage fading are achieved. This study reveals the regulation method and mechanism for the anion activity of oxide cathodes in next‐generation Li‐ion batteries. [ABSTRACT FROM AUTHOR]

Simple Summary: Boron neutron capture therapy (BNCT) is a target radiotherapy and image-guided intensity-modulated radiotherapy (IG-IMRT) that has been used for recurrent head and neck cancer. To procure better results, the current study designed to combine both as salvage treatment for this challenging problem. For the 14 patients enrolled, a high response rate and low incidence of grade 4 toxicity were seen at follow-up. Further local recurrence was the main cause of failure in spite of the larger radiation volumes and extra dose given with IG-IMRT after BNCT than with BNCT alone. Further revision of this protocol is suggested to improve our results. Background: This trial investigated the efficacy and safety of salvage boron neutron capture therapy (BNCT) combined with image-guided intensity-modulated radiotherapy (IG-IMRT) for recurrent head and neck cancer after prior radiotherapy (RT). Methods: BNCT was administered using an intravenous boronophenylalanine–fructose complex (500 mg/kg) in a single fraction; multifractionated IG-IMRT was administered 28 days after BNCT. For BNCT, the mucosa served as the dose-limiting organ. For IG-IMRT, the clinical target volume (CTV) and the planning target volume (PTV) were generated according to the post-BNCT gross tumor volume (GTV) with chosen margins. Results: This trial enrolled 14 patients, and 12 patients received combined treatment. The median BNCT average dose for the GTV was 21.6 Gy-Eq, and the median IG-IMRT dose for the PTV was 46.8 Gy/26 fractions. After a median (range) follow-up period of 11.8 (3.6 to 53.2) months, five patients had a complete response and four had a partial response. One patient had grade 4 laryngeal edema; another patient had a grade 4 hemorrhage. Most tumor progression occurred within or adjacent to the CTV. The 1-year overall survival and local progression-free survival rates were 56% and 21%, respectively. Conclusion: Despite the high response rate (64%) of this trial, there was a high incidence of in-field and marginal failure with this approach. Future studies combining BNCT with modalities other than radiation may be tried. [ABSTRACT FROM AUTHOR]

This study involves isothermal kinetic simulation to evaluate the parameters of inhibition conditions for Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) of high-risk pathogens. This is because the new type of the 2019 novel coronavirus (2019-nCoV) is continuously spreading and the importance of public health issues. Environmental disinfection and personal wearing of masks have become important epidemic prevention measures. Selection of concentration kinetics could be estimated best for E.coli and S. aureus of pathogens, 2.74 × 104 and 105 and 2.44 × 104 and 105 colony-forming units (CFU mL–1), by isothermal micro-calorimeter (TAM Air) tests, respectively. Comparisons were made of different doses of 0–70 ppm (in 20 mL test ampoule) hypochlorous acid treatment for conducting nth-order and autocatalytic reaction simulation to evaluate the inhibition reaction parameters, which determined the autocatalytic kinetic model that was beneficially applied on the E. coli and S. aureus. We developed the inhibition reaction parameters of the pathogens, which included the activation energy (Ea), the natural logarithm of pre-exponential factor (lnk0), the enthalpy of inhibition microbial growth reaction (∆H), inhibition microbial growth, and the inhibition growth analysis. Overall, we conducted isothermal kinetic simulation to understand the antimicrobial activity effects of electrolytically generated hypochlorous acid-treated pathogenic microorganisms, which will provide reference for public health and medical-related fields for SDG3, and can contribute to ensuring human health and hygiene. [ABSTRACT FROM AUTHOR]

