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We have designed and synthesized two novel pyridyl‐quinoxaline ligands, L1 and L2, as well as twelve cobalt, nickel, and copper complexes, 1–6 and 1 a–6 a. Unexpectedly, high regularities in the synthesis of both ligands and complexes were found. Further X‐ray diffraction analyses revealed that the two ligands had similar geometrical configurations, and the structures of twelve complexes were regularly divided into two categories: binuclear and mononuclear, which would be beneficial for elucidating structure‐activity relationships of metal catalysts. In addition, the experimental results showed significant variations in the catalytic performance of methyl methacrylate polymerization with different catalysts. Under the optimum reaction conditions, the mononuclear copper complex 3 a displayed a remarkably high catalytic activity of 2.76×105 g ⋅ mol−1 h−1, generating Poly(methyl methacrylate) with molecular weight of Mn=8.55×105 g ⋅ mol−1 and molecular weight distribution of Đ=1.67.This outcome suggested that copper had the potential to serve as a promising catalytic metal center. [ABSTRACT FROM AUTHOR]

A balance between the development and suppression of inflammation can always be found in the body. When this balance is disturbed, a strong inflammatory response can damage the body. It sometimes is necessary to use drugs with a significant anti-inflammatory effect, such as nonsteroidal anti-inflammatory drugs and steroid hormones, to control inflammation in the body. However, the existing anti-inflammatory drugs have many adverse effects, which can be deadly in severe cases, making research into new safer and more effective anti-inflammatory drugs necessary. Currently, numerous types of natural products with anti-inflammatory activity and distinct structural features are available, and these natural products have great potential for the development of novel anti-inflammatory drugs. This review summarizes 260 natural products and their derivatives with anti-inflammatory activities in the last two decades, classified by their active ingredients, and focuses on their structure–activity relationships in anti-inflammation to lay the foundation for subsequent new drug development. We also elucidate the mechanisms and pathways of natural products that exert anti-inflammatory effects via network pharmacology predictions, providing direction for identifying subsequent targets of anti-inflammatory natural products. [ABSTRACT FROM AUTHOR]

This study conducted pin disc friction and wear performance tests on polyethylene-lined oil pipes and four types of centralizing materials (45# steel, nylon, polytetrafluoroethylene (PTFE), and surface alloy coating) in oil fields. The friction coefficient and wear rate were tested, and the wear mechanism was analyzed using scanning electron microscopy (SEM) and three-dimensional confocal microscopy. Using a combination of experimental testing analysis and theoretical research, a comprehensive evaluation of the current wellbore centering and anti-wear technology for oil was conducted. The experimental results indicate that the usage limit of polyethylene-lined oil pipes is 400 N, and compared to metal oil pipe materials, the wear rate of both stabilizing material and tubing material is lower, indicating that it has a certain service life. From the perspective of testing load, taking into account the factors of friction coefficient and wear rate, the recommended sequence of straightening material for polyethylene lined oil pipes is (1) surface alloy coating, (2) nylon, (3) PTFE, and (4) 45# steel. [ABSTRACT FROM AUTHOR]

Whether the hole is in safe state is quite essential in the construction technology of trenchless directional horizontal hole. Many consequences caused by hole wall instability will seriously affect the normal construction of trenchless engineering. It is proved by theory and practice that when the underground excavation passes through the natural cracks in the stratum, the instability issue of the hole wall is serious. It is necessary to select mud with appropriate density to inject into the hole for auxiliary drilling, so as to ensure that no collapse or slurry leakage happens within the hole. In this paper, aiming at the trajectory optimization of trenchless horizontal well in fractured formation, a mechanical model is built, and the optimal drilling direction of horizontal well under specific working conditions is given with the help of programming calculation. [ABSTRACT FROM AUTHOR]

The in-situ stress information underground is of crucial importance for drilling and reservoir development. As the cost of direct stress measurements is high and only limited information can be obtained, the application of wellbore imaging devices made it possible to interpret the local stress state more economical. Breakout azimuths revealed by well logs are widely used to determine principal stress directions in traditional method, however strength anisotropic related to bedding planes may greatly affect breakout azimuth, width and depth, which can result in misleading for in-situ stress interpretations. Based on weak-plane borehole stability model and Mogi-Coulomb matrix strength criterion, we analyzed the relationship between in-situ stress and breakout geometry (azimuth, width and depth) both in isotropic and anisotropic formation. The results show that the azimuth of breakout is controlled by weak plane's azimuth, while steep dipping bedding plane widen the breakout and make it extending into rocks. For specific strata with determined property, breakout geometry will change regularly with the increase of the principal stress ratio. A breakout accident observed in well WFSD-2 help to illustrate the method and the magnitude of the maximum horizontal principal stress is determined. [ABSTRACT FROM AUTHOR]

For wireless communications using linear large-scale antenna arrays, we define a receiving coordinate system and parameterization strategy to facilitate the study of the impact of three-dimensional position and rotation of the arrays on the achievable spatial degrees of freedom (DoF) in line-of-sight (LOS) channels. An analytical framework based on spatial bandwidth analysis is developed, under which three elementary problems corresponding to three basic orthogonal receiving directions are investigated. For each of them, accurate, simple, and interpretable closed-form approximations for the achievable spatial DoF are derived, and the spatial region where a sufficient amount of spatial DoF is expected available is determined. The expressions can easily be integrated into large-scale system-level simulations. Some interesting and surprising observations are made from simulation studies based on the analytical results. For instance, the spatial bandwidth is shown to be approximately constant in almost the entire spatial multiplexing region. Moreover, in significant parts of this region, the optimal receive array orientation is not parallel with the transmitting array. [ABSTRACT FROM AUTHOR]

