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Target-protein-based pesticide screening has attracted wide-ranging attention on pesticide science. Pedunsaponin A (PA) is a compound isolated from the root of Pueraria peduncularis, and it has a strong toxic effect on Pomacea canaliculata. Previous studies found that Advlin (PcAdv) and neural Wiskott-Aldrich syndrome isoform X1(PcnWAS) are target proteins of PA when interacted with P. canaliculata. In this study, we modeled the two target proteins through I-Tasser and identified the pharmacophore of PA binding to the two target proteins by molecular docking. Furthermore, through virtual screening, potassium alginate was found to strongly bind to the target proteins in theory. In vivo bioassay showed that, similar to PA treatment, potassium alginate was able to induce typical poisoning symptoms on P. canaliculata, which were characterized by abnormal increase of excreta, weakening of climbing capacity, loss of gill cilia and decrease in hemocyanin content, and even cause death of P. canaliculata with a 13.33% mortality rate under 100 mg L

The dehydrative mono-/dialkylation reactions of alcohols and β-ketoacids were realized under arylboronic acid catalysis, furnishing a series of β-aryl ketones and β-ketoesters in yields of 15-99%, with CO

A catalytic α-fluorination reaction between the aryl acetic acid and selectfluor was established in the presence of a boron catalyst. A number of α-fluoro aryl acetic acids were generated in up to 96% yield, including several bioactive molecules.

This study characterized an acidic polysaccharide (OHC-LDPA) isolated from the medicinal and edible homologous plant Onosma hookeri Clarke var. longiforum Duthie. The structure of OHC-LDPA was elucidated based on the analysis of infrared, one-/two-dimensional nuclear magnetic resonance, and gas chromatography-mass spectrometry data. The immunostimulatory effects of OHC-LDPA were identified by both in vitro and in vivo models.The structure of OHC-LDPA was elucidated as a typical pectin polysaccharide, consisting of galacturonic acid, galactose, arabinose, and rhamnose as the primary sugars, with linear galacturonic acid as the main chain and arabinogalacturonic acid as the main branched components. OHC-LDPA could significantly stimulate the proliferation and phagocytosis of RAW264.7 macrophages and the release of nitric oxide in vitro. Also, it could accelerate the recovery of spleen and thymus indexes, enhance the splenic lymphocyte proliferation responses, and restore the levels of interleukin-2, interleukin-10, interferon-γ, and immunoglobulin G in the serum in a cyclophosphamide-induced immunosuppressed-mice model. In addition, OHC-LDPA could restore the intestinal mucosal immunity and reduce the inflammatory damage.OHC-LDPA could improve the immunity both in vitro and in vivo and could be used as a potential immunostimulant agent. © 2022 Society of Chemical Industry.

The umpolung Michael addition of isatin N,N′-cyclic azomethine imine 1,3-dipoles with chalcones is reported. The reaction could be finished within a very short time (0.3–2 min), with 3,3-disubstituted oxindole derivatives obtained in moderate to excellent yields with promising dr values. Unusual Michael adducts were obtained in moderate to high yields (26–98%) with low to high diastereoselectivities (0.8 : 1 to 8.5 : 1 dr). All the synthesized compounds (3, 3′, 4, 5, 5′, 7, 7′, 9 and 9′) were well characterized by FTIR, NMR, and mass spectral analyses and further confirmed by the single-crystal X-ray diffraction analysis of compounds 3aa and 4n.

As a double-edged sword, autophagy in cancer cells could either suppress or promote tumorigenesis. Nowadays, more and more natural compounds with autophagy-regulating activities exhibit therapeutic effects against various cancers. N-Heterocycle derivatives plays an important role for discovery new drugs. In this review, we summarize and classify 116 N-heterocycle derivatives with autophagy-regulating activities in the past decade into 12 classes according to structure characteristics. The structural features, bioactivities, mechanism and problems faced in this field are discussed and reported for the first time. Some of these even exhibited outstanding in vivo antitumor activities, including bisaminoquinoline (3), pancratistatin (8), 10-hydroxyevodiamine (18), lycorine (28), piperine (31) and iridium (III) complex (57), which are potential drug candidates for antitumor therapy.