Background: We aimed to analyze the radiation dose and compare survival among combined modality therapy using modern radiation techniques for patients with esophageal squamous cell carcinoma (ESCC). Methods: This retrospective study included patients with clinically staged T1‐4N0‐3M0 ESCC from 2014 to 2018. Patients who received combined modality therapies with curative intent were enrolled. The overall survival (OS) rates among combined modality therapy were compared. The clinical variables and impacts of radiation dose on survival were analyzed by the Kaplan–Meier method and Cox regression model. Results: Of the 259 patients, 141 (54.4%) received definitive concurrent chemoradiotherapy (DCCRT); 67 (25.9%) underwent neoadjuvant chemoradiotherapy followed by surgery (NCRT+S); 51 (19.7%) obtained surgery followed by adjuvant chemoradiotherapy (S+ACRT). Two‐year OS rates of the DCCRT, NCRT+S and S+ACRT group were 48.9, 61.5 and 51.2%. In the subgroup analysis of DCCRT group, the 2‐year OS of patients receiving radiation dose 55–60 Gy was 57.1%. Multivariate analyses showed that clinical stage (p = 0.004), DCCRT with 55–60 Gy (p = 0.043) and NCRT+S with pathological complete response (pCR) (p = 0.014) were significant prognostic factors for better OS. The radiation dose–survival curve demonstrated a highly positive correlation between higher radiation dose and better survival. Conclusion: Our results suggest that NCRT+S can provide a favorable survival for patients with ESCC, especially in patients who achieved pCR. The optimal radiation dose might be 55–60 Gy for patients receiving DCCRT via modern radiation techniques. Further randomized clinical studies are required to confirm the survival benefits between NCRT+S and DCCRT with escalated dose. [ABSTRACT FROM AUTHOR]

Background: To evaluate the clinical relative biological effectiveness (RBE) of carbon‐ion radiotherapy (C‐ion RT) for prostate cancer. Methods: The records of 262 patients with low‐risk prostate cancer (median age, 65 [47–80] years) treated with C‐ion RT at QST Hospital, National Institutes for Quantum Science and Technology in Japan during 2000–2018 were reviewed retrospectively. Four different protocol outcomes and prostate‐specific antigen (PSA) responses were evaluated. The median follow‐up was 8.4 years. The Kaplan–Meier method was used to estimate the biochemical or clinical failure‐free rate (BCFFR). Clinical RBE was calculated using the tumor control probability model. Results: The 5‐, 7‐, and 10‐year BCFFRs were 91.7%, 83.8%, and 73.2%, respectively. The 10‐year BCFFRs of patients who received C‐ion RT at 66 Gy (RBE) in 20 fractions, 63 Gy (RBE) in 20 fractions, and 57.6 Gy (RBE) in 16 fractions were 81.4%, 70.9%, and 68.9%, respectively. The PSA level and density during follow‐up were better in the patients treated with the lower fraction size. A higher PSA nadir and shorter time to PSA nadir were risk factors for biochemical or clinical failure by multivariate Cox regression. The tumor control probability analysis showed that the estimated clinical RBE values to achieve an 80% BCFFR at 10 years for 20, 16, and 12 fractions were 2.19 (2.18–2.24), 2.16 (2.14–2.23), and 2.12 (2.09–2.21), respectively. Conclusions: Using clinical data from low‐risk prostate cancer patients, we showed the clinical RBE of C‐ion RT decreased with increasing dose per fraction. [ABSTRACT FROM AUTHOR]

The major railroad projects in complex and difficult areas have characteristics of complex geological conditions, high incidence of natural disasters, high plateau, high cold and lack of oxygen, low level of existing infrastructure, and extremely long construction period, etc. In order to ensure high quality construction and to solve important problems such as high worker turnover rate, significant aging, and vocational skills and quality to be improved, it is imperative to promote industrialized workers. Based on major railroad projects in complex and dangerous areas, this paper conducts in-depth interviews with front-line railroad construction workers and relevant enterprise leaders. 12 influencing factors of industrialized worker training by applying rooting theory are analyzed and summarized into 6 main categories. Based on the analysis and category, a ISM-MICMAC model is constructed to analyze the interrelationship between influencing factors. The key factors are combined with the driving force dependency matrix to find out 4 key root influencing factors and put forward countermeasure suggestions to reduce their influence. This research provides reference suggestions for industrialized worker training of major railroad projects in complex and difficult areas. [ABSTRACT FROM AUTHOR]

