Dissipation and Risk Assessment of Propaquizafop in Ginseng under Field Conditions.

Propaquizafop is a highly efficient aryloxy phenoxy propionate chiral herbicide. However, the use of propaquizafop, including its safe use methods, residue patterns, dietary risk assessment, and maximum residue limits, for ginseng, a traditional Chinese medicinal plant, has not been studied. An analytical method was established for the simultaneous determination of propaquizafop and its four metabolites in ginseng soil, fresh ginseng, ginseng plant, and dried ginseng using HPLC-MS/MS. This approach showed good linearity (R2 ranging from 0.9827 to 0.9999) and limit of quantification ranging from 0.01 to 0.05 mg/kg. The intra- and interday recovery rates of this method ranged from 71.6 to 107.1% with relative standard deviation ranging from 1.3 to 23.2%. The method was applied to detect residual samples in the field, and it was found that the degradation of propaquizafop in ginseng plants and soil followed a first-order kinetic equation. R2 was between 0.8913 and 0.9666, and the half-life (t1/2) ranged from 5.04 to 8.05 days, indicating that it was an easily degradable pesticide (T1/2 < 30 days). The final propaquizafop residues in ginseng soil, plants, fresh ginseng, and dried ginseng ranged from 0.017 to 0.691 mg/kg. A dietary risk assessment was conducted on the final propaquizafop residue in fresh and dried ginseng. The results showed that the chronic exposure risk quotient values were less than 100% for fresh and dried ginseng (1.15% for fresh ginseng and 1.13% for dried ginseng). This illustrates that the dietary risk associated with the use of 10% propaquizafop emulsifiable concentrate in ginseng is very low. Thus, applying 750 mL/ha of propaquizafop on ginseng could not pose an unacceptable risk to public health. The results of the present study support the registration of propaquizafop in ginseng.

Design, Synthesis, and Antimicrobial Activity Evaluation of Ciprofloxacin-Indole Hybrids.

With the overuse and misuse of antimicrobial drugs, antibacterial resistance is becoming a critical global health problem. New antibacterial agents are effective measures for overcoming the crisis of drug resistance. In this paper, a novel set of ciprofloxacin-indole/acetophenone hybrids was designed, synthesized, and structurally elucidated with the help of NMR and high-resolution mass spectrometry. The in vitro antibacterial activities of these hybrids against gram-positive and gram-negative pathogens, including four multidrug-resistant clinical isolates, were evaluated and compared with those of the parent drug ciprofloxacin (CIP). All the target compounds (MIC = 0.0625-32 µg/mL) exhibited excellent inhibitory activity against the strains tested. Among them, 3a (MIC = 0.25-8 µg/mL) showed comparable or slightly less potent activity than CIP. The most active hybrid, 8b (MIC = 0.0626-1 µg/mL), showed equal or higher activity than CIP. Moreover, compound 8b showed superior bactericidal capability to CIP, with undetectably low resistance frequencies. Furthermore, molecular docking studies conducted showed that 8b and CIP had a similar binding mode to DNA gyrase (Staphylocouccus aureus). Thus, hybrids 3a and 8b could act as a platform for further investigations.

Synthesis and anticancer properties of celastrol derivatives involved in the inhibition of VEGF.

In this study, fourteen celastrol derivatives (1-14) were synthesised by esterification of celastrol at the 29th position. The in vitro anticancer activity of them was determined by the MTT assay. All the synthetic compounds showed significant antiproliferative activity against six cancer cells, with IC50 of the submicron molar level. The most promising compound (2) blocked the cell cycle in the G2 phase and inhibited the expression of VEGF and MMP-9 in gastric cancer cell line MGC-803. In flow cytometry analysis, compound 2 induced cancer cell apoptosis in a dose-dependent manner. In the mouse tumour xenograft model, compound 2 showed significant anti-tumour activity in vivo at the dosage of 2.5 mg/kg and 1 mg/kg, with a higher inhibition rate than 5-FU (10 mg/kg). What's more, the anticancer mechanism involved in the inhibition of VEGF and the toxicity evaluation of compound 2 were also investigated.

