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Glioblastoma (GBM), a predominant central nervous system (CNS) malignancy, is correlated with high mortality and severe morbidity. Mammalian methyltransferase-like 7B (METTL7B) as a methyltransferase has been identified to participate in cancer progression. However, its function in GBM is elusive. Accordingly, we aimed to explore the effect of METTL7B on GBM. The expression of METTL7B and EGR2 in GBM patients and GBM cells were detected by qPCR, western blots and immunohistochemical staining. Cell viability was assessed by CCK-8 assays. Cell proliferation was determined by EdU, colony formation, and tumor sphere formation assays. METTL7B shRNA was injected into the Balb/c nude mice. The size and weight of isolated tumor was measured. And the expression levels of Ki67, METTL7B and EGR1 were examined by immunohistochemical staining. METTL7B was significantly elevated, while EGR1 was downregulated in clinical GBM tissues. METTL7B upregulation was associated with the low overall survival of GBM patients. Moreover, METTL7B depletion remarkably attenuated GBM cell proliferation. Mechanistically, METTL7B overexpression inhibited EGR1 expression in GBM cells. EGR1 knockdown rescued the inhibitory effect of METTL7B depletion on GBM cell proliferation. Meanwhile, METTL7B depletion arrested more GBM cells at the G0/G1, but fewer cells at the S phase, which EGR1 knockdown reversed these effects. Furthermore, tumorigenicity analysis revealed that METTL7B promotes tumor growth of GBM cells in vivo. METTL7B contributes to the malignant progression of GBM by inhibiting EGR1 expression. METTL7B and EGR1 may be utilized as the treatment targets for GBM therapy.

Type 2 diabetes mellitus (T2DM) has become a universal and chronic global public health concern and causes multiple complex complications. In order to meet the rapidly growing demand for T2DM treatment, increased research has been focused on hypoglycemic drugs. Cyclocarya paliurus (Batal.) Iljinsk is the only living species of the genus Cyclocarya Iljinskaja, whose leaves have been extensively used as a functional tea to treat obesity and diabetes in China. An enormous amount of very recent pharmacological research on the leaves of C. paliurus has demonstrated that they carry out numerous biological activities, such as hypoglycemic, anti-inflammatory, and intestinal microbiota regulation. Multiple in vitro and in vivo studies have also shown that the extracts of C. paliurus leaves are innocuous and safe. This study aims to provide an up-to-date review of the botany, traditional uses, phytochemistry, pharmacological effects against diabetes, toxicology, and clinical studies of C. paliurus leaves, in hopes of promoting a better understanding of their role in the prevention and treatment of T2DM.

Targeted drug-delivery systems are a growing research topic in tumor treatment. In recent years, mesoporous silica nanoparticles (MSNs) have been extensively studied and applied in noninvasive and biocompatible drug-delivery systems for tumor therapy due to their outstanding advantages, which include high surface area, large pore volume, tunable pore size, easy surface modification and stable framework. The advances in the application of MSNs for anticancer drug targeting are covered and highlighted in this review, and the challenges and prospects of MSN-based targeted drug-delivery systems are discussed. This review provides new insights for researchers interested in targeted drug-delivery systems against cancer.

Wound healing is a complicated process that influences patient's life quality. Plant-based polysaccharide has recently gained interest in its use in wound dressing materials because of its biological compatibility, natural abundance, and ideal physiochemical properties. The present study reveals the potential of polysaccharide isolated from Moringa oleifera seed (MOS-PS) and its nanocomposite with silver (MOS-PS-AgNPs) as alternative materials for wound dressing. First, MOS-PS was isolated and structurally characterized by TLC, HPLC, FTIR, NMR, and GPC analyses. A green and simple method was used to synthesize AgNPs using MOS-PS as a stabilizing and reducing agent. The size, morphology, and structure of the MOS-PS-AgNPs were characterized by UV-Vis spectroscopy, X-ray diffraction, scanning electron microscopy, transmission electron microscopy, and zeta potential analysis. The results showed that the MOS-PS-AgNPs were spherically shaped, having no cytotoxicity toward mouse fibroblasts cells and promoting their in-vitro migration. Moreover, the MOS-PS-AgNPs displayed strong anti-microbial activity against wound infectious pathogenic bacteria. Finally, the MOS-PS-AgNPs were used for dressing animal wounds and its preliminary mechanism was studied by RT-PCR and histological analysis. The results showed that the MOS-PS-AgNPs can promote wound contraction and internal tissue growth well. Overall, our results indicated that the MOS-PS-AgNPs might be an excellent candidate for use as an optimal wound dressing material.

Type 2 diabetes mellitus (T2DM) has become a universal and chronic global public health concern and causes multiple complex complications. In order to meet the rapidly growing demand for T2DM treatment, increased research has been focused on hypoglycemic drugs.

A novel electrochemical method for the synthesis of α,β-epoxy ketones is reported. With KI as the redox mediator, methyl ketones reacted with aldehydes under peroxide- and transition metal-free electrolytic conditions and afforded α,β-epoxy ketones in one pot (36 examples, 52-90% yield). This safe and environmental-friendly method has a broad substrate scope and can readily provide a variety of α,β-epoxy ketones in gram-scales for evaluation of their anti-cancer activities.