Previous studies have found that temperature influences molluscicidal the activity of pedunsaponin A (PA), which may be related to the expression of Hsp70, a cold-tolerance gene in Pomacea canaliculata. We determined the temperature effect of PA and the relationship between Hsp70 and temperature sensitivity of P. canaliculata poisoned by PA. Toxicity tests resulted in LC

The rapid synthesis of novel dicyclic spiropyrrolidine was reported, using [3+2]-cycloaddition of isatin N,N′-cyclic azomethine imine 1,3-dipoles, generated from the condensation of substituted isatins and pyrazolidones, with chalcones in 2–5 min. The dicyclic spiropyrrolidine oxoindole was smoothly acquired in moderate to excellent yields (35–95%) with high diastereoselectivities (>20 : 1 dr).

An environmental-friendly and mild method has been successfully developed for the synthesis of 3-aryl-2-nitro-2,3-dihydrobenzofurans through domino Friedel–Crafts/substitution reaction of (Z)-bromonitrostyrenes with sesamol. A variety of substrates performed well in this reaction, and the corresponding 3-aryl-2-nitro-2,3-dihydrobenzofurans were obtained in excellent yields (up to 99%). Significantly, water served as the sole green solvent. Remarkably, the crude products were purified by simple filtration, washing with water and drying in oven without any organic solvents or silica gel.

In this study, a dual-emission ratiometric fluorescent sensing system is developed for the analysis of H2O2 and uric acid (UA). This sensing system is based on N, Fe-doped carbon dots (N, Fe-CDs) and bovine serum albumin (BSA)-stabilized silver nanoclusters (BSA-Ag NCs) with peroxidase activity. By the catalysis of uriase, UA was oxidized by oxygen dissolved in the solution and H2O2 is produced. The carbon site with peroxidase activity can catalyze H2O2 to generate hydroxyl radicals, which etches to the BSA-Ag NCs. At the excitation wavelength of 390 nm, there were dual emission peaks at 450 nm and 650 nm. With increasing concentration of H2O2 or UA, the red fluorescence at 650 nm for BSA-Ag NCs decreases due to the etching of BSA-Ag NCs by hydroxyl radicals, while the blue fluorescence of N, Fe-CDs is restored. Based on the relationship between the fluorescence intensity ratio (I450/I650) to detect H2O2 and UA, the linear range of H2O2 was 0.6–100 μM with a detection limit of 0.30 μM (S/N = 3), while the linear range of UA was 0.8–133 μM with a detection limit of 0.49 μM (S/N = 3). Moreover, the present method was used for the analysis of UA in human urine with satisfactory accuracy as well as recovery. This ratiometric fluorescent approach can be used for analysis of UA and H2O2 for biomedical applications.

Glabridin is a natural plant-derived compound that has been widely used in medicine and cosmetic applications. However, the fungicidal mechanism of glabridin against phytopathogens remains unclear. In this study, we determined the biological activity and physiological effects of glabridin against F. graminearum. Then the differentially expressed proteins of F. graminearum were screened. The EC50 values of glabridin in inhibiting the mycelial growth and conidial germination of F. graminearum were 110.70 mg/L and 40.47 mg/L respectively. Glabridin-induced cell membrane damage was indicated by morphological observations, DiBAC4(3) and PI staining, and measurements of relative conductivity, ergosterol content and respiratory rates. These assays revealed that the integrity of the membrane was destroyed, the content of ergosterol decreased, and the respiratory rate was inhibited. A proteomics analysis showed that 186 proteins were up-regulated and 195 proteins were down-regulated. Mechanically sensitive ion channel proteins related to transmembrane transport and ergosterol biosynthesis ERG4/ERG24, related to ergosterol synthesis were blocked. It is speculated that glabridin acts on ergosterol synthesis-related proteins to destroy the integrity of the cell membrane, resulting in abnormal transmembrane transport and an increased membrane potential. Finally, the morphology of mycelia was seriously deformed, growth and development were inhibited. As a result death was even induced.