Effect of Trichoderma viride on insoluble phosphorus absorption ability and growth of Melilotus officinalis.

Phosphorus (Pi) deficiency is a major factor of limiting plant growth. Using Phosphate-solubilizing microorganism (PSM) in synergy with plant root system which supply soluble Pi to plants is an environmentally friendly and efficient way to utilize Pi. Trichoderma viride (T. viride) is a biocontrol agent which able to solubilize soil nutrients, but little is known about its Pi solubilizing properties. The study used T. viride to inoculate Melilotus officinalis (M. officinalis) under different Pi levels and in order to investigate the effect on Pi absorption and growth of seedlings. The results found that T. viride could not only solubilizate insoluble inorganic Pi but also mineralize insoluble organic Pi. In addition, the ability of mineralization to insoluble organic Pi is more stronger. Under different Pi levels, inoculation of T. viride showed that promoted the growth of aboveground parts of seedlings and regulated the morphology of roots, thus increasing the dry weight of seedlings. The effect of T. viride on seedling growth was also reflected the increasing of chlorophyll fluorescence parameters and photosynthetic pigment content. Moreover, compared to the uninoculated treatments, inoculation of T. viride also enhanced Pi content in seedlings. Thus, the T. viride was a beneficial fungus for synergistic the plant Pi uptake and growth.

Antiseizure Properties of Histamine H3 Receptor Antagonists Belonging 3,4-Dihydroquinolin-2(1H)-Ones.

H3R is becoming an attractive and promising target for epilepsy treatment as well as the discovery of antiepileptics. In this work, a series of 6-aminoalkoxy-3,4-dihydroquinolin-2(1H)-ones was prepared to screen their H3R antagonistic activities and antiseizure effects. The majority of the target compounds displayed a potent H3R antagonistic activity. Among them, compounds 2a, 2c, 2h, and 4a showed submicromolar H3R antagonistic activity with an IC50 of 0.52, 0.47, 0.12, and 0.37 µM, respectively. The maximal electroshock seizure (MES) model screened out three compounds (2h, 4a, and 4b) with antiseizure activity. Meanwhile, the pentylenetetrazole (PTZ)-induced seizure test gave a result that no compound can resist the seizures induced by PTZ. Additionally, the anti-MES action of compound 4a fully vanished when it was administrated combined with an H3R agonist (RAMH). These results showed that the antiseizure role of compound 4a might be achieved by antagonizing the H3R receptor. The molecular docking of 2h, 4a, and PIT with the H3R protein predicted their possible binding patterns and gave a presentation that 2h, 4a, and PIT had a similar binding model with H3R.

Design, Synthesis, and Pharmacology of New Triazole-Containing Quinolinones as CNS Active Agents.

Epilepsy and major depressive disorder are the two of the most common central nervous system (CNS) diseases. Clinicians and patients call for new antidepressants, antiseizure medicines, and in particular drugs for depression and epilepsy comorbidities. In this work, a dozen new triazole-quinolinones were designed, synthesized, and investigated as CNS active agents. All compounds reduced the immobility time significantly during the forced swim test (FST) in mice at the dosage of 50 mg/kg. Compounds 3f-3j gave superior performance over fluoxetine in the FST with more reductions of the immobility time. Compound 3g also reduced immobility time significantly in a tail suspension test (TST) at the dosage of 50 mg/kg, though its anti-immobility activity was inferior to that of fluoxetine. An open field test was carried out and it eliminated the false-positive possibility of 3g in the FST and TST, which complementarily supported the antidepressant activity of 3g. We also found that almost all compounds except 3k exhibited antiseizure activity in the maximal electroshock seizure (MES) model at 100 or 300 mg/kg. Compounds 3c, 3f, and 3g displayed the ED50 of 63.4, 78.9, and 84.9 mg/kg, and TD50 of 264.1, 253.5, and 439.9 mg/kg, respectively. ELISA assays proved that the mechanism for the antiseizure and antidepressant activities of compound 3g was via affecting the concentration of GABA in mice brain. The molecular docking study showed a good interaction between 3g and the amino acid residue of the GABAA receptor. Excellent drug-like properties and pharmacokinetic properties of compound 3a-l were also predicted by Discovery Studio. These findings provided a new skeleton to develop agents for the treatment of epilepsy and depression comorbidities.

