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MicroRNAs (miRNAs) are small noncoding RNAs in eukaryotes. Plant endogenous miRNAs play pivotal roles in regulating plant development and defense responses. MicroRNA394 (miR394) has been reported to regulate plant development, abiotic stresses and defense responses. Previous reports showed that miR394 responded to P. infestans inoculation in potato, indicating that miR394 may be involved in defense responses. In this study, we further investigated its role in potato defense against P. infestans. Stable expression of miR394 in tobacco and potato enhances the susceptibility to P. infestans, which is accompanied with the reduced accumulation of ROS and down-regulation of the PTI (pattern-triggered immunity) marker genes. Besides well-known target StLCR, miR394 also targets StA/N-INVE, which encodes a chloroplast Alkaline/Neutral Invertases (A/N-INVE). Both StLCR and StA/N-INVE positively regulate late blight resistance, while miR394 degrades them. Interestingly, StA/N-INVE is located in the chloroplast, indicating that miR394 may manipulate chloroplast immunity. Degradation of StA/N-INVE may affect the chloroplast function and hence lead to the compromised ROS (reactive oxygen species) burst and reduced retrograde signaling from the chloroplast to the nucleus and cytoplasm. In summary, this study provides new information that miR394 targets and degrades StA/N-INVE and StLCR, which are positive regulators, to enhance potato susceptibility to P. infestans. [ABSTRACT FROM AUTHOR]

SARS‐CoV‐2 has evolved into a panel of variants of concern (VOCs) and constituted a sustained threat to global health. The wildtype (WT) SARS‐CoV‐2 isolates fail to infect mice, while the Beta variant, one of the VOCs, has acquired the capability to infect standard laboratory mice, raising a spreading risk of SARS‐CoV‐2 from humans to mice. However, the infectivity and pathogenicity of other VOCs in mice remain not fully understood. In this study, we systematically investigated the infectivity and pathogenicity of three VOCs, Alpha, Beta, and Delta, in mice in comparison with two well‐understood SARS‐CoV‐2 mouse‐adapted strains, MASCp6 and MASCp36, sharing key mutations in the receptor‐binding domain (RBD) with Alpha or Beta, respectively. Our results showed that the Beta variant had the strongest infectivity and pathogenicity among the three VOCs, while the Delta variant only caused limited replication and mild pathogenic changes in the mouse lung, which is much weaker than what the Alpha variant did. Meanwhile, Alpha showed comparable infectivity in lungs in comparison with MASCp6, and Beta only showed slightly lower infectivity in lungs when compared with MASCp36. These results indicated that all three VOCs have acquired the capability to infect mice, highlighting the ongoing spillover risk of SARS‐CoV‐2 from humans to mice during the continued evolution of SARS‐CoV‐2, and that the key amino acid mutations in the RBD of mouse‐adapted strains may be referenced as an early‐warning indicator for predicting the spillover risk of newly emerging SARS‐CoV‐2 variants. [ABSTRACT FROM AUTHOR]

Adsorption and purification of biological molecules with pharmacological functions over advanced adsorption materials are always a concern. In this work, manganese oxide octahedral molecular sieve (OMS‐2)‐modified ZrO2 nanocomposites (ZrO2‐OMS‐2) were fabricated and their adsorption performance towards rutin from aqueous solution was investigated. As‐obtained nanocomposites were fully characterized by N2 adsorption/desorption isothermal, ICP‐AES, XRD, SEM and TEM, which indicates that OMS‐2‐modification significantly promoted the textural properties of the nanocomposites. 10 mol% Mn amount for ZrO2‐OMS‐2 showed the optimal adsorption capacity for rutin due to the enhanced specific surface aera (104 m2/g) and better ZrO2 dispersion. The adsorption rate of 85 % was realized over 10 mg of the optimal adsorbent and the desorption rate could reach nearly 100 % in 0.2 % TFA/methanol solution. Moreover, the adsorbent could be reused for at least 3 times. The adsorption behavior was fitted the pseudo‐second‐order model and Freundlich model. Kinetic and thermodynamic studies suggested that an endothermic chemosorption from Lewis acid‐base paring on the surface of ZrO2‐OMS‐2 was responsible for the good adsorption. This work shows the positive effect of manganese oxide‐modification for ZrO2 during adsorption process and the potential of ZrO2‐based nanocomposites being adsorbents. [ABSTRACT FROM AUTHOR]

