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Ashwagandha (W. somnifera L) is a popular ethnomedicinal herb endowed with potential pharmacotherapeutic properties. In this study the ethanol extract (EE) and water extract (WE) of ashwagandha roots were qualitatively analysed using high performance liquid chromatography (HPLC), the results showed EE containing withanoside IV (a), physagulin D (b), 27-hydroxywithanone (c), withanoside V (d), withaferin A (e), withastramonolide (f), withanolide A (g), withanone (h), and withanolide B (i) as major bioactive compounds. Antioxidant potential was studied using four in vitro free radical scavenging assays and EE displayed higher antioxidant effect compared to WE for all assays. The EE also showed enzyme inhibitory effect against lipoxygenase (5-LOX) >cyclooxygenases-1 (COX-1) compared to cyclooxygenases-2 (COX-2) and to that of WE. Furthermore, EE demonstrated a potential cytotoxic effect on proliferation of A549 cells in vitro, showing IC50 values, 394.8 (24 h), 171.9 (48 h) and 126.1 (72 h) μg/mL, respectively. EE extract also exhibited induction of apoptosis in dose dependent manner confirmed with the production of ROS in A549 cells through flow cytometric analysis. The obtained results demonstrated that ashwagandha EE with high concentration of bioactive compounds could act as potential drug candidates against pro-inflammatory enzymes involved in development of inflammation and progression of lung cancer. Further, extensive research is needed to investigate the ashwagandha bioactive compounds responsible for treating inflammation, oxidative stress and lung cancer.

Nowadays, the harm of antibiotics residues in environments to human health and ecological safety has been causing more and more attention. In this paper, a biochar based iron material (MBC) was used to activate persulfate (PS) for the removal of sulfadiazine (SDZ) from aqueous solution. Experiment results indicate that the degradation and mineralization of SDZ by MBC/PS system reached 91.79 and 60 % within 60 min under the optimal reaction conditions, respectively. MBC/PS system exhibited a better performance on SDZ removal compared with MBC/H2O2 system. The addition of Cu2+ ion could enhance the degradation of SDZ by MBC/PS system. PO43-, Cl- and SO42- had a certain degree of inhibitory effect on the SDZ degradation. Both radicals and non-radical species such as SO4•-, •OH and 1O2 participated in the degradation reaction of SDZ by MBC/PS system, but •OH was the main radical species responsible for SDZ degradation. The liquid chromatograph-mass spectrometer (LC-MS) technique was used to identify the intermediate products of SDZ, and it was proposed that the degradation of SDZ might be achieved through hydrolyzation, hydroxylation, deamination and amino-oxidization processes. A possible reaction mechanism involving a synergistic effect between PS homogeneous and heterogeneous activation processes as well as both radicals and non-radicals reactions was finally proposed.

A tandem rhodium(III)-catalyzed system was established to access 3,4-dihydroisoquinolin-1(2H)-one by coupling of N-methoxy-3-methylbenzamide with 2-methylidenetrimethylene carbonate. This one-pot synthesis protocol processed smoothly under mild reaction conditions. Moreover, a total of 28 examples, broad substrate scope, and high functional-group compatibility were observed. Preliminary mechanism studies were also conducted and demonstrated that the rhodium(III) catalyst played a vital role in the C-H-allylation and N-alkylation cyclization process.

The isomerization-transalkylation coupling reaction between 2-methylnaphthalene and dimethylnaphthalene was studied over zeolite catalysts to produce them. The catalytic performance of zeolites with MWW, BEA, FAU and MFI topological structure was investigated and the reaction mechanism was discussed. The properties of zeolites were characterized by XRD, N2 adsorption-desorption, SEM, NH3-TPD, Py-FTIR and ICP. Compared with MFI zeolite with 10-membered ring channel, MWW, BEA and FAU zeolite with 12-membered ring channel showed better catalytic activity. BEA zeolite exhibited higher selectivity to dimethylnaphthalene, while MWW zeolites showed higher selectivity to 2-methylnaphthalene and the best catalytic stability. As a branch of MWW zeolites, HMCM-22 showed a 1-methylnaphthalene conversion of 70.27% and a 2-methylnaphthalene yield of 66.69%. It was worth noting that a relatively high yield of 2-methylnaphthalene (35.74%) and dimethylnaphthalene (19.00%) were obtained on HMCM-56 at the same time. This research has opened up a promising route using C10 aromatics as raw materials for the preparation of 2,6-dimethylnaphthalene, an important polyester monomer.

Summary Background & aims To date, the prevalence of Gestational diabetes mellitus (GDM) in China was 17.5%. Given the substantial relevance of GDM for medium- and long-term health of both mother and offspring and the paucity of existing data on the link between maternal diet and glucose homeostasis during pregnancy in Asian population, additional studies are needed. To examine the relevance of dietary glycemic index (GI), glycemic load (GL) and fiber intake before and during pregnancy for the development of GDM and glucose homeostasis over the course of pregnancy. Methods Cox proportional hazards analysis and linear mixed effects regressions were performed on data from 9317 women for whom three food frequency questionnaires (pre-pregnancy, 1st and 2nd trimesters) and biochemical measures during pregnancy were available. Investigated outcome variables included GDM risk, fasting plasma glucose (FPG), glycated hemoglobin (HbA1C), and homeostasis model assessment insulin resistance (HOMA-IR) in the 1st, 2nd and 3rd trimesters. Results Women in the highest tertile of dietary GI (or GL) before pregnancy, in the 1st, or the 2nd trimester respectively had a 12% (15%), 25% (23%) or 29% (25%) higher risk of developing GDM than those in the lowest tertile (all p for trend ≤ 0.02). Women with the highest dietary fiber intake before pregnancy, in the 1st or 2nd trimester had a 11%, 17% or 18% lower GDM risk (all p for trend ≤ 0.03). Moreover, increases in GI or GL and decreases in fiber intake over the course of pregnancy (1st to 3rd trimesters) were independently associated with adverse concurrent developments in FPG, HbA1C and HOMA-IR (p ≤ 0.03). Conclusions Our study indicates that dietary GI, GL and fiber intake before and during pregnancy affects glucose homeostasis of pregnant Chinese women.

Purpose: Although enzalutamide (ENZ) has been widely used to treat de novo or castration-resistant metastatic prostate cancer, resistance develops and disease progression is ultimately inevitable. There are currently no approved targeted drugs to specifically delay or overcome ENZ resistance. Experimental Design: We selected several ENZ-resistant cell lines that replicated clinical characteristics of the majority of patients with ENZ-resistant disease. A high-throughput pharmacologic screen was utilized to identify compounds with greater cytotoxic effect for ENZ-resistant cell lines, compared with parental ENZ-sensitive cells. We validated the potential hits in vitro and in vivo, and used knockdown and overexpression assays to study the dependencies in ENZ-resistant prostate cancer. Results: ABT199 (BCL-2 inhibitor) and IMD0354 (IKKB inhibitor) were identified as potent and selective inhibitors of cell viability in ENZ-resistant cell lines in vitro and in vivo which were further validated using loss-of-function assays of BCL-2 and IKKB. Notably, we observed that overexpression of BCL-2 and IKKB in ENZ-sensitive cell lines was sufficient for the emergence of ENZ resistance. In addition, we confirmed that BCL-2 or IKKB inhibitors suppressed the development of ENZ resistance in xenografts. However, validation of both BCL-2 and IKKB in matched castration-sensitive/resistant clinical samples showed that, concurrent with the development of ENZ/abiraterone resistance in patients, only the protein levels of IKKB were increased. Conclusions: Our findings identify BCL-2 and IKKB dependencies in clinically relevant ENZ-resistant prostate cancer cells in vitro and in vivo, but indicate that IKKB upregulation appears to have greater relevance to the progression of human castrate-resistant prostate cancer.