Photodynamic therapy-improved oncolytic bacterial immunotherapy with FAP-encoding S. typhimurium.

Genetically engineered bacterial cancer therapy presents several advantages over conventional therapies. However, the anticancer effects of bacterium-based therapies remain insufficient, and serious side effects may be incurred with the increase in therapeutic dosages. Photodynamic therapy (PDT) suppresses tumor growth by producing reactive oxygen species (ROS) through specific laser-activated photosensitizers (PSs). Tumor-specific PS delivery and activatable ROS generation are two critical aspects for PDT advancement. Here, we propose PDT-enhanced oncolytic bacterial immunotherapy (OBI) by using genetically engineered avirulent Salmonella expressing a fluorogen-activating protein (FAP). Upon binding to a fluorogen, FAP could be activated and generate fluorescence and ROS. The instant activation of persistent fluorescence was detected in tumors through bacterium-based imaging. In a colon cancer model, PDT-OBI showed an enhanced tumor inhibition effect and prolonged animal survival. Mechanically, PDT generated ROS, resulting in the killing of cancer cells and over-accumulated bacteria. The pathogen-associated molecular patterns and damage-associated molecular patterns released from the destroyed bacteria and cancer cells recruited and activated immune cells (macrophages, neutrophils, and dendritic cells), which released additional proinflammatory cytokines (TNF-α and IL-1ß); reduced anti-inflammatory cytokines (IL-10); and further enhanced immune cell infiltration in a positive-feedback manner, thus reducing bacterium-induced side effects and improving anticancer activities. This synergistic therapy has promising potential for cancer immunotherapy.

Clinical and pathological characteristics of familial melanoma with germline TERT promoter variants.

Around 10% of melanoma occurs in patients with a suspected familial predisposition. TERT promoter mutations are the most common somatic hotspot mutations in human cancers. However, only two families with germline mutations have been identified to date. We present detailed histological, clinical, and molecular pathologic analyses of affected patients and details of newly identified individuals in one of these previously reported families. TERT (NM_198253.3) Chr.5:1,295,161T>C (c.-57 T>C) promoter variants were detected in all melanoma-affected (n = 18) and one non-diseased family member. The median age at diagnosis was 30 years (n = 18, range 16-46 years, 2 unknown). While most primary melanomas arose on the upper extremities (n = 7, 21%) and were superficial spreading melanoma (SSM, n = 8, 24%), many primary melanomas also originated from non-UV-exposed mucosal (n = 2, 6%) and acral (n = 4, 12%) locations. One SSM sample harbored a Chr.5:1,295,228C>T TERT promoter mutation in addition to the germline Chr.5:1,295,161T>C variant, arguing additional pathway activation can support tumor pathogenesis. Patients treated with BRAF inhibitor and/or immune checkpoint inhibition (ICI) showed responses, although of limited duration. One mucosal melanoma harbored both a KIT copy number gain and an activating c.1727 p.Leu576Pro mutation. Following the modest response to ICI, subsequent KIT inhibitor (imatinib) therapy demonstrated an ongoing complete pathological response (currently 7 months).

Design, Synthesis, and Evaluation of Anticonvulsant Activities of New Triazolopyrimidine Derivatives.

