Ultrafast photodoping and effective Fermi-Dirac distribution of the Dirac particles in Bi2Se3

We exploit time- and angle- resolved photoemission spectroscopy to determine the evolution of the out-of-equilibrium electronic structure of the topological insulator Bi2Se. The response of the Fermi-Dirac distribution to ultrashort IR laser pulses has been studied by modelling the dynamics of the hot electrons after optical excitation. We disentangle a large increase of the effective temperature T* from a shift of the chemical potential mu*, which is consequence of the ultrafast photodoping of the conduction band. The relaxation dynamics of T* and mu* are k-independent and these two quantities uniquely define the evolution of the excited charge population. We observe that the energy dependence of the non-equilibrium charge population is solely determined by the analytical form of the effective Fermi-Dirac distribution.Comment: 5 Pages, 3 Figure

Ultrafast Optical Control of the Electronic Properties of ZrTe5ZrTe_5

We report on the temperature dependence of the $ZrTe_5$ electronic properties, studied at equilibrium and out of equilibrium, by means of time and angle resolved photoelectron spectroscopy. Our results unveil the dependence of the electronic band structure across the Fermi energy on the sample temperature. This finding is regarded as the dominant mechanism responsible for the anomalous resistivity observed at T* $\sim$ 160 K along with the change of the charge carrier character from holelike to electronlike. Having addressed these long-lasting questions, we prove the possibility to control, at the ultrashort time scale, both the binding energy and the quasiparticle lifetime of the valence band. These experimental evidences pave the way for optically controlling the thermoelectric and magnetoelectric transport properties of $ZrTe_5$

A New Bi-Functional Derivative of Polyethylene Glycol as Molecular Carrier for Eugenol and Ibuprofen

Eugenol (EU) and ibuprofene (IBU) were covalently bound to a bi-functionalized PEG, used as molecular carrier of drugs and the release kinetics of the two bioactive molecules was studied in vitro in buffer solution at pH 7.4, in simulated gastric fluid and in mouse plasma. The hydrolysis studies showed a specific cleavage dependent on the pH of the medium and by the presence of proteolytic enzymes in mouse plasma. Studies in vitro on the release of the parent drug from this double prodrug in various media, indicate that the adduct may be sufficiently stable to pass intact the gastrointestinal tract and release into the circulation EU and IBU. Many advantages may be achieved by the synthesis of the prodrug EU-PEG-IBU related to synergistic analgesic and anti-inflammatory effects, to the reduction of the adverse reactions and the improvement of the chemical-physical properties of the parent drugs

New Triterpenes from the Fungus Gloeophyllum odoratum

Two new triterpene acids (1, 2), together with a complex mixture of lecithins (3), were isolated from the fungus Gloeophyllum odoratum. Their structures were elucidated on the basis of extensive spectroscopic analyses. The extract of Gloeophyllum odoratum considerably inhibited thrombin (72% at a concentration of 120 g/mL); the less polar fraction of the methanolic extract from the mushroom exhibited interesting activity (47% at a concentration of 120 g/mL) against thrombin. Compounds 1 and 2 were responsible for this activity

Evidence of reduced surface electron-phonon scattering in the conduction band of Bi_{2}Se_{3} by non-equilibrium ARPES

The nature of the Dirac quasiparticles in topological insulators calls for a direct investigation of the electron-phonon scattering at the \emph{surface}. By comparing time-resolved ARPES measurements of the TI Bi_{2}Se_{3} with different probing depths we show that the relaxation dynamics of the electronic temperature of the conduction band is much slower at the surface than in the bulk. This observation suggests that surface phonons are less effective in cooling the electron gas in the conduction band.Comment: 5 pages, 3 figure

Anticancer activity of cationic porphyrins in melanoma tumour-bearing mice and mechanistic in vitro studies