Objectives: To investigate the sleep quality of women pregnant with a second child and the influencing factors and provide a scientific basis for health care guidance to clinically improve the sleep quality of pregnant women. Methods: A total of 162 women pregnant with a second child at a first-class tertiary hospital in Changsha from January to August 2018 were selected as the research subjects. General demographic characteristics were collected, and the Pittsburgh Sleep Quality Index (PSQI) scale was used to assess their sleep quality. Multivariate logistic regression analysis was used to explore the influencing factors of the sleep quality of women pregnant with a second child. Results: The PSQI score (except hypnotic drugs) and total score of pregnant women with second birth were higher than those of normal female population, and the difference was statistically significant (P < 0.05). Univariate analysis showed statistically significant differences in sleep quality among women pregnant with a second child of different ages, marital relationships, gender expectations, education levels, monthly family incomes, planned or unplanned pregnancy, and gestational weeks (P < 0.05). The results of the multi-factor analysis showed that the low education level (OR = 0.224, P = 0.001), low family monthly income (OR = 3.035, P = 0.014), expectation of gender (OR = 0.065, P = 0.038), and dissatisfaction with marital relationship (OR = 0.275, P = 0.001) were the primary risk factors of poor sleep quality of in women with second pregnant. Conclusions: The overall sleep quality of women pregnant with a second child is poor, and 37.65% have sleep quality problems. Low education levels, low family monthly incomes, fetal gender expectations, and poor relationship between husband and wife are the main factors affecting the sleep quality of women pregnant with a second child. Pregnant women with the above factors should pay attention to their sleep quality and take necessary measures for intervention and guidance to improve the level of health care during pregnancy. [ABSTRACT FROM AUTHOR]

A series of novel 4-N-phenylaminoquinoline derivatives containing a morpholine group were designed and synthesized, and their anti-cholinesterase activities and ABTS radical-scavenging activities were tested. Among them, compounds 11a, 11g, 11h, 11j, 11l, and 12a had comparable inhibition activities to reference galantamine in AChE. Especially, compound 11g revealed the most potent inhibition on AChE and BChE with IC50 values of 1.94 ± 0.13 μM and 28.37 ± 1.85 μM, respectively. The kinetic analysis demonstrated that both the compounds 11a and 11g acted as mixed-type AChE inhibitors. A further docking comparison between the 11a- and 12a-AChE complexes agreed with the different inhibitory potency observed in experiments. Besides, compounds 11f and 11l showed excellent ABTS radical-scavenging activities, with IC50 values of 9.07 ± 1.34 μM and 6.05 ± 1.17 μM, respectively, which were superior to the control, Trolox (IC50 = 11.03 ± 0.76 μM). It is worth noting that 3-aminoquinoline derivatives 12a–12d exhibited better drug-like properties. [ABSTRACT FROM AUTHOR]

For surface gravity waves propagating over a horizontal bottom that consists of a patch of sinusoidal ripples, strong wave reflection occurs under the Bragg resonance condition. The critical wave frequency, at which the peak reflection coefficient is obtained, has been observed in both physical experiments and direct numerical simulations to be downshifted from the well-known theoretical prediction. It has long been speculated that the downshift may be attributed to higher-order rippled bottom and free-surface boundary effects, but the intrinsic mechanism remains unclear. By a regular perturbation analysis, we derive the theoretical solution of frequency downshift due to third-order nonlinear effects of both bottom and free-surface boundaries. It is found that the bottom nonlinearity plays the dominant role in frequency downshift while the free-surface nonlinearity actually causes frequency upshift. The frequency downshift/upshift has a quadratic dependence in the bottom/free-surface steepness. Polychromatic bottom leads to a larger frequency downshift relative to the monochromatic bottom. In addition, direct numerical simulations based on the high-order spectral method are conducted to validate the present theory. The theoretical solution of frequency downshift compares well with the numerical simulations and available experimental data. [ABSTRACT FROM AUTHOR]