Epilepsy, a severe brain disease affecting a large population, is treated mainly by antiepileptic drugs (AEDs). However, toxicity, intolerance, and low efficiency of the available AEDs have prompted the continual attempts in the discovery of new AEDs. In this study, we discovered a skeleton of triazolopyrimidine for the development of new AEDs. The design, synthesis, in vivo anticonvulsant activity evaluation of triazolopyrimidines (3a-3i and 6a-6e), and pyrazolopyrimidines (4a-4i) are reported. We found that most triazolopyrimidines showed anticonvulsive activity in the maximal electroshock (MES) and pentetrazol (PTZ)-induced seizure models. On the contrary, pyrazolopyrimidines (4a-4i) showed weak or no protective effects. Among the tested derivatives, compound 6d, holding a median effective dose (ED50) of 15.8 and 14.1 mg/kg against MES and PTZ-induced seizures, respectively, was found to be the most potent one. Moreover, the protection index (PI) value of 6d was significantly higher than that of the available AEDs such as valproate, carbamazepine, and diazepam. The antiepileptic efficacy of compound 6d was also observed in the 3-mercaptopropionic acid and bicuculline-induced seizure models. Antagonistic effects of flumazenil and 3-MP for the anticonvulsive activity of 6d and also the radioligand-binding assay confirmed the involvement of GABA receptors, at least benzodiazepine (BZD) receptor, in the anticonvulsant activity of compound 6d. The docking study of compounds 4e and 6d with GABAA receptor confirmed and explained their affinity to the BZD receptors.

Synthesis, Antimicrobial Activity, and Molecular Docking Studies of Aminoguanidine Derivatives Containing an Acylhydrazone Moiety.

A series of aminoguanidine derivatives containing an acylhydrazone moiety was designed based on combination principles to find new antibacterial agents with wide spectra and high activities. The synthesized compounds were characterized by spectral methods and screened for their antibacterial activity. The results showed that several compounds provided great antimicrobial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). Especially, this series of compounds presented high potency against Staphylococcus aureus, among which the derivative 3f was the most promising one with a MIC value of 4 µg/mL. Compound 3d, with a tertiary butyl group, was found to have the broad spectrum inhibitory capacity, which is effective to eight strains and showed the most potent inhibitory activity against B. subtilis CMCC 63501 with a MIC value of 4 µg/mL. What's more, compound 3d also presented high activities against four multidrug-resistant strains, which were comparable or potent to oxacillin and penicillin. Molecular docking studies revealed that H-bond interaction with amino acid residue THR81 and alkyl hydrophobic interaction with residue ALA246 of FabH were crucial for their binding force and in-vitro antimicrobial activities.

Synthesis of ring-opened derivatives of triazole-containing quinolinones and their antidepressant and anticonvulsant activities.

Based on the potent antidepressant and anticonvulsant activities of the triazole-containing quinolinones reported in our previous work, a series of ring-opened derivatives of them were designed, synthesized in this work. Their antidepressant and anticonvulsant activities were screened using the forced swimming test (FST) and the maximal electroshock seizure test (MES), respectively. The results showed that compounds 4a, 5a, 6c-6e, 6g-6i, and 7 led to significant reductions in the accumulated immobility time in the FST at a dose of 50 mg/kg. Especially compound 7 exhibited higher levels of efficacy than the reference standard fluoxetine in the FST and the tail suspension test. The results of an open field test excluded the possibility of central nervous stimulation of 7, which further confirmed its antidepressant effect. Meanwhile, compounds 6a-6i and 7 showed different degrees of anticonvulsant activity in mice at the doses range from 300 to 30 mg/kg in the MES. Among them, compounds 6e and 7 displayed the ED50 of 38.5 and 32.7 mg/kg in the MES, and TD50 of 254.6 and 245.5 mg/kg, respectively. No one showed neurotoxicity at the dose of 100 mg/kg. The preliminary investigation forward to their mechanism indicated that regulation of GABAergic system might contribute to their anticonvulsive and anti-depressive action.