Glutaminyl cyclase (QC) is responsible for converting the N-terminal glutaminyl and glutamyl of the proteins into pyroglutamate (pE) through cyclization. It has been confirmed that QC catalyzes the formation of neurotoxic pE-modified Aβ in the brain of AD patients. But the effects of upregulated QC in diverse diseases have not been much clear until recently. Here, RNA sequencing was applied to identify differentially expressed genes (DEGs) in PC12 cells with QC overexpressing or knockdown. A total of 697 DEGs were identified in QC overexpressing cells while only 77 in QC knockdown cells. Multiple bioinformatic approaches revealed that the DEGs in QC overexpressing group were enriched in endoplasmic reticulum stress (ERS) related signaling pathways. The gene expression patterns of 23 DEGs were confirmed by RT-qPCR, in which the genes related to ERS showed the highest consistency. We also revealed the protein levels of GRP78, PERK, CHOP, and PARP-1, and caspase family was significantly upregulated by overexpressing QC. Moreover, overexpressing QC significantly increased apoptosis of PC12 cells in a time dependent manner. However, no significant alteration was observed in QC knockdown cells. Therefore, our study indicated that upregulated QC could induce ERS and apoptosis, which consequently trigger diseases by catalyzing the generation of pE-modified mediators.

Feline parvovirus causes infectious diseases, and Chaphamaparvovirus is a novel type of feline parvovirus. The present study aims to establish a method that can be used in clinical rapid detection of feline Chaphamaparvovirus (FeChPV), for facilitate the timely and effective diagnosis and treatment of sick animals and shorten the diagnosis time of clinical diseases. The experimental samples in this study are from 20 cats undergoing physical examination in Hefei Xin'an Animal Hospital. An SYBR Green I-based qPCR assay was performed to detect FeChPV. A pair of specific primers was designed based on the

Nonlinear tri-stable piezoelectric energy harvesters with magnetic field coupling have attracted many researchers’ interest in ambient vibration energy harvesting and conversion. In such a tri-stable piezoelectric energy harvester, the nonlinear magnetic force generated by the external magnetic field is mainly calculated by the equivalent magnetic dipole method. However, this method will give highly erroneous results when the magnetic separation distance is small. This study presents a modified magnetic force model to precisely calculate the nonlinear magnetic force exerted on the tip of the cantilever beam. Unlike the equivalent magnetic dipole method regarding the magnet as a point dipole at its body center, this model only considers the surface magnetization current of the left and right surfaces of the magnets and replaced them by the one of the center point dipoles on these associated surfaces. With this model, the nonlinear magnetic force, the potential energy, and the transition mechanism of the tri-stable piezoelectric energy harvester are numerically investigated. Experimental validations are consequently performed to testify the numerical results. Compared with the equivalent magnetic dipole method, the modified magnetic force model has a much higher accuracy to be more applicable for different magnetic separation distances, especially when the magnetic separation distance is small.

Piezoelectric ultrasonic actuators (PUA) are fascinating and precision-controlled actuators in some mechatronics systems. This study proposed an energy harvesting type piezoelectric ultrasonic actuator (H-PUA) and investigated its mechanical and energetic characteristics. The proposed H-PUA has a sandwich-type stator composed of a metal body, an exciting piezoelectric (PZT) ring and a harvesting PZT ring. The exciting PZT ring bonded on the bottom surface of the stator was used to produce a traveling wave, and the harvesting PZT ring bonded on the top surface of the stator was used to harvest the vibration-induced energy of the stator and convert it into electric energy. Sensitivity analysis method was used to optimize the stator structure. Finite element analysis using ANSYS software was performed for both the mechanical and energetic characteristics of the new actuator. A prototype H-PUA was fabricated and subsequently used to test the mechanical and energetic characteristics. When the rotor torque is zero and the pre-pressure is 100 N, the prototype H-PUA has mechanical output characteristics of no-load speed 112 rpm and stalling torque 0.78 Nm when the exciting voltage amplitude is 152 V0−p with frequency 36.0 kHz. The maximum harvesting output power of a sector area of the harvesting PZT ring reaches 54 mW when it is connected to an optimized load resistance 11 kΩ. Experiments have shown that the harvesting output energy can fully meet with the power supply demands of some low-power (i.e., mW/μW level) mechatronics systems, such as LED.

Pyroglutamate (pE) modification, catalyzed mainly by glutaminyl cyclase (QC), is prevalent throughout nature and is particularly important in mammals including humans for the maturation of hormones, peptides, and proteins. In humans, the upregulation of QC is involved in multiple diseases and conditions including Alzheimer's disease, Huntington's disease, melanomas, thyroid carcinomas, accelerated atherosclerosis, septic arthritics, etc. This upregulation catalyzes the generation of modified mediators such as pE-amyloid beta (As) and pE-chemokine ligand 2 (CCL2) peptides. Not surprisingly, QC has emerged as a reasonable target for the development of therapeutics to combat these diseases and conditions. In this manuscript the deleterious effects of upregulated QC resulting in disease manifestation are reviewed, along with progress on the development of QC inhibitors.