Background: This study aimed to investigate the clinical relevance of the immune microenvironment in patients with combined hepatocellular carcinoma and cholangiocarcinoma (cHCC‐ICC). Patients and Methods: The density of tumor‐infiltrating CD3+, CD8+, CD163+, and Foxp3+ immune cells, as well as Programmed cell death 1, Programmed cell death‐ligand 1, and Tumor necrosis factor receptor superfamily member 4, was measured in the peritumor liver, tumor invasive margin, and intratumor subregions of 56 cHCC‐ICC by immunohistochemistry. The immune index was established to stratify patients. Prognostic significance of immune cell subsets and immune indices was evaluated. Results: The distribution of immune cells was highly heterogeneous among different subregions of cHCC‐ICC. As compared with the hepatocellular carcinoma (HCC) component, the lower density of CD8+ T cells and higher intensity of Foxp3+ Tregs and immune checkpoints in the intrahepatic cholangiocarcinoma (ICC) component may indicate a stronger immune evasive ability of ICC. Based on clustering classification or a combination of random forest and lasso‐cox, two models of immune indices were established and both were identified as independent prognostic factors for cHCC‐ICC patients. The selected immune variables in the immune prognostic models derived from both HCC and ICC subregions, indicating that the prognosis of cHCC‐ICC patients was a complex interaction of both components. Conclusions: The immune contexture was heterogeneous among different subregions of cHCC‐ICC patients and contributed differently to patient prognosis. Immune score based on the densities of immune cells might serve as a promising prognostic predictor for cHCC‐ICC patients. [ABSTRACT FROM AUTHOR]

The adoption of the PPP model in urban infrastructure construction is a new feature that drives the dual benefits of urban economy and society. The cooperation between public and private sectors needs to use incentive and restraint mechanisms to motivate the enthusiasm of stakeholders to participate in project construction investment, thereby obtaining economic and social benefits. Through the empirical case study, this study found that the effectiveness of incentive mechanism is mainly determined by the government's reward to the private sector in the project and its active efforts. The utility of incentive mechanism is the key to determine the unique constraint control power of the government. In order to demonstrate the validity of the research method in project implementation, a model based on incentive and constraint mechanism in PPP projects is established. The results show that there are differences in the decision standards during project operation phase. The incentive and restraint mechanism has the strongest role and risk sharing ability in the PPP projects, and has the highest difficulties on supervision of income constraint. The findings of this study can help stakeholders avoid the risk sharing and improve social equity of the PPP model in urban construction and operation. [ABSTRACT FROM AUTHOR]

A series of novel quinazolinone derivatives bearing a disulfide bond were designed and synthesized. Their in vitro antiproliferative activities were evaluated using CCK-8 assay against SMMC-7721, Hela, A549 and MCF-7 human cancer cell lines and normal cell lines L929. The preliminary bioassay results demonstrated that all compounds 7a-7h, 8a-8h and 9a-9h exhibited antiproliferation with various degrees, and some compounds showed better effects than positive control 5-fluorouracil against different cancer cell lines. Among these compounds, 8c and 9f showed significant antiproliferative activity against SMMC-7721 cells with IC50 values of 2.88 and 2.56 μM, respectively. In Hela cells, compounds 9c and 9d showed highly effective biological activity with IC50 values of 3.16 and 2.68 μM, respectively. Compounds 7a and 9a exhibited good inhibitory effect against A549 cells with IC50 values of 3.53 and 3.54 μM, respectively. In MCF-7 cells, compounds 7e, 8e and 9e displayed excellent activity with IC50 values of 1.26, 1.12 and 1.85 μM, respectively. Besides, most of the tested compounds showed low cytotoxic effect against the normal cell lines L929. Biological evaluation indicated that all the tested compounds possessed antibacterial activity with certain degrees. [ABSTRACT FROM AUTHOR]