In the 21st century, cancer is the major public health problem worldwide. Based on the important roles of protein tyrosine kinase, the accelerated hunt for potent small-molecule tyrosine kinase inhibitors has led to the success of 30 newly inhibitors in this family for the cancer therapy in last five years. In this review, we updated their synthesis methods, and compared the original research routes with the optimized routes for each PTK inhibitor against different target, in order to make an outlook on the future synthesis of potential PTK inhibitors for anticancer therapy.

Aconitine linoleate (11) isolated from the Aconitum sinchiangense W. T. Wang exhibited significant anti-tumor activity. Based on this, a series of novel lipo-diterpenoid alkaloids were synthesized and evaluated for their anticancer activities against MCF-7 and MCF-7/ADR cell lines. Seventeen compounds, including 18–20, 22, 24–32, 36, 39, 41–42 possessed higher anti-proliferative activities (IC50

Pseudorabies virus (PRV), belonging to the family Herpesviridae, is a pathogen of Aujeszky’s disease leading great economic losses to pig industry. Re-outburst of pseudorabies implies that new control measures are urgent needed. The present study provides a candidate drug for PRV infection that kaempferol possesses the ability to inhibit PRV replication in a dose-dependent manner in vitro. Kaempferol at a concentration of 52.40 μM could decrease PRV-induced cell death by 90%. Kaempferol with a IC50 of 25.57μM is more effective than acyclovir (Positive control) with a IC 50 of 54.97 μM. Mode of action study indicated that kaempferol inhibited viral penetration and replication stages and virus load was decreased by 4-fold and 30-fold, respectively. Addition of kaempferol within 16 hours post infection (hpi) could significantly inhibit virus replication, and the DNA copies were decreased by almost 15-fold when kaempferol was added at 2 hpi. Kaempferol could regulate NF-κB and MAPKs signal pathways involved in PRV infection and change the levels of the target genes of MAPKs (ATF-2 and c-Jun) and NF-κB (IL-1α, IL-1β and IL-2) signaling pathways. All the results indicated that kaempferol has the ability to be an alternative control measure for PRV infection.¶ These authors contribute equally to this work and should be considered as the first author.

Two oleanane-type triterpenoid saponins named pedunsaponin D (1) and pedunsaponin E (2) were isolated from the roots of Pueraria peduncularis. The structures of the new compounds were elucidated based on chemical and physicochemical evidence as follows: pedunsaponin D, 3-O-β-glucopyranosyl-(1-3)-β-glucuronopyranosyl-3β,15α,23α-trihydroxy-11,13(18)-oleanadien-16-one (1); pedunsaponin E, 3-O-β-glucopyranosyl-(1-2)-β-glucopy ranosyl(1-2)[β-glucopyranosyl(1-3)-β-glucuronopyranosyl]-3β-hydroxy-16-oxoolean-12-en-30-oic acid (2). The two compounds showed moderate molluscicidal activity.[Formula: see text].

Purification, characterization and biological activities of polysaccharides from Lycium barbarum pedicel were investigated in this study. Two polysaccharides, PLBP-I-I and PLBP-II-I, were obtained from water extracts by anion exchange chromatography and gel filtration. Structural elucidation based on IR, 1H NMR, and 13C NMR spectra indicated that these two fractions were typical pectic polysaccharides, with homogalacturonan and rhamnogalacturonan type I regions and arabinogalactan side chains, and some of the galacturonic acid units were methyl esterified. Both fractions exhibited potent complement fixating activity and pro-antioxidant defense capacity, and those two fractions showed different activities. The higher complement fixation activity was obtained in fraction PLBP-I-I, while the higher pro-antioxidant defense capacity was obtained in fraction PLBP-II-I, which may be due to the structural differences between those two fractions. Thus, the pedicel of L. barbarum could be used as a potential source for natural immunomodulator and antioxidant.