Inflammatory bowel disease (IBD) is a chronic inflammatory intestinal disorder that is difficult to cure and characterized by periods of relapse. To face the challenges of limited treatment strategies and drawbacks of conventional medications, developing new and promising strategies as well as safe and effective drugs for treatment of IBD has become an urgent demand for clinics. The imbalance of Th17/Treg is a crucial event for the development of IBD, and studies have verified that correcting the imbalance of Th17/Treg is an effective strategy for preventing and treating IBD. Recently, a growing body of studies has indicated that phytochemicals derived from natural products are potent regulators of Th17/Treg, and exert preferable protective benefits against colonic inflammation. In this review, the great potential of anti-colitis agents derived from natural products through targeting Th17/Treg cells and their action mechanisms for the treatment or prevention of IBD in recent research is summarized, which may help further the development of new drugs for IBD treatment.

Alzheimer's disease (AD) is one of the most common neurodegenerative causes of dementia, the pathology of which is still not much clear. It′s challenging to discover the disease modifying agents for the prevention and treatment of AD over the years. Emerging evidence has been accumulated to reveal the crucial role of up‐regulated glutaminyl cyclase (QC) in the initiation of AD. In the current study, the QC inhibitory potency of a library consisting of 1621 FDA‐approved compounds was assessed. A total of 54 hits, 3.33 % of the pool, exhibited QC inhibitory activities. The Ki of the top 5 compounds with the highest QC inhibitory activities were measured. Among these selected hits, compounds affecting neuronal signaling pathways and other mechanisms were recognized. Moreover, several polyphenol derivatives with QC inhibitory activities were also identified. Frameworks and subsets contained in these hits were analyzed. Taken together, our results may contribute to the discovery and development of novel QC inhibitors as potential anti‐AD agents., Up‐regulated glutaminyl cyclase (QC) has a crucial role in the initiation of Alzheimer's disease (AD).The QC inhibitory potency of a library containing 1621 FDA‐approved compounds was investigated. Molecule scaffolds and motifs contained in these hits (3.33 % of the pool) are suggested to be combined into the design of new fragment like libraries targeting QC. This approach may support the development of novel QC inhibitors as potential anti‐AD agents.

Polymers with aggregation-induced emission (AIE) characteristics have aroused tremendous interest because of their potential applications in large-area flexible display and luminescent self-assembling, and as stimuli-responsive and porous materials. However, the design of AIE-active polymers is always not as easy as that of small molecules because their properties are hard to predict. In some cases, the polymers prepared from the AIE-active monomers show the aggregation-caused quenching (ACQ) instead of AIE effect. To understand the structure-property relationship of the polymers constructed from the AIE monomers, in this paper, two pyrazine-containing AIE monomers were utilized to construct luminescent polymers by click polymerization. The photophysical property investigation indicates that the polytriazole containing tetraphenylpyrazine units is AIE-active, whereas that bearing 2,3-dicyano-5,6-diphenylpyrazine units suffers from the ACQ effect. Through systematical investigation, the cause for such difference was unveiled. Thus, this work provides a useful guidance for further design of AIE-active polymers.

A procedure is described to measure curcumin (C), demethoxycurcumin (DMC), bisdemethoxycurcumin (BDMC), tetrahydrocurcumim (TC) and their glucuronidated metabolites (CG, DMCG, and BDMCG) in plasma, brain, liver and tumor samples. The procedure involves converting the analytes to their boron difluoride derivatives and analyzing them by combined liquid chromatography coupled to an ion trap mass spectrometer operating in the negative ion MSn scan mode. The method has superb limits of detection of 0.01 nM for all curcuminoids and 0.5 nM for TC and the glucuroniated metabolites, and several representative chromatograms of biological samples containing these analytes are provided. In addition, the pharmacokinetic profile of these compounds in one human who daily consumed an over-the-counter curcuminoid product shows the peak and changes in circulating concentrations achieved by this mode of administration.

Ferroptosis is an iron- and lipotoxicity-dependent regulated cell death that has been implicated in various diseases, such as cancer, neurodegeneration and stroke. The biosynthesis of phospholipids, coenzyme Q10, and glutathione, and the metabolism of iron, amino acids and polyunsaturated fatty acid, are tightly associated with cellular sensitivity to ferroptosis. Up to now, only limited drugs targeting ferroptosis have been documented and exploring novel effective ferroptosis-modulating compound is needed. Natural bioactive products are conventional resources for drug discovery, and some of them have been clinically used against cancers and neurodegenerative diseases as dietary supplements or pharmaceutic agents. Notably, increasing evidence demonstrates that natural compounds, such as saponins, flavonoids and isothiocyanates, can either induce or inhibit ferroptosis, further expanding their therapeutic potentials. In this review, we highlight current advances of the emerging molecular mechanisms and disease relevance of ferroptosis. We also systematically summarize the regulatory effects of natural phytochemicals on ferroptosis, and clearly indicate that saponins, terpenoids and alkaloids induce ROS- and ferritinophagy-dependent ferroptosis, whereas flavonoids and polyphenols modulate iron metabolism and nuclear factor erythroid 2-related factor 2 (NRF2) signaling to inhibit ferroptosis. Finally, we explore their clinical applications in ferroptosis-related diseases, which may facilitate the development of their dietary usages as nutraceuticals.