CO2 reservoirs are widely distributed within the Yingcheng Formation in the Songliao Basin, but the extreme horizontal heterogeneity of CO2 content causes difficulties in the exploration and exploitation of methane. Former studies have fully covered the lithology, structure, and distribution of the reservoirs high in CO2 content, but few are reported about migration and accumulation of CO2. Using the East Changde Gas Field as an example, we studied the accumulation mechanisms of CO2 gas. Two original types of accumulation model are proposed in this study. The fault-controlled accumulation model refers to gas accumulation in the reservoir body that is cut by a basement fault (the West Xu Fault), allowing the hydrocarbon gas generated in the lower formation to migrate into the reservoir body through the fault, which results in a relatively lower CO2 content. The volcanic conduit-controlled accumulation model refers to a reservoir body that is not cut by the basement fault, which prevents the hydrocarbon gas from being mixed in and leads to higher CO2 contents. This conclusion provides useful theories for prediction of CO2 distribution in similar basins and reservoirs. [ABSTRACT FROM AUTHOR]

In the present study, the synthesis of novel 1,3,4-thiadiazole derivatives bearing disulfide bond are accomplished in good yields with employing a convergent synthetic route, and their in vitro antiproliferative activities were screened against human cancer cell lines A549, Hela, SMMC-7721, and normal cell lines L929 by CCK-8 assay. Meanwhile, all compounds were evaluated for their in vitro antimicrobial activities against Gram-negative bacteria Escherichia coli and Gram-positive bacteria Staphylococcus aureus strains. Screening results indicated that some of the tested compounds 6a-6h, 7a-7h, and 8a-8h possessed better antiproliferative activity than positive control 5-fluorouracil. Compounds 7f, 7h, and 8h displayed significant antitumor activities against SMMC-7721 cells with IC50 values 2.37, 3.80, and 2.72 µM, respectively. Compounds 6g, 7g, 7h, and 8g showed great antitumor effects against Hela cells with IC50 values 1.29, 2.56, 3.43, and 2.14 µM, respectively. Compounds 6e, 8a, and 8h exhibited highly effective antiproliferative activities against A549 cells with IC50 values 3.43, 2.12, and 3.81 µM, respectively. Most of tested compounds exerted weak cytotoxic effects on normal human cell line L929. Biological evaluation indicated that all the tested compounds possessed antimicrobial activity with certain degrees. [ABSTRACT FROM AUTHOR]

Purpose: Selective internal radiation therapy (SIRT) is an effective treatment strategy for unresectable hepatocellular carcinoma (HCC) patients. However, the prognoses of patients with portal vein thrombosis, extra-hepatic metastases, or residual tumors remain poor when treated with SIRT alone. In these patients, sequential external beam radiotherapy (EBRT) may offer a chance of salvage. Here, we reported the clinical outcomes and the detailed dosimetry analysis of 22 patients treated with combination therapy. Methods: Between October 2011 and May 2015, 22 consecutive patients who underwent EBRT after yttrium-90 (90Y) SIRT were included in this study. The post-SIRT 90Y bremsstrahlung SPECT/CT of each patient was transferred to dose distribution by adopting the local deposition hypothesis. The patient-specific 3-dimensional biological effective dose distribution of combined SIRT and EBRT was generated. The overall survival and safety were evaluated. The relationship between dosimetric parameters and liver toxicity was analyzed. Results: The mean administered activity of SIRT was 1.50 GBq (range: 0.5–2.8). The mean prescribed dose of EBRT was 42.3 Gy (range: 15–63) in 14 fractions (range: 5–15) and was targeted to the residual liver tumor in 12 patients (55%), portal vein thrombosis in 11 patients (50%), and perihilar lymphadenopathies in 4 patients (18%). The overall 1-, 2-, and 3-year survival rates were 59.8%, 47.9%, and 47.9%, respectively. Overall, 8 patients (36%) developed > grade 2 liver toxicities, and the Child-Pugh score prior to EBRT strongly affected the toxicity risk. A dosimetry analysis restricted to 18 Child-Pugh A/B patients showed that the V100 (The fraction of normal liver exposed to more than 100 Gy) to V140 significance differed between patients who did or did not experience hepatotoxicity. The V110 was the strongest predictor of hepatotoxicity (18.6±11.6% vs 29.5±5.8%; P = 0.030). Conclusion: Combined therapy is feasible and safe if patients are carefully selected. Specifically, 3-dimensional dosimetry is crucial for the evaluation of efficacy and toxicity. The normal liver V100 to V140 values of the combined dose should be as low as possible to minimize the risk of liver toxicity. [ABSTRACT FROM AUTHOR]