ZnO with three different morphologies were synthesized by hydrothermal method with sodium citrate, polyethylene glycol 2000 (PEG2000) and cetyltrimethylammonium bromide (CTAB) as surfactants, and zinc acetate as the precursor. The phase structure and morphology of zinc oxide were investigated by X-ray diffractometry (XRD), scanning- and transmission electron microscopy (SEM/TEM), while vector network analysis was involved in the characterization of the electromagnetic parameters of the samples. The effect of different surfactants on the structure, morphology, and electromagnetic absorption properties of zinc oxide was also investigated. ZnO obtained with CTAB as the surfactant showed an excellent wave absorption performance at the frequency range of 9.93–18 GHz by adjusting the sample's matching thickness. When this was 5.39 mm, a minimum return loss of − 52.86 dB was obtained at 17.76 GHz, while at 5.74 mm, the effective absorption bandwidth reached 2.32 GHz (15.68–18 GHz).

This study reveals an uncovered mechanism for the regulation of polyamine homeostasis through protein arginyl citrullination of antizyme (AZ), a natural inhibitor of ornithine decarboxylase (ODC). ODC is critical for the cellular production of polyamines. AZ binds to ODC dimers and promotes the degradation of ODC via the 26S proteasome. This study demonstrates the protein citrullination of AZ catalyzed by peptidylarginine deiminase type 4 (PAD4) both in vitro and in cells. Upon PAD4 activation, the AZ protein was citrullinated and accumulated, leading to higher levels of ODC proteins in the cell. In the PAD4-overexpressing and activating cells, the levels of ODC enzyme activity and the product putrescine increased with the level of citrullinated AZ proteins and PAD4 activity. Suppressing cellular PAD4 activity reduces the cellular levels of ODC and downregulates cellular polyamines. Furthermore, citrullination of AZ in the C-terminus attenuates AZ function in the inhibition, binding, and degradation of ODC. This paper provides evidence to illustrate that PAD4-mediated AZ citrullination upregulates cellular ODC and polyamines by retarding ODC degradation, thus interfering with the homeostasis of cellular polyamines, which may be an important pathway regulating AZ functions that is relevant to cancer biology.

Herein, we develop a novel 3D composite aerogel (3D PB/GMA) and apply it to the real-time monitoring of H2O2 secretion from living cells. The 3D PB/GMA shows an obvious porous structure and superior peroxidase-like activity. The electrochemical sensor based on 3D PB/GMA shows an excellent electrocatalytic performance towards H2O2. When applied to the real-time tracking of H2O2 secretion from living cells, it can satisfactorily distinguish cancer cell lines from normal cell lines, revealing a good application potential in pathological diagnosis.

Integrating metal–organic frameworks (MOFs) of different components or structures together and exploiting them as electrochemical sensors for electrochemical sensing has aroused great interest. Furthermore, the incorporation of noble metals with MOFs is conducive to the improvement of catalytic performance. In this work, Pd@UiO-66-on-ZIF-L nanomaterials were successfully synthesised onto a self-supported flexible carbon cloth (Pd@UiO-66-on-ZIF-L/CC) through a novel strategy called MOF-on-MOF. Then, Au nanoparticles were electrodeposited onto Pd@UiO-66-on-ZIF-L/CC to obtain Au–Pd@UiO-66-on-ZIF-L/CC, which can serve as an excellent electrocatalyst for the reduction of hydrogen peroxide (H2O2). The obtained flower-like Pd@UiO-66-on-ZIF-L/CC hybrid MOF changes the structure of the monomeric MOF alone and adds more attachment sites. The synergy of the bimetals greatly improved the catalytic performance of the as-developed sensor. Electrochemical experiment results show that the proposed sensor based on Au–Pd@UiO-66-on-ZIF-L/CC has an extended linear range from 1 μM to 19.6 mM with a sensitivity of 390 μA mM−1 cm−2, and a low limit of detection (LOD) of 21.2 nM (S/N = 3). Moreover, it has good anti-interference, reproducibility, repeatability and excellent stability. Furthermore, the real-time in situ detection of H2O2 secreted from human adenocarcinomic alveolar basal epithelial cells (A549 cells) was achieved by culturing cells on Au–Pd@UiO-66-on-ZIF-L/CC, which indicates the potential of the sensor for applications in cancer pathology. Both the synthesis strategy and the sensor design provide new methods and ideas for the production of ultrasensitive H2O2 electrochemical sensors.

Preah Vihear temple is one of the most significant representatives of the ancient Angkorian temples listed as United Nations Educational, Scientific and Cultural Organization (UNESCO) World Heritage Sites. The surfaces of this Angkor sandstone monument are covered with deteriorated materials, broadly called "sediments" here, resulting from a long time of weathering of the sandstone. The sediments might adversely affect the ancient sandstone substratum of this cultural heritage, and the potential risk from them is essential information for current strategies and on-going protection and management. The extracted DNA from the sediment samples of this temple was used for Illumina high-throughput sequencing analysis, resulting in approximately 12 Gb of metagenomic dataset. The results of this shotgun metagenomic analysis provided a thorough information of the phylogenetic groups presented in the microbiome of the sediment samples, indicating that potential metabolic activities, involving different geomicrobiological cycles, may occur in this microbiome. The phylogenetic result revealed that the majority of metagenomic reads were affiliated with Proteobacteria, Acidobacteria, Actinobacteria, and Bacteroidetes at the phylum level. The metabolic reconstruction results indicated that the important geomicrobiological cycling processes include carbon sequestration, and nitrogen and sulfur transformation as the potentially active ones in the sediments of the sampling sites. Specifically, the dissimilatory nitrate reduction to ammonium (DNRA) and the newly discovered complete ammonia oxidation (comammox) were retrieved from this metagenomic dataset. Furthermore, the genetic information on the presence of acid-producing processes by sulfur- and ammonia-oxidizing bacteria and archaea in this metagenomic dataset suggested that the microbial flora in these samples has the potential to participate in the degradation of sandstone cultural heritage by producing acids. N-15 isotope amendment and incubation analysis results confirmed the presence of active denitrification, but not anammox activity at this temple. These results are important for our knowledge on the microbial community composition and microbial biodeterioration processes affecting this sandstone cultural heritage and will aid in the protection and management of the ancient Preah Vihear temple.Key Points• Microbiota on Preah Viher temple was analyzed using NGS.• Nitrate-N transformation by DNRA, comammox, and denitrifcation was detected.• N-15 isotope analysis confirmed the active denitrifcation, but not Anammox.• Accumulation of nitrate is a result of less active removal by denitrification.

The catalytic promiscuity of MML, lipase from Mucor miehei, was reported to catalyze direct aldol reactions between aromatic aldehydes and cyclic ketones in water, ionic liquids, and deep eutectic solvents at 50 °C. Water can promote the catalytic activity of MML. A wide range of aromatic aldehydes reacted with cyclic ketones to provide the corresponding aldol products with high yields (up to 87.2%) and moderate to good diastereoselectivity (up to 3:97 dr).