The intelligent design or development of dual‐functional catalysts using non‐precious metals especially for the oxygen evolution reaction (OER) in sustainable energy systems and degradation of organic pollutants is still a difficult and a significant challenge. Furthermore, the development of these catalysts is of great importance in terms of energy security and solution of the environmental problems. To meet these requirements, herein, we describe the synthesis of a Ni‐ion doped Birnessite@Cryptomelane (Ni2+/B@Cr) hybrid structure as a bifunctional efficient catalyst for the OER in neutral media and degradation of dye pollutants. The Ni2+/B@Cr catalyst exhibited a sharp onset potential at 390 mV (vs. RHE) and achieved a current density of 1 mA cm−2 at a low ƞ of 430 mV with a Tafel slope of ~96 mV dec−1. The results of electrochemical impedance spectroscopy (EIS) studies indicated that Ni intercalation into birnessite layer and heterostructure of the hybrid electrocatalyst Ni2+/B@Cr increased the conductivity by lowering the resistance of charge transfer (Rct = 4.82 Ω) and oxygen evolution processes (ROER = 4.13 Ω). The durability assay identified Ni2+/B@Cr as stable electrocatalyst with 10% loss of activity after long‐term stability tests (10 h, under 500‐mV overpotential). In addition, the Ni2+/B@Cr achieved high (86.67 s−1 g−1) and rapid (173 s) catalytic performance for the reduction of methylene blue (MB). Overall, this paper presents a low‐cost production strategy for the design of highly efficient bifunctional catalysts, offering boosted electrocatalytic and degradation performance for water oxidation and organic dye contamination, respectively. [ABSTRACT FROM AUTHOR]

Aims: Single‐dose pharmacokinetic (PK) studies in healthy subjects have been the design of choice for bioequivalence determination for decades. This preference has been recently extended to PK similarity studies of proposed biosimilars. However, PK similarity studies can be complicated by the effect of immunogenicity response on drug disposition. The impact is exacerbated when there is an imbalance in host‐specific immunological characteristics of subjects between the test and reference groups. Such complications remain poorly understood. The purpose of this communication is to show that the impact of immunogenicity response on PK similarity determination can be critical, using adalimumab as an example. Methods: Data for adalimumab concentrations and immunogenicity response over 10 weeks were obtained from 133 healthy subjects receiving a 40 mg dose of Humira® in a PK similarity study. Also, a population PK model with a mechanistic construct for delineating the interplay between adalimumab disposition and antidrug antibodies response was utilized to estimate via simulation the probability that a PK similarity study would fail in typical study settings. Results: The simulations showed that the immunogenicity response can have a profound impact on the outcome of PK similarity determination. As such, the probability of failing to achieve the similarity conclusion increased to 51.9%, from 13.8% in the absence of immunogenicity response. Conclusion: This study provides a model‐based framework for better understanding of how a PK similarity study can be optimally designed and for interpretation of the outcome of PK similarity determination when the drug disposition is affected in the presence of immunogenicity response. [ABSTRACT FROM AUTHOR]

A background calibration technique for time-interleaved analogue-to-digital converter (TIADC) over Sub-Nyquist frequency timing mismatch is proposed. When the input signal only satisfies the Nyquist sampling theorem of the overall TIADC rather than sub-ADC, both directions of estimation based on correlation and compensation based on differentiator may be opposite to the actual value, which results in a failure calibration. In this Letter, the authors propose a calibration direction correction algorithm which can detect and correct the calibration direction and assure an effective calibration in the whole Nyquist frequency of TIADC. Simulation results show that, for a four-channel 12-bit 1 GS/s TIADC, with $f_{\rm in}/f_{\rm s}=0.45$fin/fs=0.45 , signal to noise and distortion ratio (SNDR) is improved from 30.1 to 73.2 dB. [ABSTRACT FROM AUTHOR]