Background Porphyrin TMPyP4 (P4) and its C14H28-alkyl derivative (C14) are G-quadruplex binders and singlet oxygen (1O2) generators. In contrast, TMPyP2 (P2) produces 1O2 but it is not a G-quadruplex binder. As their photosensitizing activity is currently undefined, we report in this study their efficacy against a melanoma skin tumour and describe an in vitro mechanistic study which gives insights into their anticancer activity. Methods Uptake and antiproliferative activity of photoactivated P2, P4 and C14 have been investigated in murine melanoma B78-H1 cells by FACS, clonogenic and migration assays. Apoptosis was investigated by PARP-1 cleavage and annexin-propidium iodide assays. Biodistribution and in vivo anticancer activity were tested in melanoma tumour-bearing mice. Porphyrin binding and photocleavage of G-rich mRNA regions were investigated by electrophoresis and RT-PCR. Porphyrin effect on ERK pathway was explored by Western blots. Results Thanks to its higher lipophylicity C14 was taken up by murine melanoma B78-H1 cells up to 30-fold more efficiently than P4. When photoactivated (7.2 J/cm2) in B78-H1 melanoma cells, P4 and C14, but not control P2, caused a strong inhibition of metabolic activity, clonogenic growth and cell migration. Biodistribution studies on melanoma tumour-bearing mice showed that P4 and C14 localize in the tumour. Upon irradiation (660 nm, 193 J/cm2), P4 and C14 retarded tumour growth and increased the median survival time of the treated mice by ~50% (P <0.01 by ANOVA), whereas porphyrin P2 did not. The light-dependent mechanism mediated by P4 and C14 is likely due to the binding to and photocleavage of G-rich quadruplex-forming sequences within the 5\u2032-untranslated regions of the mitogenic ras genes. This causes a decrease of RAS protein and inhibition of downstream ERK pathway, which stimulates proliferation. Annexin V/propidium iodide and PARP-1 cleavage assays showed that the porphyrins arrested tumour growth by apoptosis and necrosis. C14 also showed an intrinsic light-independent anticancer activity, as recently reported for G4-RNA binders. Conclusions Porphyrins P4 and C14 impair the clonogenic growth and migration of B78-H1 melanoma cells and inhibit melanoma tumour growth in vivo. Evidence is provided that C14 acts through light-dependent (mRNA photocleavage) and light-independent (translation inhibition) mechanisms. Keywords: Melanoma B78-H1 cells; Cationic porphyrins; Biodistribution; C57/BL6 mice; Ras genes; G4-RNA; ERK pathwa

CHOLANE AND LANOSTANE DERIVATIVES: ANTIMICROBIAL EVALUATION

Steroids are natural compounds with several important applications in many fields of research, such as medicinal chemistry, pharmacology, supramolecular chemistry and nanotechnology.In particular, bile acids such as lithocholic acid (LCA) and ursodeoxycholic acid (UDCA) have been considered quite useful as starting points for a rich and different set of medicinal chemistry activities. Besides, the discovery of bioactive ingredients from plants and fungi is always the main target in medicinal chemistry. The lanostane-type triterpenoid 3b-hydroxylanosta-8,24-diene-21-oic acid (Trametenolic acid, TMA) was the main bioactive component of Gloeophyllum odoratum, which was reported to possess widely bioactivities, including tumor cell anti-proliferation effects (for example, human HL-60 leukemia, human KB epidermoid carcinoma, murine L1210 leukemia cells, Caski, HT-3, T-24, etc.), inhibition of enzyme activity (human thrombin, bovine trypsin and so on).Nevertheless, trametenolic acid was scarcely investigated as antimicrobial agent. Structurally, bile acids (LCA and UDCA) and trametenolic acid are similar since they may be regarded as consisting of two components, a rigid steroid nucleus and an aliphatic side chain possessing a carboxyl group. On the basis of these considerations, six new compounds bearing a guanidine moiety in their side chain were synthesized using LCA, UDCA and TMA as starting materials. The parent bile acids, TMA and their resulting derivatives were evaluated for antimicrobial activity against S. aureus, B. subtilis and M. smegmatis. The derivative 3a-hydroxy-23-guanidino-5b-cholane showed the best activity, with MIC values of 12.5 \u3bcM against S. aureus, 5 \u3bcM against B. subtilis and 50 \u3bcM against M. smegmatis. The cytotoxic activity of bile acids, trametenolic acid and derivatives was also evaluated against HT-29 cell lin