Furan, which has been identified as possibly carcinogenic for humans, can be induced to different food items by thermal treatment. In accordance with the previous studies and risks associated with prevalence of furan in food, it is necessary to be acknowledged of amounts of furan formed in different thermally processed foods for human awareness. In this study, Headspace Solid-Phase Microextraction Gas Chromatography–Mass Spectrometry (HS-SPME-GC/MS) was optimized for simultaneous determination of furan, furfural, 2-methylfuran and 2-pentylfuran for the first time from different dried fruits and roasted nuts. The method was proved to be valid for determination of all analytes at 50 °C for 25 min, stirring at 700 rpm and 20% NaCl (W/V) using 50/30 μm divinlybenzene/carboxen/polysimethylsiloxane (DVB/CAR/PDMS) fibre. All analytes were baseline-separated at HP 5-MS column in less than 13 min and obtained results have shown prevalence of furan, furfural and 2-pentylfuran in the studied matrices; however, 2-pentylfuran was more prevalent in the roasted nuts than dried fruits and 2-methylfuran has not shown considerable prevalence in both matrices. Moreover, this method was validated in terms of linearity, precision, recovery, specificity, limit of detection and limit of quantification depending on analytes and sample matrices. Hence, the present method was proved to be highly sensitive, specific and robust with good precision and accuracy and suitable for monitoring these furan derivatives in the studied matrices.

In this work, a cloth-based chemiluminescence (CL) biosensor has been firstly presented for highly sensitive determination of long PCR amplicons. Under the action of a hybridization chain reaction, a good deal of hemin/G-quadruplex DNAzyme molecules are produced, which can effectively enhance the CL signal. Moreover, effective cloth-based DNA biosensors can be fabricated by sequential wax screen-printing and surface-modification processes. Especially, the integration of a desirable hydrophobic barrier and gravity/capillary flow onto the flow channel of the cloth-based device makes the biosensor easy to be fabricated and to be associated with a flow CL. For the luminol/H2O2-based CL system, the signals are triggered by the hemin/G-quadruplex DNAzyme and are recorded by a low-cost CCD. Under optimized conditions, the determination range of target DNA is 0.002–20,000 pM and its limit of detection is calculated to be 1.1 fM. The results show that the proposed CL biosensor has a good analytical performance, such as high detectability and specificity, wide linear range, and receivable reproducibility and stability. Finally, the proposed biosensor is proven by the fact that this method can successfully detect the target DNA prepared from the Listeria monocytogenes–spiked milk samples. Therefore, it is believed to have the potential application prospects in food safety and environmental monitoring.

Tris(2-chloroethyl) phosphate (TCEP), a typical chlorinated organophosphate ester (OPE), is an emerging contaminant of global concern because of its frequent occurrence, potential toxic effects, and persistence in the environment. In this study, we investigated the microbial TCEP biotransformation and the development of microbial communities in sediment microcosms with repeated TCEP amendments. The TCEP degradation fitted pseudo-zero-order kinetics, with reaction rates of 0.068 mg/(L h) after the first spike of 5 mg/L and 1.85 mg/(L h) after the second spike of 50 mg/L. TCEP was mainly degraded via phosphoester bond hydrolysis, evidenced by the production of bis(2-chloroethyl) phosphate (BCEP) and mono-chloroethyl phosphate (MCEP). Bis(2-chloroethyl) 2-hydroxyethyl phosphate (TCEP-OH), phosphoric bis(2-chloroethyl) (2-oxoethyl) ester (TCEP-CHO), phosphoric acid bis(2-chloroethyl)(carboxymethyl) ester (TCEP-COOH), and 2-chloroethyl 2-hydroxyethyl hydrogen phosphate (BCEP-OH) were also identified as microbial TCEP transformation products, indicating that TCEP degradation may follow hydrolytic dechlorination and oxidation pathways. Microbial community compositions in TCEP-amended microcosms shifted away from control microcosms after the second TCEP spike. Burkholderiales and Rhizobiales were two prevalent bacterial guilds enriched in TCEP-amended microcosms and were linked to the higher abundances of alkaline and acid phosphatase genes and genes involved in the metabolism of 2-chloroethanol, a side product of TCEP hydrolysis, indicating their importance in degrading TCEP and its metabolites.

Pepsin was found to catalyze asymmetric cross aldol reactions of aromatic and polycyclicaromatic aldehydes with cyclic ketones in ionic liquids and deep eutectic solvents for the first time. Pepsin exhibited high catalytic activity and excellent stereoselectivity in ionic liquids and deep eutectic solvents in the presence of moderate water. High yields of up to 93.1%, excellent enantioselectivities of up to 96% ee, and good diastereoselectivities of up to 5:95 dr were achieved.

To unravel changes in the structures and digestibility of sweet potato starch in the roots during postharvest storage (0 to 20 days), starches are isolated and characterized in terms of amylose content, polyphenols amount, molecular molar mass (Mw), molecular reassociation and multi-scale reassociated structures after cooking. Results reveal that starch digestibility decreases with a concomitant increase on resistant starch (RS) fraction during the first 10 days. These changes are associated with an increase of ordered structures, amylose and polyphenols content as well as the starch fractions with molecular weight of (2.0–2.5) × 107 g/mol. However these trends get reversed at higher postharvesting periods. Correlation matrices reveal that the short-range ordered structures and starch molecular reassociation behavior of starch paste and polyphenol content are the key factors in determining the RS content. Besides, the short-range ordered structures, specific starch molecular weight distribution and amylose of starch paste can be tailored for modulating the digestibility by controlling the postharvest storage time. This study opens a promising pathway to tailor starch digestibility via simply controlling the postharvest storage time of starch-containing crops.

In this study, a series of organo difluoroboron probes with a BF2 benzamide moiety was designed, prepared and evaluated. Among them, 2c displayed the best optical and biological properties, and may be used as a useful near-infrared fluorescent probe for the detection of Aβ plaques and neurofibrillary tangles in AD.

Background Developing an ideal wound dressing that meets the multiple demands of safe and practical, good biocompatibility, superior mechanical property and excellent antibacterial activity is highly desirable for wound healing. Bacterial cellulose (BC) is one of such promising class of biopolymers since it can control wound exudates and can provide moist environment to a wound resulting in better wound healing. However, the lack of antibacterial activity has limited its application. Methods and results We prepared a flexible dressing based on a bacterial cellulose membrane and then modified it by chemical crosslinking to prepare in situ synthesis of nZnO/BCM via a facile and eco-friendly approach. Scanning electron microscopy (SEM) results indicated that nZnO/BCM membranes were characterized by an ideal porous structure (pore size: 30~ 90 μm), forming a unique string-beaded morphology. The average water vapor transmission of nZnO/BCM was 2856.60 g/m2/day, which improved the moist environment of nZnO/BCM. ATR-FITR further confirmed the stepwise deposition of nano-zinc oxide. Tensile testing indicated that our nanocomposites were flexible, comfortable and resilient. Bacterial suspension assay and plate counting methods demonstrated that 5wt. % nZnO/BCM possessed excellent antibacterial activity against S.aureus and E. coli, while MTT assay demonstrated that they had no measurable cytotoxicity toward mammalian cells. Moreover, skin irritation test and histocompatibility examination supported that 5wt. % nZnO/BCM had no stimulation to skin and had acceptable biocompatibility with little infiltration of the inflammatory cells. Finally, by using a bacteria-infected (S. aureus and E. coli) murine wound model, we found that nZnO/BCM could prevent in vivo bacterial infections and promote wound healing via accelerating the re-epithelialization and wound contraction, and these membranes had no obvious toxicity toward normal tissues. Conclusion Therefore, the constructed nZnO/BCM has great potential for biomedical applications as an efficient antibacterial wound dressing.

