Production of Terretonin N and Butyrolactone I by Thermophilic Aspergillus terreus TM8 Promoted Apoptosis and Cell Death in Human Prostate and Ovarian Cancer Cells

The anticancer activity of terretonin N (1) and butyrolactone I (2), obtained from the thermophilic fungus Aspergillus terreus TM8, was intensively studied against prostate adenocarcinoma (PC-3) and ovary adenocarcinoma (SKOV3) human cell lines. According to this study, both compounds showed potent cytotoxicity towards ovarian adenocarcinoma cells (SKOV3) with IC₅₀ 1.2 and 0.6 μg/mL, respectively. With respect to metastatic prostate cells (PC-3), the two compounds 1 and 2 showed a significantly promising cytotoxicity effect with IC₅₀ of 7.4 and 4.5 μg/mL, respectively. The tested fungal metabolites showed higher rates of early and late apoptosis with little or no necrotic apoptotic pathway in all treated prostate adenocarcinoma (PC-3) and ovary adenocarcinoma (SKOV3) human cell lines, respectively. The results reported in this study confirmed the promising biological properties of terretonin N (1) and butyrolactone I (2) as anticancer agents via the induction of cellular apoptosis. However, further studies are needed to elucidate the molecular mechanism by which cellular apoptosis is induced in cancer cells.     

Formulation of Piperine–Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation

The present research work is designed to prepare and evaluate piperine liposomes and piperine–chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (−7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC₅₀ when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.     

Theoretical study of the structural and energetic properties of platinum clusters with up to 60 atoms

Structural Chemistry - Applying a theoretical approach that combines an efficient and fast global optimization based on genetic algorithms (GA) to search in structure space and the parameterized...     

Chalepin and Chalepensin: Occurrence,Biosynthesis and Therapeutic Potential

Dihydrofuranocoumarin, chalepin (1) and furanocoumarin, chalepensin (2) are 3-prenylated bioactive coumarins, first isolated from the well-known medicinal plant Ruta chalepensis L. (Fam: Rutaceae) but also distributed in various species of the genera Boenminghausenia, Clausena and Ruta. The distribution of these compounds appears to be restricted to the plants of the family Rutaceae. To date, there have been a considerable number of bioactivity studies performed on coumarins 1 and 2, which include their anticancer, antidiabetic, antifertility, antimicrobial, antiplatelet aggregation, antiprotozoal, antiviral and calcium antagonistic properties. This review article presents a critical appraisal of publications on bioactivity of these 3-prenylated coumarins in the light of their feasibility as novel therapeutic agents and investigate their natural distribution in the plant kingdom, as well as a plausible biosynthetic route.     

Timing performance of ZnO:Ga nanopowder composite scintillators

The implementation of nanocrystal‐based composite scintillators as a new generation of ultrafast particle detectors is explored using ZnO:Ga nanopowder. Samples are characterized with a spectral‐time resolved photon counting system and pulsed X‐rays, followed by coincidence time resolution (CTR) measurements under 511 keV gamma excitation. Results are comparable to CTR values obtained using bulk inorganic scintillators. Bringing the ZnO:Ga nanocrystal's timing performance to radiation detectors could pave the research path towards sub‐20 ps time resolution as shown in this contribution. However, an efficiency boost when placing nanopowders in a transparent host constitutes the main challenge in order to benefit from sub‐nanosecond recombination times. (© 2016 WILEY‐VCH Verlag GmbH &Co. KGaA, Weinheim)     

Charge transport in anodic TiO2 nanotubes studied by terahertz spectroscopy

We report on the photoelectrochemical and terahertz measurements, of the charge transport properties of 1 μm thick self‐organized TiO₂ nanotube layers, prepared by the anodization of titanium. We provide evidence regarding the complexity of electron transport, and dynamics in the nanotubes. Shortly after photoexcitation, charge mobilites in amorphous and crystalline nanotubes are similar, but still lower compared to the bulk anatase. The mobility subsequently decreases due to trapping‐detrapping processes. The recombination rate in anatase nanotubes is much slower than in the amorphous ones, enabling the material to reach an internal photon to electron conversion efficiency exceeding 60%.     