Here, L1 (2‐(pyridin‐2‐yl)quinoxaline) and L2 ((1‐((1H‐pyrrol‐2‐yl)ethylidene)benzene‐1,2‐diamine) ⋅ (1‐(1H‐pyrrol‐2‐yl)ethanone)) were synthesized and reacted with CoCl2 ⋅ 6H2O and NiCl2 ⋅ 6H2O to produce complexes 1–4. We found several interesting pieces of crystal structure information. Firstly, ligands L1 and L2 with completely different molecular structures were obtained by reacting the precursors containing similar N‐heterocycles with 1,2‐diaminobenzene. Secondly, in methanol and DMF solvents, 1 showed two structures, the binuclear and mononuclear cobalt complexes 1 a and 1 b. Finally, the structure of 4 showed the formation of a new 2 : 1 type ligand at eutectic L2 in the presence of a Ni2+ template. Upon treatment with AIBN, 1–4 showed moderate to high activities for MMA polymerization, producing PMMA with low to high molecular weights (2.02∼73.03×104 g⋅mol‐1) and moderate dispersity indices (PDI: 1.72∼3.32). Moreover, 1 b displayed higher catalytic activities (up to 1.138×105 g mol−1 ⋅ h−1), which was 20 times higher than that of 3 and more than 7 times higher than that of 1 a. [ABSTRACT FROM AUTHOR]

Anisotropic strata are frequently encountered in deep drilling engineering, especially for the rock with fracture structures. The problem of instability in highly deviated well in this kind of rock stratum is prominent as the strength of fractured rocks is weakened and the directions of fractures, in-situ stress and borehole axis can be complex. A model is built in this paper to assess the safety of drilling considering the influences of well trajectory, in-situ stress and fractures. The results show that: the fractures with different dip angles have important influence on the failure area and the collapse pressure. It is quite necessary to select the safe drilling trajectory in fractured formations as this is the economical and convenient approach. For some directional drilling, the determination of safe mud weight should be cautious. The in-situ stress difference, pore pressure and fracture strength parameters have significant effects on well collapse pressure. The above model calculation under specific working conditions can easily evaluate the safety and stability of wells drilling in all directions in fractured formation, so as to provide reference for well trajectory design of highly deviated wells. [ABSTRACT FROM AUTHOR]

A homologous series of five-membered heterocyclic ketoximes is synthesized by condensation reactions of 2-acetylpyrrole, 2-acetylthiophene, and 2-acetylfuran with hydroxylamine hydrochloride. These compounds were fully characterized by X-ray single-crystal diffraction, elemental analysis, 1H NMR, IR, UV-Vis, and fluorescence spectra. Interesting isomerization phenomena are observed for these heterocyclic ketoximes by different characterization methods. By means of 1H NMR and X-ray single-crystal diffraction, it was found that 2-acetylpyrrole oxime (1) exists as the Z -type geometric isomer, 2-acetylfuran oxime (3) exists as the E -isomer, while 2-acetylthiophene oxime (2) is identified as a mixture of Z- and E -isomers. To study the above phenomena further, quantum chemical calculations of total energy, dipole moment, E HOMO, E LUMO, and other parameters of each heterocyclic ketoxime were carried out by Density functional theory (DFT). The theoretical calculations were in good accordance with the experimental spectroscopic results. [ABSTRACT FROM AUTHOR]

A phytochemical investigation of the barks of Eucommia ulmoides Oliv. resulted in the isolation of 18 flavonoids (1-18). The new compound, eucommiaflavone (1) was structurally elucidated by various spectroscopic analyses. In particular, Mo2(OAc)4-induced circular dichroism (ICD) analysis was applied to determine the absolute configuration of 1. Furthermore, five flavonoids (4, 9, 11, 13, and 15) revealed significant in vitro hepatoprotective activity against D-galactosamine-induced cytotoxicity in human hepatoma HepG2 cells. [ABSTRACT FROM AUTHOR]

This study proposes a novel miniaturized circularly polarized (CP) ultrahigh frequency (UHF) quadrifilar helix antenna for spaceborne applications. The dual‐band operation is realized using four inverted‐U shaped helical strips (IUSHSs) that are rotated and alternately arranged on the four faces of a hollow polyimide cuboid in a sequential rotation manner, which effectively reduces the size of the antenna. Furthermore, the four IUSHSs are connected by a cross‐shape strip at the top of the antenna to control the dual resonant frequencies, resulting in a small dual‐band frequency ratio. The proposed antenna is both lightweight and robust when compared with the conventional miniaturized CP antennas operating at similar bands with similar performance. In particular, its compact radiator provides effective miniaturized spaceborne solution without the need of high‐dielectric coefficient materials. A device for spaceborne application that operates at 402/505 MHz is designed, fabricated, measured, and in‐orbit tested with a weight of 651 g and an effective size of 0.161 × 0.161 × 0.228 λ3402MHz (λ402MHz is the wavelength at 402 MHz). The measured gain and axial ratio of the proposed antenna are better than 5.32 dBi and 2.18 dB, respectively, within 2 and 12 MHz bandwidth for the two bands. The test results proved that the methods used to design the proposed antenna are effective. [ABSTRACT FROM AUTHOR]

Three new phenylethanol glycosides (1-3) and one known analogue (4) were isolated from the seeds of Aesculus chinensis Bge. var. chekiangensis. To the best of our knowledge, this represents the first isolation of phenylethanol glycosides from the genus of Aesculus, which enriched its chemical composition. Structure elucidations were performed via extensive NMR and HRESIMS data together with comparison with literature data. Thereafter, the isolated compounds were assayed for their neuroprotective activities against CoCl2-induced cytotoxicity in PC12 cells and compound 3 exhibited moderate activity. [ABSTRACT FROM AUTHOR]

