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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]

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]

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]

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]

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]

Guided by intergroup contact theory, this study examined participants' communication with their most frequent contact with an invisible physical disability and their attitudes and stereotypes toward people with disabilities. Results indicated that participants' perceptions of communication frequency and quality with the contact and the contact's disclosure about disability all had a significant indirect effect on attitudes and stereotypes through social support and intergroup anxiety sequentially. Contact quality had significant negative direct and indirect effects on endorsement of stereotypes and a significant positive indirect effect on attitudes. Protective disclosure had a significant positive indirect effect on cognitive attitudes through social support. [ABSTRACT FROM AUTHOR]

Guided by intergroup contact and communication accommodation theories, this study tested the effects of U.S. participants' (N = 286) communication with their most frequent contact who had a visible physical disability and its effects on attitudes toward and stereotypes of people with disabilities as a whole. As predicted, mediation analysis showed the type of interability contact (i.e., nonfamily = 1 and family = 2), and participants' perceptions of their own communication accommodation during interability interactions with the contact had significant indirect effects on the improvement of attitudes toward and reduction of stereotypes about people with disabilities through relational solidarity and intergroup anxiety as sequential mediators. In addition, communication accommodation had significant positive direct effects on intergroup attitudes. These findings provide insights into the important role played by interability contact, especially in the family context and communication accommodation in developing positive relationships in order to reduce anxiety, prejudices, and biases toward people with disabilities. [ABSTRACT FROM AUTHOR]

This study investigates the relationship between interability communication (i.e., communication frequency and identity accommodation) and interability attitudes and disability stereotyping through intergroup anxiety and whether the relationship varies with disability salience. Results indicated that participants' report of communication frequency with their disability-contact had a significant direct effect on the dependent variables (i.e., interability attitudes and disability stereotyping). Moderated mediation results revealed that when salience was low, communication frequency enhanced positive interability attitudes and reduced disability stereotyping through reduced anxiety. Additionally, perceptions of identity accommodation were positively associated with interability attitudes. However, when salience was moderate and high, identity accommodation reduced positive interability attitudes and elevated negative disability stereotyping through an increase in intergroup anxiety. Discussion focuses on the complementary nature of communication accommodation and intergroup contact theories, and thus illustrates the complex role played by identity accommodation in the interability context. • This study examined people without disabilities' communication with people with visible physical disabilities. • Communication frequency and identity accommodation enhanced positive interability attitudes. • Enacting identity accommodation elevated people without disabilities' intergroup anxiety when disability salience was high. • Low disability salience enhanced generalization from communication to broader and better interability attitudes. • Findings illustrate the complementary nature of communication accommodation and intergroup contact theories. [ABSTRACT FROM AUTHOR]

This experiment examines whether exposure to outgroup members' self-presentation on Facebook and ingroup members' accommodative versus nonaccommodative responses influence perceptions of outgroup members' social attractiveness and attitudes toward the target outgroup. U.S. college students (N = 865) saw one of four fictitious Facebook pages with wall posts representing a Chinese international student's self-presentation (positive vs. negative) and the student's U.S. Facebook friends' response (accommodative vs. nonaccommodative). The Chinese international student's U.S. Facebook friends were ingroup members with respect to the U.S. college student participants. Participants who viewed outgroup members with positive (compared to negative) self-presentation and ingroup accommodation (compared to nonaccommodation) perceived the outgroup target as more socially attractive. Perceptions of the outgroup target generalized to both affective and behavioral attitudes toward the Chinese outgroup. However, direct effects in our mediated model yielded some complex effects wherein negative self-presentation and communication partner nonaccommodation yielded more positive attitudinal effects. We discuss these findings in terms of the complex dynamics of intergroup accommodation in the online space. • In line with CAT, this experimental study examined intercultural online interactions involving outgroup self-presentation and ingroup non/accommodative responses on Facebook. • The effect of the ingroup members' communication accommodation on perceptions of outgroup members' social attractiveness was stronger than the valence of the outgroup member's own self-presentation. • The perceptions of social attractiveness mediate the effect of intercultural interactions on affective and behavioral attitudes. • Nonaccommodative responses can yield positive effects, perhaps due to sympathy. • Findings move CAT toward next phase focusing on communication & technology. [ABSTRACT FROM AUTHOR]