The synthesis of novel spiropyrrolidine oxindole derivatives was reported, using Ag-catalyzed [3+2] cycloaddition of azomethine ylides generated in situ from the condensation of substituted isatins and primary α-amino acid esters with chalcones. Products bearing four consecutive stereocenters, including spiroquaternary stereocenters fused in one ring structure, were smoothly acquired in moderate to high yields (50–95%) with good to excellent diastereoselectivities (11 : 1 → 20 : 1 dr). Furthermore, product 4a underwent reduction, oxidation, hydrolysis and amidization to give the corresponding alcohol, dihydropyrrole, pyrrole, acid and amide, respectively, in good yields. The synthesized compounds (>100 examples) were well characterized through different spectroscopic techniques, such as single crystal XRD, FTIR, NMR, and mass spectral analysis.

A high incidence of cancer has given rise to the development of more anti-tumor drugs. From 2015 to 2020, fifty-six new small-molecule anticancer drugs, divided into ten categories according to their anti-tumor target activities, have been approved. These include TKIs (30 drugs), MAPK inhibitors (3 drugs), CDK inhibitors (3 drugs), PARP inhibitors (3 drugs), PI3K inhibitors (3 drugs), SMO receptor antagonists (2 drugs), AR antagonists (2 drugs), SSTR inhibitors (2 drugs), IDH inhibitors (2 drugs) and others (6 drugs). Among them, PTK inhibitors (30/56) have led to a paradigm shift in cancer treatment with less toxicity and more potency. Each of their structures, approval statuses, applications, SAR analyses, and original research synthesis routes have been summarized, giving us a more comprehensive map for further efforts to design more specific targeted agents for reducing cancer in the future. We believe this review will help further research of potential antitumor agents in clinical usage.

Haemophilus parasuis , a symbiotic bacteria of upper respiratory tract of swine, is the etiological agent of Glasser's disease, which is characterized by fibrinous polyserositis. Emodin, exhibits antibacterial activity against H. parasuis , yet the action mode has not been fully understood. In present study, isobaric tag for relative and absolute quantification (iTRAQ) method was applied to analyze the global protein alteration of H. parasuis in response to 16 μg/mL Emodin. In total, 338 proteins exhibiting significant differential expressions were identified. It was speculated that, through application of bioinformatics analysis to theses differentially expressed proteins, Emodin mainly inhibited some key proteins expression of ABC transport system, carbohydrate metabolism pathway and bacterial cell division by inhibiting the ribosome synthesis, resulting in the growth inhibition of H. parasuis. Remarkably, nine virulence-associated proteins were detected differently expressed, further experiments revealed that after treatment with Emodin, H. parasuis could be inhibited to adhere to and invade into porcine kidney epithelial cells (PK-15 line) and exhibited increased sensitivity to serum complement in a concentration-dependent manner. Phagocytosis assay showed Emodin also could enhance phagocytic activity of porcine alveolar macrophages PAM to H. parasuis. These results indicated that Emodin also can attenuate virulence of H. parasuis and reduce infection. Biological significance The Glasser's disease caused by H. parasuis has become a typical bacterial disease and cause serious economic loss to the swine industry around the world. Antibiotics are extensively used to control the infection, but increasing antibiotic resistance has been a severe problem. Hence, novel treatment agents are needed. So far, few antibacterial agents were reported that could control H. parasuis infection. In the present study, the state-of-the-art quantitative proteomic technology was applied to uncover underlying action mechanism of Emodin. This study extends understanding of antibacterial effect of Emodin to H. parasuis at molecular level and provides useful information for further investigations. Moreover, our results provide theoretical foundation for the practical application of Emodin.