Synthesis and evaluation of antimicrobial and anticancer activities of 3-phenyl-1-phenylsulfonyl pyrazoles containing an aminoguanidine moiety.

A series of 3-phenyl-1-phenylsulfonyl pyrazoles containing an aminoguanidine moiety was designed, synthesized, and evaluated for their antimicrobial and anticancer activities. The majority of the target compounds showed broad-spectrum antimicrobial activity against the tested strains, with minimum inhibitory concentration (MIC) values ranging from 2 to 64 µg/ml. Compound 5k, showing the most potent antimicrobial activity against Bacillus subtilis CMCC 63501 and multidrug-resistant Staphylococcus aureus ATCC 43300 with an MIC value of 2 µg/ml, was the most promising one in this series. It was also effective for S. aureus ATCC 33591 and multidrug-resistant Escherichia coli ATCC BAA-196 at higher concentrations. The bactericidal time-kill kinetics test illustrated that compound 5k had rapid bactericidal potential. Docking results exhibited that compound 5k showed various kinds of binding to the FabH receptor, reflecting that 5k could bind with the active site well. All compounds showed excellent activity against the investigated cancer cells, with IC50 values ranging from 1.90 to 54.53 µM. Among them, compound 5f showed prominent cytotoxicity with IC50 = 1.90 µM against A549 cells, while exhibiting lower inhibitory activity against 293T cells (IC50 = 41.72 µM), indicating that it has the potential for a good therapeutic index as an anticancer drug.

Constructed Ag NW@Bi/Al core-shell nano-architectures for high-performance flexible and transparent energy storage device.

Flexible and transparent energy storage devices (FTESDs) have recently attracted much attention for use in wearable and portable electronics. Herein, we developed an Ag nanowire (NW) @Bi/Al nanostructure as a transparent negative electrode for FTESDs. In the core-shell nanoarchitecture, the Ag NW percolation network with excellent conductivity contributes superior electron transport pathways, while the unique nanostructure provides an effective interface contact between the current collector and electroactive material. As a result, the electrode delivers a high capacity of 12.36 mF cm-2 (3.43 µA h cm-2) at 0.2 mA cm-2. With a minor addition of Al, the coulombic efficiency of the electrode remarkably increases from 65.1% to 83.9% and the capacity retention rate improves from 53.8% to 91.9% after 2000 cycles. Moreover, a maximum energy density of 319.5 µW h cm-2 and a power density of 27.5 mW cm-2 were realized by an interdigital structured device with a transmittance of 58% and a potential window of 1.6 V. This work provides a new negative electrode material for high-performance FTESDs in the next-generation integrated electronics market.

Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety.

Histamine H3 receptors (H3R) antagonists/inverse agonists are becoming a promising therapeutic approach for epilepsy. In this article, novel nonimidazole H3R antagonists/inverse agonists have been designed and synthesised via hybriding the H3R pharmacophore (aliphatic amine with propyloxy chain) with the 1,2,4-triazole moiety as anticonvulsant drugs. The majority of antagonists/inverse agonists prepared here exerted moderate to robust activities in cAMP-response element (CRE) luciferase screening assay. 1-(3-(4-(3-Phenyl-4H-1,2,4-triazol-4-yl)phenoxy)propyl)piperidine (3l) and 1-(3-(4-(3-(4-chlorophenyl)-4H-1,2,4-triazol-4-yl)phenoxy)propyl)piperidine (3m) displayed the highest H3R antagonistic activities, with IC50 values of 7.81 and 5.92 nM, respectively. Meanwhile, the compounds with higher H3R antagonistic activities exhibited protection for mice in maximal electroshock seizure (MES)-induced convulsant model. Moreover, the protection of 3m against the MES induced seizures was fully abrogated when mice were co-treated with RAMH, a CNS-penetrant H3R agonist, which suggested that the potential therapeutic effect of 3m was through H3R. These results indicate that the attempt to find new anticonvulsant among H3R antagonists/inverse agonists is practicable.