Guided by communication accommodation theory, the current study examined the effects of accent stereotyping on native English speakers' (N = 243) perceptions of and willingness to communicate with the nonnative speaker and willingness to accommodate to Hispanic/Latino Americans in general. Accent stereotyping was manipulated through two experimental conditions: presence or absence of an explicit and negative stereotype in a written paragraph. After reading the paragraph, participants listened to a recording of an English speaker with a moderate, native-Spanish accent. Using PROCESS, results revealed participants in the stereotype condition rated the speaker as less socially attractive than the control condition, indicating accent stereotyping negatively affected perceptions of social attractiveness of the moderately accented speaker. Additionally, results indicated significant indirect effects of negative accent stereotyping on willingness to communicate with the speaker and willingness to accommodate to Hispanic/Latino out-group members sequentially through perceived social attractiveness and communication anxiety. [ABSTRACT FROM AUTHOR]

Using a content analytic approach, this study examined young adults’ retrospective written accounts about their perceived communication with family and nonfamily elders in conflict situations to uncover conflict initiating factors and management styles. Results revealed that old-to-young criticism (especially in nonfamily contexts) and competition were the most frequently reported conflict initiating factor and management style in intergenerational relationships. Also, results indicated that family elders’ use of the competing and avoiding styles were reciprocated by young adults. [ABSTRACT FROM AUTHOR]

This study examined Chinese daughters-in-law's (N = 287) perceptions of the husband's conflict management styles in their dyadic interaction regarding mother/daughter-in-law conflicts and associations with marital satisfaction and relational satisfaction with the mother-in-law. Results showed that the problem-solving style was perceived to be used most by the husband, followed by the accommodating, avoiding, and competing styles. In addition, the problem-solving and accommodating styles were positively associated, whereas the competing and avoiding styles were negatively associated with judgments of communication appropriateness and effectiveness, and the relational satisfaction variables. Furthermore, results indicated a moderator effect of shared family identity on the associations between perceptions of the husband's conflict management styles and relational satisfaction with the mother-in-law. Implications of the findings were discussed with reference to the prior literature on interpersonal conflict management, the Common Ingroup Identity Model, family relationships, as well as culture change in China. [ABSTRACT FROM AUTHOR]

A series of novel Mahkoside A derivatives was synthesized, and their in vitro cytotoxic activities were evaluated against the human cancer cell line Ec-9706. A Preliminary structure-activity relationship study showed compounds 7 and 8 have obvious cytotoxic activities (IC50: 30.0 and 12.5 µg · mL-1, respectively). [ABSTRACT FROM AUTHOR]

Abstract: Dibutyltin oxide (DBTO) was first utilized for the deacetylation of steroid and diterpene esters. The results showed the deprotection of acetylated steroids and diterpenes separately with moderate catalysis dibutyltin oxide in methanol selectively removed part acetyl groups of these substrates, whereas several functional groups of the steroids and diterpenes were retained and neither isomerization nor degradation of these substrates was observed. It seems that the acetyl groups with lower steric hindrance or near carbonyl, alkoxy, or hydroxyl groups can be cleaved by the reaction, whereas the acetyl groups with higher steric hindrance or without carbonyl, alkoxy, or hydroxyl groups neighboring were retained under the same conditions. One of the interesting results obtained was the selective hydrolysis of the 3β-O-acetyl group in the presence of the 6β group in 3β,6β-Di-O-acetyl-5α-hydroxypregn-16-en-20-one. This allows for subsequent introduction of one unit at C-3 and the other unit at C-6. This procedure is useful for the synthesis of a series of closely related isomers of 3β,5α,6β-trihydroxypregn-16-en-20-one and other widespread polyhydroxysteroids in marine organisms and some terrestrial species. [Copyright &y& Elsevier]

A new phenolic glycoside (1), mahkoside A, together with six known compounds including mangiferin (2), kaempferol-3- O -β-d-glucoside (3), dodecanoic acid (4), palmitic acid (5) ethyl stearate (6) and sucrose (7), were isolated from the pit of Mahkota dewa. Their structures were identified on the basis of spectroscopic analysis. All the compounds were isolated from the title plant for the first time. [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. [ABSTRACT FROM AUTHOR]