Esophageal cancer is one of the leading cause of cancer mortality in the world. Due to the increased drug and radiation tolerance, it is urgent to develop novel anticancer agent that triggers nonapoptotic cell death to compensate for apoptosis resistance. In this study, we show that treatment with gypenoside L (Gyp-L), a saponin isolated from Gynostemma pentaphyllum, induced nonapoptotic, lysosome-associated cell death in human esophageal cancer cells. Gyp-L-induced cell death was associated with lysosomal swelling and autophagic flux inhibition. Mechanistic investigations revealed that through increasing the levels of intracellular reactive oxygen species (ROS), Gyp-L triggered protein ubiquitination and endoplasm reticulum (ER) stress response, leading to Ca2+ release from ER inositol trisphosphate receptor (IP3R)-operated stores and finally cell death. Interestingly, there existed a reciprocal positive-regulatory loop between Ca2+ release and ER stress in response to Gyp-L. In addition, protein synthesis was critical for Gyp-L-mediated ER stress and cell death. Taken together, this work suggested a novel therapeutic option by Gyp-L through the induction of an unconventional ROS-ER-Ca2+-mediated cell death in human esophageal cancer.

Glutaminyl cyclase (QC) plays an important role in the pathogenesis of Alzheimer's disease (AD) and can be a potential target for the development of novel anti-AD agents. However, the study of QC inhibitors are still less. Here, phenol-4' (R1-), C5-OH (R2-) and C7-OH (R3-) modified apigenin derivatives were synthesized as a new class of human QC (hQC) inhibitors. The efficacy investigation of these compounds was performed by spectrophotometric assessment and the structure-activity relationship (SAR) was evaluated. Molecular docking was also carried out to analyze the binding mode of the synthesized flavonoid to the active site of hQC.

Alzheimer's disease (AD) is a multifactorial and socioeconomically burdensome disease. In view of the failures of anti-AD candidates, we should try to rethink what we did before and what we should do next, in part at least. Research shows that the more neurotoxic factor, pyroglutamate-Aβs, and the more important inflammatory mediators, pyroglutamate-CCL2, both contribute to the initiation of AD specifically and the generation of N-terminal intramolecular cyclization catalyzed by glutaminyl cyclase quality control, the over-expression of which correlates positively with the severity of AD. Subsequently, lowering pyroglutamate-Aβs and pyroglutamate-CCL2 levels by quality control inhibition using small molecule inhibitors could be expected as an amazing strategy for the prevention and treatment of AD.

Piezoelectric ceramics are fascinating function materials and have good electromechanical coupling properties that can be used to develop various types of composite devices. Recently, piezoelectric composite devices with multifunctional demands have been extensively desired due to the remarkable developments of mechatronics systems. This paper focuses on developing a novel multifunctional composite device by using one single PZT ring, in which a piezoelectric actuator, a sensor and an energy harvester are embedded. The composite device is mainly composed of a rotary rotor and a piezoelectric vibrator, the piezoelectric vibrator is formed by a metal elastomer mechanically bonded together with a piezoelectric ceramic ring. The piezoelectric ceramic ring is polarized into three regions to produce the actuating, sensing and energy harvesting functions. The mathematical model of the composite device was derived and validated by experiment. A prototype was fabricated and the experiments including the mechanical, energetic and transient characteristics were performed and discussed. The results indicate that the composite device reaches the maximum torque, no-load speed and mechanical power of 0.674 Nm, 118 rpm and 2.65 W when it is excited by a voltage signal with amplitude 67 V and frequency 40 kHz; the results also show that the maximum extracted power of the composite device reaches 305 mW when the load resistance is 11.6 kΩ, the composite device has a rapid response speed with startup time less than 5 ms and shutdown time less than 1 ms.

Because of the crucial roles of upregulated glutaminyl cyclase (QC) in the initiation and development of Alzheimer's disease (AD), QC inhibitors are supposed as disease-modifying agents for the treatment of AD. And reported compounds encourage this hypothesis greatly based on the remarkable anti-AD effects in vivo. To illustrate the mechanism in detail, the actions of a selected QC inhibitor (23) were assessed firstly in a cell system here. It was demonstrated that QC activities and the generation of pyroglutamate-modified β-amyloids in PC12 cells were both inhibited obviously after the treatment of 23. A total of 13 and 15 genes were up- and downregulated significantly in treated cells by RNA-sequencing analysis. Quantitative real-time polymerase chain reaction, enzyme-linked immunosorbent assay, WB, and immunofluorescence analysis supported the effects of 23 on the transcriptome of PC12 cells consequently. The expressions of chaperones, heat shock proteins (HSP) 70, and 90, were upreglutated, while gene expression of actin and the level of encoded protein were reduced significantly in PC12 cells with the treatment. Furthermore, the regulations of ribosome were observed after the treatment. These results indicate the potency of 23 to improve the translation, expression and folding regulation of proteins and affect the multivalent cross-linking of cytoskeletal protein and other proteins subsequently in the cell system and might contribute to the understanding of the mechanism of QC inhibitor as potential anti-AD agents.

The anionic polytriazole PI with a weight-average molecular weight of 190 300 was facilely and directly prepared in an excellent yield of 98.1% in 6 h by the well-established Cu(I)-catalyzed click polymerization of 4,4′-diazido-2,2′-stilbenedisulfonic acid disodium salt hydrate (1) and AIE-active tetraphenylethene (TPE)-containing diyne (2) under mild reaction conditions. PI is soluble in high polar solvents, and thermally stable with 5% loss of its weight at temperatures higher than 290 °C. The photo-physical property investigation showed that PI possesses the unique feature of aggregation-enhanced emission (AEE). By taking this feature, PI could be used for the specific detection of aluminum ions with a threshold as low as 31 ppb, which could potentially be used for strict drinking water purity control of the aluminum ion content.