Here Fe‐doped on manganese oxide octahedral molecular sieve (Fe‐OMS‐2) has been successfully synthesized and used as an efficient catalyst for acid orange 7 degradation in the presence of peroxymonosulfate in aqueous solutions. Then Fe‐OMS‐2 has been characterized by inductively coupled plasma optical emission spectrometry, N2 adsorption‐desorption isotherms, transmission electron microscopy, X‐ray diffraction and X‐ray photoelectron spectroscopy. Fe‐OMS‐2 catalyst exhibits higher efficiency for the degradation of acid orange 7 in comparison with OMS‐2. Then various amounts of Fe‐OMS‐2, AO7 concentration and PMS concentration have also been tested for the degradation of acid orange 7. In addition, the catalyst Fe‐OMS‐2 has been successfully reused 5 times without significant decrease in catalytic activity by simple filtration. [ABSTRACT FROM AUTHOR]

Two different synthetic strategies have been employed, wet‐impregnation vs. pre‐incorporation, to control the localization of Cu from interior to external surface of α‐MnO2 octahedral molecular sieves (OMS‐2). CuOx/OMS‐2 exhibits dispersed granular CuOx (x=1 or 0.5) attached and located at the external surface of OMS‐2, whereas Cu‐OMS‐2 shows Cu location within OMS‐2. These results indicate that the catalyst CuOx/OMS‐2 is significantly more active than Cu‐OMS‐2 and OMS‐2 itself in the degradation of organic pollutants. In addition, the catalyst CuOx/OMS‐2 has been successfully reused 10 times without significant decrease in catalytic activity. This work highlights the role of the catalyst location in molecular sieve on the catalytic efficiency of the metal and rationalizes the catalyst optimization in nanocatalyst engineering. [ABSTRACT FROM AUTHOR]

On 3 January 2019, the Chang'e‐4 (CE‐4) touched down on the Von Karman crater located inside the South Pole‐Aitken Basin, providing for the first time the opportunity for in situ measurements of the lunar regolith at the farside of the Moon. The CE‐4 ground penetrating radar reveals that fine‐grained regolith, coarse impact ejecta, and fractured bedrocks lie beneath the exploration path of the Yutu‐2 rover. The variations of regolith permittivity with depth and the radargrams indicate that the CE‐4 site has a fine‐grained regolith layer thickness of 11.1 m, which is about 1.3–3 times higher than the in situ measurement results at the Apollo and Chang'e‐3 (CE‐3) sites except for Apollo 16, possibly due to a faster weathering rate of ejecta deposits compared with coherent basalt substrates. The penetration depth of CE‐4 is about 2.85 times (in terms of round‐way delay) deeper than CE‐3, probably due to the differences in abundances of ilmenite and rocks in the regolith. Plain Language Summary: CE‐4 is the first craft in history to land on the lunar farside. Its rover is equipped with a ground‐penetrating radar (GPR), the same as the one mounted on the CE‐3 rover, which uses pulses of electromagnetic energy to reveal the subsurface structure and properties, especially useful to study the lunar soil layer ("regolith") that mantles most of the lunar surface. The results from the GPR show that the thickness of the regolith at the CE‐4 site is 1.3–3 times higher than the in situ measurements at the Apollo 11,12,14,15, 17, and CE‐3 sites even though the ages of the surfaces of Apollo 11 and Apollo 17 are thought to be comparable with that of the CE‐4 site. It implies a faster regolith growth speed at the CE‐4 site. The mineral mix of the surface materials at the CE‐4 site is different from that at the CE‐3: this results in less radar signal attenuation, thus increasing the detection limit up to the depth of 35 m, 2.85 times deeper than the CE‐3. Key Points: The LPR measurements at the CE‐4 landing site reveal that the shallow structure comprises of fine‐grained regolith, coarse impact ejecta, and fractured bedrocksThe CE‐4 landing site has a thicker regolith layer (~11 m) compared with the CE‐3, hinting at a longer weathering historyA lower abundance of ilmenite and rocks in the regolith at the CE‐4 site allows 2.85 times the penetration depth compared with CE‐3 site [ABSTRACT FROM AUTHOR]

Cryptomelane‐type manganese oxide (OMS‐2) was synthesized successfully using urea hydrogen peroxide (urea⋅H2O2) as the reductant in an acidic buffer solution. As‐prepared crystalline material was fully characterized by XRD, BET, XPS, SEM and HRTEM. The results demonstrate that OMS‐2 has nanofiber with short nanorod morphologies, very rich oxygen vacancy defects and more exposed crystal facets compared with ones synthesized with other H2O2‐containing reductants. These unique properties make nanostructural OMS‐2 an excellent heterogeneous catalyst in aerobic oxidation reactions, such as selective oxidation of mercaptan and oxygenation of alkylarenes. [ABSTRACT FROM AUTHOR]

