Perisomalien A,a new cytotoxic scalarane sesterterpene from the fruits of Periploca somaliensis

Abstract

The CHCl₃ fraction of MeOH extract of Periploca somaliensis (family Asclepiadaceae) fruits afforded a new scalarane sesterterpene, namely perisomalien A (1), along with lupeol acetate (2), β-amyrin (3), cycloart-23Z-ene-3β,25-diol (4), and β-sitosterol-3-O-β-D-glucopyranoside (5). Their chemical structures were established by various spectroscopic analyses, in addition to comparison with the formerly reported data. Moreover, the cytotoxic activity of these metabolites was assessed towards MCF-7, HepG2, and HCT-116 tumour cell lines using sulforhodamine B (SRB) assay. Compound 4 showed the most potent cytotoxic profile with IC₅₀ 9.0?µM towards MCF-7, compared to doxorubicin (IC₅₀ 0.18?µM). Also, 1 and 4 possessed the most potent effect towards HepG2 with IC₅₀s 26.7 and 25.9?μM, respectively. In addition, all tested compounds showed cytotoxic effects with IC₅₀ values ranging from 19.9 to 39.3?µM against HCT-116.     

Bioactive Tryptophan-Based Copper Complex with Auxiliary β-Carboline Spectacle Potential on Human Breast Cancer Cells: In Vitro and In Vivo Studies

Biocompatible tryptophan-derived copper (1) and zinc (2) complexes with norharmane (β-carboline) were designed, synthesized, characterized, and evaluated for the potential anticancer activity in vitro and in vivo. The in vitro cytotoxicity of both complexes 1 and 2 were assessed against two cancerous cells: (human breast cancer) MCF7 and (liver hepatocellular cancer) HepG2 cells with a non-tumorigenic: (human embryonic kidney) HEK293 cells. The results exhibited a potentially decent selectivity of 1 against MCF7 cells with an IC₅₀ value of 7.8 ± 0.4 μM compared to 2 (less active, IC₅₀ ~ 20 μM). Furthermore, we analyzed the level of glutathione, lipid peroxidation, and visualized ROS generation to get an insight into the mechanistic pathway and witnessed oxidative stress. These in vitro results were ascertained by in vivo experiments, which also supported the free radical-mediated oxidative stress. The comet assay confirmed the oxidative stress that leads to DNA damage. The histopathology of the liver also ascertained the low toxicity of 1.     

Large eddy simulations of partially premixed ethanol dilute spray flames using the flamelet generated manifold model

The paper presents Large Eddy Simulations (LESs) for the Sydney ethanol piloted turbulent dilute spray flames ETF2, ETF6, and ETF7. The Flamelet Generated Manifold (FGM) approach is employed to predict mixing and burning of the evaporating fuel droplets. A methodology to match the experimental inflow spray profiles is presented. The spray statistical time-averaged results show reasonable agreement with mean and RMS data. The Particle Size Distribution (PSD) shows a good match downstream of the nozzle exit and up to x/D = 10. At x/D = 20 and 30 the PSD is under-predicted for droplets with mean diameter D10 > 20μm and over-predicted for the smaller size droplets. The simulations reasonably predict the reported mean flame structure and length. The effect of increasing the carrier velocity (ETF2–ETF7) or decreasing the liquid fuel injection mass flow rate (ETF2–ETF6) is found to result in a leaner, shorter flame and stronger spray–flow interactions. Higher tendency to local extinction is observed for ETF7 which is closer to blow-off compared to ETF2 and has higher scalar dissipation rates, higher range of Stokes number, and faster droplet response. The possible sources of LES-FGM deviations from the measurements are discussed and highlighted. In particular, the spray time-averaged statistical error contribution is quantified and the impact of the inflow uncertainty is studied. Sensitivity analysis to the pre-vaporized nozzle fuel mass fraction show that such small inflow perturbations (by ±?2% for the ETF2 flame) have a strong impact on the flame structure, and the droplets’ dynamics. Conditional scatter plots show that the flame exhibits wide range of mixing conditions and bimodal mixing lines particularly at upstream locations (x/D?相似文献   

Retention Behavior of Neutral and Positively and Negatively Charged Solutes on an Immobilized‐Artificial‐Membrane (IAM) Stationary Phase

The retention behavior of neutral, positively charged, and negatively charged solutes on the IAM.PC.DD2 stationary phase was investigated and compared. A set of monofunctional compounds and complex drugs (steroids, nonsteroidal anti‐inflammatory drugs, and β‐blockers) were selected for this study, i.e., neutral solutes and solutes with acidic or basic functionalities which are positively charged or negatively charged at pH 7.0. The correlation between the retention factor log k_w at pH 7.0 on the IAM.PC.DD2 stationary phase and the partition coefficient log P_oct or the distribution coefficient log D_7.0 showed that the retention mechanism depends on the charge state and structural characteristics of the compounds. The neutrals were least retained on the IAM.PC.DD2 stationary phase, and positively charged solutes were more retained than negatively charged ones. This implies that the retention of the charged solutes is controlled not only by lipophilicity but also by the electrostatic interaction with the phospholipid, with which positively charged solutes interact more strongly than negatively charged ones.     