Rhizoma coptidis has been used for a long time in China owing to its anti‐bacterial, anti‐diabetes, anti‐hyperlipidemia and anti‐obesity activities. However, the in vivo biotransformation of Rhizoma coptidis is still unclear to date. In this study, a three‐step strategy using UPLC‐Q‐TOF/MS was applied to clarify the in vivo absorbed constituents and metabolites in rats after oral administration of Rhizoma coptidis. First, alkaloids in Rhizoma coptidis extract were identified. Second, six abundant alkaloids (berberine, palmatine, coptisine, epiberberine, jatrorrhizine, and columbamine) were selected as representative prototypes and the metabolic fates of them in rats were investigated to obtain a database of Rhizoma coptidis‐derived metabolites. Finally, the metabolic profiles of Rhizoma coptidis were fully elucidated based on the above‐mentioned results. In summary, 29 alkaloids were identified in Rhizoma coptidis, and a database of Rhizoma coptidis‐derived metabolites was obtained with 144 characterized metabolites. A total of 89 xenobiotics including 12 absorbed constituents and 77 metabolites were identified in dosed rat biosamples. Major metabolic pathways of Rhizoma coptidis were hydroxylation, reduction, methylation, demethylation, demethylenation, desaturation, glucuronidation and sulfation. This is the first systematic study on the in vivo absorbed constituents and metabolic profiling of Rhizoma coptidis and will be beneficial for its further studies. [ABSTRACT FROM AUTHOR]

User-centric ultra-dense network (UDN) has been considered a key enabler of high data rate and high reliable vehicle-to-infrastructure (V2I) communication. In this paper, an analytical framework is developed based on stochastic geometry to characterize the uplink V2I transmission performances, in terms of the outage probability, the average vehicle throughput and the average spatial throughput, particularly resolving two important but not well-understood factors in such networks: the spatial correlation in the interference powers among the cooperative roadside units (RSUs) as caused by the shared set of co-channel vehicles, and the combined vertical distance (CVD) owing to the lane width and the antenna height difference between the vehicle and the RSUs. Exact analytical expressions of the outage probability are derived for the general multiple association cases, a far-distance approximation method is introduced to reduce the computational complexity, and lower and upper bounds are obtained corresponding to two extreme assumptions of the spatial interference correlation. We show that the impacts of the spatial interference correlation can be significant and ignoring the correlation can lead to non-optimal system deployment, and that the far-distance approximation can approach well with the exact results. Meanwhile, although CVD diminishes the V2I uplink transmission performances, the diminution can be mitigated through RSU cooperation. [ABSTRACT FROM AUTHOR]

A novel very‐high frequency (VHF) band spaceborne phased antenna array for satellite‐automatic identification system/VHF data exchange (SAT‐AIS/VDE) applications operating at 159 MHz is proposed in this letter. Element phase shifting is achieved by controlling each element mechanical rotation angle rather than the phase shifter behind each element. Thanks to the new working scheme, the proposed array shows several advantages over its former counterpart, including low cost, high power capacity, and broad phase‐shifting bandwidth. This letter explains the basic principle, and presents a preliminary study on element rotation angle controlled phased antenna array technology, and an eight‐element‐array which is implemented on solar panel supporting plate is designed to validate the concept. [ABSTRACT FROM AUTHOR]

Due to the rapidly increasing global interest in the use of herbs, phytomedicines and other natural products as medical or complementary remedies, concerns about the clinical medication safety have drawn much attention worldwide. Particularly, many natural ingredients exhibit inhibitory effects on cytochrome P450 (CYP) enzymes, which are the most important Phase I metabolism enzymes in liver. CYP2C9 is one of the most abundant CYP enzymes and responsible for the metabolism of over 15% clinical drugs, including oral sulfonylurea hypoglycemics, nonsteroidal anti-inflammatory agents, selective cyclooxygenase-2 inhibitors, antiepileptics, angiotensin II receptor inhibitors and anticoagulants. Diclofenac (4'-hydroxylase) and tolbutamide (methylhydroxylation) are widely used as probe substrates for CYP2C9. To date, numerous natural products have been reported to have the capabilities of inhibiting the catalytic activity of CYP2C9 and further influencing the pharmacokinetic and pharmacodynamic behaviors of drugs that are mainly metabolized by CYP2C9, leading to potential herb-drug interactions. Moreover, some fatal adverse interactions may occur for drugs with a narrow therapeutic window when they are coadministered with a CYP2C9 inhibitor, especially irreversible inactivators. For the purpose of better understanding the interactions of natural products with CYP2C9, we comprehensively reviewed the characteristics of CYP2C9, the natural ingredients that inhibit CYP2C9, the related research approaches and strategies, the types of inhibition and the underlying mechanisms. [ABSTRACT FROM AUTHOR]