Chinese alkaline noodle (CAN) is one of popular staple foods in Asia. Whole wheat flour (WWF) is healthier than refined wheat flour (WF). This study investigated the effect of substitution level of WWF on physicochemical and sensory properties of CAN. Results showed that increasing WWF amount significantly reduced tensile strength (TS) and extensibility (E) of cooked CAN, but increased TS/E ratio from 6.05 to 13.22 mN/mm. High WWF substitution (>60 %) significantly increased cooking loss and decreased the elasticity of CAN. CAN prepared with WWF had darker, redder and yellower color than control. However, free and bound phenolics and DPPH radical scavenging capacity of CAN obviously increased with the amount of WWF. CAN with 0-40 % WWF had similar sensory scores in color, flavor, texture and overall preferences. The study suggests that healthy whole grain CAN with higher phytochemicals and acceptable eating quality can be produced by using 20-40 % WWF. [ABSTRACT FROM AUTHOR]

A series of novel nonsymmetrical disulfides bearing 1,2,4-triazole moiety were designed, synthesized, and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, Hela, A549, and normal cell lines L929 by CCK-8 assay. The preliminary bioassay results demonstrated that most of the tested compounds 8a- r exhibited good antiproliferative activities, and some compounds showed better effects than positive control 5-fluorouracil against various cancer cell lines. Among these compounds, compound 8l showed significant antiproliferative activity against SMMC-7721 cells with IC value of 2.97 μM. Compound 8f displayed highly effective biological activity against Hela cells with IC value of 3.51 μM. Compound 8d exhibited the best inhibitory effect against A549 cells with IC value of 2.79 μM. Furthermore, some of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituent groups are vital for improving the potency and selectivity of this class of compounds. [ABSTRACT FROM AUTHOR]

Purpose: Medulloblastoma (MB) is the most commonly occurring malignant pediatric brain tumor worldwide. However, a recent study found that the treatment outcomes in those with high-risk disease receiving conventional treatment were suboptimal. This study aimed to assess outcomes and treatment strategies for specific histologic subtypes of pediatric MB. Methods: A total of 114 pediatric patients (age < 20 years) diagnosed with MB between March 1998 and August 2011 were retrospectively reviewed; 52 that were treated with surgery followed by adjuvant radiotherapy (RT) and chemotherapy (CHT) were included. Results: The 5-year overall survival (OS) and relapse-free survival (RFS) rates were 73 and 69%, respectively. Median time to relapse was 17 months with a median survival time of 6 months after relapse. Patients of average risk had a better 5-year OS rate compared with high-risk patients ( p = 0.027). The 5-year RFS of high-risk patients was lower compared with average risk ( p = 0.038). A greater proportion of patients with large cell/anaplastic (LC/A) MB had recurrence than classic MB with 5-year RFS rate of 34 and 76%, respectively ( p = 0.001), and OS rate of 56 and 76%, respectively ( p = 0.04). Conclusion: High-risk group and histology of LC/A were the most significant factors associated with worse OS and RFS. Patients with LC/A-MB had higher relapse rates and worse survival than those with classic MB. LC/A-MB carries a high risk for recurrence and should be treated with the more aggressive strategies. [ABSTRACT FROM AUTHOR]