An air-stable supported Cu(I) catalyst, CuI@PS-Phen, was designed and synthesized. CuI@PS-Phen can efficiently catalyze the click polymerization of diynes a and diazides b to produce soluble and thermally stable polytriazoles with high molecular weights (M w up to 30800), and low copper residue content (down to 190 ppm) in high yields (up to 94.2%) under mild reaction conditions without the exclusion of oxygen.

To help produce hypoallergenic food, this study investigated reducing the allergenicity and improving the functional properties of bovine β-lactoglobulin (βLG) by covalent conjugation with (-)-epigallo-catechin 3-gallate (EGCG) and chlorogenic acid (CA). The covalent bond between the polyphenols and the amino acid side-chains in βLG was confirmed by MALDI-TOF-MS and SDS-PAGE. Structural analysis by fluorescence spectroscopy, circular dichroism (CD) and Fourier transform infrared (FTIR) indicated that the covalent conjugate of EGCG and CA led to the changed protein structure of βLG. Western blot analysis and enzyme-linked immunosorbent assay indicated that conjugation of βLG with these polyphenols was effective in reducing the IgE-binding capacity of βLG. The conjugates maintained the retinol-binding activity without denaturation the protein and enhanced the thermal stability with high antioxidant activity. The study provides an innovative approach to producing hypoallergenic food.

Downregulation of apoptotic signal pathway and activation of protective autophagy mainly contribute to the chemoresistance of tumor cells. Therefore, exploring efficient chemotherapeutic agents or isolating novel natural products that can trigger nonapoptotic and nonautophagic cell death such as lysosome-associated death is emergently required. We have recently extracted a saponin, gypenoside L (Gyp-L), from Gynostemma pentaphyllum and showed that Gyp-L was able to induce nonapoptotic cell death of esophageal cancer cells associated with lysosome swelling. However, contributions of vacuolization and lysosome to cell death remain unclear. Herein, we reveal a critical role for NADPH oxidase NOX2-mediated vacuolization and transcription factor EB (TFEB) activation in lysosome-associated cell death. We found that Gyp-L initially induced the abnormal enlarged and alkalized vacuoles, which were derived from lipid rafts dependent endocytosis. Besides, NOX2 was activated to promote vacuolization and mTORC1-independent TFEB-mediated lysosome biogenesis. Finally, raising lysosome pH could enhance Gyp-L induced cell death. These findings suggest a protective role of NOX2-TFEB-mediated lysosome biogenesis in cancer drug resistance and the tight interaction between lipid rafts and vacuolization. In addition, Gyp-L can be utilized as an alternative option to overcome drug-resistance though inducing lysosome associated cell death.

The “thio-click” polymerization is a well-expanded concept of click polymerization. Among the click polymerizations, the thiol–yne click polymerization is less developed and still in its infancy stage. In general, UV light, elevated temperature, amine, or transition metal complexes is needed to catalyze the thiol–yne click polymerization, which greatly complicates the experimental operation and limits its application. In this work, a facile and powerful thiol–yne click polymerization was developed, which could be carried out under very mild conditions without using external catalyst. Simply mixing the aromatic diynes (1a–1e) and dithiols (2–4) with equivalent molar ratio in THF at 30 °C will readily produce soluble and regioregular functional poly(vinylene sulfide)s (PIa–PIe, PII, and PIII) with high molecular weights (Mw up to 85 200) in excellent yields (up to 97%) after as short as 2 h. Furthermore, no double addition product of an ethynyl group was found. This catalyst-free thiol–yne click polymerizat...

Accurate determination of the squeeze-film damping in rare air is crucial for the design of high-Q MEMS devices. In the past, for the MEMS structures with no perforations, there have been two approaches to treating the squeeze-film damping in rare air: the approach based on the continuum assumption and the approach using molecular dynamics (MD) method. The amount of squeeze-film damping can be controlled by providing perforations in microstructures. To model perforation effects on squeeze-film damping, many methods have been proposed. However, almost all the previous methods are based on the continuum assumption. Only one paper focuses on analytical modeling of squeeze-film damping of a perforated microplate using the MD method. Hutcherson and Ye (J Micromech Microeng 14:1726–1733, 2004) developed a novel MD method to model the squeeze-film damping in free molecular regime. The method possesses high computational efficiency. However, their work is valid only for non-perforated rectangular microplate. This paper presents a numerical MD approach for calculating the squeeze-film damping of a perforated rectangular plate and a perforated circular plate in free molecular regime. In Hutcherson and Ye’s work, the microplate is non-perforated. After each collision with the non-perforated plate, all the molecules are reflected to the substrate. In this paper, the plate is perforated. For the molecules in the air gap striking the surface of the perforated microplate, some of the molecules are reflected to the substrate. The rest leave the air gap through the perforations. This paper is an extension of the work done by Hutcherson and Ye (J Micromech Microeng 14:1726–1733, 2004). The accuracy of the present numerical MD approach is verified by comparing its results with the experimental results available in the literature and the finite element method results.