A novel generalized polarization-space modulation (GPSM) is proposed for polarized multiple-input multiple-output (MIMO) systems with a limit number of radio frequency (RF) chains. In the spatial domain, multiple dual-polarized (DP) transmit antennas are activated, and then combinations of those indices are used to convey information. While in the polarization domain, depending on the random input bits, only one polarization state is selected for each active DP transmit antenna to transmit information following the rule of the polarized shift keying. At the receiver, the maximum likelihood detector is employed as a benchmark to detect information bits being used to select the polarization state and activated DP antennas. In the detector, imperfect channel state information (CSI) is taken into account. Two less computationally complex detectors, i.e., a linear detector and a sphere decoding (SD) detector are proposed to relieve the computational burden. Sacrificing the average bit error probability (ABEP) performance, the proposed linear detector can reduce the computational complexity significantly. The proposed SD detector can achieve the optimum ABEP performance, while reducing computational complexity by reducing the search space. A closed-form union upper bound (UUB) on the ABEP of the GPSM system with imperfect CSI at the receiver is analytically derived and validated through simulations. From the UUB, a loose asymptotic bound on the ABEP, which sheds light on deriving the diversity gain and the coding gain, is derived. Numerical results show that the signal-to-noise ratio loss caused by increasing the number of transmit antennas is less than 3 dB while the spectral efficiency is increased by 7 b/z/Hz. Therefore, the GPSM can be a promising candidate of down link massive MIMO systems to achieve a high spectral efficiency with a limit number of RF chains. [ABSTRACT FROM AUTHOR]

Two new isoflavone glucosides, 3′-methoxyneopuerarin A (1) and 3′-methoxyneopuerarin B (2), together with nine known isoflavones including puerarin (3), neopuerarin A (4), neopuerarin B (5), daidzin (6), daidzein (7), 3′-methoxypuerarin (PG-3) (8), puerarin xyloside (9), mirificin (10), 3′-hydroxypuerarin (11) were isolated from the water extraction of the dried roots of Pueraria lobata (Willd.) Ohwi. Their structures were elucidated by the means of spectroscopic and chromatographic analysis methods. All compounds were evaluated for their hepatoprotective activity on HepG2 cells. All of them showed statistically significant hepatoprotective effect. [ABSTRACT FROM AUTHOR]

Two new flavonoid glycosides, 2′,4′-dihydroxydihydrochalcone-4-O-β-d-glucopyranoside (1) and medicarpin-3-O-β-d-apiofuranosyl (1 → 2)-β-d-glucopyranoside (2), together with 34 known flavonoids were isolated from the 75% EtOH extract of the dried roots of Glycyrrhiza uralensis Fisch. Their structures were elucidated on the basis of spectroscopic analyses. The flavonoids were classified into ten sub-types, namely, dihydrochalcone (1), pterocarpans (2–4), flavones (5–6), flavanones (7–11), chalcones (12–15), retro-chalcones (16–18), isoflavans (19–21), isoflavones (22–28), 3-arylcoumarins (29–30), and coumestans (31–36). The isolated flavonoids were evaluated for in vitro hepatoprotective activity against d-galactosamine-induced toxicity in human hepatoma HepG2 cells. [ABSTRACT FROM AUTHOR]

1.Corydaline, an isoquinoline alkaloid obtained from the rhizomes of Corydalis yanhusuo, exhibits anti-acetylcholinesterase, anti-angiogenic, anti-allergic and gastric-emptying activities. In this study, a rapid and reliable ultra-performance liquid chromatography coupled to quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF-MS) method was developed and employed for the comprehensive study of the metabolites of corydaline in rats. 2.Altogether, 43 metabolites were identified in the plasma (11), bile (9), urine (34) and feces (21) of rats after oral administration of corydaline at a dose of 4.5mg/kg. 3.It was demonstrated that demethylation, hydroxylation, sulfation and glucuronidation were the major metabolic transformation pathways. Among these, two metabolites were identified as tetrahydropalmatine and isocorybulbine, and 33 phase I and phase II products were inferred to be new metabolites arising from the in vivo metabolism of corydaline. 4.Importantly, this research provides scientific and reliable support for full understanding of the metabolic profiles of corydaline and the results could help to elucidate its safety and efficacy. [ABSTRACT FROM AUTHOR]

Longhu Rendan (LHRD), a Chinese traditional compound medicine, has a remarkable treatment effect on motion sickness for about half a century. However, the role of LHRD in atherosclerosis treatment is still unclear. In this study, LHRD treatment significantly diminished total cholesterol (TC), triglyceride (TG), and low-density lipoprotein cholesterol (LDL-C) levels in apolipoprotein E gene-knockout (ApoE-/-) mice fed with high fat and high cholesterol diet (western diet). Besides, LHRD treatment significantly reduced atherosclerotic lesion and plaques formation in both aortic roots and aortic trees. Furthermore, immunofluorescence staining in aortic roots demonstrated that LHRD treatment inhibited lectin-like oxidized low-density-lipoprotein receptor-1 (LOX-1) expression in atherosclerotic plaques. These results indicated that LHRD ameliorated atherosclerosis via reducing serum levels of TC, TG, and LDL-C as well as LOX-1 expression, subsequently attenuating atherosclerotic lesion and lipid deposition. In conclusion, LHRD could significantly attenuate experimental atherosclerosis and might be a novel potential drug for the prevention and treatment of atherosclerosis. [ABSTRACT FROM AUTHOR]

Abstract: The calyces of Physalis alkekengi var. franchetii (Chinese Lantern, JDL) are well‐known as traditional Chinese medicine owing to its various therapeutic effects. However, the bioactive constituents responsible for the pharmacological effects of JDL and their metabolites in vivo are still unclear to date. In this paper, an ultra‐high‐pressure liquid chromatography coupled with quadrupole time‐of‐flight mass spectrometry (UHPLC/Q‐TOF‐MS/MS) method was established to identify absorbed constituents and in vivo metabolites in rat biological fluids after oral administration of JDL. Based on the proposed strategy, 33 compounds were observed in dosed rat biosamples. Twelve of 33 compounds were indicated as prototype components of JDL, and 21 compounds were predicted to be metabolites of JDL. Finally, the metabolic pathways were proposed, which were glucuronidation, sulfation, methylation and dehydroxylation for flavonoid constituents and sulfonation and hydroxylation for physalin consitituents. This is the first systematic study on the absorbed constituents and metabolic profiling of JDL and will provide a useful template for screening and characterizing the ingredients and metabolites of traditional Chinese medicine. [ABSTRACT FROM AUTHOR]