Abstract: 4-Chloro-4-deoxy-α-d-galactopyranose, 1,2,3,6-tetra-O-acetyl-4-chloro-4-deoxy-α-d-galactopyranose and 1,2,3,6-tetra-O-acetyl-4-chloro-4-deoxy-β-d-galactopyranose were readily prepared from 1,4:3,6-dianhydro-β-d-fructofuranosyl 4-chloro-4-deoxy-α-d-galactopyranoside. In the study, we found an interesting anomerization phenomenon of 4-chloro-4-deoxy-d-galactose. The molar ratio of α and β anomers in solution is about 1:2 when the anomerization reaches a dynamic equilibrium, and the β anomer could completely convert to the α anomer in the process of crystallization and precipitation. The acetylation of 4-chloro-4-deoxy-d-galactopyranose is kinetically controlled, and the configuration of the starting galactose determines the configuration of the resulting acetates. The influence of the chloro group at C-4 and the O-acetyl group at the anomeric carbon on the galactopyranose ring conformations is discussed, based upon the crystallographic data for the α and β anomers of 1,2,3,6-tetra-O-acetyl-4-chloro-4-deoxy-d-galactopyranose. [Copyright &y& Elsevier]

This study examined young adults' written accounts of intergenerational communication in conflict situations in the People's Republic of China. Using a content analysis approach, this study identified five major types of initiating factors that precipitated intergenerational conflict. Old-to-young criticism was most frequent, followed by illegitimate demand and rebuff. The least frequent initiating factors included young-to-old criticism and disagreement/generation gap. In addition, results indicated that more rebuffs were from nonfamily elders than from family elders, whereas disagreement with family elders was more frequent than with non-family elders. Proportionally speaking, no differences emerged between family and nonfamily elders for criticism (both old-to-young and young-to-old) and illegitimate demand. Results are discussed with respect to research in intergenerational communication, interpersonal conflict, and the Chinese socio-cultural norm of hierarchy and filial piety. [ABSTRACT FROM AUTHOR]

A simplified finite element method (FEM) simulation method has been established and validated for analyzing the sound absorption mechanism of structures with periodic axisymmetric cavities. Combined with genetic algorithm, the simplified FEM method is used to optimize the sound absorption coefficient of the structure containing periodic cylindrical cavities and variable cross section cavities. The result of variable section cavities is much better than the case of cylindrical cavities. The effect of cavity shape on sound absorption mechanism is discussed through energy dissipation, structure deformation and modal analysis of the absorption structures. It is found that the cavity structure resonances include bending vibration of the surface layer and radial motion of particles near the cavities. The radial motion also changes along the axial direction. Adding geometric design parameters of the cavity cross section are conducive to moving the radial mode to low frequency. The radial vibration has a great influence on absorption performance, which is more conducive to promoting the conversion of longitudinal waves into transverse waves with more energy dissipation. Finally, a better sound absorption performance is obtained by introducing the material parameter of Young's modulus into the optimization model, indicating that comprehensive consideration of geometry and material parameters for optimization is expected to obtain the desired sound absorption structure in engineering practice. [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]

Abstract: Treatment of 3β-hydroxyl-5-Δ steroids with anhydrous FeCl3 in CH2Cl2 afforded reasonable yields of the corresponding alkyl chlorides with a retention of configurations. The structures of the chlorine-exchanging products were determined by NMR and HRMS spectra. The absolute configurations were confirmed by X-ray crystal analysis of 3β-chloro-androst-5-en-17-one. The generality and scope of the reaction were also investigated. [Copyright &y& Elsevier]

In order to study the effects of isovolumic hemodilution and its combination with Danshen solution on acute ischemic reperfused canine myocardium, 24 adult hybrid dogs were used and divided into four groups. Group I was the control group, groups II-IV were treated with Dextron 40, Danshen solution and a combination of the two, respectively. The results showed that either Dextron 40 or Danshen solution alone had a significant increase of ±dp/dt — max when compared with group I (p < 0.05). Although no significant difference existed between group II and III, the former showed more rapid action. The combination of the two therapies improved ± dp/dt — max and LVSP, and significantly reduced the necrotic sizes and the MDA contents in the ischemic myocardia compared with not only group I, but also group II or group III (all p < 0.05). The results suggest that isovolumic hemodilution or Danshen may protect the ischemic reperfused myocardium and the former may come into action more rapidly, and that the combination of the two may show a better synergism than each one of the two by itself. [ABSTRACT FROM AUTHOR]