The first example of InCl3-catalyzed polycyclotrimerization of diynes to generate regioregular hyperbranched polymers was developed. The InCl3/2-iodophenol-catalyzed polycyclotrimerization of aromatic/aliphatic diynes in chlorobenzene readily furnished soluble 1,3,5-trisubstituted benzene-cored hyperbranched polyarylenes with high weight-averaged molecular weights (up to 37200) in high yields (up to 87.8%). Thanks to its low cost and moisture-tolerance, this catalytic system is promising to be widely applied in preparation of regioregular functional hyperbranched polymers with unique properties.

Panax ginseng C. A. Mey has been used as a traditional medicine and functional food in Asia for thousands of years for its improvement of human immunity and metabolism and its antitumor and antifatigue activities. This study reports the impact of storage conditions and storage period on the quality of P. ginseng. The contents of four major ginsenosides in P. ginseng and phosphorylation activities of Akt of ginseng extracts were affected by both storage conditions and storage period. In contrast, the ATP generation capacity of ginseng extracts was affected by storage conditions, but not by storage period. The results showed that the quality of P. ginseng could be well maintained at a relative humidity between 70% and 90%, and dry conditions might decrease the quality of P. ginseng. Through dual-index evaluation, the present study extended our knowledge on the changes of ginsenosides and bioactivities in P. ginseng with respect to different storage conditions and storage periods.

The metal-free click polymerization (MFCP) of azide and alkyne has become a powerful tool for the synthesis of functional polytriazoles. Among which, the MFCP of propiolate and azide has been used to prepare functional linear poly(aroxycarbonyltriazole)s (PACTs). Their hyperbranched analogues, however, have been rarely prepared. In this paper, hyperbranched PACTs with satisfactory molecular weights and high regioregularities were synthesized in high yields by the MFCP of tripropiolates (1) and tetraphenylethene (TPE)-containing diazide (2) under the optimized reaction conditions without protection from oxygen and moisture. The resultant polymers are soluble in common organic solvents and thermally stable, with 5% loss of their weights at temperatures higher than 330 °C. The polymers exhibit high refractive indices with low chromatic dispersion. Thanks to their contained TPE units, the polymers show the unique feature of aggregation-induced emission, and their aggregates can function as fluorescent sensors...

Ligustrum purpurascens, named as "Ku ding cha", has been used as a kind of functional tea in southern China for about two thousand years, which has the effects on diuresis, anti-hypertension, weight-loss and anti-inflammation.This study was aimed to investigate the immune enhancement effects of the crude phenylethanoid glycosides (CPGs) from Ligustrum. Purpurascens on mice and analyze the chemical profiles of phenylethanoid glycosides in the CPGs.The immune functions enhancing potential of CPGs was determined using serum hemolysin antibody, phagocytosis, splenocyte antibody production, and NK cells activity assays. The contents of five major constituents in the crude glycosides of Ligustrum purpurascens were determined by using liquid chromatography, other five glycosides were deduced according to their UV and MS spectra compared with the literature as well.In the immunizing experiment, mice treated with different doses of CPGs showed an increase (p0.01) in the haemagglutination titre compared with the control group. The increases (p0.05) were found to be significant at doses of 440 mg/kg and 1.32 g/kg in the experiments of antibody production of spleen cells, MΦ phagocytosis of chicken RBCs and NK cell activity. Further chemical characterization yielded 10 constituents from CPGs, five glycosides were quantified by HPLC and the structures of other five compounds were speculated according to their UV and MS spectra.The results suggested that phenylethanoid glycosides from Ligustrum purpurascens have immunomodulatory effects on mice.

In our effort to develop novel plant-derived acaricides, we examined the contact and fumigant toxicity of Asarum heterotropoides (Asarum sieboldii Miquel) essential oil constituents to the house dust mite Dermatophagoides farinae (Acari: Pyroglyphidae). Ten constituents, including methyl eugenol (relative amount 42.18 %), were identified by gas chromatography-mass spectroscopy (GC-MS) in the A. sieboldii Miq. essential oil. In contact toxicity tests, methyl eugenol (4.2 μg/cm(2), 24 h LD50) was most toxic to D. farinae, followed by benzyl benzoate (9.1 μg/cm(2)), A. sieboldii Miq. essential oil (37.7 μg/cm(2)), and dibutyl phthalate (DBP 57.9 μg/cm(2)). The potency of methyl eugenol and A. sieboldii Miq. essential oil was higher than benzyl benzoate and DBP, with mortalities of 100, 100, 94.6, and 13.2 %, respectively, after 2.5 h of exposure. In the vapor phase mortality bioassay, methyl eugenol and A. sieboldii Miq. essential oil resulted in 100 % mortality in closed containers after 24-h exposure, but only 4.7 and 7.9 %, respectively, in open containers, indicating that the toxicity in these tests was largely due to the vapor phase. Methyl eugenol and A. sieboldii Miq. essential oil merit further study as potential D. farinae control compounds.