A series of novel benzisoselenazolone derivatives bearing 1,3,4-thiadiazole moiety were designed, synthesized and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, MCF-7, A549, and normal cell lines L929 by CCK-8 assay. The bioassay results demonstrated that most of the tested compounds showed potent antitumor activities, and some compounds exhibited better effects than positive control ebselen and ethaselen against various cancer cell lines. Among these compounds, compound 7l showed significant antiproliferative activity against SMMC-7721 cells, with IC values of 2.18 μM. Compound 7j exhibited the best inhibitory effect against MCF-7 cells, with IC values of 2.89 μM. Compounds 7e and 7i displayed highly effective antitumor activities against A549 cells, with IC values of 2.33 and 2.33 μM, respectively. Furthermore, most of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituents of benzoylmethylthio-moiety at position-2 on 1,3,4-thiadiazole are vital for modulating antiproliferative activities against various tumor cell lines. [ABSTRACT FROM AUTHOR]

Browser with Rich Internet Application (RIA) Web pages could be a powerful user interface for handling sophisticated data and applications. Then the RIA solutions would be a potential method for viewing and manipulating the most data generated in clinical processes, which can accomplish the main functionalities as general picture archiving and communication system (PACS) viewing systems. The aim of this study is to apply the RIA technology to present medical images. Both Digital Imaging and Communications in Medicine (DICOM) and non-DICOM data can be handled by our RIA solutions. Some clinical data that are especially difficult to present using PACS viewing systems, such as ECG waveform, pathology virtual slide microscopic image, and radiotherapy plan, are as well demonstrated. Consequently, clinicians can use browser as a unique interface for acquiring all the clinical data located in different departments and information systems. And the data could be presented appropriately and processed freely by adopting the RIA technologies. [ABSTRACT FROM AUTHOR]

A new flavonol glycoside, kaempferol 3-O-α-L-rhamnopyranosyl (1 → 6)-O-[β-D-glucopyranosyl (1 → 2)-O-β-D-galactopyranosyl (1→2)]-O-β-D-glucopyranoside (1), together with a known compound, kaempferol 3-O-β-D-glucopyranosyl (1 → 2)-O-β-D-galactopyranosyl (1 → 2)-O-β-D-glucopyranoside (2) was isolated from the seeds of Nigella glandulifera. Their structures were elucidated on the basis of spectral analysis, including ESI–MS, ESI–MS/MS, HR-ESI–MS, DQF–COSY, TOCSY, HSQC and HMBC techniques. [ABSTRACT FROM PUBLISHER]

Multiscale classification has potential advantages for monitoring industrial processes generally driven by events in different time and frequency domains. In this study, we adopt stationary wavelet transform for multiscale analysis and propose an applicable scale selection method to obtain the most discriminative scale features. Then using the multiscale features, we construct two classifiers: (1) a supported vector machine (SVM) classifier based on classification distance, and (2) a Bayes classifier based on probability estimation. For the SVM classifier, we use 4-fold cross-validation and grid-search to obtain the optimal parameters. For the Bayes classifier, we introduce dimension reduction techniques including kernel Fisher discriminant analysis (KFDA) and principal component analysis (PCA) to investigate their influence on classification accuracy. We tested the classifiers with two simulated benchmark processes: the continuous stirred tank reactor (CSTR) process and the Tennessee Eastman (TE) process. We also tested them on a real polypropylene production process. The performance comparison among the classifiers in different scales and scale combinations showed that when datasets present typical scale features, the multiscale classifier had higher classification accuracy than conventional single scale classifiers. We also found that dimension reduction can generally contribute to a better classification in our tests. [ABSTRACT FROM AUTHOR]

