Phytochemical Analysis, Antioxidant and Enzyme-Inhibitory Activities, and Multivariate Analysis of Insect Gall Extracts of Picea koraiensis Nakai.

Picea koraiensis Nakai (PK) is an evergreen tree. It plays an important role in landscaping and road greening. Insect galls of PK are formed by parasitism of the adelgid Adelges laricis. Except for phenolics, other chemical constituents and biological activity of insect gall from PK are still unknown. Thus, here, we performed phytochemical and biological activity analyses of PK insect gall extracts, aiming to turn waste into treasure and serve human health. PK insect gall extracts were prepared using seven solvents. Antioxidant activities of the extracts were examined via antioxidant assays (radical and oxidizing substance quenching, metal chelating, and reducing power). The inhibitory activities of the extracts were determined toward the key human-disease-related enzymes α-glucosidase, α-amylase, cholinesterase, tyrosinase, urease, and xanthine oxidase. The content of numerous active constituents was high in the methanol and ethanol extracts of PK insect gall, and these extracts had the highest antioxidant and enzyme-inhibitory activities. They also showed excellent stability and low toxicity. These extracts have potential for use as stabilizers of olive and sunflower seed oils.

Three Polyoxovanadates-Based Organic-Inorganic Hybrids: Structural Variation, Bifunctional Electrocatalytic Activities, and Computational Studies.

Three bimetallic organic-inorganic hybrids based on the [V2O6]2- building unit, [Cu(pty)(V2O6)]·H2O (1), [Cu(pty)(V2O6)] (2), [Cu(tpy)(V2O6)] (3), (pty = 4'-(4″-pyridyl)-2,2':6',2″-terpyridine, tpy = 2,2':6',2″-terpyridine), were synthesized via a one-pot method. Hybrid 1 has a 1D straight chain architecture with [V2O6]2- clusters and Cu-pty complexes; hybrids 2 and 3 possess a 2D sheet structure including 10-membered rings assembled from four [Cu(pty)]2+ motifs and six [V2O6]2- clusters in 2, and two [Cu(tpy)]2+ units and eight [V2O6]2- clusters in 3. Noteworthy, hybrids 1-3 can be employed as bifunctional electrocatalysts for electroreduction of nitrite and electrooxidation of ascorbic acid. Additionally, theoretical calculations including the molecular electrostatic potential and the frontier molecular orbital were performed to estimate the electronic structure of hybrids 1-3. The natural bond orbital analysis was also calculated to interpret the electron charge distribution.

Design, synthesis and evaluation of dihydrotriazine derivatives-bearing 5-aryloxypyrazole moieties as antibacterial agents.

In the present investigation, a series of dihydrotriazine derivatives-bearing 5-aryloxypyrazole moieties were synthesized and their structures were confirmed by different spectral tools. The biological evaluation in vitro revealed that some of the target compounds exerted good antibacterial and antifungal activity in comparison with the reference drugs. Among these novel hybrids, compound 10d showed the most potent activity with minimum inhibitory concentration values (MIC) of 0.5 µg/mL against S. aureus 4220, MRSA 3506 and E. coli 1924 strain. The cytotoxic activity of the compounds 6d, 6m, 10d and 10g was assessed in MCF-7 and HeLa cells. Growth kinetics study showed significant inhibition of bacterial growth when treated with different conc. of 10d. In vitro enzyme study implied that compound 10d exerted its antibacterial activity through DHFR inhibition. Moreover, significant inhibition of biofilm formation was observed in bacterial cells treated with MIC conc. of 10d as visualized by SEM micrographs. Twenty-nine target compounds were designed, synthesized and evaluated in terms of their antibacterial and antifungal activities.

Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties.

In an attempt to search for more potent positive inotropic agents, two series of [1,2,4]triazolo[4,3-a] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties were synthesized and their positive inotropic activities evaluated by measuring left atrial stroke volume in isolated rabbit heart preparations. Several compounds showed favorable activities compared with the standard drug, milrinone. Compound 6c was the most potent agent, with an increased stroke volume of 12.53% ± 0.30% (milrinone: 2.46% ± 0.07%) at 3 × 10-5 M. The chronotropic effects of compounds having considerable inotropic effects were also evaluated.