Resveratrol (3,5,4'-trihydroxystilbene, RSV) is a natural potential anti-aging polyphenolic compound frequently used as a nutritional supplement against several diseases. However, the underlying mechanisms by which resveratrol regulates postovulatory aging of oocytes are still insufficiently known. In this study, we found that resveratrol could delay postovulatory aging and improve developmental competence of oocytes through activating selective mitophagy in the mouse. Resveratrol could maintain spindle morphology but it disturbed cortical granule (CG) distribution during oocyte aging. This might be due to upregulated mitophagy, since blocking mitophagy by cyclosporin A (CsA) treatment affected oocyte quality by damaging mitochondrial function and it decreased embryonic development. In addition, we also observed an involvement of FoxO3a in regulating mitophagy in aging oocytes following resveratrol treatment. Taken together, our results provide evidence that mitophagy induced by resveratrol is a potential mechanism to protect against postovulatory oocyte aging.

The evolution of oxygenic photosynthesis is a pivotal event in Earth’s history because the O2 released fundamentally changed the planet’s redox state and facilitated the emergence of multicellular life. An intriguing hypothesis proposes that hydrogen peroxide (H2O2) once acted as the electron donor prior to the evolution of oxygenic photosynthesis, but its abundance during the Archean would have been limited. Here, we report a previously unrecognized abiotic pathway for Archean H2O2 production that involves the abrasion of quartz surfaces and the subsequent generation of surface-bound radicals that can efficiently oxidize H2O to H2O2 and O2. We propose that in turbulent subaqueous environments, such as rivers, estuaries and deltas, this process could have provided a sufficient H2O2 source that led to the generation of biogenic O2, creating an evolutionary impetus for the origin of oxygenic photosynthesis., Hydrogen peroxide (H2O2) has been proposed as an electron donor for photosynthesis before water, however, the amount of H2O2 available on early Earth was thought to be limited. Here the authors propose a new abiotic pathway wherein abrasion of quartz surfaces would have provided enough H2O2.

The potential for aerobic and anaerobic microbial natural attenuation of PCBs in freshwater sediments is described by PCB congener, quantitative PCR, and 16S rRNA gene amplicon sequencing datasets generated, in duplicate, from 27 sediment samples collected from a PCB-contaminated freshwater lagoon (54 samples total). Sediment samples were subjected to a hexane PCB extraction protocol and the concentrations of 209 PCB congeners were determined in hexane extracts by gas chromatography with a tandem mass spectrometry detection. DNA was extracted from sediments sediment samples and used for qPCR and 16S rRNA amplicon sequencing. The abundance of 16S rRNA genes (i.e., Dehalococcoides and putative dechlorinating Chloroflexi) and functional genes (i.e., reductive dehalogenase (rdhA) and biphenyl dioxygenase (bphA)) associated with aerobic and anaerobic PCB biodegradation, along with the total 16S rRNA genes abundance, was determined by SYBR green qPCR. The microbial community composition and structure in all sediment samples was obtained by 16S rRNA gene amplicon sequencing. Primers targeting the 16S rRNA gene V4 region were used to produce 16S rRNA gene amplicons that were sequencing with the high-throughput Illumina MiSeq platform and sequencing chemistry. The 16S rRNA gene sequencing dataset along with PCB congener and qPCR datasets included as metadata, could be reused in meta-analyses that aim to determine microbial community interactions in contaminated environments, and uncover relationships between microbial community structure and environmental variable (e.g., PCB congener concentrations).

Zinc-anode-based electrochromic devices (ZECDs) are emerging as the next-generation energy-efficient transparent electronics. We report anatase W-doped TiO2 nanocrystals (NCs) as a Zn2+ active electrochromic material. It demonstrates that the W doping in TiO2 highly reduces the Zn2+ intercalation energy, thus triggering the electrochromism. The prototype ZECDs based on W-doped TiO2 NCs deliver a high optical modulation (66% at 550 nm), fast spectral response times (9/2.7 s at 550 nm for coloration/bleaching), and good electrochemical stability (8.2% optical modulation loss after 1000 cycles). Highlights: 1 A reversible Zn2+ insertion in anatase TiO2 nanocrystals is reported for the first time.2 This is the first report regarding TiO2 for zinc-anode-based electrochromic devices, which will subsequently broaden its applications to zinc-ion electrochemical cells.3 A prototype device based on the TiO2 nanocrystals delivers a high optical modulation, fast response times, and robust electrochemical stability.

Improving the strength of grey cast iron wheel hubs will improve the safety of automobiles and have a great significance for energy saving and environmental protection. This paper systematically compares the calculation results of Python-based precipitation calculation and JmatPro software simulation with experiments. The results show that with a low mass fraction of niobium (0.098%) cuboid Niobium Carbide (NbC) precipitates do not form in the liquid phase, however, an elongated NbC niobium-rich phase may form during the solidification process and in the solid phase. However, cuboid NbC precipitates can be precipitated from the liquid phase when the niobium mass fraction is higher (0.27%, 0.46%). These results indicate that with the increasing niobium content the amount, particle size, and initial precipitation temperature of niobium carbide precipitated in the matrix structure will increase. According to the observation and statistical analysis of the microstructure, it is found that tensile strength will be improved with an increase in niobium content due to the refinement of the graphite and pearlite interlamellar spacing. In this paper, adding less than 0.32% of Nb to grey cast iron is recommended, considering the comprehensive cost and the effect of niobium in the material structure.

An efficient and practical approach for the synthesis of medicinally important acridones was developed from anthranils and commercially available arylboronic acids by a tandem copper(I)-catalyzed electrophilic amination/Ag(I)-mediated oxidative annulation strategy. This new and straightforward protocol displayed a broad substrate scope (25 examples) and high functional group tolerance. What's more, a possible mechanistic proposal was also presented.

Highlights A reversible Zn2+ insertion in anatase TiO2 nanocrystals is reported for the first time.This is the first report regarding TiO2 for zinc-anode-based electrochromic devices, which will subsequently broaden its applications to zinc-ion electrochemical cells.A prototype device based on the TiO2 nanocrystals delivers a high optical modulation, fast response times, and robust electrochemical stability. Supplementary Information The online version contains supplementary material available at 10.1007/s40820-021-00719-y., Zinc-anode-based electrochromic devices (ZECDs) are emerging as the next-generation energy-efficient transparent electronics. We report anatase W-doped TiO2 nanocrystals (NCs) as a Zn2+ active electrochromic material. It demonstrates that the W doping in TiO2 highly reduces the Zn2+ intercalation energy, thus triggering the electrochromism. The prototype ZECDs based on W-doped TiO2 NCs deliver a high optical modulation (66% at 550 nm), fast spectral response times (9/2.7 s at 550 nm for coloration/bleaching), and good electrochemical stability (8.2% optical modulation loss after 1000 cycles). Supplementary Information The online version contains supplementary material available at 10.1007/s40820-021-00719-y.