Synthesis, antibacterial and anticancer activity, and docking study of aminoguanidines containing an alkynyl moiety.

Two series of aminoguanidines containing an alkynyl moiety were designed, synthesised, and screened for antibacterial and anticancer activities. Generally, the series 3a-3j with a 1,2-diphenylethyne exhibited better antibacterial activity than the other series (6a-6k) holding 1,4-diphenylbuta-1,3-diyne moiety antibacterial activity. Most compounds in series 3a-3j showed potent growth inhibition against the tested bacterial strains, with minimum inhibitory concentration (MIC) values in the range 0.25-8 µg/mL. Compound 3g demonstrated rapid and persistent bactericidal activity at 2 × MIC. The resistance study revealed that resistance of the tested bacteria towards 3g is not easily developed. Molecular docking studies revealed that compounds 3g and 6e bind strongly to the LpxC and FabH enzymes. Moreover, excellent activity of selected compounds against the growth of cancer cell lines A549 and SGC7901 was also observed, with IC50 values in the range 0.30-4.57 µg/mL. These findings indicate that compounds containing the aminoguanidine moiety are promising candidates for the development of new antibacterial and anticancer agents.

Design, synthesis, and evaluation of anticonvulsant activities of benzoxazole derivatives containing the 1,2,4-triazolone moiety.

A novel series of benzoxazole derivatives containing 1,2,4-triazolone (5a-m) was designed. These compounds were synthesized in order to screen their anticonvulsant activities by the maximal electroshock seizure (MES) model and the subcutaneous pentylenetetrazole (sc-PTZ) seizure model in mice. The rotarod test was used to evaluate their neurotoxicities. Most of the compounds showed anti-MES activities at 100 and 300 mg/kg. Compound 5f, which showed potential anticonvulsant activity in the MES model with ED50 values of 22.0 mg/kg, was considered as the most promising one in this study. It exhibited greater safety than that of carbamazepine and valproate regarding neurotoxicity. The efficacy of compound 5f in inhibiting the tonic seizures and death induced by the convulsants 3-mercaptopropionic acid and BIC was also verified. In an enzyme-linked immunosorbent assay, compound 5f and the positive drug phenytoin significantly increased the γ-aminobutyric acid (GABA) level in the mouse brain. Further, pretreatment with an inhibitor of the GABA synthesizing enzyme dramatically raised the ED50 value of 5f in the MES model. These results confirmed that the compound 5f plays its anticonvulsive action via regulating the GABA function in the brain. Also, a docking study of the compound 5f in the benzodiazepine (BZD) binding site of the GABAA receptor confirmed possible binding of the compound 5f with BZD receptors.

Anticonvulsive activity of duloxetine: A new choice for the epileptic patients with depression.

The aim of this study was to investigate the antiepileptic effects of duloxetine in the maximal electroshock test and convulsions induced by four compounds: Pentylenetetrazole, 3-mercaptopropionic acid, thiosemicarbazide, and bicuculline. Duloxetine exhibited moderate anticonvulsive activity with an ED50 (median effective dose) of 48.21 mg/kg in the maximal electroshock test in mice. The anticonvulsive action of duloxetine was also confirmed in chemical-induced seizure tests, where this drug decreased tonic convulsions. Single administration of duloxetine (6.25-25 mg/kg) significantly increased the anticonvulsant effects of valproate, carbamazepine, and oxcarbazepine in the maximal electroshock test. Furthermore, pretreatment with thiosemicarbazide (an inhibitor of GABA synthesis enzyme) significantly increased the ED50 of duloxetine, suggesting the GABAergic system may contribute to the anticonvulsive action of duloxetine. These results support the use of duloxetine in the treatment of coexisting depression and epilepsy.

Hexagonal and Square Patterned Silver Nanowires/PEDOT:PSS Composite Grids by Screen Printing for Uniformly Transparent Heaters.