Astragaloside IV (AS-IV), a main active substance isolated from Astragalus membranaceus Bunge, has been shown to have multiple pharmacological effects. Endothelial cell protein C receptor (EPCR) is a marker of inflammation, and is also a major member of protein C (PC) anti-coagulation system. EPCR can be cut off from the cell surface by tumor necrosis factor-α converting enzyme (TACE), which is controlled through mitogen-activated protein kinase (MAPK) and protein kinase C (PKC) pathways. To develop novel therapeutic drug for EPCR shedding, the effect of AS-IV was studied in phorbol-12-myristate 13-acetate (PMA)-induced human umbilical vein endothelial cells (HUVECs) and the potential molecular mechanism of AS-IV action was investigated. The results showed that AS-IV could significantly inhibit PMA-induced EPCR shedding. In further study, AS-IV suppressed the expression and activity of TACE. In addition, AS-IV could decrease the phosphorylation of MAPK such as janus kinase (JNK) and p38, and inhibit activation of PKC through the prevention of non-phosphorylation and phosphorylation of specific PKC isoforms in PMA-stimulated HUVECs. These findings indicate that AS-IV may be used as a natural medicine to treat EPCR-related systemic inflammation and cardiovascular diseases by targeting MAPK and PKC pathway.

Pomacea canaliculata is an invasive snail that can adversely affect biodiversity, agricultural crop yields and human health. Schima superba, which belongs to the Theaceae family, exhibits insecticidal and antibacterial activity, but few studies have focused on its potential molluscicidal activity. In this study, we systematically evaluated the molluscicidal activity of S. superba extract against P. canaliculata in a variety of conditions, including multiple exposure intervals (24, 48 and 72 h), temperatures (15, 20 and 25 °C) and shell diameters (1.5 ± 0.2, 2.5 ± 0.2 and 3.5 ± 0.2 cm). The molluscicidal activities of a 10% microemulsion of S. superba extract were tested on rice in plastic pots filled with mud at different exposure intervals (1, 3, 5 and 7 days). In addition, we isolated and purified the active components from S. superba extract and described them. S. superba was highly toxic to P. canaliculata; the LC50 values for the crude extract at 72 h were 12.25 mg L−1 (15 °C), 11.31 mg L−1 (20 °C), 8.33 mg L−1 (25 °C) with 2.5 ± 0.2 cm shell diameter and 9.43 mg L−1 (1.5 ± 0.2 cm shell diameter), 9.48 mg L−1 (2.5 ± 0.2 cm shell diameter), 10.06 mg L−1 (3.5 ± 0.2 cm shell diameter) at 25 °C. There was a positive correlation between the molluscicidal activity of the extract and treatment temperature after 24 h of treatment, but there was no clear correlation beyond 24 h. In addition, there was no statistically significant correlation between the molluscicidal activity of the extract and shell diameters. Pot trials showed that the crude extract effectively controlled P. canaliculata at 8 and 10 mg L−1. We isolated and characterized two pentacyclic triterpenoid saponins from S. superba, maetenoside B and sasanquasaponin III, which had high molluscicidal activity. This study provides an important foundation for future research on the potential value of S. superba as a molluscicide.

The present study investigated acute and subchronic toxicity and safety pharmacology of modified pulsatilla granules (MPG) to provide a basis for a comprehensive understanding of MPG toxicity. The results of acute toxicity testing showed that the median lethal dose of MPG was more than 5000 mg kg−1, suggesting that MPG was considered as practically non-toxic. The subchronic toxicity study for 30 days was conducted by daily oral administration at doses of 375, 750 and 1 500 mg kg−1 in Sprague-Dawley rats. The results of subchronic toxicity study showed that the body weight and relative organ weight were not significantly changed by administration of MPG. The clinical chemistry study showed that MPG could induce kidney and liver damages. In histopathological, mild lesions in liver and kidney were also observed, suggesting that the liver and kidney might be potential target organs of MPG. In the safety pharmacology study, MPG did not exhibited any side effects to rats in cardiovascular system, respiratory system and central nervous system. These results suggested that MPG could be considered safe for veterinary use.

A new synthetic method for 2-arylindoles has been developed, the process through Suzuki coupling reaction of 3-bromoindoles with hindered boronic acid catalyzed by Pd(OAc)2/PCy3, and a series of 2-arylindoles have been synthesized in moderate to high yields.

