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Novel phenothiazine-dithiocarbamate analogues were designed by molecular hybridization strategy and synthesized and evaluated for their anticancer activity in vitro against three selected cancer cell lines (EC-109, MGC-803, and PC-3). The preliminary structure-activity relationship (SAR) for this phenothiazine-dithiocarbamate hybrids is explored. Among all analogues, 2-oxo-2-(10H-phenothiazin-10-yl)ethyl 4-ethylpiperazine-1-carbodithioate (8a) showed the most potent inhibitory activity with an [Formula: see text] value of [Formula: see text] against PC-3 cells. In addition, compound 8a could arrest the cell cycle at the G1 phase and regulate the expression of G1 checkpoint-related proteins, suggesting that phenothiazine-dithiocarbamate hybrids might be useful as cell cycle blockers.

A series of 5,6-diaryl-1,2,4-triazines hybrids bearing a 1,2,3-triazole linker were synthesized by molecular hybridization strategy and evaluated for antiproliferative activity against three selected cancer cell lines (MGC-803, EC-109 and PC-3). The first structure-activity relationship (SAR) for these 5,6-diaryl-1,2,4-triazines is explored in this report with evaluation of 15 variants of the structural class. Among these chemical derivatives, 3-(((1-(4-fluorobenzyl)-1H-1,2,3-triazol-4-yl)methyl)thio)-5,6-diphenyl-1,2,4-triazine (11E) showed the more potent inhibitory effect against three cell lines than 5-Fu. Cellular mechanism studies in MGC-803 cells elucidated 11E inhibited colony formation and arrested cell cycle at G2/M phase. Furthermore, compound 11E caused morphological changes, decreased mitochondrial membrane potential, and induced apoptosis through the apoptosis-related proteins in MGC-803 cells. It was the first time, to our knowledge, that 5,6-diaryl-1,2,4-triazines bearing a 1,2,3-triazole linker were used as potential apoptosis inducers.

A series of novel formononetin-dithiocarbamate derivatives were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell line (MGC-803, EC-109, PC-3). The first structure-activity relationship (SAR) for this formononetin-dithiocarbamate scaffold is explored in this report with evaluation of 14 variants of the structural class. Among these analogues, tert-butyl 4-(((3-((3-(4-methoxyphenyl)-4-oxo-4H-chromen-7-yl)oxy)propyl)thio)carbonothioyl)piperazine-1-carboxylate (8i) showed the best inhibitory activity against PC-3 cells (IC50 = 1.97 μM). Cellular mechanism studies elucidated 8i arrests cell cycle at G1 phase and regulates the expression of G1 checkpoint-related proteins in concentration-dependent manners. Furthermore, 8i could inhibit cell growth via MAPK signaling pathway and inhibit migration via Wnt pathway in PC-3 cells.

In order to enhance and toughen the polymer resin with hollow glass microspheres (HGM), polyurethane coating modification was carried out on HGM. The paper aims to explore the conditions and formulas of the physical coating and chemical coating. The physical method is to dissolve thermoplastic polyurethane elastomer in solvent and add HGM to prepare samples. In chemical method, HGM, alcohol component, and isocyanate component are added into solvent, and polymerization reaction is carried out under appropriate conditions to obtain samples. The coating effects and whether there was adhesion between the microspheres were observed through an optical microscope. The results showed that the polyurethane concentration of 4% was suitable for physical method. The reaction temperature of 80 °C is suitable for chemical method. The product synthesized by infrared spectroscopy was polyurethane, and the reaction time was 120 min according to the observation results of optical microscope. The effects of glycerol and toluene-2,4-diisocyanate (TDI) dosage on the thickness of the coating layer were explored through thermogravimetric analysis and optical microscope. This study provides a reference for the preparation of polyurethane-coated HGM 'soft-coated hard' core-shell structure, so that it can be used as a modifier to improve the comprehensive properties of resin. [ABSTRACT FROM AUTHOR]

There is an emerging paradigm shift in oncology that seeks to emphasize molecularly targeted approaches for cancer prevention and therapy. Chalcones (1,3-diphenyl-2-propen-1-ones), naturally-occurring compounds with widespread distribution in spices, tea, beer, fruits and vegetables, consist of open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α, β-unsaturated carbonyl system. Due to their structural diversity, relative ease of chemical manipulation and reaction of α, β-unsaturated carbonyl moiety with cysteine residues in proteins, some lead chalcones from both natural products and synthesis have been identified in a variety of screening assays for modulating important pathways or molecular targets in cancers. These pathways and targets that are affected by chalcones include MDM2/p53, tubulin, proteasome, NF-kappa B, TRIAL/death receptors and mitochondria mediated apoptotic pathways, cell cycle, STAT3, AP-1, NRF2, AR, ER, PPAR-γ and β-catenin/Wnt. Compared to current cancer targeted therapeutic drugs, chalcones have the advantages of being inexpensive, easily available and less toxic; the ease of synthesis of chalcones from substituted benzaldehydes and acetophenones also makes them an attractive drug scaffold. Therefore, this review is focused on molecular targets of chalcones and their potential implications in cancer prevention and therapy.