Transparent conductive films with hexagonal and square patterns were fabricated on poly(ethylene terephthalate) (PET) substrates by screen printing technology utilizing a poly(3,4-ethylenedioxythiophene) poly(styrenesulfonate) (PEDOT:PSS) and silver nanowire (Ag NWs) composite ink. The printing parameters-mesh number, printing layer, mass ratio of PEDOT:PSS to Ag NWs and pattern shape-have a significant influence on the photoelectric properties of the composite films. The screen mesh with a mesh number of 200 possesses a suitable mesh size of 74 µm for printing clear and integrated grids with high transparency. With an increase in the printing layer and a decrease in the mass ratio of PEDOT:PSS to Ag NWs, the transmittance and resistance of the printed grids both decreased. When the printing layer is 1, the transmittance and resistance are 85.6% and 2.23 kΩ for the hexagonal grid and 77.3% and 8.78 kΩ for the square grid, indicating that the more compact arrangement of square grids reduces the transmittance, and the greater number of connections of the square grid increases the resistance. Therefore, it is believed that improved photoelectric properties of transparent electrodes could be obtained by designing a printing pattern with optimized printing parameters. Additionally, the Ag NWs/PEDOT:PSS composite films with hexagonal and square patterns exhibit high transparency and good uniformity, suggesting promising applications in large-area and uniform heaters.

Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.

Thirty-six N-arylsulfonyl-3-substituted indoles were designed and synthesized by combining the N-arylsulfonylindoles with aminoguanidine, semicarbazide, and thiosemicarbazide, respectively. Their antibacterial activities were screened, and cytotoxic activities were evaluated. The results showed that aminoguanidines (6) exhibited much better antibacterial activity than semicarbazides (7) and thiosemicarbazides (8). Most compounds in series 6 showed potent inhibitory activity against the tested bacterial strains, including multidrug-resistant strains, with MIC values in the range of 1.08-23.46 µM. The cytotoxic activity of the compounds 6c, 6d, 6h, 6j, 6k and 6l was assessed in two human cancer cell lines A590 and SGC7901, and one human normal cell line HEK 293T. The results indicated that compounds selected exhibited excellent activity against the tested cancer cells with IC50 values in the range of 1.51-15.12 µM suggesting the potential of them as new antibacterial and anticancer agents. What's more, the results of resistance study revealed that resistance of the tested bacteria toward 6d is not easily developed. Molecular docking studies revealed that the aminoguanidine and arylsulfonylindole moieties played a significant role in binding the target site of E. coli FabH-CoA receptor.

[Fabrication of a Biomass-Based Hydrous Zirconium Oxide Nanocomposite for Advanced Phosphate Removal].

Wheat straws were modified by 3-chloro-2-hydroxypropyl trimethylammonium chloride (CTA) to obtain aminated wheat straw St-N'. The optimum synthetic conditions were determined to be NaOH with 30% mass fraction, CTA of 100 mL, reaction temperature of 80℃, and reaction time of 3 h, which was verified by orthogonal experiments. Nano-sized hydrous zirconium oxides (HZO) were immobilized into St-N' by an in situ precipitation method to obtain the nanocomposite St-N'-Zr. The SEM, TEM, XRD, and BET results indicated that the nano-sized HZO with 50-100 nm sizes were uniformly loaded onto the inner surface of the biomass-based carrier St-N' that was amorphous in nature. A Langmuir adsorption isotherm fitted the adsorption process well, and the maximum adsorption amount was calculated to be 33.90 mg·g-1. The optimal pH range was 1.8-6.0, displaying good removal capacity of phosphate in acidic waters. In the presence of high levels of competing anions, the phosphate adsorption still retained more than 70% of the original amount, showing the higher preference of St-N'-Zr towards phosphate than towards the commercial anion exchanger D-201. After 10 cycles of adsorption-desorption, the removal efficiency remained stable, confirming the good regeneration ability and potential application of St-N'-Zr.