Transcriptomes, genomes, and proteomes have played important roles in the search for drug targets. To determine the molluscicidal mechanism of pedunsaponin A against Pomacea canaliculata, RNA-seq technology was adopted to analyze the differentially expressed genes (DEGs) in the P. canaliculata transcriptome after treatment with pedunsaponin A. As a result, 533 DEGs were identified, among which 255 genes were significantly upregulated and 278 genes were significantly downregulated. According to the analysis of Gene Ontology (GO) functions, we found that the DEGs were significantly enriched in the viral life cycle, UDP-glucose 4-epimerase activity, guanylate cyclase activity, the cyclic guanosine monophosphate (cGMP) biosynthetic process, and the cGMP metabolic process. The Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway results showed that the DEGs were mainly involved in the hedgehog signaling pathway, phagosome, cytosolic DNA-sensing pathway, retinoic acid-inducible gene I like (RIG-I-like) receptor signaling pathway, bacterial secretion system, and nuclear factor-kappa B (NF-kappa B) signaling pathway. The above results indicated that pedunsaponin A causes a metabolic disorder, anomalous opening of membrane ion channels, and an imbalance in osmotic pressure between the interior and exterior of cells, eventually resulting in the death of cells involved in immune defense and influencing the immune response of P. canaliculata.

Pomacea canaliculata hemocytes are the main functional cells in the immune defense system, and hemocyte destruction disrupts the immune response mechanism of P. canaliculata, resulting in abnormal growth, development, reproduction, and even death. Our previous study found that Pedunsaponin A significantly affects P. canaliculata hemocyte structure. This study further investigated the damaging effects of Pedunsaponin A on P. canaliculata hemocytes. The cell mortality rate results showed that the hemocyte mortality was significantly increased after treatment with Pedunsaponin A, and the mortality rate exhibited a significant positive correlation with treatment time and dose. The membrane potential results showed that the cell membranes of P. canaliculata hemocytes exhibited time-dependent membrane depolarization after 40 mg/L Pedunsaponin A treatment. At 36 h, the cell depolarization rate in the Pedunsaponin A treatment group was 41.43%, which was significantly greater than the control group (6.24%). The cytoskeleton results showed that Pedunsaponin A led to disordered and dispersed arrangement of microfilaments and changes in the cytoskeletal structure. The apoptosis and cell cycle results showed that Pedunsaponin A induced apoptosis and influenced the cell cycle to some extent. These results showed that the cell membrane and cytoskeleton of P. canaliculata hemocytes were damaged after treatment with Pedunsaponin A, which led to an increase in cell mortality, dysfunction, cell cycle abnormalities and apoptosis. This study provides a foundation for further identification of the site of Pedunsaponin A activity on hemocytes.

Porous uranium oxide hollow sphere nanoparticles were synthesized in ionic liquids under hydrothermal conditions. Various precipitating agents and ionic liquids were investigated to determine their respective impact on the resultant uranium oxide morphologies. Using hydrazine hydrate as precipitating agent and N-butyl pyridinium bromide as templating agent, a porous-hollow structure was created with a surface area of 1958 m2.g−1 and an average pore diameter of 30 nm. The nanoparticles revealed high peroxidase-mimicking activity. This was evaluated by using the peroxidase substrate 3,3′,5,5′-tetramethylbenzidine (TMB) that is catalytically oxidized by H2O2 to give oxidized TMB (oxTMB) which is blue (with an absorption peak at 652 nm). The material was used as a nanozyme for colorimetric detection of Sn2+. Meanwhile, it is found that BSA strongly improves the catalytic activity of the nanozyme, while Sn(II) inhibits its activity. Thus, a colorimetric method for Sn2+ detection was designed. The method works in the 0.5–100 μM Sn(II) concentration range and has a lower detection limit of 0.36 μM (at S/N = 3).