• Chalcone-dithiocarbamates were novel apoptosis inducers. • 12d arrested cell cycle at G2/M phase and induced DNA damage. • 12d induced ROS-mediated apoptosis by catalase inhibition. • 12d inhibited epithelial-mesenchymal transition process. Novel chalcone-dithiocarbamate hybrids were designed, synthesized and evaluated for antiproliferative activity against selected cancer cell lines (MGC803, MCF7, and PC3). Among these analogues, (E)-2-oxo-2-((4-(3-(3,4,5-trimethoxyphenyl)acryloyl)phenyl)amino)ethyl-4-(2-hydroxyethyl)piperazine-1-carbodithioate (12d) showed the best inhibitory activity against PC3 cells (IC 50 = 1.05 μM). Cellular mechanism studies elucidated 12d could inhibit colony formation, arrest cell cycle at G2/M phase and induce DNA damage against PC3 cells. Compound 12d also induced mitochondrial apoptosis by caspase activation, MMP decrease, ROS production and catalase (CAT) inhibition. Importantly, 12d inhibited epithelial-mesenchymal transition (EMT) process by regulating EMT-related proteins (E-cadherin, N-cadherin, Vimentin, MMP2, MMP9). These results indicated that 12d is a promising lead compound and deserves further investigation for prevention and treatment of human prostate cancer. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

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-4 H -chromen-7-yl)oxy)propyl)thio)carbonothioyl)piperazine-1-carboxylate ( 8i ) showed the best inhibitory activity against PC-3 cells (IC 50 = 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. [ABSTRACT FROM AUTHOR]

A series of nine novel 1,2,3-triazole-chalcone derivatives were designed using the molecular hybridisation approach and synthesised by click chemistry. Most of the synthesised compounds exhibited moderate to good antiproliferative activity against oesophagus, gastric and neuroendocrine cancer cell lines, but a compound containing a p-bromo group in the A ring and a [(4,5-dihydrothiazol-2-yl)thio]methyl group attached at the 4-position of a p-[3-(1,2,3-triazol-1-yl)propyloxy] group in the B ring showed the highest activity with an IC50 value of 8.16 μM against neuroendocrine cancer cells. The structure activity relationships of all nine compounds were discussed. [ABSTRACT FROM AUTHOR]

A series of 3-aminopropyloxy derivatives of chalcone were synthesised and evaluated for their antiproliferative activity against liver, gastric and neuroendocrine cancer cell lines. Most of the synthesised compounds exhibited moderate to good activity against all three cancer cell lines, but in particular, a 3-(pyrrolidin-1-yl)propyloxy chalcone containing a 3,4,5-trimethoxyphenyl group showed the highest antiproliferative activity with an IC50 value of 2.74 μM against liver cancer cells. [ABSTRACT FROM AUTHOR]

Nine chalcone derivatives containing an N-heterocyclic compound attached by its nitrogen atom to one of the benzene rings were prepared and evaluated for their antiproliferative activity against liver, gastric and neuroendocrine cancer cell lines. Most of the synthesised compounds exhibited moderate to good activity against all three cancer cell lines, but in particular, a chalcone containing a 4-(imidazol1yl)phenyl group and a 3,4,5-trimethoxyphenyl group showed the highest antiproliferative activity with an IC50 value of 5.39 μM against liver cancer cells. [ABSTRACT FROM AUTHOR]

A series of novel dithiocarbamate–chalcone derivates were designed, synthesized and evaluated for antiproliferative activity against three selected cancer cell lines (EC-109, SK-N-SH and MGC-803). Majority of the synthesized compounds exhibited moderate to potent activity against all the cancer cell lines assayed. Particularly, compounds II2 and II5 exhibited the excellent growth inhibition against SK-N-SH with IC 50 values of 2.03 μM and 2.46 μM, respectively. Further mechanism studies revealed that compound II2 could obviously inhibit the proliferation of SK-N-SH cells by inducing apoptosis and arresting the cell cycle at G0/G1 phase. [ABSTRACT FROM AUTHOR]

A series of novel coumarin derivatives were synthesized from commercially available chemical agents. All prepared compounds were evaluated for their in vitro antiproliferative activity against five selected human cancer cell lines (EC109, MGC-803, PC-3, MCF-7, and EC9706) and their in vitro antimicrobial activity against E. coli and M. albicans. 4-(3-Bromopropoxy)-2 H-chromen-2-one exhibited the highest growth inhibition against MGC-803 cell line (IC 47.7 μM) and 7-(2-bromoethoxy)-2 H-chromen-2-one exhibited the highest growth inhibition against MCF-7 cell line (IC 48.3 μM). The latter compound was also the most active against E. coli (MIC 0.27 μg/ml). [ABSTRACT FROM AUTHOR]