Communicating male sexual dysfunction: The medicalization and psychologization of sexual experiences in Chinese online medical consultations.

Previous research shows that men who experience erectile or sexual dysfunction may feel uncomfortable discussing their sexual experiences in face-to-face clinical encounters. Part of the reason is the stigma and embarrassment associated with discussing private sexual matters. This study examines how e-patients, or more precisely advice-seekers, and doctors communicate about sexual dysfunction in online medical consultations (OMCs). We conducted a Theme-Oriented Discourse Analysis of relevant OMCs on CH Doctor, a Chinese medical consultation website, to understand how individuals with perceived sexual dysfunction articulate their conditions and how doctors on the platform respond and provide recommendations to these individuals. Our analysis reveals that OMCs afford advice-seekers a place to openly discuss their sexual health issues and gain empowerment from doctors who assist in mitigating the associated social stigma. Upon detailed discourse analysis, however, we find that individuals seeking advice often interpret their sexual experiences as symptoms of illness that requires medical intervention. In response, doctors tend to validate these advice-seekers' preliminary self-diagnoses by treating their conditions as medical issues and characterizing them as psychosocial problems caused by stress and anxiety. Aligning with a critical sociological perspective that views sexual dysfunction as socially constructed problems referenced against dominant norms of sexual functioning, we argue that the medicalization and psychologization of certain sexual behaviors by doctors and advice-seekers discursively reinforce and legitimize essentialist views of hetero-coital sexual interaction. Such views reify penile-vaginal intercourse and ejaculation as the only standard, successful, and desirable form of sexual activity. This may further induce fear and anxiety among adult men whose sexual behaviors do not realistically align with these norms.

Fighting rumors to fight COVID-19: Investigating rumor belief and sharing on social media during the pandemic.

The outbreak of the coronavirus disease (COVID-19) pandemic, a significant health threat, influenced information-related behaviors and induced increased rumor-sharing behaviors on social media. Fighting COVID-19 thus entails the need to fight the rumors as well, providing a strong motivation to explore rumor-related behavior during this extraordinary period. From the perspective of information acquisition, we predicted that information acquisition from social and traditional media would interactively influence rumor-related decisions (i.e., rumor belief and sharing) and that critical thinking would shape this relationship. Through a survey of 2424 individuals who used social media during the pandemic, we found that information acquisition from social media was negatively related to rumor sharing and that rumor belief mediated this relationship. Meanwhile, information acquisition from traditional media weakened the negative effect of information acquisition from social media on rumor belief, and critical thinking alleviated the positive effect of rumor belief on rumor sharing. This study contributes to the literature by explaining the diffusion of COVID-19 rumors on social media from an information perspective and revealing how different information sources and thinking styles come into conflict in rumor decisions.

Quantitative detection of surface defect using laser-generated Rayleigh wave with broadband local wavenumber estimation.

Laser ultrasonic technology has been widely used in surface defect detection attribute to its non-contact, non-destructive and high spatial resolution characteristics. This paper proposes a surface defect quantitative detection method using laser-generated Rayleigh wave with broadband local wavenumber estimation. In this method, considering the broadband characteristics of laser-generated Rayleigh wave, the broadband local wavenumber estimation is presented to achieve the defect imaging accurately, and then the defect geometric parameters are estimated based on image segmentation. A surface defect detection experiment using the laser ultrasonic detection system is conducted to verify the effectiveness of the proposed method. The experimental results show that the proposed method has superior imaging effect for vertical and inclined defects than the standing wave energy method or reflected wave energy method. Besides, the geometric parameters such as length, width, and inclination angle of a surface defect can be accurately identified by the proposed method, the errors of vertical defects are 1.6% in length and 4.0% in width respectively, as well as the maximum and minimum error of inclined defects are 5.0% and 1.28% in inclination angle respectively. The research results provide a potential application for the fast and non-destructive surface defect detection of metal structures.