β-Amyloid (Aβ) plaques and Tau tangles are cognitive impairment markers vital for diagnosing and preventing Alzheimer's disease (AD). To systematically explore the relationship between the number or position of nitrogen atoms and their optical properties and biological properties, five series of new N, O-coordinated organo-difluoroboron probes were introduced as binding scaffolds for Aβ plaques and Tau tangles. These probes exhibited suitable optical properties for near-infrared (NIR) imaging. Probe 4PmNO-2 (4-((1E,3E)-4-(1,1-difluoro-1H-1λ4,9λ4-pyrimido[1,6-c][1,3,5,2]oxadiazaborinin-3-yl)buta-1,3-dien-1-yl)-N,N-dimethylaniline) displayed the excellent emission maximum (716 nm in PBS), a high quantum yield (61.4% in CH2Cl2), and a high affinity for synthetic Aβ1–42 (Kd = 23.64 ± 1.08 nM) and Tau (K18) aggregates (Kd = 26.38 ± 1.29 nM), as well as for native Aβ plaques and NFTs in the brain tissue from AD patients. 4PmNO-2, with significantly enhanced fluorescence (Aβ1–42, 136 fold; Tau (K18), 96 fold) and the highest initial brain uptake (11.57% ID/g at 2 min) in normal ICR mice, was evaluated further. In vivo NIR fluorescent imaging studies in living Aβ and Tau transgenic mice revealed that it could differentiate healthy and diseased animals. Further ex vivo fluorescent staining studies showed that 4PmNO-2 specifically bound to Aβ plaques and Tau tangles in transgenic mice. In summary, the probe 4PmNO-2 may be a useful near-infrared fluorescence (NIRF) probe for AD biomarkers.

A novel polysaccharide (CMP-2B) was purified from Centipeda minima by anion-exchange and gel-permeation chromatography. Structural characterization revealed that CMP-2B was a homogeneous heteropolysaccharide with an average molecular weight of 113.193 KDa. CMP-2B was made up of mannose, galacturonic acid, galactose and arabinose with a molar ratio of 0.27:0.12:0.42:0.17. The backbone chain of CMP-2B consisted of 3,6)-α-D-Manp-(1 and 4,6)-β-D-Galp-(1, and the branches were comprised of 4)-α-D-GalpA-(1, 6)-β-D-Galp-(1, T-α-L-Araf-(1 and 3)-α-L-Araf -(1. Besides, the results of antioxidant assays revealed that CMP-2B possessed signifcant free radical scavenging ability. Moreover, the results of hypoglycemic assays showed that CMP-2B displayed α-glucosidase inhibitory activities, and could significantly improve glucose consumption, glycogen synthesis and the activity of pyruvate kinase of insulin-resistance HepG2 cells. Overall, these results suggested that CMP-2B could be a new source for functional foods.

Chronic pain is a costly health problem that impairs health-related quality of life when not effectively treated. Regulating the transition from acute to chronic pain is a new therapeutic strategy for chronic pain that presents a major clinical challenge. The underlying mechanisms of pain transition are not entirely understood, and strategies for preventing this transition are lacking. Here, a hyperalgesic priming model was used to study the potential mechanism by which γ-aminobutyric acid receptor type A (GABAAR) in the dorsal root ganglion (DRG) contributes to pain transition. Furthermore, electroacupuncture (EA), a modern method of acupuncture, was administered to regulate pain transition, and the mechanism underlying EA’s regulatory effect was investigated. Hyperalgesic priming was induced by intraplanar injection of carrageenan (Car)/prostaglandin E2 (PGE2). The decrease in mechanical withdrawal threshold (MWT) induced by PGE2 returned to baseline 4 h after injection in NS + PGE2 group, and still persisted 24 h after injection in Car + PGE2 group. Lower expression of GABAAR in the lumbar DRG was observed in the model rats. Furthermore, activating or blocking GABAAR could reversed the long-lasting hyperalgesia induced by Car/PGE2 injection or produced a persistent hyperalgesia. In addition, GABAAR may be involved in Protein Kinase C epsilon (PKCε) activation in the DRG, a mark molecular of pain transition. EA considerably increased the mechanical pain thresholds of hyperalgesic priming model mammals in both the acute and chronic phases. Furthermore, EA upregulated the expression of GABAAR and inhibited the activation of PKCε in the DRG. In addition, peripheral administration of picrotoxin blocked the analgesic effect of EA on the model rats and abolished the regulatory effect of EA on PKCε activation. These findings suggested that GABAAR plays a key role in both the transition from acute to chronic pain and the analgesic effect of EA on hyperalgesic priming.

Intraneuronal neurofibrillary tangles composed of Tau aggregates have been widely accepted as an important pathological hallmark of Alzheimer's disease. A current therapeutic avenue for treating Alzheimer's disease is aimed at inhibiting Tau accumulation with small molecules such as natural flavonoids. Liquid–liquid phase separation (LLPS) of Tau can lead to its aggregation, and Tau aggregates can then be degraded by autophagy. However, it is unclear whether natural flavonoids modulate the formation of phase-separated Tau droplets or promote autophagy and Tau clearance. Here, using confocal microscopy and fluorescence recovery after photobleaching assays, we report that a natural antioxidant flavonoid compound myricetin slows LLPS of full-length human Tau, shifting the equilibrium phase boundary to a higher protein concentration. This natural flavonoid also significantly inhibits pathological phosphorylation and abnormal aggregation of Tau in neuronal cells and blocks mitochondrial damage and apoptosis induced by Tau aggregation. Importantly, using coimmunoprecipitation and Western blotting, we show that treatment of cells with myricetin stabilizes the interaction between Tau and autophagy-related protein 5 (ATG5) to promote clearance of phosphorylated Tau to indirectly limit its aggregation. Consistently, this natural flavonoid inhibits mTOR pathway, activates ATG5-dependent Tau autophagy, and almost completely suppresses Tau toxicity in neuronal cells. Collectively, these results demonstrate how LLPS and abnormal aggregation of Tau are inhibited by natural flavonoids, bridging the gap between Tau LLPS and aggregation in neuronal cells, and also establish that myricetin could act as an ATG5-dependent autophagic activator to ameliorate the pathogenesis of Alzheimer's disease.

Malathion (MAL) is a common organophosphorus pesticide and affects both animal and human reproduction. However, the mechanisms regarding how MAL affects the mammalian oocyte quality and how to prevent it have not been fully investigated. In this study, we used porcine oocyte as a model and proved that MAL impaired porcine oocyte quality in a dose-dependent manner during maturation. MAL decreased the first polar body extrusion, disrupted spindle assembly and chromosome alignment, impaired cortical granules (CGs) distribution, and increased reactive oxygen species (ROS) level in oocytes. RNA-seq analysis showed that MAL exposure altered the expression of 2,917 genes in the porcine maturated oocytes and most genes were related to ROS, the lipid droplet process, and the energy supplement. Nevertheless, these defects could be remarkably ameliorated by adding melatonin (MLT) into the oocyte maturation medium. MLT increased oocyte maturation rate and decreased the abnormities of spindle assembly, CGs distribution and ROS accumulation in MAL-exposed porcine oocytes. More important, MLT upregulated the expression of genes related to lipid droplet metabolism (PPARγ and PLIN2), decreased lipid droplet size and lipid peroxidation in MAL-exposed porcine oocytes. Finally, we found that MLT increased the blastocysts formation and the cell numbers of blastocysts in MAL-exposed porcine oocytes after parthenogenetic activation, which was mediated by reduction of ROS levels and maintaining lipid droplet metabolism. Taken together, our results revealed that MLT had a protective action against MAL-induced deterioration of porcine oocyte quality.