This experimental study, extending the communication accommodation theory and the Communication Predicament of Disability Model, examined people with disabilities' perceptions of four manipulated communication styles and tested the effects on their cognitive, emotional, and behavioral responses. Results revealed that participants in the integrative talk condition judged the coworker as the most competent and satisfying and had the least anxiety, followed by a relational talk, dismissive talk, and directive talk. Additionally, integrative talk resulted in the least internalized stigma and the highest likelihood of participants using accommodative response strategies, such as problem-solving and obliging. Furthermore, results revealed indirect effects of the communication styles on communication competence, satisfaction, stigma, and response strategies through communication anxiety. [ABSTRACT FROM AUTHOR]

Aberrant histone lysine methylation that is controlled by histone lysine methyltransferases (KMTs) and demethylases (KDMs) plays significant roles in carcinogenesis. Infections by tumor viruses or parasites and exposures to chemical carcinogens can modify the process of histone lysine methylation. Many KMTs and KDMs contribute to malignant transformation by regulating the expression of human telomerase reverse transcriptase (hTERT), forming a fused gene, interacting with proto-oncogenes or being up-regulated in cancer cells. In addition, histone lysine methylation participates in tumor suppressor gene inactivation during the early stages of carcinogenesis by regulating DNA methylation and/or by other DNA methylation independent mechanisms. Furthermore, recent genetic discoveries of many mutations in KMTs and KDMs in various types of cancers highlight their numerous roles in carcinogenesis and provide rare opportunities for selective and tumor-specific targeting of these enzymes. The study on global histone lysine methylation levels may also offer specific biomarkers for cancer detection, diagnosis and prognosis, as well as for genotoxic and non-genotoxic carcinogenic exposures and risk assessment. This review summarizes the role of histone lysine methylation in the process of cellular transformation and carcinogenesis, genetic alterations of KMTs and KDMs in different cancers and recent progress in discovery of small molecule inhibitors of these enzymes.

In this chapter, we focus on Communication Accommodation Theory (CAT)'s utility for analyzing one under-studied domain of intergroup communication, namely police-civilian encounters. By so doing, we focus on one aspect of institutional talk where a power imbalance is clearly evident. In addition to presenting recent self-report data relevant to this initiative, new intercultural data from China, Taiwan and the US, are also introduced. But first, we overview some important assumptions and concepts of the theory, interlaced with a selection of empirical research studies.

Along with Saudi women's increased presence and participation in mixed-gender workforces and the current government's reform initiative, Saudi Vision 2030, their communication opportunities with male coworkers have also increased. Guided by intergroup contact theory, the current online survey tested the influences of Saudi female journalists' (N = 198) report of communication quantity and communication quality with male coworkers on their affective attitudes toward Saudi men and intention to quit the current job. Supporting our hypotheses, results indicated that Saudi female journalists' communication quality with male coworkers was positively associated with affective attitudes toward men. In addition, results revealed a significant positive indirect effect of communication quality with male coworkers on affective attitudes toward men and a significant negative indirect effect on intention to quit through intergroup anxiety. These findings are discussed regarding prior literature on intergroup contact theory and Saudi women in the workplace. [ABSTRACT FROM AUTHOR]

From the perspectives of Saudi female journalists, the current study examined the predictive associations between gender discrimination, supervisor support, government support, and work-related outcomes (i.e., job stress and job satisfaction). Supporting our predictions, regression analyses results revealed that perceptions of gender discrimination were positively and perceptions of supervisor support were negatively associated with job stress. In addition, we found that perceptions of supervisor support and government support had positive associations with job satisfaction. Findings are discussed considering women's participation in the media industry in Saudi Arabia in relation to gender discrimination, supervisor and government support of women. [ABSTRACT FROM AUTHOR]