Abstract: A concise and practical approach for synthesis of 2,5‐disubstituted oxazole has been developed via a TsOH(p‐Methylbenzene sulfonic acid)/I2‐mediated tandem dehydrogenation oxidative cyclization of phenylacetylene and benzylamine. Desired products in high yields have been obtained. [ABSTRACT FROM AUTHOR]

Bococizumab (RN316/PF-04950615), a humanized monoclonal antibody, binds to secreted proprotein convertase subtilisin/kexin type 9 (PCSK9) and prevents its downregulation of low-density lipoprotein receptor, leading to improved clearance and reduction of low-density lipoprotein cholesterol (LDL-C) in plasma. A mechanism-based drug-target binding model was developed, accounting for bococizumab, PCSK9, and LDL-C concentrations and the effects of concomitant administration of statins. This model was utilized to better understand the pharmacokinetic/pharmacodynamic (PK/PD) data obtained from 3 phase 1 and 2 phase 2a clinical studies. First, simulations performed with this model demonstrated that the conventional method of the area-under-the-curve ratio for bioavailability determination underestimated the subcutaneous bioavailability of bococizumab due to its target-mediated disposition. Second, a covariate model component for statin effects on bococizumab PK/PD was characterized, including a description of the decreased baseline LDL-C, increased baseline PCSK9, and increased LDL-C lowering with concomitant use of statins. Last, the impact of the dosing regimens with and without a dose holiday on bococizumab's LDL-C-lowering effectiveness was shown to be predictable due to the well-characterized PK-PD relationship. [ABSTRACT FROM AUTHOR]

Aims To evaluate potential differences between PF-05280586 and rituximab sourced from the European Union (rituximab-EU) and USA (rituximab-US) in clinical response (Disease Activity Score in 28 Joints [DAS28] and American College of Rheumatology [ACR] criteria), as part of the overall biosimilarity assessment of PF-05280586. Methods A randomised, double-blind, pharmacokinetic similarity trial was conducted in patients with active rheumatoid arthritis refractory to anti-tumour necrosis factor therapy on a background of methotrexate. Patients were treated with 1000 mg of PF-05280586, rituximab-EU or rituximab-US on days 1 and 15 and followed over 24 weeks for pharmacokinetic, clinical response and safety assessments. Key secondary end points were the areas under effect curves for DAS28 and ACR responses. Mean differences in areas under effect curves were compared against respective reference ranges established by observed rituximab-EU and rituximab-US responses using longitudinal nonlinear mixed effects models. Results The analysis included 214 patients. Demographics were similar across groups with exceptions in some baseline disease characteristics. Baseline imbalances and group-to-group variation were accounted for by covariate effects in each model. Predictions from the DAS28 and ACR models tracked the central tendency and distribution of observations well. No point estimates of mean differences were outside the reference range for DAS28 or ACR scores. The probabilities that the predicted differences between PF-05280586 vs. rituximab-EU or rituximab-US lie outside the reference ranges were low. Conclusions No clinically meaningful differences were detected in DAS28 or ACR response between PF-05280586 and rituximab-EU or rituximab-US as the differences were within the pre-specified reference ranges. TRIAL REGISTRATION Number: NCT01526057. [ABSTRACT FROM AUTHOR]

Aims Pharmacokinetic (PK) similarity was assessed among PF-05280586 (a proposed biosimilar) vs. rituximab sourced from the European Union (rituximab-EU) and the United States (rituximab-US). Pharmacodynamics (PD), overall safety and immunogenicity were also evaluated. Methods Patients with active rheumatoid arthritis on a background of methotrexate and inadequate response to one or more tumour necrosis factor antagonist therapies were randomized to intravenous PF-05280586, rituximab-EU or rituximab-US 1000 mg doses on study days 1 and 15. Results A total of 220 patients were randomized to receive study treatment as assigned. Of these, 198 met per-protocol population criteria for inclusion in the PK data analysis. PF-05280586, rituximab-EU and rituximab-US exhibited similar PK profiles following administration of assigned study drug on days 1 and 15. The 90% confidence intervals of test-to-reference ratios for Cmax, AUCT, AUC0-∞ and AUC2-week were within the bioequivalence margin of 80.00-125.00% for comparisons of PF-05280586 with rituximab-EU, PF-05280586 with rituximab-US, and rituximab-EU with rituximab-US. All treatments resulted in a rapid and profound reduction in CD19+ B cells and sustained profound B cell suppression up to week 25. The incidence of antidrug antibody (ADA) response ( n = 7, 10 and 9 for PF-05280586, rituximab-EU and rituximab-US, respectively), time to ADA emergence and ADA titres were similar across treatments. None of the ADA-positive samples was positive for neutralizing activity. No clinically meaningful differences in adverse events were identified. Conclusions The study demonstrated PK similarity among PF-05280586, rituximab-EU and rituximab-US. In addition, all treatments showed comparable CD19+ B cell depletion PD responses, as well as safety and immunogenicity profiles. [ABSTRACT FROM AUTHOR]