We report on the fabrication of an amphiphilic random copolymer-based colorimetric and fluorescent chemosensor for Fe 3+ ions that was prepared by free radical polymerization of a novel rhodamine-based Fe 3+ -recognizing monomer, R6GEM, with N -vinylpyrrolidone (NVP). Because of its amphiphilic property, the copolymer P(NVP-co-R6GEM) can self-assemble into micelles, which allows it to be used as a chemosensor in aqueous solution. Upon addition of Fe 3+ ions to the micelle solution, visual color change and fluorescence enhancement were observed. Moreover, other metal ions did not induce obvious changes to the absorption and fluorescence spectra. The water dispersibility and biocompatibility of these polymer micelles could provide a new strategy for detecting analytes in environmental and biological systems.

This study characterized the acaricidal activity of constituents of patchouli oil extracted from (Pogostemon cablin (Blanco) BENTH) against the house dust mite, Dermatophagoides farinae. A new compound, 2-(1,3-dihydroxy-but-2-enylidene)-6-methyl-3-oxo-heptanoic acid (DHEMH), was isolated from patchouli oil and characterized by (1)H-NMR, (13)C-NMR, LC-MS and elemental analysis (EA). This active component was identified as the hydrolysate of pogostone. Fifteen other constituents found in patchouli oil were also identified by GC-MS, including patchouli alcohol and pogostone. LD(50) studies carried out over 24 h using contact toxicity tests identified DHEMH as the most toxic compound to D. farinae (2.04 μg/cm(2)), followed by patchouli oil (6.11 μg/cm(2)), benzyl benzoate (BP) (9.31 μg/cm(2)) and dibutyl phthalate (DBP) (58.52 μg/cm(2)). In vapor phase toxicity tests, all of these compounds were more effective in closed than open containers, indicating that the most efficient mode of delivery for these compounds is the vapor phase. These results indicate that DHEMH and patchouli oil merit further study as potential agents for the control of D. farinae.

A novel easily available turn-on fluorescent polymeric chemosensor poly(VP-co-GMA-g-RhBH) based on water-soluble copolymer with pendant rhodamine B moiety was synthesized, which showed highly selective and sensitive recognition toward Hg2+ in pure water over a wide range of tested metal ions with remarkably enhanced fluorescent intensities and also clear color changes from colorless to pink. In addition, the response of poly(VP-co-GMA-g-RhBH) to Hg2+ is very quick without any time delay. The combination of water solubility and positive fluorescence response as well as color change is hence particularly promising for the practical utility of this sensor.

A novel, easily available colorimetric and fluorescent double-sensor 1 based on Salicylaldehyde bis-Schiff has been investigated in this work. The sensor exhibits highly selective and sensitive recognition toward Cu2+ in aqueous solution via a naked eye colour change from colourless to yellow and toward Al3+ via a significant fluorescent enhancement in ethanol over a wide range of tested metal ions. This represents the first reported Salicylaldehyde Schiff-based sensor capable of detecting both Cu2+ and Al3+ using two different modes.

Acteoside is one kind of phenylethanoid glycoside, which has shown a lot of biological activities. This article reviewed the study progress of acteoside, such as distribution, preparation, identification, and bioactivities.

SUMMARYObjective.This paper assessed the potential of traditional Chinese medicine (TCM) preparations for using as environmentally acceptable and alternative commercial acaricides.Methods.22 kinds of TCM, which contained abundant essential oils and showed insecticidal effects, were collected. Samples extracted with petroleum ether, ethyl acetate and methanol were tested against house dust mitesDermatophagoides farinaeand their toxicity assessed.Results.The results showed that 3 TCM ofCinnamonum cassia, Eugenia caryophyllataandPogostemon cablinhave higher activity, and the parallel tests showed that the petroleum ether extract had higher activities (0·0046 mg/cm2, 0·005 mg/cm2and 0·006 mg/cm2respectively, 24 h, LD50) than the extracts of ethyl acetate and methanol. The acaricidal activity of the ethyl acetate extracts fromC. cassia,P. cablinandAsarum sieboldii(0·00144 mg/cm2, 0·00347 mg/cm2and 0·05521 mg/cm2respectively, 24 h, LD50) were almost comparable to that of benzyl benzoate and dibutyl phthalate. However, the methanolic extracts of were less effective.Conclusions.This study shows the use of extracts with petroleum ether ofC. cassia,P. cablinandE. caryophyllataas eco-friendly biodegradable agents for the control of the house dust mite.

Exploring novel anticancer agents that can trigger non-apoptotic or non-autophagic cell death is urgent for cancer treatment. In this study, we screened and identified an unexplored anticancer activity of gypenoside L (Gyp-L) isolated from Gynostemma pentaphyllum. We showed that treatment with Gyp-L induces non-apoptotic and non-autophagic cytoplasmic vacuolation death in human hepatocellular carcinoma (HCC) cells. Mechanically, Gyp-L initially increased the intracellular reactive oxygen species (ROS) levels, which, in turn, triggered protein ubiquitination and unfolded protein response (UPR), resulting in Ca(2+) release from endoplasm reticulum (ER) inositol trisphosphate receptor (IP3R)-operated stores and finally cytoplasmic vacuolation and cell death. Interruption of the ROS-ER-Ca(2+) signaling pathway by chemical inhibitors significantly prevented Gyp-L-induced vacuole formation and cell death. In addition, Gyp-L-induced ER stress and vacuolation death required new protein synthesis. Overall, our works provide strong evidence for the anti-HCC activity of Gyp-L and suggest a novel therapeutic option by Gyp-L through the induction of a unconventional ROS-ER-Ca(2+)-mediated cytoplasmic vacuolation death in human HCC.