Guided by the theoretical frameworks of communication accommodation theory and conflict management, this study examines U.S. older participants' (65 or older) written conflict scenario either with a grandchild or a nonfamily young adult. Using content analysis approach, we analyzed these written conflict scenarios to uncover major conflict initiating factors and conflict management styles. Results revealed that intergenerational conflict initiated by old-to-young criticism (more frequently reported in conflicts with nonfamily young adults) or disagreement/generation gap (more frequently reported in conflicts with grandchildren) was reported most frequently followed by young-to-old rebuff, cumulative annoyance, and young-to-old criticism. Additionally, results indicated that older adults used the problem-solving style most frequently when disagreement/generation gap initiated the conflict, especially in the family contexts; both young and older adults used the competing style most frequently when old-to-young criticism initiated the conflict, especially in nonfamily contexts. Furthermore, the use of the competing and problem-solving styles by young adults was significantly associated with the use of the same styles by older adults and vice versa, indicating both positive and negative reciprocation in intergenerational conflict. Results in general show that young and older adults manage intergenerational conflicts in different ways in family versus nonfamily contexts. [ABSTRACT FROM AUTHOR]

Guided by intergroup contact theory, this survey study investigated whether the formation of pseudo-socioemotional ties with well-known LGBT media personas in China (i.e., parasocial relationships) could reduce cisgender heterosexual Chinese participants' anxiety toward and prejudice against the LGBT community. Results indicated a significant indirect effect of parasocial relationship with LGBT media personas on prejudice against this community through intergroup anxiety: the parasocial relationship was negatively associated with intergroup anxiety, which was consequently associated with less prejudice. Moreover, results indicated the direct effect of parasocial relationships with LGBT media personas on prejudice was moderated by participants' direct contact with LGBT members: parasocial relationships reduced prejudice only for those who had more direct contact with LGBT individuals. These findings add nuances and create boundary conditions to intergroup contact theory and bear significant practical implications for the Chinese LGBT community. [ABSTRACT FROM AUTHOR]

We examined intergenerational communication and conflict management styles in China. Older and younger Chinese adults were randomly assigned to evaluate one of four conversation transcripts in which an older worker criticizes a young co-worker. The young worker's communication was varied across the transcripts to reflect four conflict management styles: competing, avoiding, accommodating, and problem-solving. As expected, older participants favored the accommodating style over the problem-solving style. Young adults either preferred the problem-solving style to the accommodating style, as predicted, or judged the two styles as equally positive. The results illustrate the juxtaposition of tradition and modernization/globalization in the changing Chinese cultural context, and demonstrate how such cultural changes are reflected in interpersonal communication between the generations. Keywords: Globalization; China; Intergenerational Communication; Conflict; Filial Piety

Commercials shown on 3 Chinese TV stations in the summer of 2000 are analyzed to expose the dominant value themes. The 13 value themes identified are compared with previous conceptualizations and are discoursed in the context of globalization and Chinese cultural change.

From the theoretical perspectives of anxiety and uncertainty management and intergroup contact, this study examined U.S. American participants' (N = 487) perceptions of conflict management styles with Chinese international students. Specifically, this study tested the indirect effects of participants' perceptions of contact quality with the Chinese in general and strength of Chinese international students' identification with home culture on conflict management styles through intergroup communication anxiety and social attraction. A conflict scenario was set in a typical class project context in which the American participants experienced a conflict with a Chinese international student. Results indicated that participants' perceptions of contact quality with the Chinese and Chinese international students' identification with their home culture had positive indirect effects on the problem‐solving style and negative indirect effects on the competing and avoiding styles through intergroup communication anxiety. In addition, quality of contact had positive direct and indirect effects on the accommodating style through social attraction of Chinese international students. Findings in this study generally indicated important ways in which contact experiences with outgroup members, intergroup communication anxiety, and outgroup membership influence specific communication behaviours during a conflict episode. Findings are discussed in light of prior literature and theories of intergroup contact, anxiety, and integrated threat. [ABSTRACT FROM AUTHOR]

Hippo signalling pathway plays a crucial role in tumorigenesis and cancer progression. In this work, we identified an N-aryl sulphonamide-quinazoline derivative, compound 9i as an anti-gastric cancer agent, which exhibited potent antiproliferative ability with IC50 values of 0.36 μM (MGC-803 cells), 0.70 μM (HCT-116 cells), 1.04 μM (PC-3 cells), and 0.81 μM (MCF-7 cells), respectively and inhibited YAP activity by the activation of p-LATS. Compound 9i was effective in suppressing MGC-803 xenograft tumour growth in nude mice without obvious toxicity and significantly down-regulated the expression of YAP in vivo. Compound 9i arrested cells in the G2/M phase, induced intrinsic apoptosis, and inhibited cell colony formation in MGC-803 and SGC-7901 cells. Therefore, compound 9i is to be reported as an anti-gastric cancer agent via activating the Hippo signalling pathway and might help foster a new strategy for the cancer treatment by activating the Hippo signalling pathway regulatory function to inhibit the activity of YAP. [ABSTRACT FROM AUTHOR]