Cathelicidins are pleiotropic antimicrobial peptides largely described for innate antimicrobial defenses and, more recently, immunomodulation. They are shown to modulate a variety of immune or nonimmune host cell responses. However, how cathelicidins are expressed by β cells and modulate β-cell functions under steady-state or proinflammatory conditions are unknown. We find that cathelicidin-related antimicrobial peptide (CRAMP) is constitutively expressed by rat insulinoma β-cell clone INS-1 832/13. CRAMP expression is inducible by butyrate or phenylbutyric acid and its secretion triggered upon inflammatory challenges by IL-1β or LPS. CRAMP promotes β-cell survival in vitro via the epidermal growth factor receptor (EGFR) and by modulating expression of antiapoptotic Bcl-2 family proteins: p-Bad, Bcl-2, and Bcl-xL. Also via EGFR, CRAMP stimulates glucose-stimulated insulin secretion ex vivo by rat islets. A similar effect is observed in diabetes-prone nonobese diabetic (NOD) mice. Additional investigation under inflammatory conditions reveals that CRAMP modulates inflammatory responses and β-cell apoptosis, as measured by prostaglandin E2 production, cyclooxygenases (COXs), and caspase activation. Finally, CRAMP-deficient cnlp-/- mice exhibit defective insulin secretion, and administration of CRAMP to prediabetic NOD mice improves blood glucose clearance upon glucose challenge. Our finding suggests that cathelicidins positively regulate β-cell functions and may be potentially used for intervening β-cell dysfunction-associated diseases. [ABSTRACT FROM AUTHOR]

This study evaluated the performance of an algal membrane bioreactor (A-MBR) for secondary wastewater effluent polishing and determined the membrane fouling behavior and dominance of algae in the A-MBR. The continuous flow A-MBR (effective volume = 7.2 L) was operated with low biomass wastage for more than 180 days, resulting in an average algal mixed liquor suspended solid concentration of 4922 mg/L. At the influent concentrations of 43 mg/L COD, 1.6 mg/L total phosphorus (TP), and 11.8 mg/L total nitrogen (TN), the effluent COD, TP and TN concentrations were 26 ± 6 mg/L, 0.7 ± 0.3 mg/L, and 9.6 ± 1.2 mg/L, respectively. High-density algae cultivation facilitated P adsorption and chemical precipitation. However, the TN removal efficiency was only 14% because of low biomass wastage. Although bacteria represented less than 2% of the total biomass in the AMBR, bacterial growth in the secondary wastewater effluent accelerated membrane fouling. [ABSTRACT FROM AUTHOR]

An efficient methodology to access a library of 1,2,4,5-tetrasubstituted imidazoles from a broad range of amidines and α,β-unsaturated aldehydes/ketones via a C(sp2)-H amination has been developed. This method represents a new and simple way to prepare highly substituted imidazoles from easily available starting materials, inexpensive catalysts, and with good functional group tolerance in good to excellent yields. [ABSTRACT FROM AUTHOR]

The plant-specific WUSCHEL-related HOMEOBOX (WOX) transcription factors play important roles in key developmental processes, but knowledge regarding functional characterization ofWOX genes in poplar remains limited. To reveal genes and signaling pathways associated with adventitious rooting in poplar, here we isolated and characterized two WOX genes through the rapid amplification of cDNA ends (RACE), sequence aligning, expression profiling, protoplast transfection and poplar transformation. Detailed information about the sequence similarity, structural features, evolutionary relationships, expression patterns and subcellular localization of the two genes were revealed. Overexpression of either PeWOX11a or PeWOX11b not only increased the number of adventitious roots on the cuttings but also induced ectopic roots in the aerial parts of transgenic poplars. Meanwhile, their overexpression in transgenic poplars affected axillary bud and leaf development. These results suggest that PeWOX11a and PeWOX11b were involved in multiple developmental processes of poplar, especially in adventitious root formation. Our results provide new insights into themolecularmechanisms underlying adventitious root formation of poplar. [ABSTRACT FROM AUTHOR]