Rice starch-Gallic acid (GA) complex (RSP-GA) was prepared by high pressure homogenization (HPH), and the effect of GA on the digestibility and multi-structure of rice starch under HPH was investigated. The results showed that, after HPH, the digestibility of starch substantially changed in the reduced rapidly digestible starch (RDS) content, and increased resistant starch (RS) after interacting with GA. In particular, the RS content of RSP-GA ranged from 5.4% to 29.7%, which were much higher than that of rice starch (1.6%). Meanwhile, the results indicated that rice starch and GA were aggregated by hydrogen bonding and van der Waals forces to form a single helix V7 type complex during HPH processing. Moreover, with the increase addition of GA, the fractal structure of the RSP-GA is converted into a mass fractal structure, and the aggregate structure gradually became compact due to the enhancement of rearrangement and aggregation behavior of the degraded starch molecular chains. It thus reduced the accessibility of the starch molecules to digestive enzymes. These results demonstrated that HPH and GA complexation could be beneficial to control the digestion of starch products with desired digestibility.

Background Differentiated embryo chondrocyte 1 (DEC1) is a helix-loop-helix transcription factor that directly binds to the class B E-box in target genes. DEC1 exerts both pro-survival and pro-apoptotic effects in a cell- and tissue-dependent manner. Its actions play role the progression of cancer remains unclear. Methods We first examined the functional roles of DEC1 using the transient promoter reporter assay. Then, the knockdown of DEC1 expression was performed with the short hairpin RNA strategy in HeLa and A2058 cancer cell lines to check the cell cycle and mitochondrial function profile using the flow cytometry and Seahorse assays. We later clarified the role of DEC1 in the tumorigenesis using the colony formation, anchorage-independent growth assay, and cellular proliferation analysis. Results In the present study, we tested two guanide-containing drugs, metformin and phenformin, and found that both exhibit cytotoxicity against HeLa cervical carcinoma and A2058 melanoma cells. This effect was mediated, at least in part, through activation of the AMPK pathway; degradation of important cellular proteins, such as DEC1 and p53; and suppression of mitochondrial function, colony formation, and anchorage-independent cell proliferation. Our results further suggest that the cytotoxicity of metformin and phenformin reflect the impact of the repressive actions of DEC1 on gene expression, including DEC1 itself. This in turn suppresses both anchorage-independent growth and cell proliferation. Conclusion These findings provide several lines of evidence suggesting that DEC1 activity contributes to tumorigenicity and that the antitumor properties of biguanides reflect their ability to inhibit DEC1 functions.

Vinyl chloride (VC) is a common groundwater contaminant and known human carcinogen. Three major bacterial guilds are known to participate in VC biodegradation: aerobic etheneotrophs and methanotrophs, and anaerobic organohalide-respiring VC-dechlorinators. We investigated the spatial relationships between functional genes representing these three groups of bacteria (as determined by qPCR) with chlorinated ethene concentrations in a surficial aquifer at a contaminated site. We used cryogenic soil coring to collect high-resolution aquifer sediment samples and to preserve sample geochemistry and nucleic acids under field conditions. All samples appeared to be anaerobic (i.e., contained little to no dissolved oxygen). VC biodegradation associated functional genes from etheneotrophs (etnC and/or etnE), methanotrophs (mmoX and/or pmoA), and anaerobic VC-dechlorinators (bvcA and/or vcrA) coexisted in 48% of the samples. Transcripts of etnC/etnE and bvcA/vcrA were quantified in contemporaneous groundwater samples, indicating co-located gene expression. Functional genes from etheneotrophs and anaerobic VC-dechlorinators were correlated to VC concentrations in the lower surficial aquifer (p

Effect of different contents of ground ginger [0%, 1%, 3%, 5%, and 7% (w/w)] on flour quality, dough and biscuit characteristic and acrylamide content were investigated. Texture results showed that by adding 1% (w/w) ground ginger, hardness of dough, hardness and chewiness of biscuit decreased, which was beneficial for biscuit making. Moreover, the L* value of biscuit dropped while the a* and b* value rose with the increase of ginger contents, indicating darker, redder and yellower biscuits. Sensory score of biscuits became worse but acrylamide content reduced with the addition of ground ginger. The phenol hydroxyl group of gingerol played a more important role in the reaction of formation of acrylamide than the side chain. Finally, biscuit with 1% ground ginger content showed good texture, color and acceptable sensory evaluation, as well as lowering the acrylamide content by 6.2%.

Ran Zhang,1,2 Yi Liang,1 Shuxiang Wei1 1Department of Orthopedics, Liuzhou General Hospital, Liuzhou 545006, Guangxi, China; 2The Department of Orthopedics, The Affiliated Liuzhou General Hospital of Guangxi University of Technology, Liuzhou 545006, Guangxi, China Background: Angiogenesis and bone formation are vital for fracture healing. Nerve growth factor (NGF) not only promotes neuronal survival but also enhances the proliferation and differentiation of osteoblasts. Vascular endothelial growth factor (VEGF) plays an important role in angiogenesis. However, the potential correlation of NGF and VEGF levels with fracture healing in patients with traumatic brain injury (TBI) remains unclear.Methods: This study enrolled 22 patients with clavicle fracture and concomitant TBI (CFT group) and 25 patients with clavicle fracture alone (CF group). Serum NGF levels were measured with ELISA. The expressions of NGF, VEGF, and CD31 in callus tissues were measured with immunohistochemistry.Results: The fracture healing time in CFT group (82.22±13.61 days) was significantly shorter than that in CF group (127±25.05 days; P

Purpose: Morphine is often used for the treatment of moderate and severe cancer pain, but long-term use can lead to morphine tolerance. Methods for effectively inhibiting morphine tolerance and the related mechanism of action are of great significance for the treatment of cancer pain. Previous studies have shown that electroacupuncture (EA) can inhibit the occurrence of morphine tolerance, but the mechanism is not yet clear. The aim of the present study was to explore the signaling pathway by which EA attenuates the development of bone cancer pain (BCP)-morphine tolerance (MT). Materials and methods: Changes in the paw withdrawal threshold (PWT) of rats with bone cancer pain-morphine tolerance were observed in a study of EA combined with intrathecal injection of a PI3K inhibitor (LY294002) or agonist (insulin-like growth factor-1 [IGF-1]). We also tested the protein expression of phosphorylated phosphatidylinositol 3-kinase (p-PI3K), phosphorylated protein kinase B (p-Akt), phosphorylated c-Jun NH2-terminal kinase 1/2 (p-JNK1/2), and β-arrestin2 in the L4-6 spinal dorsal horn of rats. Results: The protein expression of p-PI3K, p-Akt, p-JNK1/2, and β-arrestin2 was upregulated in the L4-6 spinal dorsal horn of rats with bone cancer pain and bone cancer pain-morphine tolerance. EA delayed the occurrence of morphine tolerance in rats with bone cancer pain and downregulated the protein expression of p-PI3K, p-Akt, p-JNK1/2, and β-arrestin2 in the L4-6 spinal dorsal horn of rats with bone cancer pain-morphine tolerance. Intrathecal injection of LY294002 attenuated the development of morphine tolerance and downregulated the protein expression of p-Akt, p-JNK1/2, and β-arrestin2 in the spinal dorsal horn of rats with bone cancer pain-morphine tolerance. In addition, the inhibitory effect of EA on morphine tolerance was reversed by IGF-1. Conclusion: The mechanism underlying the ability of EA to attenuate morphine tolerance may be associated with inhibition of the PI3K/Akt/JNK1/2 signaling pathway.