Proverbs listed by Chinese college students, who are often at the leading edge of cultural change, provide a window into the dynamic interplay of traditionality and modernity. Using thematic analysis, Study 1 examined popular proverbs listed frequently by Chinese college students (n = 298) and the embedded values. Study 2, which was a survey, examined Chinese college students' (n = 240) endorsement of individualism, collectivism, and the values identified in Study 1, and the predictive associations of individualism and collectivism with the values. Findings in Study 1 revealed 103 frequently listed proverbs and eight embedded values (i.e., Learnedness, Diligence, Practical Orientation, Collective Orientation, Social Relationship, Moral Virtue, Free Spirit, and Optimism). Findings in Study 2 indicated participants endorsed Practical Orientation and Learnedness the most, followed by Diligence, Moral Virtue, Social Relationship, Collective Orientation, Optimism, and Free Spirit. Furthermore, although Chinese young adults are more individualistic than collectivistic, collectivism remains a stronger predictor of the values uncovered in the proverbs. The value dynamics in general revealed tensions and harmony between Confucianism and Daoism and the hybridisation of tradition, modernisation, and Western individualism, thus reflecting the complexity of Chinese young adults' social psychology. [ABSTRACT FROM AUTHOR]

Abstract Background Previous studies have demonstrates that, after nerve injury, extracellular signal-regulated protein kinase (ERK) activation in the spinal cord-initially in neurons, then microglia, and finally astrocytes. In addition, phosphorylation of ERK (p-ERK) contributes to nociceptive responses following inflammation and/or nerve injury. However, the role of spinal cells and the ERK/MAPK pathway in cancer-induced bone pain (CIBP) remains poorly understood. The present study analyzed activation of spinal cells and the ERK/MAPK pathway in a rat model of bone cancer pain. Results A Sprague Dawley rat model of bone cancer pain was established and the model was evaluated by a series of tests. Moreover, fluorocitrate (reversible glial metabolic inhibitor) and U0126 (a MEK inhibitor) was administered intrathecally. Western blots and double immunofluorescence were used to detect the expression and location of phosphorylation of ERK (p-ERK). Our studies on pain behavior show that the time between day 6 and day 18 is a reasonable period ("time window" as the remaining stages) to investigate bone cancer pain mechanisms and to research analgesic drugs. Double-labeling immunofluorescence revealed that p-ERK was sequentially expressed in neurons, microglia, and astrocytes in the L4-5 superficial spinal cord following inoculation of Walker 256 cells. Phosphorylation of ERK (p-ERK) and the transcription factor cAMP response element-binding protein (p-CREB) increased in the spinal cord of CIBP rats, which was attenuated by intrathecal injection of fluorocitrate or U0126. Conclusions The ERK inhibitors could have a useful role in CIBP management, because the same target is expressed in various cells at different times.

The purpose of the present work was to evaluate the inhibitory effects of different phenolic extracts from non- and ultra-high-pressure- (UHP-) treated palm fruits and their main phenolic compounds against pancreatic lipase and α-glucosidase and to further analyze the interaction and inhibitory mechanisms of two main phenolics (caffeic acid and catechin). Results showed that the free, esterified, and insoluble-bound phenolic fractions from the non- and UHP-treated fruits demonstrated good inhibitory effects towards two enzymes. The insoluble-bound phenolic fraction, regardless of UHP treatment, presented the strongest inhibitory capacities, and UHP treatment significantly upgraded the inhibitory effects of these phenolic fractions (lipase IC50 : 78.01 vs. 72.50 μg/mL; α-glucosidase IC50 : 76.42 vs. 64.51 μg/mL). Catechin and caffeic acid, main phenolic compounds detected in all phenolic fractions of the fruits, showed similar efficiencies on inhibiting the two enzymes, which were consistent with the findings observed by molecular docking analysis. Moreover, these two phenolic compounds exhibited a synergy effect on inhibiting pancreatic lipase and α-glucosidase at a relatively high combination concentration with the ratio of 1 : 1. Therefore, the present work may be helpful for further application of palm fruits as food supplements or nutraceuticals to control energy intake to improving some chronic metabolic diseases. [ABSTRACT FROM AUTHOR]