ABSTRACT The polymerization strategy plays a vital role in the preparation of functional microspheres. In this work, fluorescent poly (styrene- co-glycidyl methacrylate) (PSt-GMA) microspheres were synthesized via one-stage and two-stage dispersion polymerization with 4-Bis(5-phenyl-1,3-oxazol-2-yl)benzene (POPOP) as fluorescence agent. SEM and DLS were adopted to characterize the properties of prepared microspheres. The UV-vis and fluorescence spectroscopy were used to analyze the mechanisms of two-stage dispersion polymerization. The experimental results showed that the size distribution and fluorescence intensity of prepared microspheres could be improved by two-stage dispersion polymerization compared to one-stage dispersion polymerization. In addition, according to UV-vis, the interactions between POPOP and Poly (N-vinyl pyrrolidone) (PVP) as well as POPOP and Glycidyl methacrylate (GMA) could affect the particle size and its distribution. UV-vis and fluorescence spectra implied that the POPOP existed outside of the particle's core via two-stage strategy. The monomer conversion of styrene was similar at the beginning of reaction; however, the monomer conversion of styrene by two-stage strategy was higher than that of by one-stage strategy. In a word, two-stage dispersion polymerization could prepare fluorescent microspheres with the monodispersion micrometer-size and high quality. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015, 132, 41927. [ABSTRACT FROM AUTHOR]

An efficient method for the synthesis of 3-alkylated indoles is described. The oxidative cross-coupling reaction of diphenylmethane derivatives with indoles at the C-3 position was achieved employing the N,N-dimethylcarbamoyl moiety as an auxiliary group in the presence of iron(II) chloride (FeCl2) and 2,3-dichloro-5,6-dicyanoquinone (DDQ). [ABSTRACT FROM AUTHOR]

Aims The pharmacokinetic ( PK) similarity between PF-05280014, a proposed trastuzumab biosimilar, trastuzumab sourced from European Union (trastuzumab- EU) or from United States (trastuzumab- US) was evaluated. Safety and immunogenicity were also assessed. Methods In this phase 1, double-blind trial ( NCT01603264), 105 healthy male volunteers were randomized 1:1:1 to receive a single 6 mg kg−1 intravenous dose of PF-05280014, trastuzumab- EU, or trastuzumab- US, and evaluated for 70 days. Drug concentration-time data were analyzed by non-compartmental methods. PK similarity for the comparisons of PF-05280014 to each of trastuzumab- EU and trastuzumab- US, and trastuzumab- EU to trastuzumab- US were determined using the standard 80.00% to 125.00% bioequivalence criteria. Results Baseline demographics for the 101 subjects evaluable for PK were similar across all arms. The three products exhibited similar PK profiles with target-mediated disposition. The 90% CIs for the ratios of Cmax [ABSTRACT FROM AUTHOR]

An efficient and simple protocol for N-bromosuccinimide (NBS)-mediated styrenes using amides as the nitrenoid source has been developed. This affords desired products in moderate to good yields without using transition metal catalyst under very mild reaction condition. [ABSTRACT FROM AUTHOR]

An efficient one-pot of benzimidazole and benzotriazole from carbonyl compounds and tosylhydrazide has been accomplished via copper powder-catalyzed N-H bond insertion affording N-alkylated products in good yields. The reaction can tolerate a wide range of carbonyl compounds, such as aryl, alkyl, heterocyclic and α,β-unsaturated ketones, and aldehydes. [ABSTRACT FROM AUTHOR]