1. Physalin A is a bioactive withanolide isolated from the natural plantPhysalis alkekengivar.franchetii(Solanaceae), a common traditional Chinese herbal medicine. This study aims to investigate the metabolites of physalin Ain vivo. 2. Two metabolites (M1andM2) were characterized as sulfonate metabolites in the feces obtained from rats treated with physalin A orally at a dose of 15 mg/kg/day for 3 days, by application of a UPLC-Q/TOF-MS method. Furthermore, formation of the two sulfonate metabolites was verified by chemical synthesis and NMR, including1H NMR,13C NMR and two-dimensional NMR. The structures ofM1andM2were identified to be 3α-sulfo-2,25β,27-trihydrophysalin A and 3α,27-disulfo-2,25α-dihydrophysalin A, respectively. 3. In summary, this study indicated that physalin A could be biotransformed to sulfonate metabolites with strong polarity, which contributed to the elimination of physalin A. A rare metabolic pathway has been revealed in this study. [ABSTRACT FROM AUTHOR]

Heterogeneous networks (HetNets) are envisioned as a key solution to address the ever increasing capacity demand in wireless networks. With the deployment of enhanced radio access technologies, the non-ideal backhaul will become a potential network bottleneck. However, the impact of backhaul capacities (BCs) on the network coverage and offloading are not well understood. To address these issues, using tools from stochastic geometry, we propose a tractable framework for analyzing the impact of BCs on the network coverage and the optimal offloading bias in HetNets with cell range expansion (CRE) and time domain enhanced inter-cell interference coordination (eICIC) techniques. Conditioned on guaranteeing the minimum quality of service (QoS) of serving users, the coverage probability is derived as a function of offloading bias and BC parameters. We show how non-ideal backhaul alters the network coverage and the optimal bias. Compared with the perfect backhaul case, the optimal coverage and the optimal bias exhibit different behaviors in the case of limited BC. [ABSTRACT FROM AUTHOR]

Physalis pubescens L. has been used as a traditional folk medicine in China. Comprehensive studies aimed at identifying the bioactive constituents are still lacking. In the course of searching bioactive secondary metabolites from P. pubescens L., phytochemical investigation of the fruits of P. pubescens L. led to the isolation of one new eremophilane glycoside, 1β,3α-dihydroxy-7α-eremophila-911-dien-3-O-[α-L-arabinopyranosyl-(l→6)]-β-D-glucopyranoside (1), and six known glycosides (2–7). Their structures were established via extensive spectroscopic data including 1D and 2D NMR and HRESIMS. Cytotoxic effects against six human cancer cell lines (C4-2B, A375, A375-S2, 786-O, Caki-2, and ACHN) and one human normal hepatic cell line (L02) were evaluated and compounds 1 and 2 exhibited moderate cytotoxicity against C4-2B and A375 cell lines with IC50 values in the range of 6.78–28.3 μM. The study indicates that the fruits of P. pubescens L. have the potential to be used for drug discovery. [ABSTRACT FROM AUTHOR]

The single-radio-frequency (RF) multiple-input-multiple-output (MIMO) system has been proposed to pursue a high spectral efficiency while keeping a low hardware cost and complexity. Recently, the available degrees of freedom (DoF) in the polarization domain has been exploited to reduce the size of the transmit antenna array and provide 1 bit per channel use (bpcu) multiplexing gain for the single-RF MIMO system. Nevertheless, the polarization domain resource still has the potential to provide a higher multiplexing gain in the polarized single-RF MIMO system. In this paper, we propose a generalized polarization shift keying (PolarSK) modulation scheme that uses polarization states in the dual-polarized transmit antenna as an information-bearing unit to increase the overall spectral efficiency. At the receiver, the optimum maximum likelihood (ML) detector is employed to investigate the ultimate performance limit of the PolarSK. A closed-form union upper bound on the average bit error probability (ABEP) of the PolarSK with the optimum ML receiver is derived. Inspired by the analytic ABEP, a constellation diagram optimization algorithm is proposed. To reduce the computational complexity of the receiver, a linear successive interference cancellation (SIC) detection algorithm and a sphere-decoding (SD) detection algorithm are introduced. Through numerical results, performances of the proposed PolarSK in terms of ABEP and computational complexity are analyzed. Furthermore, the PolarSK is analyzed over measured indoor channels. Numerical and measurement results show that the PolarSK scheme outperforms the state-of-the-art dual-polarized/unipolarized SM schemes. [ABSTRACT FROM PUBLISHER]

Nine pairs of megastigmane enantiomers ( 1a/ 1b- 9a/ 9b), comprising two new compounds (6 S,9 R)-blumenol C ( 7b), (6 S,9 S)-blumenol C ( 8b), two pairs of enantiomers (+)-(6 R)-eucomegastigmane A ( 1a), (−)-(6 S)-eucomegastigmane A ( 1b), (+)-(3 S,4 S)-eucomegastigmane B ( 5a), (−)-(3 R,4 R)-eucomegastigmane B ( 5b) isolated by chiral resolution firstly, and twelve known compounds, were isolated from the leaves of Eucommia ulmoides Oliver. Their structures were elucidated based on extensive spectroscopic analysis. Absolute configurations of the megastigmane enantiomers were assigned by comparing experimental ECD and OR with calculated ECD and OR. Docking-based virtual screening of all compounds showed that megastigmane enantiomers have weak intermolecular interactions with the binding site residues of angiotensin-converting enzyme (ACE) and angiotensin II type 1 receptor (ATR). [ABSTRACT FROM AUTHOR]