Two rare guanidine-type alkaloids, Buthutin A (1) and Buthutin B (2), along with two other compounds (3, 4), were isolated from Buthus martensii Karsch, and determined using extensive spectroscopic data analysis and high resolution-mass spectrometry. Compound 1 showed the most potent inhibition on AChE and BChE with IC50 values of 7.83 ± 0.06 and 47.44 ± 0.95 μM, respectively. Kinetic characterization of compound 1 confirmed a mixed-type of AChE inhibition mechanism in accordance with the docking results, which shows its interaction with both catalytic active (CAS) and peripheral anionic (PAS) sites. The specific binding of compound 1 to PAS domain of AChE was also confirmed experimentally. Moreover, compounds 1 and 3 exhibited satisfactory biometal binding abilities toward Cu2+, Fe2+, Zn2+ and Al3+ ions. These results provide a new evidence for further development and utilization of B. martensii in health and pharmaceutical products. [ABSTRACT FROM AUTHOR]

Simple Summary: The supplement of TNuF, a total nutrition formula, before cancer diagnosis significantly enhanced the anticancer effect of radiotherapy against primary tumor and lung metastasis in tumor-bearing mice. Meanwhile, TNuF improved cancer related sarcopenia. We supposed that these benefits are related to the regulations of cell proliferation, angiogenesis, and immunity in tumor microenvironment. (1) Background: Radiotherapy (RT) is one of the major treatments for non-small cell lung cancer, but RT-associated toxicities usually impede its anticancer effect. Nutrient supplementation has been applied for cancer prevention or a complementary measure to anticancer therapy. Here, we explored the influence of total nutrition supplementation before and after cancer occurrence on the anticancer benefit and side effects of RT. (2) Methods: C57BL/6JNarl mice were inoculated with Lewis lung carcinoma cells and then treated with radiotherapy. TNuF, a total nutrition formula, was prescribed by oral gavage. In the preventive groups, TNuF supplementation started from seven days before tumor inoculation. In the complementary groups, TNuF supplementation began after tumor inoculation. (3) Results: TNuF successfully enhanced the anticancer effect of RT against primary tumor and lung metastasis. Additionally, the complementary supplement improved the high serum TNF-α level and the wasting of sartorius muscle in mice receiving RT. In histologic and molecular analysis, TNuF was observed to modulate EGFR, apoptosis, and VEGF and PD-1/PD-L1 pathways. Furthermore, the anticancer benefit of the preventive supplement was comparable to that of the complementary administration. (4) Conclusions: Our results demonstrated that the prescription of the TNuF total nutrition formula before and after cancer diagnosis attains similar benefits in testing subjects with typical anticancer RT. TNuF is also a potential sensitizer to anti-PD-1 immune therapy. [ABSTRACT FROM AUTHOR]

Non-small-cell lung cancer (NSCLC) causes high mortality. Radiotherapy is an induction regimen generally applied to patients with NSCLC. In view of therapeutic efficacy, the outcome is not appealing in addition to bringing about unwanted side effects. Total nutrition is a new trend in cancer therapy, which benefits cancer patients under radiotherapy. Male C57BL/6JNarl mice were experimentally divided into five groups: one control group, one T group (borne with Lewis lung carcinoma but no treatment), and three Lewis lung carcinoma-bearing groups administrated with a total nutrition formula (T + TNuF group), a local radiotherapy plus daily 3 Gy in three fractions (T + R group), or a combination TNuF and radiotherapy (T + R + TNuF group). These mice were assessed for their mean tumor volumes, cachectic symptoms and tumor metastasis. TNuF administration significantly suppressed tumor growth and activated apoptotic cell death in NSCLC-bearing mice under radiation. The body-weight gain was increased, while the radiation-induced cachexia was alleviated. Analysis of mechanisms suggests that TNuF downregulates EGFR and VEGF signaling pathways, inhibiting angiogenesis and metastasis. In light of radiation-induced tumor cell death, mitigation of radiation-induced cachexia and inhibition of tumor cell distant metastasis, the combination of TNuF and radiotherapy synergistically downregulates EGFR and VEGF signaling in NSCLC-bearing mice. [ABSTRACT FROM AUTHOR]