Modeling of tsunami generation and propagation by a spreading curvilinear seismic faulting in linearized shallow-water wave theory

The processes of tsunami evolution during its generation in search for possible amplification mechanisms resulting from unilateral spreading of the sea floor uplift is investigated. We study the nature of the tsunami build up and propagation during and after realistic curvilinear source models represented by a slowly uplift faulting and a spreading slip-fault model. The models are used to study the tsunami amplitude amplification as a function of the spreading velocity and rise time. Tsunami waveforms within the frame of the linearized shallow-water theory for constant water depth are analyzed analytically by transform methods (Laplace in time and Fourier in space) for the movable source models. We analyzed the normalized peak amplitude as a function of the propagated uplift length, width and the average depth of the ocean along the propagation path.     

Flow‐Through Assay of Quinine Using Solid Contact Potentiometric Sensors Based on Molecularly Imprinted Polymers

Miniaturized potentiometric membrane sensors for quinine incorporated with molecular imprinted polymer (MIP) were synthesized and implemented. Planar PVC based polymeric membrane sensors containing quinine‐methacrylic and/or acrylic acid‐ethylene glycol methacrylate were dispensed into anisotropically etched wells on polyimide wafers. The determination of quinine was carried out in acidic solution at pH 6, where positively charged species predominated prevalently. The suggested miniaturized planner sensors exhibited marked selectivity, sensitivity, long‐term stability and reproducibility. At their optimum conditions, the sensors displayed wide concentration ranges of 4.0×10^?6–1.0×10^?2mol L^?1 and 1.0×10^?5–1.0×10^?2 mol L^?1 with slopes of about 61.3–55.7 mV decade^?1; respectively. Sensors exhibit detection limits of 1.2×10^?6 and 8.2×10^?6 mol L^?1 upon the use of methacrylic and acrylic acid monomers in the imprinted polymer, respectively. Validation of the assay method according to the quality assurance standards (range, within‐day repeatability, between‐day variability, standard deviation, accuracy, and good performance characteristics) which could assure good reliable novel sensors for quinine estimation was justified. Application of the proposed flow‐through assay method for routine determination of quinine in soft drinks was assayed and the results compared favorably with data obtained by the standard fluorimetric method.     

The fractional coupled KdV equations： Exact solutions and white noise functional approach

Variable coefficients and Wick-type stochastic fractional coupled KdV equations are investigated. By using the mod- ified fractional sub-equation method, Hermite transform, and white noise theory the exact travelling wave solutions and white noise functional solutions are obtained, including the generalized exponential, hyperbolic, and trigonometric types.     

Computational study of decaying annular vortex flow using the Rε/k − ε turbulence model

In this article, we present three dimensional CFD study of turbulent vortex flow in an annular passage using OpenFOAM 1.6. The vortex flow is generated by introducing the flow through a tangential entry to the passage. For the analysis presented in this article, turbulence was modeled using the R_ε/k − ε model, in addition, a comparison between such model with the standard k − ε model was conducted and discussed. The main characteristics of the flow such as vortex structure and recirculation zone were investigated. It was found that flow is subjected to Rankine vortex structure with three forced vortex regimes and a free vortex region near to the outer wall. The phenomenon of vortex decay was investigated by depicting the swirl number trend along the axial direction of the flow domain. It was found that the vortex decay is subjected to an exponential decay behavior. New coefficients for the exponential decay correlation were derived based on local values of velocity components in different radial planes.     

The acoustical influence of balcony depth and parapet form: experiments and simulations

The influence of balcony depth and parapet form on the acoustical performance of building facades close to roadways have been investigated. Various depths and two inclinations of parapet have been modeled on an eight floor building. Pyramid ray-tracing simulations and scale model measurements have been carried out. The predicted and measured A-weighted sound pressure level reductions over the balcony back wall and in free field conditions have been compared. The results have been used to derive empirical equations for predicting protection as a function of geometrical parameters. The protection obtained by various parapet depths ranges between 4 and 8 dB(A), while an additional protection of between 0.5 and 4 dB(A) can be obtained by inclining the parapets.     

A green approach to the synthesis of 2,3‐diaminophenazine using a photocatalytic system of CdFe2O4/TiO2 nanoparticles

In recent years, the development of novel green chemistry routes for the synthesis of organic compounds has become very attractive to many research groups. Nanoparticles have been widely used because of their potential applications in catalysis, environmental remediation, electronic fields, biomedical, and industrial fields. In this article, a rapid, efficient, and simple approach was applied for the synthesis of 2,3‐diaminophenazine using a new photocatalytic system of CdFe₂O₄/TiO₂ nanoparticles in water as a benign solvent. The structure of the synthesized CdFe₂O₄/TiO₂ nanoparticle was confirmed using different methods such as transmission electron microscope (TEM), X‐ray diffraction (XRD), and magnetic measurements. It was found that the rate and yield of the photocatalytic synthesis of 2,3‐diaminophenazine were improved using CdFe₂O₄/TiO₂ nanoparticles compared to other methods.