A series of novel chalcone-1,2,3-triazole-azole hybrids were designed, synthesized and evaluated for their antiproliferative activity against three selected cancer cell lines (SK-N-SH, EC-109 and MGC-803). Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Particularly, compound I-21 showed the most excellent antiproliferative activity with an IC50 value of 1.52 μM against SK-N-SH cancer cells. Further mechanism studies revealed that compound I-21 induced morphological changes of SK-N-SH cancer cells possibly by inducing apoptosis. Novel chalcone-1,2,3-triazole-azole derivatives in this work might be a series of promising lead compounds to develop anticancer agents for treating neuroblastoma. [ABSTRACT FROM AUTHOR]

Two new compounds, 2 S -hydroxyl-jiadifenolide ( 1 ) and jiadifenlactone acid ( 2 ), and eight known compounds were isolated from the fruits of Illicium jiadifengpi . Their structures were analysed using several spectroscopic techniques, including 1D-, 2D-NMR and HR-ESI-MS experiments. The anti-hepatitis B virus (HBV) activities of the isolates were evaluated via HBV transfection of the Hep G2.2.15 cell line. The inhibitory rates of the most active compounds, compounds 4 and 5, on the HBeAg and HBsAg expression were 28.85 ± 3.15% and 17.53 ± 1.81% and 37.93 ± 2.74% and 23.47 ± 9.52% at concentrations of 64.94 μM and 61.35 μM, respectively. [ABSTRACT FROM AUTHOR]

Highlights: [•] LC–MS/MS was used for the determination of eight banned dyes in complex food. [•] A simple sample treatment procedure without further cleanup was developed. [•] Most of the analytes have satisfactory LODs and LOQs depending on matrices. [ABSTRACT FROM AUTHOR]

NEDDylation process regulates multiple physiological functions and signaling pathways, which are still in an equilibrium that favors the survival and proliferation of tumor cells. Unlike inhibitors, NEDDylation agonists are rarely studied. In this work, novel 1,2,4-triazine-dithiocarbamate derivatives were synthesized and evaluated for antiproliferative activity against MGC-803, PC-3 and EC-109 cells. Among them, compound K3 displayed the most potent activity MGC-803, PC-3 and EC-109 cells with IC 50 values of 2.35, 5.71 and 10.1 μM, respectively, which were more potent than 5-FU. Further cellular mechanisms suggested that compound K3 inhibited the cell viability, induced proliferation inhibition, arrested cell cycle at G2/M phase and induced cell apoptosis in MGC-803 and HGC-27 cells. Importantly, compound K3 could interact with NAE1 to promote the NEDDylation of MGC-803 and HGC-27 cells. The promotion of NEDDylation resulted in the degradation of c-IAP and YAP/TAZ, which leads to the induction of cell apoptosis and inhibition of proliferation in MGC-803 and HGC-27 cells. Therefore, as a NEDDylation agonist, compound K3 could effectively inhibit gastric cancer cells. Here, we reported NEDDylation promotion induced by compound K3 , which could inhibit the cancer cell lines MGC-803 and HGC-27 and induce the cancer cell apoptosis via prompting the degradation of c-IAP and YAP/TAZ. [Display omitted] ● Novel 1,2,4-triazine dithiocarbamate derivatives were designed and prepared. ● K3 as a NEDDylation agonist exhibited potent antiproliferative activity. ● K3 promoted the NEDDylation, resulting in degradation of c-IAP and YAP/TAZ. ● K3 inhibited gastric cancer cells via promoting degradation of c-IAP and YAP/TAZ. [ABSTRACT FROM AUTHOR]

A new C18-diterpenoid alkaloid, kirinenine A (1), was isolated from the root of Aconitum kirinense, along with eight known diterpenoid alkaloids. The structures of all compounds were characterized on the basis of extensive NMR and MS analyses and by comparison with literature values, and the new one was further confirmed by X-ray crystallographic diffraction. All the compounds were isolated from the title plant for the first time. [ABSTRACT FROM AUTHOR]