Exploring rumor behavior during the COVID-19 pandemic through an information processing perspective: The moderating role of critical thinking.

In the midst of the pervasive disruption caused by the proliferation of rumors, it is unclear how individuals react to such information. Guided by the SOR theory (Stimuli-Organism-Response), our study investigates the association between different information sources (stimuli), emotions experienced by individuals (organism), and resulting rumor behaviors such as sharing and refuting (response). Furthermore, we examine the moderating role of individual critical thinking in this process. Using the COVID-19 pandemic as a study scenario, we collected questionnaire data from 4588 respondents. Our results reveal a large positive association between pandemic-related information and feelings of fear. Additionally, a medium negative correlation between fear and rumor sharing was observed while a moderate positive correlation between fear and rumor refuting was identified. Moreover, we found that individual critical thinking abilities can effectively moderate the relationship between fear and online COVID-19-related information and strengthen the link between fear and rumor sharing while weakening the link between fear and rumor refuting. Additionally, our study indicates that an individual's fear plays a mediating role in the relationship between information sources and rumor behavior. Our findings shed light on the information processing mechanisms underlying rumor behaviors and yield practical and policy implications for managing them.

Synthesis and in-vitro inotropic evaluation of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides.

We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-phenyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit-heart. Several compounds were developed from, and showed favorable activities compared with the standard drug milrinone. Compound 5o was the most potent with an increased stroke volume of 9.17 ± 0.14% (milrinone 2.47 ± 0.08%) at 3 × 10⁻5 M in our in-vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated.

Four new dual-functional electro-catalysts formed from small molybdenum clusters and Cu-pyridyl complexes.

By changing N-heterocyclic ligands in the same Mo7/Cu/N-ligand reaction systems, four new organic-inorganic hybrids based on isopolymolybdates, [Cu2(tpy)2(ß-Mo8O26)0.5(γ-Mo8O26)0.5]·0.25H2O (1), [Cu2(tpy)2(H2O)2(ß-Mo8O26)] (2), [Cu(bpy)(Mo3O10)]·H2O (3), and [Cu(bpy)(H2O)(ß-Mo8O26)0.5]0.5 (4) (tpy = 2,2':6',2''-terpyridine and bpy = 2,6-bis(pyrazol-1-yl) pyridine), were prepared using hydrothermal methods at different pH values. X-ray structural analysis shows that compound 1 has a 1D {-ß-[Mo8O26]-Cu2-γ-[Mo8O26]}n straight chain structure with mixed ß-[Mo8O26] and γ-[Mo8O26] polyoxoanions; compound 2 possesses a 3D supramolecular structure based on [Cu(tpy)]2+ motifs and ß-[Mo8O26] clusters; and compound 3 has a 1D chain structure built from [Cu(bpy)]2+ and [Mo3O10]2- units. In compound 4, [ß-Mo8O26] clusters are linked by [Cu(bpy)]2+ motifs to give rise to a 2D sheet structure including {(ß-Mo8O26)4Cu4} 8-membered rings. Cyclic voltammograms of compounds 1-4 display discrepant dual-functional electro-catalytic activities toward the reduction of nitrite and the oxidation of ascorbic acid in acidic solution. Electrocatalytic tests indicate that the [Mo3O10]2--based organic-inorganic hybrid exhibits better electro-catalytic performances than [Mo8O26]4--type hybrids towards oxidation and reduction.

Synthesis and positive inotropic evaluation of 2-(4-(4-substituted benzyloxy)-3-methoxybenzyl)-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-methyl[1,2,4]triazolo[4,3-a]quinolin-7-yl)-acetamides.

