New designed DNA light switch Ruthenium complexes as DNA photocleavers and Topoisomerase I inhibitors

Two ruthenium complexes containing a new ligand phipz (phipz = 2‐(1,10‐phenanthroline)‐1H‐imidazo[4,5‐b]phenazine) were designed and synthesized. These complexes were found to inhibit the DNA supercoiled relaxation mediated by topoisomerase I (topo I), cleave DNA under irradiation and bind to calf thymus DNA through intercalative mode. Furthermore, complex 2 shows higher photocleavage activity, topo I inhibition activity and DNA affinity than complex 1 . Additionally, introduction of phenazine unit may be the reason that two complexes exhibit DNA ‘light switch’ behavior. The present work shows that two complexes might be potential as new DNA ‘light switches’, DNA photocleavers and topo I inhibitors.     

Study of three rotating radio transients with FAST

Rotating radio transients(RRATs) are peculiar astronomical objects whose emission mechanism remains under investigation.In this paper, we present observations of three RRATs, J1538+2345, J1854+0306 and J1913+1330, carried out with the Fivehundred-meter Aperture Spherical radio Telescope(FAST). Specifically, we analyze the mean pulse profiles and temporal flux density evolutions of the RRATs. Owing to the high sensitivity of FAST, the derived burst rates of the three RRATs are higher than those in previous reports. RRAT J1854+0306 exhibited a time-dynamic mean pulse profile, whereas RRAT J1913+1330 showed distinct radiation and nulling segments on its pulse intensity trains. The mean pulse profile variation with frequency is also studied for RRAT J1538+2345 and RRAT J1913+1330, and the profiles at different frequencies could be well fitted with a cone-core model and a conal-beam model, respectively.     

Quantum transport in topological semimetals under magnetic fields (II)

Research about two-dimensional (2D) materials is growing exponentially across various scientific and engineering disciplines due to the wealth of unusual physical phenomena that occur when charge transport is confined to a plane. The applications of 2D materials are highly affected by the electrical properties of these materials, including current distribution, surface potential, dielectric response, conductivity, permittivity, and piezoelectric response. Hence, it is very crucial to characterize these properties at the nanoscale. The Atomic Force Microscopy (AFM)-based techniques are powerful tools that can simultaneously characterize morphology and electrical properties of 2D materials with high spatial resolution, thus being more and more extensively used in this research field. Here, the principles of these AFM techniques are reviewed in detail. After that, their representative applications are further demonstrated in the local characterization of various 2D materials’ electrical properties.

     

Pressure controllable phase transition in MoTe2 by the interlayer band occupancy

High pressure can effectively control the phase transition of MoTe₂ in experiment, but the mechanism is still unclear. In this work, we show by first-principles calculations that the phase transition is suppressed and $1T^{\prime }$ phase becomes more stable under high pressure, which originates from the pressure-induced change of the interlayer band occupancies near the Fermi energy. Specifically, the interlayer states of $1T^{\prime }$ phase tend to be fully occupied under high pressure, while they keep partially occupied for the $T_d$ phase. The increase of the band occupancies makes the $1T^{\prime }$ phase more favorable in energy and prevents the structure changing from $1T^{\prime }$ to $T_d$ phase. Moreover, we also analyze the superconductivity under high pressure based on BCS theory by calculating the density of states and phonon spectra. Our results may shed some light on understanding the relationship between the interlayer band occupancy and crystal stability of MoTe₂ under high pressures.     