Abstract: Two benzophenone glucopyranosides have been isolated from the nut shell part of Mahkota Dewa. The structures were identified as 2,4′,6-trihydroxy-4-methoxy-benzophenone-2-O-β-d-glucoside (Mahkoside A) and 2,4′,6-trihydroxy-4-methoxy-6″-acetyl-benzophenone-2-O-β-d-glucoside (Mahkoside B). Mahkoside B was recognized as a novel compound. Furthermore, a series of benzophenone glucopyranoside derivatives (compounds 3–18) were synthesized and their bioactivities were characterized. Our results demonstrated that compound 18 has significant cytotoxicity against two esophageal cancer cell lines, stomach cancer cell line and prostate cancer cell line, with IC50 less than 10μM, indicating its potential activity against cancer cells. [Copyright &y& Elsevier]

[Display omitted] Bruton tyrosine kinase (BTK) is a key kinase in the B cell antigen receptor signal transduction pathway, which is involved in the regulation of the proliferation, differentiation and apoptosis of B cells. BTK has become a significant target for the treatment of hematological malignancies and autoimmune diseases. Ibrutinib , the first-generation BTK inhibitor, has made a great contribution to the treatment of B cell malignant tumors, but there are still some problems such as resistance or miss target of site mutation. Therefore, there is an imperative need to develop novel BTK inhibitors to overcome these problems. Besides, proteolysis targeting chimera (PROTAC) technology has been successfully applied to the development of BTK degradation agents, which has opened a fresh way for the BTK targeted treatment. This paper reviews the biological function of BTK, the discovery and development of BTK targeted drugs as a promising cancer therapy. It mainly reviews the binding sites and structural characteristics of BTK, structure–activity relationships, activity and drug resistance of BTK inhibitors, as well as potential treatment strategies to overcome the resistance of BTK, which provides a reference for the rational design and development of new powerful BTK inhibitors. [ABSTRACT FROM AUTHOR]

The chalcone and quinoline scaffolds are frequently utilized to design novel anticancer agents. As the continuation of our work on effective anticancer agents, we assumed that linking chalcone fragment to the quinoline scaffold through the principle of molecular hybridization strategy could produce novel compounds with potential anticancer activity. Therefore, quinoline-chalcone derivatives were designed and synthesized, and we explored their antiproliferative activity against MGC-803, HCT-116, and MCF-7 cells. Among these compounds, compound 12e exhibited a most excellent inhibitory potency against MGC-803, HCT-116, and MCF-7 cells with IC50 values of 1.38, 5.34, and 5.21 µM, respectively. The structure–activity relationship of quinoline-chalcone derivatives was preliminarily explored in this report. Further mechanism studies suggested that compound 12e inhibited MGC-803 cells in a dose-dependent manner and the cell colony formation activity of MGC-803 cells, arrested MGC-803 cells at the G2/M phase and significantly upregulated the levels of apoptosis-related proteins (Caspase3/9 and cleaved-PARP) in MGC-803 cells. In addition, compound 12e could significantly induce ROS generation, and was dependent on ROS production to exert inhibitory effects on gastric cancer cells. Taken together, all the results suggested that directly linking chalcone fragment to the quinoline scaffold could produce novel anticancer molecules, and compound 12e might be a valuable lead compound for the development of anticancer agents. [ABSTRACT FROM AUTHOR]

This study examined intergenerational communication schemas by investigating young adults' cognitive representations of communication with older adults in Taiwan. Forty-one Taiwanese college students described conversations with an older adult in response to a variety of interviewer prompts. Transcripts were read and content analyzed by the first two authors. To capture the characteristics of the conversation descriptions, eleven coding dimensions were generated based on schema theory, and all conversation descriptions were coded along these dimensions. Coding results were submitted to hierarchical cluster analysis, yielding five schemas: Mutually satisfying, helping, mixed feelings, small talk, and mutually unpleasant conversations. Results are discussed in terms of similarities and differences from Harwood, McKee and Lin's (2000) study, schema theory, intergenerational communication, and Chinese cultural norms. [ABSTRACT FROM AUTHOR]

FAK is a nonreceptor intracellular tyrosine kinase which plays an important biological function. Many studies have found that FAK is overexpressed in many human cancer cell lines, which promotes tumor cell growth by controlling cell adhesion, migration, proliferation, and survival. Therefore, targeting FAK is considered to be a promising cancer therapy with small molecules. Many FAK inhibitors have been reported as anticancer agents with various mechanisms. Currently, six FAK inhibitors, including GSK-2256098 (Phase I), VS-6063 (Phase II), CEP-37440 (Phase I), VS-6062 (Phase I), VS-4718 (Phase I), and BI-853520 (Phase I) are undergoing clinical trials in different phases. Up to now, there have been many novel FAK inhibitors with anticancer activity reported by different research groups. In addition, FAK degraders have been successfully developed through "proteolysis targeting chimera" (PROTAC) technology, opening up a new way for FAK-targeted therapy. In this paper, the structure and biological function of FAK are reviewed, and we summarize the design, chemical types, and activity of FAK inhibitors according to the development of FAK drugs, which provided the reference for the discovery of new anticancer agents. [ABSTRACT FROM AUTHOR]