Magnesium (Mg) is one of essential plant nutrients needed for optimal growth, yield and quality formation. Also, soil application of Mg fertilizer has been shown to be an effective approach to improve vegetable Mg nutrition. Leafy vegetables can accumulate relatively high levels of heavy metals in the above-ground plant parts. However, it remains unclear as to whether soil-applied Mg affects the vegetable nutritional quality and human health risk of heavy metals from field-grown Chinese cabbage. Here we conducted a two-year, two-crop cycle field experiment in south-western China to evaluate crop yield, vegetable nutrition and heavy metal accumulation in Chinese cabbage supplied with varying levels of Mg (0–90 kg ha−1). Soil application of Mg did not increase the cabbage yield. However, it did increase the vegetable vitamin C and water-soluble protein content by 20.0 % and 57.9 % with 45 and 22.5 kg Mg ha−1 application, respectively, compared to control. The nitrate content of Mg-supplied (45 kg ha−1) cabbages was significantly lower, by about 14 %, than the control. Further, it also significantly decreased the accumulation of cadmium and nickel in the above-ground tissues by reducing their uptake from soil to root or their translocation from root to shoot. Magnesium application, however, increased chromium uptake. A human health risks assessment nonetheless showed that the contribution of chromium from Mg-supplied plants to threshold hazard quotient and threshold carcinogenic risk were indeed much lower than that of cadmium and nickel, proving the value of crop Mg supplementation for ameliorating non-carcinogenic and carcinogenic risks to humans with the consumption of Chinese cabbage. Here we show that soil application of Mg in the range of 22.5–45 kg ha−1 to Chinese cabbage will significantly improve its nutritional qualities and alleviate the potential human health risks of heavy metals associated with Chinese cabbage consumption.

The pollution of heavy metals and organic compounds has received increased attention in recent years. In the current study, a novel biochar-based iron oxide composite (FeYBC) was successfully synthesized using pomelo peel and ferric chloride solution through one-step process at moderate temperature. Results clearly demonstrate that FeYBC exhibited more efficient removal of Cr(VI) and/or phenol compared with the pristine biochar, and the maximum adsorption amounts of Cr(VI) and phenol by FeYBC could reach 24.37 and 39.32 mg g−1, respectively. A series of characterization data suggests that several iron oxides such as Fe2O3, Fe0, FeOOH and Fe3O4 were formed on the FeYBC surface as well as oxygen-containing groups. Thermodynamics study indicates that Cr(VI) and phenol adsorption by FeYBC were endothermic and exothermic processes, respectively. Langmuir adsorption isotherm and pseudo-second order models could better explain the Cr(VI) and phenol adsorption behaviors over FeYBC. The Cr(VI) adsorption might be primarily achieved through the ion exchange and surface complexation and reduction, whereas the π–π interaction and electron donor–acceptor complex mainly contributed to phenol adsorption. The findings indicate that the biochar-based iron oxide composites material was an efficient adsorbent for the remediation of industrial effluents containing Cr(VI) and phenol.

Peroxisome proliferator-activated receptor gamma (PPARγ) is a master regulator of adipogenesis and lipogenesis. To understand its roles in fiber formation and fat deposition in skeletal muscle, we successfully generated muscle-specific overexpression of PPARγ in two pig models by random insertion and CRISPR/Cas9 transgenic cloning procedures. The content of intramuscular fat was significantly increased in PPARγ pigs while had no changes on lean meat ratio. PPARγ could promote adipocyte differentiation by activating adipocyte differentiating regulators such as FABP4 and CCAAT/enhancer-binding protein (C/EBP), along with enhanced expression of LPL, FABP4, and PLIN1 to proceed fat deposition. Proteomics analyses demonstrated that oxidative metabolism of fatty acids and respiratory chain were activated in PPARγ pigs, thus, gathered more Ca2+ in PPARγ pigs. Raising of Ca2+ could result in increased phosphorylation of CAMKII and p38 MAPK in PPARγ pigs, which can stimulate MEF2 and PGC1α to affect fiber type and oxidative capacity. These results support that skeletal muscle-specific overexpression of PPARγ can promote oxidative fiber formation and intramuscular fat deposition in pigs.

A novel way of lipase-catalyzed synthesis of monocaffeoyl monofatty acyl glycerols (MCMFGs), caffeic acid derivatives, with improved lipophilicity was investigated. The monocaffeoyl monopalmitoyl glycerol (MCMPG), monocaffeoyl monooleoyl glycerol (MCMOG) and monocaffeoyl monolinoleoyl glycerol (MCMLG) were prepared by Lypozyme 435 catalysis between 1-MCG and fatty acids. High 1-monocafferol glycerol (1-MCG) conversion (>98.26%) and the maximum yields of MCMPG (26.26%), MCMOP (35.37%) and MCMLP (45.43%) were obtained. The MCMFGs (>95%) were purified by preparative chromatography and their structures were verified by HPLC-MS/MS and 13C NMR. The ionization and viscosity of fatty acids were major factors during the synthesis of MCMFGs. Subsequently, the antioxidant assays supported that the MCMFGs are effective antioxidants and their antioxidant properties decreased by the “block” effect of their fatty acyl groups on catechol group. This study lighted not only the application of MCMFGs in industry, but also the further design of phenol lipids.

Background: Human ornithine decarboxylase (ODC) is a well-known oncogene, and the discovery of ODC enzyme inhibitors is a beneficial strategy for cancer therapy and prevention. Methods: We examined the inhibitory effects of a variety of flavone and flavonol derivatives on ODC enzymatic activity, and performed in silico molecular docking of baicalein, 7,8-dihydroxyflavone and myricetin to the whole dimer of human ODC to investigate the possible binding site of these compounds on ODC. We also examined the cytotoxic effects of these compounds with cell-based studies. Results: Baicalein, 7,8-dihydroxyflavone and myricetin exhibited significant ODC suppression activity with IC50 values of 0.88 &micro, M, 2.54 &micro, M, and 7.3 &micro, M, respectively, which were much lower than that of the active-site irreversible inhibitor &alpha, DL-difluoromethylornithine (IC50, the half maximal inhibitory concentration, of approximately 100 &micro, M). Kinetic studies and molecular docking simulations suggested that baicalein, and 7,8-dihydroxyflavone act as noncompetitive inhibitors that are hydrogen-bonded to the region near the active site pocket in the dimer interface of the enzyme. Baicalein and myricetin suppress cell growth and induce cellular apoptosis, and both of these compounds suppress the ODC-evoked anti-apoptosis of cells. Conclusions: Therefore, we suggest that the flavone or flavonol derivatives baicalein, 7,8-dihydroxyflavone, and myricetin are potent chemopreventive and chemotherapeutic agents that target ODC.