A rapid and sensitive liquid chromatography with tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of luteolin, luteolin-7- O- β-D-glucopyranoside, physalin A, physalin D and physalin L in rat plasma. Scutellarein and dexamethasone were used as the internal standards (IS). Plasma samples were prepared by liquid-liquid extraction with ethyl acetate. The five constituents were separated on an Acquity UPLC BEH C18 column (100 mm × 2.1 mm, 1.7 μm). A gradient elution procedure was used with acetonitrile (A)-0.1% aqueous formic acid (B). Mass spectrometric detection was performed in negative ion multiple reaction monitoring mode with an electrospray ionization (ESI) source. This method showed good linearity ( r2 > 0.997) over a concentration range of 2.0-500 ng/mL with a lower limit of quantification of 2.0 ng/mL for all five compounds. The inter- and intra-day accuracy ranged from 91.7 to 104%, and precisions (RSD) were <6.46% for all analytes. The extraction recoveries of all analytes were >85%. This validated method was successfully applied for the first time to the pharmacokinetic study of five ingredients after oral administration of 70% ethanol extract of Chinese lantern in rats. [ABSTRACT FROM AUTHOR]

Rationale Palmatine (PAL), a protopalmatine alkaloid, is an active constituent in a number of medicinal plants. In order to obtain a comprehensive and systematic metabolic profile of PAL, we investigated its metabolites in plasma, liver tissue, bile, urine, and feces samples after intragastrical administration to Sprague-Dawley rats with a dose of 100 mg/kg/day. Methods In this study, a rapid and sensitive method by ultra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC/QTOF-MS), and Metabolynx™ software with the mass defect filter (MDF) technique was developed for screening and identification of the metabolites. The structural elucidation of the metabolites was performed by comparing their molecular weights and fragment ions with those of the parent drug. Results As a result, a total of 58 metabolites were identified in rat biological samples including 46 metabolites in urine, 18 metabolites in plasma, 34 metabolites in bile, 26 metabolites in liver tissue, and 10 metabolites in feces. Among them, six major metabolites were fully confirmed using reference standards and others were identified by retention time, accurate mass and fragment ions. Conclusions These results indicated that phase I reactions (demethylation and hydroxylation) and phase II reaction (glucuronidation and sulfation) were the main metabolic pathways of PAL in vivo. This research enhances our understanding of metabolism of PAL in rats, and provides useful information on the action mechanism of PAL. Copyright © 2017 John Wiley & Sons, Ltd. [ABSTRACT FROM AUTHOR]

Thirteen phenones were obtained from the 70% ethanol extract of Paeonia suffruticosa Andrews. Their structures were determined on the basis of chemical methods and spectral data. Among them, compound 1 was identified as a new compound, and compounds 5 and 13 were obtained from genus Paeonia for the first time. The inhibitory effects of isolated compounds (1–12) on nitric oxide (NO) production in lipopolysaccharide-activated macrophages were evaluated, and NO production was suppressed significantly by compound 7. [ABSTRACT FROM AUTHOR]

Objective: The transition from child mental health services to adult mental health services can be challenging for patients. Transition is a critical aspect of continuity of care but little is known of the profile of the patients who makes such transitions and their unique characteristics, which could place special demands on subsequent mental health services. The Adult Neurodevelopmental Service at the Institute of Mental Health, Singapore is the first integrated service for adults with neurodevelopmental disorders and psychiatric co-morbidities in Southeast Asia. This audit aims to analyse the profile and characteristics of patients who have made this transition to ensure that the service addresses their specific needs. Methods: The electronic records of 50 patients who were seen in 2015 were analysed in relation to socio-demographics, diagnosis and psychiatric co morbidities, pharmacotherapy, functioning and illness severity scores. Results: All patients except 3(6%) were seen as outpatients. 41(82%) of whom were male and 9(18%) female with the mean age of 21.1 years (SD±2.68). 32(64%) had autistic spectrum disorder, 28(56%) had intellectual disability and 8(16%) had attention deficit/hyperactivity disorder. Co morbid psychiatric disorders included anxiety disorders (16%), mood disorders (14%), psychotic disorders(8%), and obsessive-compulsive disorders(8%). Risperidone and fluoxetine were the most commonly used antipsychotics and antidepressants respectively. The mean initial clinical global impression score was 4.05(SD±0.87) ± 0.87), and the mean global assessment scale was 53.78(SD±9.42) in patients who were scored. Conclusion: Patients in transition from a child to adult mental health services are a complex and vulnerable group which requires services adapted to their unique needs. Analysing the profile of these patients is critical in evolving the service to meet the needs of this group of young patients to achieve an ideal level of care. [ABSTRACT FROM AUTHOR]

To obtain the optimal coefficient matrix for the integer-forcing (IF) linear receiver, the successive minima problem (SMP) on lattices needs to be solved. By decomposing SMP into a series of subspace avoiding problems (SAP) and developing a modified sphere-decoding (SD) algorithm based on the Schnorr-Euchner (SE) enumeration strategy to solve each instance of SAP, two practical algorithms are constructed to solve SMP exactly for real and complex lattices respectively. The initial radius and the starting position on the search-tree of the SAP algorithm are optimized by exploiting the intermediate results obtained in previous rounds. As compared to the Minkowski reduction algorithm, the proposed complex SMP algorithm brings not only more freedom in lattice code design, but also computation reduction in finding the coefficient matrix. Moreover, benefiting from the tree-search initialization optimization, the proposed real SMP algorithm can bring even more computation reduction when the system size is large. However, the proposed algorithms achieve practically the same performance as Minkowski reduction for the IF linear receiver, as the Minkowski-reduced basis approximates successive minima very closely. [ABSTRACT FROM PUBLISHER]