Carbon dots-doped CeO2 (CeO2-CDs) with enhanced peroxidase-like activity and fluorescent carbon dots (CDs) were prepared by one-pot hydrothermal method in this work. The morphology, surface groups and enzymatic properties of CeO2-CDs and optical properties of CDs were studied in detail. The enzyme activity of CeO2-CDs was higher than CeO2 due to the smaller particle size. O-phenylenediamine (OPD) as peroxidase substrate can be catalyzed to fluorescent o-phenylenediamine (oxOPD) by CeO2-CDs, and the UV–vis absorption of oxOPD overlapped partly with the fluorescence emission of CDs. Hence, the fluorescence intensity of CDs would be decreased by oxOPD due to the inner filter effect. Based on this, a sensitive and selective ratiometric fluorescence method for H2O2 and cholesterol was developed. The detection ranges for H2O2 and cholesterol are 1.67 µM-2.01 mM and 1.66 µM-1.65 mM with the detection limits are 0.35 µM and 0.49 µM (3Ϭ), respectively. Moreover, this method has been successfully used to detect cholesterol in human serum.

Background of the Study. As a widely used traditional medicine, Galla Chinensis is rich in tannins. However, there are few detailed studies about pharmaceutical preparations of Galla Chinensis tannin extract (GTE). In the present experiments, for better application and to investigate the possibility that Galla Chinensis tannin extract can be used as an antidiarrheal drug, we prepared Galla Chinensis oral solution (GOS). Materials and Methods. GOS was prepared with GTE, and its physicochemical and microbiological stability was evaluated. The oral acute toxicity of GOS was calculated by the 50% lethal dose (LD50). The antidiarrheal activity was determined in a castor oil-induced diarrhea model in mice through diarrhea symptoms, fluid accumulation ratio, and percentage of distance moved by charcoal meal. Results. The tannin content of GTE was 47.75%. GOS could endure a high temperature without a significant decrease of tannin content. After storage for six months, the tannin content of GOS was still more than 90%. GOS was determined to be nontoxic. Meanwhile, GOS showed significant antidiarrheal activity in a castor oil-induced diarrhea model in mice (P<0.01). Conclusion. The results suggested that GOS is an effective and stable antidiarrheal drug that can be used to complement other therapies.

BACKGROUND Pueraria peduncularis (Grah. ex Benth.) Benth., which belongs to the Leguminosae family, exhibits resistance to many crop pests in agricultural production. Pomacea canaliculata is an important invasive snail in rice fields and causes severe yield losses. To evaluate the toxicity of P. peduncularis to P. canaliculata, in this study the molluscicidal activity of root extracts of P. peduncularis was tested against P. canaliculata; the active compounds were isolated, and the structures of these compounds were analysed using nuclear magnetic resonance (NMR) analysis and mass spectral analysis. RESULTS Our results showed that the molluscicidal activity of the root crude extract differed between P. canaliculata with different shell diameters after treatment for 72 h. The median lethal concentration (LC50) was 5.511 mg L−1 against snails of 1.5 ± 0.2 cm diameter and 12.383 mg L−1 against snails of 2.5 ± 0.2 cm diameter. Furthermore, two active ingredients isolated from root methanol extracts were identified as pedunsaponin A and pedunsaponin C. Both pedunsaponin A and pedunsaponin C showed strong molluscicidal activities, with LC50 values of 3.893 and 4.252 mg L−1, respectively, against snails with shell diameters of 1.5 ± 0.2 cm after treatment for 72 h. CONCLUSION Pueraria peduncularis extracts exhibit high molluscicidal activity and have great potential value for exploring a molluscicide to control Pomacea canaliculata. © 2016 Society of Chemical Industry

Duck enteritis virus (DEV) is a double-stranded DNA virus belonging to the alphaherpesvirinae subfamily of the herpesviridae. Although vaccines were wildly used in controlling this disease, some infection could still not be prevented and led to significant economic losses as a result of mortality and decreased egg production. However, there is no antiviral drug against DEV. Resveratrol was identified to exert its antiviral activity by inhibiting the DEV replication in preliminary investigations. In the present study, we confirmed that resveratrol significantly reduced the mortality of ducklings which infected with a virulent strain of DEV. With resveratrol treatment, the survival rate increased by almost 80% at 8 days post infection (dpi). Pathological symptoms of ducklings caused by DEV were also relieved by resveratrol. The virus load in blood and tissues were effectively depressed when compared with the untreated group. In the assay of immune cytokines, the resveratrol exerted a dual-regulation effect. These results suggest that resveratrol is expected to be a new alternative control measure for DEV infection.