In an attempt to search for more potent positive inotropic agents, a series of 2-(4-(4-substituted benzyloxy)-3-methoxybenzyl)-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-methyl[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides was synthesized and their positive inotropic activities were evaluated by measuring left atrium stroke volume on isolated rabbit-heart preparations. Several compounds showed favorable activity compared with the standard drug Milrinone among which 2-(4-(4-(2-chlorobenzyloxy)-3-methoxybenzyl)-1,4-diazepan-1-yl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamide 6e was found to have the most desirable potency with the 6.79 +/- 0.18% increased stroke volume (Milrinone: 1.67 +/- 0.64%) at a concentration of 1 x 10(-5) M in our in-vitro study. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.

Synthesis of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol-6-yl)acetamides as inotropic agents.

We describe the synthesis and positive inotropic evaluation of a series of 2-(4-substitutedbenzylpiperazin-1-yl)-N-(2-oxo-2,3-dihydrobenzooxazol-6-yl)acetamides by measuring left atrial stroke volume in preparations of isolated rabbit hearts. Several compounds were developed from and showed favorable activities compared with the standard drug milrinone. Compound 4l was the most potent with an increased stroke volume of 11.78 ± 0.18% (milrinone 6.36 ± 0.13%) at 1 × 10(-4) M in our in-vitro study. The chronotropic effects of compounds having inotropic effects were also evaluated.

Synthesis and antitumor activity of dehydroepiandrosterone derivatives on Es-2, A549, and HepG2 cells in vitro.

A series of dehydroepiandrosterone derivatives containing an acid ester was synthesized and evaluated for their antitumor activity on ES-2, A549, and HepG2 cells by the MTT assay. Most compounds showed antitumor activity, while compounds 1c, 2i, and 2o exhibited more potential inhibitory effects compared with dehydroepiandrosterone on ES-2 cells, A549 cells, and HepG2 cells, respectively.

Synthesis of new chalcone derivatives bearing 2,4-thiazolidinedione and benzoic acid moieties as potential anti-bacterial agents.

A series of chalcone derivatives bearing the 2,4-thiazolidinedione and benzoic acid moieties (8a-s) were synthesized, characterized, and evaluated for their anti-bacterial activity. Among the tested compounds, the most effective were 8a, 8h, 8k, 8n and 8q with MIC value in the range of 0.5-4 µg/mL against six Gram-positive bacteria (including multidrug-resistant clinical isolates). None of the compounds exhibited any activity against the Gram-negative bacteria Escherichia coli 1356 and E. coli 1682 at 64 µg/mL.

Synthesis of 2-(4-substitutedbenzyl-[1,4]diazepan-1-yl)-n-(1-methyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides as inotropic agents.

In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)acetamides were synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume in isolated rabbit heart preparations. Some of these derivatives exhibited favorable activity compared with the standard drug, milrinone, among which 2-(4-(4-methylbenzyl)-[1,4]-diazepan-1-yl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamide (6m) was the most potent, increasing stroke volume by 8.38±0.16% (milrinone 2.45± 0.06%) at 3 x 10(-5) m. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.

Synthesis and anti-tumor evaluation of panaxadiol derivatives.

A series of panaxadiol derivatives have been synthesized by the simple acylation of the 3-hydroxy group of panaxadiol. The anti-tumor activities of the synthesized compounds were evaluated against a panel of human tumor cell lines by the standard MTT assay. Compounds 2, 11, 12, 13, 14, 15 and 16 showed stronger antiproliferative activities than that of Rg3 and PD on the growth of the distinct cancer cell lines in vitro.

Synthesis of 2-(4-substitutedmethylpiperazin-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamides and their positive inotropic evaluation.

In an attempt to search for more potent positive inotropic agents, a series of 2-(4-substitutedmethylpiperazin-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamides were synthesized and their positive inotropic activities were evaluated by measuring left atrium stroke volume on isolated rabbit heart preparations. Several compounds showed favorable activities compared with the standard drug, milrinone, among which 2-(4-(4-methylbenzyl)piperazin-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamide 4e showed the most potent activity with the 5.09+/-0.00% increased stroke volume (milrinone 1.67+/-0.64%) at a concentration of 1x10(-5)M in our in vitro study. The chronotropic effects of those compounds having significant inotropic effects were also evaluated in this work.