Background/aim Quinazolinone is a privileged chemical structure employed for targeting various types of cancer. This study aimed to demonstrate the antitumor activity of synthesized 6,7-disubstituted-2-(3-fluorophenyl) quinazolines (HoLu-11 to HoLu-14). Materials and methods The cytotoxicity was assessed by the sulforhodamine B (SRB) assay. The cell cycle was examined by flow cytometry. The expression levels of cell cycle- and apoptosis-related proteins were estimated by western blotting. A xenograft animal model was used to explore the antitumor effects of HoLu-12. Results Among four synthetic quinazolinone derivatives, HoLu-12 significantly reduced the viability of oral squamous cell carcinoma (OSCC) cells. HoLu-12 induced G2/M arrest and increased the expression of cyclin B, histone H3 (Ser10) phosphorylation, and cleaved PARP, indicating that HoLu-12 could induce mitotic arrest and then apoptosis. Moreover, the combination of HoLu-12 and 5-fluorouracil (5-FU) displayed synergistic toxic effect on OSCC cells. HoLu-12 significantly inhibited tumor growth in vivo. Conclusion HoLu-12 induces mitotic arrest and leads to apoptosis of OSCC cells. Furthermore, HoLu-12 alone or in combination with 5-FU is a potential therapeutic agent for OSCC.

Certain sucrose mono-esters display excellent emulsifying properties as well as a range of other useful physicochemical characteristics that follow from their amphipathic nature. Accordingly, they are playing increasingly important roles in various food manufacturing industries. In this study, an homologous series of 6-O-acylsucrose mono-esters with long and very long fatty acid-derived acyl side-chains has been prepared via enzymatic transesterification. The surface-active properties as well as the antibacterial and antitumor activities of these esters have been studied. Their HLB values were 10.3–15.7 while the mean droplet sizes of the emulsions formed with soybean, colza and olive oils were 380–563 nm. Oil-water emulsions incorporating some of them are more stable, even under conditions of thermal and ionic stress, than those prepared using commercial sucrose esters. Additionally, these esters display activities against Gram-positive bacteria and certain fungi as well as exerting antiproliferative effects on six tumor cell lines. Taken together, these results suggest that the title esters could have considerable utility in the food industry by serving as emulsifiers, as preservatives and even as functional foods.

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) causing the current pandemic, coronavirus disease 2019 (COVID-19), has taken a huge toll on human lives and the global economy. Therefore, effective treatments against this disease are urgently needed. Here, we established a fluorescence resonance energy transfer (FRET)-based high-throughput screening platform to screen compound libraries to identify drugs targeting the SARS-CoV-2 main protease (Mpro), in particular those which are FDA-approved, to be used immediately to treat patients with COVID-19. Mpro has been shown to be one of the most important drug targets among SARS-related coronaviruses as impairment of Mproblocks processing of viral polyproteins which halts viral replication in host cells. Our findings indicate that the anti-malarial drug tafenoquine (TFQ) induces significant conformational change in SARS-CoV-2 Mproand diminishes its protease activity. Specifically, TFQ reduces the α-helical content of Mpro, which converts it into an inactive form. Moreover, TFQ greatly inhibits SARS-CoV-2 infection in cell culture system. Hence, the current study provides a mechanistic insight into the mode of action of TFQ against SARS-CoV-2 Mpro. Moreover, the low clinical toxicity of TFQ and its strong antiviral activity against SARS-CoV-2 should warrant further testing in clinical trials.

As a common foodborne pathogen, Escherichia coli O157:H7 produces toxins causing serious diseases. However, traditional methods failed in detecting E. coli O157:H7 cells in the viable but non-culturable (VBNC) state, which poses a threat to food safety. This study aimed at investigating the formation, control, and detection of the VBNC state of E. coli O157:H7. Three factors including medium, salt, and acid concentrations were selected as a single variation. Orthogonal experiments were designed with three factors and four levels, and 16 experimental schemes were used. The formation of the VBNC state was examined by agar plate counting and LIVE/DEAD® BacLightTM bacterial viability kit with fluorescence microscopy. According to the effects of environmental conditions on the formation of the VBNC state of E. coli O157:H7, the inhibition on VBNC state formation was investigated. In addition, E. coli in the VBNC state in food samples (crystal cake) was detected by propidium monoazide-polymerase chain reaction (PMA-PCR) assays. Acetic acid concentration showed the most impact on VBNC formation of E. coli O157:H7, followed by medium and salt concentration. The addition of 1.0% acetic acid could directly kill E. coli O157:H7 and eliminate its VBNC formation. In crystal cake, 25, 50, or 100% medium with 1.0% acetic acid could inhibit VBNC state formation and kill E. coli O157:H7 within 3 days. The VBNC cell number was reduced by adding 1.0% acetic acid. PMA-PCR assay could be used to detect E. coli VBNC cells in crystal cake with detection limit at 104 CFU/ml. The understanding on the inducing and inhibitory conditions for the VBNC state of E. coli O157:H7 in a typical food system, as well as the development of an efficient VBNC cell detection method might aid in the control of VBNC E. coli O157:H7 cells in the food industry.

Electrochemical (EC) sensors have been widely developed for DNA detection, but they are seldom used in a simple, economic, and efficient manner. In this work, for the first time, EC cloth-based DNA sensors (ECDSs) are developed as a new class of EC DNA sensors, without the need for cumbersome chip fabrication and high-cost peripheral facilities. Carbon ink- and solid wax-based screen printing were used to produce ultracheap sensing devices (the cost of one sensor is estimated to be $0.045). Also, a CdTe QDs/MWCNTs nanocomposite (CdTe-MWCNTs) was applied to modify the sensing interface to obtain a stronger EC signal. Specifically, the newly developed double linear hybridization chain reaction (DL-HCR) greatly amplified the EC signal, relative to the conventional linear HCR. Under optimized conditions, target DNA (TD) samples (75-bp DNA fragments prepared via PCR amplification) were determined in a range from 20 fM to 5 nM, with a detection limit of 8.74 fM and relative standard deviations of 2.04% and 4.75% for intra- and inter-assays at 50 pM TD, respectively. Additionally, the ECDSs had an acceptable storage stability and high selectivity. Importantly, the ECDSs, coupled with simple enzyme digestion, could detect genomic DNA from Listeria monocytogenes (L. monocytogenes), and a detection limit of 0.039 ng/μL was obtained. When coupled with enzyme digestion and PCR amplification, the ECDSs could determine L. monocytogenes in milk samples, with detection limits of approximately 1.64 × 104 and 11 CFU/mL. These results demonstrate that the method offers a broad prospect for cost-effective, reliable, and highly sensitive gene-sensing applications.

The effects of thermomechanical treatment and guar gum (GG) addition on the in vitro digestibility of rice starch have been investigated. Rice starch added with GG at concentrations of 0, 0.025, 0.05, 0.075, or 0.10 g/100 g (wet basis) was subject to a micro-extrusion process. The in vitro digestibility, predicted glycemic index (pGI), and multi-scale structures (granule, lamellar, crystalline, and molecular structures) were examined. Micro-extruded rice starch (MERS) with GG presented reduced digestion rate and pGI, a higher degree of structural ordering, and altered crystalline, single-helical and double-helical structures. Using Pearson correlation analysis, the relationships among extrusion, the molecular interaction and multi-scale structure, and the digestibility were established. The content of resistant components (RC) was positively correlated with crystallinity (r = 0.836, p