Glycyrrhizin (GZ), the main active component of licorice, is a widely used therapeutic in the clinic. Depending on the disease, the treatment may involve a long course of high dose GZ. Another component of licorice, glycyrrhetinic acid (GA), is the main active metabolite of GZ and is thought to be responsible for the majority of the pharmacological properties of GZ. Therefore, GZ and GA are both used for therapeutic purposes. In addition, GZ and GA are also widely used to sweeten and flavor foods. Due to this widespread, multifaceted use of these substances, potential drug interactions with GZ and GA have recently gained attention. Along these lines, this review covers the known effects of GZ and GA on drug-metabolizing enzymes and efflux transporters. We conclude that both GZ and GA may have an effect on the activity of CYPs. For example, GZ may induce CYP3A activity through activation of PXR. Also, GZ and GA may affect glucuronidation in rats and humans. Furthermore, 18β-GA is a potent inhibitor of P-gp, while GZ and GA are inhibitors of MRP1, MRP2 and BCRP. The pharmacokinetics and pharmacodynamics of many medications may be altered when used concurrently with GZ or GA, which is also covered in this review. Overall, GZ, GA or related products should be taken with caution when taken with additional medications due to the possible drug interactions. [ABSTRACT FROM AUTHOR]

A fast joint sorting and reduction (FJSR) algorithm is proposed, which involves elementary column operations only, to assist the successive interference cancellation (SIC) detection for multiple‐input multiple‐output (MIMO) systems. Simulation results show that the FJSR‐aided SIC detector achieves good error performance especially when the system scales up, yet requires only a few extra basis updates over the optimal‐ordered SIC detector regardless of the system size. This suggests that FJSR is particularly advantageous to small‐to‐medium scale MIMO systems with strict delay constraints. [ABSTRACT FROM AUTHOR]

Eight eudesmane-type sesquiterpenes - phaeusmanes A-H ( 1- 8) - isolated for the first time in this work, and four others ( 9- 12) isolated for the first time from plants in this work, together with fourteen known eudesmane derivatives, were isolated from the rhizomes of Curcuma phaeocaulis. Their structures were elucidated by 1D and 2D NMR and CD spectroscopy and HRMS. Compound 8 is the first example of a nitrogen-containing eudesmane-type sesquiterpene isolated from the genus Curcuma. Furthermore, inhibitory effects of the isolated compounds on NO production in lipopolysaccharide-activated macrophages were evaluated. Compounds 1, 6, 10, 19, 22, and 24 showed strong inhibitory activities on NO production with IC50 values of 3.2, 4.8, 1.2, 0.8, 3.8, and 0.8 μ M, respectively. Preliminary structure-activity relationships for these compounds are proposed. A possible biogenetic pathway for nitrogen-containing eudesmane-type sesquiterpene 8 is postulated. [ABSTRACT FROM AUTHOR]

The Spatial Modulation (SM) transmission scheme boosts the spectral efficiency and achieves the multiplexing gain by activating a single transmit antenna in each time slot. Radio wave propagation characteristics determined by the environment is a decisive factor for the SM system. In this paper, we investigate the performance of the SM scheme over real-world 4x4 Multi-Input Multi-Output (MIMO) channels measured in typical indoor scenarios. Firstly, a MIMO channel sounder is established. Based on the sounder, 15150 complex 4x4 MIMO channel matrices are measured inside a typical teaching building under both Line of Sight (LOS) and None Line of Sight (NLOS) scenarios. Secondly, by comparing the SM system over the measured channel and commonly-used channel models, we prove that both the Independently and Identically Distribute (i.i.d.) Rayleigh and the Spatial Correlation (SC) channel model are oversimplified, and that only practical experiences can yield definitive answers to the achievable real-world system performance. Thirdly, the Average Bit Error Probability (ABEP) performance of the SM system is studied based on the measured data under a variety of system configurations. The study of different receive antenna array settings (4x4, 4x2 and 4x1 MIMO setups) approves the significance of combining scheme at the receiver. SM systems employing different signal constellations (Binary Phase Shift Keying (BPSK), Quadrature Phase Shift Keying (QPSK) and 16 Quadrature Amplitude Modulation (16QAM)) are also investigated and some interesting results are revealed. Lastly, performance assessment of SM against State-Of-The-Art (SOTA) MIMO schemes (Space-Time Block Code (STBC) and Vertical Bell Labs Layered Space-Time (V-BLAST) code) is conducted. Results show that for a 4x4 MIMO, the low-complexity SM scheme outperforms both STBC and V-BLAST. [ABSTRACT FROM PUBLISHER]