ABSTRACT A guanidine-based oligomer grafted with a reactive cationic surfactant was designed and synthesized through Michael addition in an attempt to combine its antibacterial and emulsification properties. This was also an excellent and efficient strategy for preparing more kinds of guanidine derivatives. Fourier transform infrared spectroscopy, 1H-NMR, and 13C-NMR showed that the guanidine-based oligomer grafted with reactive cationic surfactant was synthesized successfully. The antimicrobial activity and antimicrobial mechanism were investigated with several approaches. The antimicrobial activity results indicated that the introduction of a cationic surfactant into the guanidine-based oligomer effectively raised the antimicrobial activity and showed a synergistic effect. The UV absorption at 260 nm was used to detect the dynamic antimicrobial process of the modified guanidine oligomer. Further, the results of scanning electron microscopy and atomic force microscopy implied that the antimicrobial mechanism of the modified guanidine oligomer changed the permeability of the cell membrane of the bacteria and caused the leakage of intracellular components of the Escherichia coli cells. © 2013 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 130: 3489-3497, 2013 [ABSTRACT FROM AUTHOR]

ABSTRACT The purpose of this study was to assess whether autologous uncultured bone marrow-derived mononuclear cells (BMMNCs) combined with modified cannulated screw would accelerate the healing of canine femoral neck fracture. BMMNCs were encapsulated within fibrin glue (FG) and implanted into the fractured femoral neck via modified cannulated screw in experiment group, and the control group was treated by modified cannulated screw. Gross observation, radiological examination, histological analysis, and blood vessel microdensity counting were used to compare bone healing of each group at 1, 2, and 3 months. FG was confirmed as an ideal cell-delivery vehicle for BMMNCs proliferation and differentiation in vitro testing. In vivo animal testing, faster new bone formation and fracture healing were confirmed by gross observation, radiological examination, histological analysis in experimental group than in control group at all times points. The blood vessel microdensity counting increased gradually both in the experimental group and control group, but was more obviously in experimental group at 3 months ( p < 0.01). These data suggest that autologous BMMNCs combined with modified cannulated screw treatment is an effective therapy for femoral neck fracture and thus, may be an option for clinical applications. © 2013 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 31:1302-1307, 2013 [ABSTRACT FROM AUTHOR]

Arenes and electron‐deficient olefins can be oxidatively coupled through a biomimetic Pd(OAc)2‐catalyzed transformation. CH activation of the arene partner is effected under reaction conditions of low catalyst loading, normal oxygen pressure, and using p‐benzoquinone and iron phthalocyanine as electron‐transfer mediators (ETMs). By controlling catalyst loading, the reaction can be made selective for either mono‐ or diarylation. [ABSTRACT FROM AUTHOR]

Children with gastroesophageal reflux disease (GERD) may benefit from gastric acid suppression with proton pump inhibitors such as pantoprazole. Effective treatment with pantoprazole requires correct dosing and understanding of the drug’s kinetic profile in children. The aim of these studies was to characterize the pharmacokinetic (PK) profile of single and multiple doses of pantoprazole delayed-release tablets in pediatric patients with GERD aged 6 to 11 years (study 1) and 12 to 16 years (study 2). Patients were randomly assigned to receive pantoprazole 20 or 40 mg once daily. Plasma pantoprazole concentrations were obtained at intervals through 12 hours after the single dose and at 2 and 4 hours after multiple doses for PK evaluation. PK parameters were derived by standard noncompartmental methods and examined as a function of both drug dose and patient age. Safety was also monitored. Pantoprazole PK was dose independent (when dose normalized) and similar to PK reported from adult studies. There was no evidence of accumulation with multiple dosing or reports of serious drug-associated adverse events. In children aged 6 to 16 years with GERD, currently available pantoprazole delayed-release tablets can be used to provide systemic exposure similar to that in adults. [ABSTRACT FROM PUBLISHER]

J Oral Pathol Med (2010) 39: 63–68 Background: The chemokine SDF-1 and its receptor CXCR4 play active role in the metastasis and proliferation of several malignancies. Methods: In this study, we used an immunohistochemical technique in 91 specimens of oral squamous cell carcinoma (SCC), and flow cytometry technique in oral SCC cell line, and then evaluated the role of proliferation of CXCR4 using MTT assay in oral SCC cell line. Results: The expression of CXCR4 in 91 specimens of oral SCC was 62.6% and in oral SCC cell line was 68.6%. There was a significant association between the expression of CXCR4 and lymph node metastasis ( P = 0.012), tumor size ( P = 0.01), UICC stage ( P = 0.016), tumor histology grade ( P < 0.001). SDF-1 stimulated proliferation of oral SCC cell and CXCR4 neutralization by monoclonal antibodies decreased proliferation. Conclusions: Our results suggest that CXCR4 might be a novel biomarker to evaluate the biological behavior of oral SCC. CXCR4 inhibitors or antagonists might be potential anticancer agents to suppress tumor proliferation. [ABSTRACT FROM AUTHOR]