Modulation of autophagy has been increasingly regarded as a promising cancer therapeutic approach. In this study, we screened several ginsenosides extracted from Panax ginseng and identified ginsenoside Ro (Ro) as a novel autophagy inhibitor. Ro blocked the autophagosome-lysosome fusion process by raising lysosomal pH and attenuating lysosomal cathepsin activity, resulting in the accumulation of the autophagosome marker MAP1LC3B/LC3B and SQSTM1/p62 (sequestosome 1) in various esophageal cancer cell lines. More detailed studies demonstrated that Ro activated ESR2 (estrogen receptor 2), which led to the activation of NCF1/p47PHOX (neutrophil cytosolic factor 1), a subunit of NADPH oxidase, and subsequent reactive oxygen species (ROS) production. Treatment with siRNAs or inhibitors of the ESR2-NCF1-ROS axis, such as N-acetyl-L-cysteine (NAC), diphenyleneiodonium chloride (DPI), apocynin (ACN), Tiron, and Fulvestrant apparently decreased Ro-induced LC3B-II, GFP-LC3B puncta, and SQSTM1, indicating that ROS instigates autophagic flux inhibition triggered by Ro. More importantly, suppression of autophagy by Ro sensitized 5-fluorouracil (5-Fu)-induced cell death in chemoresistant esophageal cancer cells. 5-Fu induced prosurvival autophagy, and by inhibiting such autophagy, siRNAs against BECN1/beclin 1, ATG5, ATG7, and LC3B enhanced 5-Fu-induced autophagy-associated and apoptosis-independent cell death. We observed that Ro potentiates 5-Fu cytotoxicity via delaying CHEK1 (checkpoint kinase 1) degradation and downregulating DNA replication process, resulting in the delayed DNA repair and the accumulation of DNA damage. In summary, these data suggest that Ro is a novel autophagy inhibitor and could function as a potent anticancer agent in combination therapy to overcome chemoresistance.

The azide-alkyne click polymerization (AACP) has emerged as a powerful tool for the synthesis of functional polytriazoles. While, for the Cu(I)-catalyzed AACP, the removal of the catalytic Cu(I) species from the resulting polytriazoles is difficult, and the research on the recyclability and reusability of the catalyst remains intact. Herein, we reported the first example of using recyclable and reusable supported Cu(I) catalyst of CuI@A-21 for the AACP. CuI@A-21 could not only efficiently catalyze the AACP but also be reused for at least 4 cycles. Moreover, pronounced reduction of copper residues in the products was achieved. Apart from being a green and cost-effective polymer synthesis strategy, this method will also broaden the application of AACP in material and biological sciences and provide guidelines for other polymerizations with metal catalysts.

This study characterized the acaricidal activity of constituents of patchouli oil extracted from (Pogostemon cablin (Blanco) BENTH) against the house dust mite, Dermatophagoides farinae. A new compound, 2-(1,3-dihydroxy-but-2-enylidene)-6-methyl-3-oxo-heptanoic acid (DHEMH), was isolated from patchouli oil and characterized by 1H-NMR, 13C-NMR, LC-MS and elemental analysis (EA). This active component was identified as the hydrolysate of pogostone. Fifteen other constituents found in patchouli oil were also identified by GC-MS, including patchouli alcohol and pogostone. LD50 studies carried out over 24 h using contact toxicity tests identified DHEMH as the most toxic compound to D. farinae (2.04 μg/cm2), followed by patchouli oil (6.11 μg/cm2), benzyl benzoate (BP) (9.31 μg/cm2) and dibutyl phthalate (DBP) (58.52 μg/cm2). In vapor phase toxicity tests, all of these compounds were more effective in closed than open containers, indicating that the most efficient mode of delivery for these compounds is the vapor phase. These results indicate that DHEMH and patchouli oil merit further study as potential agents for the control of D. farinae.

A new rhodamine-based reversible chemosensor (2) was synthesized, which exhibits high sensitivity and selectivity for Cu(2+) but no significant response toward other competitive metal ions in aqueous solution. Upon the addition of Cu(2+), the spirolactam ring of 2 was opened and the solution color changed from colorless to red. Strangely, an unexpected fluorescence quenching was observed, which is contrary to the fluorescence turn-on of the most rhodamine-based chemosensors. The likely novel sensing mechanism has been proposed.

To extract, identify and purify the major allergens of Pseudosciaena crocea in order to evaluate the immunological activities.Pseudosciaena crocea proteins were extracted by Coca's buffer. Allergens of the Pseudosciaena crocea were identified by SDS-polyacrylamide gel electrophoresis (SDS-PAGE) and Western-Blotting. Major allergens were isolated by ion exchange chromatagraphy (IEC) and their immunological activities were evaluated by Western-Blotting with the serum of patients as 1st antibody.The molecular weight of the Pseudosciaena crocea protein were between 8-116 kD. The molecular weight of the major allergens of Pseudosciaena crocea were 54, 29, 27, 14 kD. The concentration of allergens of Pseudosciaena crocea after isolated by IEC were highly improved and the immunological activities were kept.The allergens of Pseudosciaena crocea were detected and identified by immunological activity.