Stationary shapes of deformable particles moving at low Reynolds numbers

We introduce an iterative solution scheme in order to calculate stationary shapes of deformable elastic capsules which are steadily moving through a viscous fluid at low Reynolds numbers. The iterative solution scheme couples hydrodynamic boundary integral methods and elastic shape equations to find the stationary axisymmetric shape and the velocity of an elastic capsule moving in a viscous fluid governed by the Stokes equation. We use this approach to systematically study dynamical shape transitions of capsules with Hookean stretching and bending energies and spherical resting shape sedimenting under the influence of gravity or centrifugal forces. We find three types of possible axisymmetric stationary shapes for sedimenting capsules with fixed volume: a pseudospherical state, a pear-shaped state, and buckled shapes. Capsule shapes are controlled by two dimensionless parameters, the Föppl-von-Kármán number characterizing the elastic properties and a Bond number characterizing the driving force. For increasing gravitational force the spherical shape transforms into a pear shape. For very large bending rigidity (very small Föppl-von-Kármán number) this transition is discontinuous with shape hysteresis. The corresponding transition line terminates, however, in a critical point, such that the discontinuous transition is not present at typical Föppl-von-Kármán numbers of synthetic capsules. In an additional bifurcation, buckled shapes occur upon increasing the gravitational force.     

Current fluctuations in nanopores: The effects of electrostatic and hydrodynamic interactions

Using nonequilibrium Langevin dynamics simulations of an electrolyte with explicit solvent particles, we investigate the effect of hydrodynamic interactions on the power spectrum of ionic nanopore currents. At low frequency, we find a power-law dependence of the power spectral density on the frequency, with an exponent depending on the ion density. Surprisingly, however, the exponent is not affected by the presence of the neutral solvent particles. We conclude that hydrodynamic interactions do not affect the shape of the power spectrum in the frequency range studied.     

Effect of nonlinear correlations on the statistics of return intervals in multifractal data sets

We study the statistics of return intervals between events above a certain threshold in multifractal data sets without linear correlations. We find that nonlinear correlations in the record lead to a power-law (i) decay of the autocorrelation function of the return intervals, (ii) increase in the conditional return period, and (iii) decay in the probability density function of the return intervals. We show explicitly that all the observed quantities depend both on the threshold value and system size, and hence there is no simple scaling observed. We also demonstrate that this type of behavior can be observed in real economic records and can be used to improve considerably risk estimation.     

Correcting saturation effects of the arterial input function in dynamic susceptibility contrast-enhanced MRI: a Monte Carlo simulation

To prevent systematic errors in quantitative brain perfusion studies using dynamic susceptibility contrast-enhanced magnetic resonance imaging (DSC-MRI), a reliable determination of the arterial input function (AIF) is essential. We propose a novel algorithm for correcting distortions of the AIF caused by saturation of the peak amplitude and discuss its relevance for longitudinal studies. The algorithm is based on the assumption that the AIF can be separated into a reliable part at low contrast agent concentrations and an unreliable part at high concentrations. This unreliable part is reconstructed, applying a theoretical framework based on a transport-diffusion theory and using the bolus-shape in the tissue. A validation of the correction scheme is tested by a Monte Carlo simulation. The input of the simulation was a wide range of perfusion, and the main aim was to compare this input to the determined perfusion parameters. Another input of the simulation was an AIF template derived from in vivo measurements. The distortions of this template was modeled via a Rician distribution for image intensities. As for a real DSC-MRI experiment, the simulation returned the AIF and the tracer concentration-dependent signal in the tissue. The novel correction scheme was tested by deriving perfusion parameters from the simulated data for the corrected and the uncorrected case. For this analysis, a common truncated singular value decomposition approach was applied. We find that the saturation effect caused by Rician-distributed noise leads to an overestimation of regional cerebral blood flow and regional cerebral blood volume, as compared to the input parameter. The aberration can be amplified by a decreasing signal-to-noise ratio (SNR) or an increasing tracer concentration. We also find that the overestimation can be successfully eliminated by the proposed saturation-correction scheme. In summary, the correction scheme will allow DSC-MRI to be expanded towards higher tracer concentrations and lower SNR and will help to increase the measurement to measurement reproducibility for longitudinal studies.