Abstract: Objective: To evaluate the efficacy and safety of oxycodone hydrochloride controlled-release (CR) tablets (Oxycontin®, Mundipharma International Limited, Cambridge, UK), 5 mg, 10 mg, 20 mg, and 40 mg in relieving moderate to severe non-cancer pain. Method: Two multi-center, open-label, prospective, self-controlled clinical trial, used identical protocols. All the subjects were patients with moderate to severe non-cancer pain. The clinical data were collected in the natural course of clinical treatment. Results: Treatments with oxycodone CR tablets was associated with fast onset on pain relief; 85.2% of patients in study 1 and 91.8% of patients in study 2 achieved pain relief within 1 hour of drug administration. Clinical efficacy: Both studies demonstrated that oxycodone CR tablets showed good clinical efficacy for relieving both moderate and severe non-cancer pain. Patients experienced sustained pain relief from the first week of treatment. Patients in both study 1 and study 2 experienced a dramatic pain score reduction (as assessed by VAS) after the first week of treatment. Safety profile: During oxycodone CR treatment, use of concomitant medications decreased significantly. A few patients developed ADRs in the first week, which decreased significantly as the treatment continued. Constipation was the most common ADR in the first week, which decreased to 10% of patients from the second week of treatment. Conclusion: Oxycodone CR tablets demonstrated fast onset of pain control and superior efficacy for relieving both moderate and severe non-cancer pain, as well as significant reductions in the number of concomitant medications, demonstrating a good safety profile. [Copyright &y& Elsevier]

Aim: Arteriovenous fistula (AVF) is usually surgically created in a patient’s upper extremity to provide adequate blood flow during haemodialysis. Blood flow distal to an AVF is altered and theoretically could change pulse oximetry (SpO2) reading, systemic blood pressure and skin temperature. The authors conducted a prospective case–control study to measure changes in these parameters in the upper extremity of patients who have had an AVF. Methods: In patients with an upper extremity AVF, the authors conducted a prospective case–control study using the patient’s own non-AVF upper extremity as the control. The authors evaluated other factors that may have influenced blood flow changes distal to an AV fistula like gender, presence of AVF aneurysm, peripheral vascular disease, diabetes mellitus and vasodilator therapy. Results: Thirty patients were enrolled, skin temperature and blood pressure were significantly altered in the hand distal to the AVF, but there was no significant change in the SpO2. Conclusion: An upper extremity AVF alters blood pressure and temperature measurements when compared with the contralateral non-AVF side, but there is no difference in SpO2 provided an adequate signal quality is detected. [ABSTRACT FROM AUTHOR]

We developed and evaluated simple sequence repeat (SSR) markers derived from expressed sequence tags (ESTs) of Liriodendron tulipifera. Characteristics of 15 EST-SSR loci were investigated using 33 L. tulipifera individuals. The number of alleles per locus ranged from two to five. The expected and observed heterozygosities ranged from 0.216 to 0.751 and from 0.182 to 0.97, respectively. These loci were further tested for their cross-species transferability to Liriodendron Chinense. Because of their high level of polymorphism and transferability, our 15 single-locus EST-SSR markers will be valuable tools for research on mating system, population genetics and systemic evolution of Liriodendron. [ABSTRACT FROM AUTHOR]

CuCl2 supported on TiO2 nanopowder efficiently catalyzes the aerobic oxidative cyclization reaction of 2-aminopyridine derivatives and ketones to give imidazopyridines. [ABSTRACT FROM AUTHOR]

A mixed Cu/Zn-catalyst supported on Al2O3-TiO2 is used as catalyst for the cyclocondensation of 2-aminopyridines or amidine hydrochlorides with nitriles to give the corresponding 1,2,4-triazoles. [ABSTRACT FROM AUTHOR]

An efficient and convenient protocol for the synthesis of N-alkylated benzimidazoles and benzotriazoles using carbonyl compounds as alkylating agents is developed. [ABSTRACT FROM AUTHOR]

The title reaction proceeds with a relatively low catalyst loading. [ABSTRACT FROM AUTHOR]