Tubulin has been regarded as an attractive and successful molecular target in cancer therapy and drug discovery. Vicinal diaryl is a simple scaffold found in many colchicine site tubulin inhibitors, which is also an important pharmacophoric point of tubulin binding and anti-cancer activity. As the continuation of our research work on colchicine binding site tubulin inhibitors, we designed and synthesized a series of diarylamide N-containing heterocyclic derivatives by the combination of vicinal diaryl core and N-containing heterocyclic skeletons into one hybrid though proper linkers. Among of these compounds, compound 15b containing a 5-methoxyindole group exhibited the most potent inhibitory activity against the tested three human cancer cell lines (MGC-803, PC-3 and EC-109) with IC50 values of 1.56 μM, 3.56 μM and 14.5 μM, respectively. Besides, the SARs of these compounds were preliminarily studied and summarized. The most active compound 15b produced the inhibition of tubulin polymerization in a dose-dependent manner and caused microtubule network disruption in MGC-803 cells. Therefore, compound 15b was identified as a novel tubulin polymerization inhibitor targeting the colchicine binding site. In addition, the results of molecular docking also suggested compound 15b could tightly bind into the colchicine binding site of β-tubulin. [ABSTRACT FROM AUTHOR]

• V7 exhibited the potent antiproliferative activity against MGC803 cells. • V7 induced cell cycle G2/M phase arrest. • V7 induced apoptosis against MGC803 cells. • V7 inhibited NEDDylation and MAPK pathways. A series of novel indole derivatives were synthesized and evaluated for their antiproliferative activity against three selected cancer cell lines (MGC803, EC-109 and PC-3). Among these analogues, 2-(5-methoxy-1 H -indol-1-yl)- N -(4-methoxybenzyl)- N -(3,4,5-trimethoxyphenyl)acetamide (V7) showed the best inhibitory activity against MGC803 cells with an IC 50 value of 1.59 μM. Cellular mechanisms elucidated that V7 inhibited colony formation, induced apoptosis and arrested cell cycle at G2/M phase. Importantly, indole analogue V7 inhibited NEDDylation pathway and MAPK pathway against MGC803 cells. [ABSTRACT FROM AUTHOR]

Abstract: Jiadifenlactone A (1), the first example of cleavage of bond [4, 9] of the seco-prezizaane-type sesquiterpenoid with a unique 9-membered ring moiety, together with its biosynthetic related compound 2, were isolated from the fruits of Illicium jiadifengpi. The structure of 1 and its relative configuration were determined by spectroscopic methods and single-crystal X-ray diffraction analysis. The inhibitory rates of compound 1 on the HBeAg and HBsAg expressions were 37.91±2.78% and 17.21±3.78%, respectively. [Copyright &y& Elsevier]

Abstract: Henrylactone F (1), an unusual nor-sesquiterpene lactone, together with a pair of stereoisomers, henrylactone G (2) and anislactone B (3), was discovered from the fruits of Illicium henryi. Their structures were elucidated based on extensive spectroscopic data analyses as well as X-ray diffraction. The anti-hepatitis B virus (HBV) activity of the isolates against the HBV transfected Hep G2.2.15 cell line was evaluated. Anislactone B (3) possessed a high therapeutic index (TI=43.4) on HBeAg secretion of the Hep G2.2.15 cell line with an IC50 value of 0.079±0.035mM. [Copyright &y& Elsevier]

NEDDylation is a post-translational modification of a protein, which transfers Ubiquitin like protein NEDD8 (Neuronal Precursor Cell-expressed Developmentally Down-regulated Protein 8) to the lysine residue of the product through a three-stage enzymatic reaction, and widely regulates many biological processes, such as cell cycle signal transduction and immune recognition. In the past ten years, we have witnessed tremendous progress in the study of protein ubiquitination modification, from modification mechanisms to drug development. Which suggests that inhibition of NEDDylation is an effective way to inhibit tumor. A variety of biological detection methods have been developed during the development of the inhibitor. In this review, we briefly introduced the modification process and substrates of NEDDylation, and discussed detection methods of NEDDylation activity in detail. This review will provide an up-to-date and comprehensive review of the methods for detecting NEDDylation activity that will contribute to NEDDylation inhibitor development. [ABSTRACT FROM AUTHOR]