The keyhole effect causes a dramatic performance degradation to Multiple-Input Multiple-Output (MIMO) systems. The main contribution of this letter is the analytical performance evaluation of Spatial Modulation MIMO (SM-MIMO) systems over the keyhole channel. The closed-form Pairwise Error Probability (PEP) is derived with accuracy verified by simulations. Based on the PEP, the achievable diversity gain is extracted and shown to be no more than 1 under any configuration. In addition, a tight Average Bit Error Probability (ABEP) upper bound is given. Numerical results demonstrate that compared to independent fading scenarios, the keyhole channel causes a significant performance degradation to the SM-MIMO system. It is shown that SM-MIMO schemes outperforms Space-Time Block Code (STBC) and V-BLAST schemes over the keyhole channel. Therefore, among multiple antenna transmission schemes, SM-MIMO schemes are better choices for systems that may experience the keyhole effect. However, owing to the inherent unfitness of the keyhole channel for multiple antenna transmission, SM-MIMO schemes are still inferior to SISO/SIMO schemes. [ABSTRACT FROM PUBLISHER]

Severe wellbore stability issues were reported while drilling in laminated formation with weak planes such as beddings. To accurately determine the safe mud weight according to the changing environment is of primary importance for safety control of drilling. Considering both the elastic and strength anisotropy of bedding formation, a novel theoretical model is established and the stress and failure around wellbores are analyzed. The accuracy and applicability of the theoretical model is verified by in situ field data. For the purpose of fulfilling real-time prediction, the method flowchart of programming is also provided. The results show that the model built can be conveniently used to predict the stress distribution, failure area, and collapse and fracture pressure while drilling, and rather good predictions can be made compared to real field data. In addition, the inhomogeneity of in situ stress and elastic parameters affect the upper limit of the safe mud weight window (SMWW) greater than the lower limit. Negative SMWW may appear with the direction change of the wellbore or weak plane, especially when the azimuths of them change. As to the magnitude of SMWW, the anisotropic effects of Young's modulus are greater than the Poisson's ratio. The method established in this paper can greatly help with the precise prediction of wellbore stability as drilling proceeds in bedding formation. [ABSTRACT FROM AUTHOR]

abstract 1. Paeonol, a major component of Paeonia suffruticosa Andrews, is used in clinical situations in China as a natural anti-inflammatory agent. The aim of the present study is to investigate the metabolism of paeonol in humans. 2. Six metabolites were isolated from human urine after oral administration of paeonol, and their structures were elucidated as resacetophenone (M1), resacetophenone-2-O-sulfate (M2), 2-hydroxy-4-methoxyacetophenone-5- O-sulfate(M3), 2-hydroxy-4-methoxyacetophenone-5-O-glucopyranuronoside (M4), 2-hydroxyacetophenone-4- O-glucopyranuronoside (M5) and 2,5-dihydroxy-4-methoxyacetophenone(M6) by a series of analyses involving mass spectrometry, 1H NMR, 13C NMR and NOESY spectra. 3. In addition, three more metabolites 2,4-dihydroxyacetophenone-5-O-sulfate (M7), paeonol-2-Oglucopyranuronoside (M8) and paeonol-2-O-sulfate (M9), were identified in human urine by using a UPLC/Q-TOF– MS/MS method. 4. This is the first study of paeonol metabolism in humans. Based on the identified metabolites, possible metabolic pathways of paeonol in humans are proposed. Paeonol is metabolized mainly by hydroxylation and demethylation to give the corresponding phase I metabolites, M1, M6 and 2,4,5-trihydroxyacetophenone, and which then underwent conjugation with glucuronic acid or sulfuric acid to form phase II metabolites, [ABSTRACT FROM AUTHOR]

The time of arrival (ToA) and received signal strength (RSS) estimation errors are modelled based on channel measurements in a non‐line‐of‐sight indoor environment. It is found interesting that their errors are largely independent. Suboptimal hybrid ToA/RSS ranging estimators are derived in closed form based on the obtained error models, and shown to achieve near‐optimal performance. The performance of all the estimators improves as the bandwidth increases. [ABSTRACT FROM AUTHOR]

The article reports on the synthesis of functional diamines 3,3'-diaminochalcone and bis(3-aminophenyl)-3,5-bis(trifluoromethyl)phenyl phosphine oxide. According to the authors, overall yields were pegged at 78 and 70 percent. The copolymides prepared exhibited high levels of solubility in organic solvents and thermal stability up to 450 degrees Celsius. They also report that copolymides that contain chalcone and phosphine oxide moieties in the main chain exhibited high levels of adhesiveness and photoreactivity.

Klebsiella pneumoniae is an opportunistic pathogen posing an urgent threat to global public health, and the capsule is necessary for K. pneumoniae infection and virulence. Phage-derived capsule depolymerases have shown great potential as antivirulence agents in treating carbapenem-resistant K. pneumoniae (CRKP) infections. However, the therapeutic potential of phages encoding depolymerases against CRKP remains poorly understood. In this study, we identified a long-tailed phage SRD2021 specific for mucoid CRKP with capsular K47 serotype, which is the predominant infectious K-type in Asia. Genome sequencing revealed that ΦSRD2021 belonged to the Drulisvirus genus and exhibited a capsular depolymerase domain in its tail fiber protein. A transposon-insertion library of host bacteria was constructed to identify the receptor for ΦSRD2021. We found that most phage-resistant mutants converted to a nonmucoid phenotype, including the mutant in wza gene essential for capsular polysaccharides export. Further knockout and complementation experiments confirmed that the Δwza mutant avoided adsorption by ΦSRD2021, indicating that the K47 capsular polysaccharide is the necessary receptor for phage infection. ΦSRD2021 lysed the bacteria mature biofilms and showed a therapeutic effect on the prevention and treatment of CRKP infection in the Galleria mellonella model. Furthermore, ΦSRD2021 also reduced the colonized CRKP in mouse intestines significantly. By recognizing the host capsule as a receptor, our results showed that ΦSRD2021 may be used as a potential antibacterial agent for K47 serotype K. pneumoniae infections. [ABSTRACT FROM AUTHOR]