A general procedure for the tandem arylation reaction of arylbromide with heteroaryl compounds was developed by using Pd(PPh3)2Cl2/(&plusmn, )-BINAP (1,1&prime, Binaphthalene-2,2&prime, diylbis (diphenylphosphane)) as catalytic system. Both sulphur- and oxygen-containing heterocycles were also employed as an efficient reagent for arylation, which gave moderate to excellent yields with moderate to good regioselectivities (5:1 to &gt, 20:1 ir (isomer ratio)). Except for dihydrobenzofurans, indolines and indolinones, this type of tandem reaction was also expanded to synthesize isochromanes. The synthesized new compounds were well characterized through different spectroscopic techniques, such as 1H and 13C NMR (nuclear magnetic resonance), and mass spectral analysis.

In this study, using diethylenetriaminepentaacetic acid (DPTA), diethylenetriamine (DETA) and Fe (NO3)3.9H2O, Fe, N co-doped carbon dots (Fe, N-CDs) were successfully synthesized by a simple one-pot hydrothermal method. Fe, N-CDs possessed fluorescence and peroxidase-like properties. When H2O2 was present, o-phenylenediamine (OPD) can be oxidized by Fe, N-CDs to oxidized phenylenediamine (oxOPD), and oxOPD further quenched the fluorescence of Fe, N-CDs because of inner filter effect. There were two peaks at 450 nm and 560 nm for the system of Fe, N-CDs and oxOPD. Results showed that the concentration of H2O2 can not only affect the fluorescence intensity but also the color of the oxOPD. Considering that the xanthine oxidase can oxidize xanthine to produce H2O2, thus, a ratiometric fluorescent and colorimetric dual-signal sensor for H2O2 and xanthine was developed. This new method was demonstrated to have high sensitivity and excellent selectivity for determination of H2O2 and xanthine. The detection limits (LOD) for H2O2 and xanthine were 0.047 μM and 0.02 μM with a ratiometric fluorescence method, and were 0.05 μM and 0.023 μM with a colorimetric method, respectively. This dual-signal sensor was used successfully for xanthine detection in human serum and urine.

Fluorescent nitrogen-doped carbon dots (CDs) were prepared via hydrothermal method at 190 °C for 10 h using rhizobium from soy as the carbon and nitrogen source. Their optical properties, structure, morphology, and functional groups were characterized in detail and the results showed that they possess unique excitation-dependent fluorescence behavior, with average diameter 4.5 ± 2.0 nm and good water dispersibility. Due to the overlap of the UV-vis absorbance of chlortetracycline hydrochloride (CCH) and the fluorescence excitation band of CDs, the fluorescence of the prepared CDs can be quenched by CCH selectively and sensitively. The changes of the fluorescence intensity of CDs have a good linear relationship with the concentration of CCH in a wide concentration range of 5-100 μM, with a detection limit of 0.254 μM. This present method has been successfully applied to determine the CCH in water with recovery ranging from 96.0% to 100.7%.

A rapid, sensitive, and highly selective method for determining nitrite in food has been developed. This method is based on the reaction of nitrite with the amino group of 3,3,5,5-tetramethylbenzidine (TMB) to form a diazonium salt, and then the diazonium salt and glucosamine hydrochloride are coupled to each other to form an orange compound. The optimal conditions for maximum color and other analytical parameters were studied. A colorimetric method for nitrite detection has been developed with an outstanding correlation coefficient (R2 = 0.9944), a wide linear range (1-75 μM) and 0.73 μM limit of detection (at S/N = 3) for nitrite ions. This method was successfully applied to the determination of nitrite in a variety of foods and gave recoveries in the range between 100.16% and 103.07%, demonstrating that the accuracy, reliability and potential application of this assay for monitoring nitrite in foods.