Chalcone is a common scaffold found in many biologically active compounds. The chalcone scaffold was also frequently utilized to design novel anticancer agents with potent biological efficacy. Aiming to continue the research of effective chalcone derivatives to treat cancers with potent anticancer activity, fourteen amino chalcone derivatives were designed and synthesized. The antiproliferative activity of amino chalcone derivatives was studied in vitro and 5-Fu as a control group. Some of the compounds showed moderate to good activity against three human cancer cells (MGC-803, HCT-116 and MCF-7 cells) and compound 13e displayed the best antiproliferative activity against MGC-803 cells, HCT-116 cells and MCF-7 cells with IC50 values of 1.52 μM (MGC-803), 1.83 μM (HCT-116) and 2.54 μM (MCF-7), respectively which was more potent than the positive control (5-Fu). Further mechanism studies were explored. The results of cell colony formatting assay suggested compound 10e inhibited the colony formation of MGC-803 cells. DAPI fluorescent staining and flow cytometry assay showed compound 13e induced MGC-803 cells apoptosis. Western blotting experiment indicated compound 13e induced cell apoptosis via the extrinsic/intrinsic apoptosis pathway in MGC-803 cells. Therefore, compound 13e might be a valuable lead compound as antiproliferative agents and amino chalcone derivatives worth further effort to improve amino chalcone derivatives' potency. [ABSTRACT FROM AUTHOR]

On the basis and continuation of our previous studies on anti-tubulin and anti-gastric cancer agents, novel tertiary amide derivatives incorporating benzothiazole moiety were synthesized and the antiproliferative activity was studied in vitro. Preliminary structure activity relationships (SARs) were explored according to the in vitro antiproliferative activity results. Some of compounds could significantly inhibit the proliferation of three cancer cells (HCT-116, MGC-803 and PC-3 cells) and compound F10 exhibited excellent antiproliferative activity against HCT-116 cells (IC 50 = 0.182 μM), MGC-803 cells (IC 50 = 0.035 μM), PC-3 cells(IC 50 = 2.11 μM) and SGC-7901 cells (IC 50 = 0.049 μM). Compound F10 effectively inhibited tubulin polymerization (IC 50 = 1.9 μM) and bound to colchicine binding site of tubulin. Molecular docking results suggested compound F10 could bind tightly into the colchicine binding site of β-tubulin. Moreover, compound F10 could regulate the Hippo/YAP signaling pathway. Compound F10 activated Hippo signaling pathway from its very beginning MST1/2, as the result of Hippo cascade activation YAP were inhibited. And then it led to a decrease of c-Myc and Bcl-2 expression. Further molecular experiments showed that compound F10 arrested at G2/M phase, inhibited cell colony formatting and induced extrinsic and intrinsic apoptosis in MGC-803 and SGC-7901 cells. Collectively, compound F10 was the first to be reported as a new anticancer agent in vitro via inhibiting tubulin polymerization and activating the Hippo signaling pathway. Image 1 • Novel tertiary amide derivatives containing benzothiazole moiety were designed and prepared. • Compound F10 displayed excellent antiproliferative activity against gastric cancer cell lines. • Compound F10 acted as a novel colchicine site tubulin polymerization inhibitor with an IC 50 value of 1.9 μM. • Compound F10 activated Hippo signaling pathway. [ABSTRACT FROM AUTHOR]

Abstract: A new series of tanshinone IIA (DIIA) derivatives were synthesized through the reaction of brominated tanshinone IIA (1-Br DIIA) and aromatic acids in the presence of K2CO3. Twenty compounds were synthesized, and all of them were novel. Vasodilative activities for synthesized compounds were valuated in vitro on the contractile response of vascular thoracic aorta smooth muscle from Wistar rats. The results showed that most compounds exhibited a concentration-dependent inhibition on the contractile response of norepinephrine. Four prepared compounds, 4, 5, 8 and 13 revealed relatively remarkable vasodilative activity. [Copyright &y& Elsevier]