Dose‐dependent exposure profile and metabolic characterization of notoginsenoside R1 in rat plasma by ultra‐fast liquid chromatography–electrospray ionization–tandem mass spectrometry

Notoginsenoside R₁ (NGR₁), a diagnostic protopanaxatriol‐type (ppt‐type) saponin in Panax notoginseng, possesses potent biological activities including antithrombotic, anti‐inflammatory, neuron protection and improvement of microcirculation, yet its pharmacokinetics and metabolic characterization as an individual compound remain unclear. The aim of this study was to investigate the exposure profile of NGR₁ in rats after oral and intravenous administration and to explore the metabolic characterization of NGR₁. A simple and sensitive ultra‐fast liquid chromatographic–tandem mass spectrometric method was developed and validated for the quantitative determination of NGR₁ and its major metabolites, and for characterization of its metabolic profile in rat plasma. The blood samples were precipitated with methanol, quantified in a negative multiple reaction monitoring mode and analyzed within 6.0 min. Validation parameters (linearity, precision and accuracy, recovery and matrix effect, stability) were within acceptable ranges. After oral administration, NGR₁ exhibited dose‐independent exposure behaviors with t_1/2 over 8.0 h and oral bioavailability of 0.25–0.29%. A total of seven metabolites were characterized, including two pairs of epimers, 20(R)‐notoginsenoside R₂/20(S)‐notoginsenoside R₂ and 20(R)‐ginsenoside Rh₁/20(S)‐ginsenoside Rh₁, with the 20(R) form of saponins identified for the first time in rat plasma. Five deglycometabolites were quantitatively determined, among which 20(S)‐notoginsenoside R₂, ginsenoside Rg₁, ginsenoside F₁ and protopanaxatriol displayed relatively high exploration, which may partly explain the pharmacodynamic diversity of ginsenosides after oral dose.     

Pharmacokinetics of salvianolic acid B,rosmarinic acid and Danshensu in rat after pulmonary administration of Salvia miltiorrhiza polyphenolic acid solution

A sensitive and accurate LC–MS/MS method was established for quantifying salvianolic acid B (Sal B), rosmarinic acid (Ros A) and Danshensu (DA) in rat plasma. Salvia miltiorrhiza polyphenolic acid (SMPA), active water‐soluble ingredients isolated and purified from Salvia miltiorrhiza Bge included Sal B, Ros A and DA. The pharmacokinetic analysis of Sal B, Ros A and DA after pulmonary administration of SMPA solution to rat was performed by LC–MS/MS. Results from the pharmacokinetic studies showed that the peak concentration of DA was 21.85 ± 6.43 and 65.39 ± 3.83 ng/mL after pulmonary and intravenous administration, respectively. DA was not detected at 2 h after administration. The absolute bioavailabilities of Sal B and Ros A were respectively 50.37 ± 27.04 and 89.63 ± 12.16% after pulmonary administration of 10 mg/kg SMPA solution in rats. The absolute bioavailability of Sal B increased at least 10‐fold after pulmonary administration, compared with oral administration. It was concluded that the newly established LC–MS/MS method was suitable for describing the pharmacokinetic characteristics of Sal B, Ros A and DA in rat after pulmonary administration of SMPA solution. The data from this study will provide a preclinical insight into the feasibility of pulmonary administration of SMPA.     

Effect of ethanediamine on bio-polishing of cotton fabrics with cellulase

n-Propylamine and n-butylamine showed an inhibitory effect on cellulase A and cellulase B, while ethanediamine displayed a positive effect on both of these cellulases. Relative filter paper activity and relative CMCase activity of cellulase A and cellulase B measured at 50 °C were increased by 16.0 and 25.2 %, and 18.9 and 13.9 %, respectively, by the appearance of ethanediamine at a certain concentration. Also the addition of ethanediamine maintained the thermal stability of cellulase A and B at 65 °C to some extent and showed a stronger stabilizing effect on cellulase A than cellulase B. Third, the addition of ethanediamine within a certain concentration range enhanced the bio-polishing effect of cotton fabric enzymatic treatment at 50 °C to some extent, obtaining a close bio-polishing effect of cotton fabrics treated at 50 °C; the addition of ethanediamine saved some of the dose of cellulase A and B. Last but not least, the appearance of ethanediamine broadened the operating temperature of cellulase A to 65 °C, and it had a less positive effect on cellulase B at 65 °C.