Luminescence of ZnS-AgAlS2

The procedure of synthesizing the ZnS-AgAlS₂ phosphor are described. It is shown that this phosphor has three emission bands and three excitation band groups for these emission bands. The temperature- and concentration-dependent shifts of the emission and excitation bands are noted along with the changes which occur in the emission band intensities with changes in temperature and concentration. An explanation of the observed effects is offered.     

Functional human 5-HT6 receptor assay for high throughput screening of chemical ligands and binding proteins

Continuous identification and validation of novel drug targets require the development of rapid, reliable, and sensitive cell-based high-throughput screening (HTS) methods for proposed targets. Recently, the 5-HT(6) receptor (5-HT(6)R), a member of the class of recently discovered 5-HT receptors, has received considerable attention for its possible implications in depression, cognition, and anxiety. However, the cellular signaling mechanisms of 5-HT(6)R are poorly understood due to the lack of selective 5-HT(6)R ligands. In the present study, we examined functional coupling of the human 5-HT(6)R, 5-HT(7A)R, or 5-HT(7B)R with various Galpha-proteins (Galpha(15), Galpha(qs5), or Galpha(qG66Ds5)) to develop a reliable cell-based HTS method for 5-HT receptors. Among variable couplings between 5-HT receptors and G-proteins, we found that functional coupling of human 5-HT(6)R with Galpha(qG66Ds5) produced the highest levels of Ca(2+) signaling in HEK293 cells as measured by the fluorescence-based HTS plate reader, FDSS6000. After validation of this new 5-HT(6)R HTS system (Z'-factor = 0.56) in 96-well plates and characterization of the pharmacological profile of the 5-HT(6)R, we screened approximately 500 synthetic chemical compounds including butanamide and benzenesulfonamide derivatives. Based on this preliminary screening, we found that the butanamide derivative LSG11104 produced an IC(50) value of 6.3 microM. This compound will serve as a lead structure for further chemical modification to develop novel 5-HT(6)R ligands. Furthermore, we demonstrated that this HTS method can be utilized to identify proteins that modulate 5-HT(6)R function and present Fyn tyrosine kinase as an example, which is already known as a 5-HT(6)R interacting protein. Taken together, these results suggest that the 5-HT(6)R/Galpha(qG66Ds5) FDSS6000 system can be utilized to screen for selective 5-HT(6)R ligands and to examine any functional relationships between 5-HT(6)R and its binding proteins.     

Intermolecular Double Prins‐Type Cyclization: A Facile and Efficient Synthesis of 1,6‐Dioxecanes

Double or nothing : The title reaction converts a range of aromatic aldehydes and allenylmethyl/allyl silanes into 1,6‐dioxecane derivatives in good to excellent yields (see scheme; Ar=aryl, Tf=triflate, THF=tetrahydrofuran, TMS=trimethylsilyl). In addition, the bisdiene product has been transformed into the corresponding tricyclic compound through a Diels–Alder reaction.

     

γ–α Solid–solid transition of isotactic polypropylene

X-ray diffraction patterns have been taken as a function of time and temperature on a sample of polypropylene held under high pressure (4.14 kbar) for 180 hr. at a temperature of 248°C. and subsequently cooled to room temperature. The molded sample initially crystallizes in the triclinic γ–phase but transforms to the γ–phase at elevated temperatures. The rate of conversion from γ to α is a function of time and temperature and tends to approach a constant value with increasing time. The nature of the thermal changes occurring in the sample was also studied by differential scanning calorimetry. It appears that at low scan speeds, there is a solid–solid transformation from the α-phase to the γ–phase, but at high scan speeds, the γ–phase melts without conversion to the α-phase.     

Influence of pressure on yield and fracture in polymers

Some new data on the effects of pressure on a poly(p-oxybenzoyl) polymer are presented and existing data on various other polymers are reviewed and analyzed. It is demonstrated that the effect of pressure on the elastic response of a polymer depends on the location of T_g relative to room temperature, and that the modulus-pressure data can be used to estimate the pressure shift of T_g. Also, the pressure coefficient of the modulus increase can be deduced from considerations of finite strain elasticity theory. There is a marked increase of tensile and compressive yield strengths with pressure and this can be interpreted in terms of a Mohr-Coulomb type of yield criterion. In some polymers, hydrostatic pressure inhibits cold drawing and reduces the elongation to fracture. However, in other polymers which at atmospheric pressure fracture prior to yielding, increasing the pressure above some critical value can cause significant increases in ductility. This effect is utilized to show that even rigid high-temperature polymers, like polymide, can be successfully cold extruded at room temperature if a proper high-pressure environment is present. The nature of the changes occurring near the brittle-ductile transition pressure have been investigated by use of the scanning electron microscope and the possible influence of the pressure medium has been examined. SEM pictures of fracture surfaces and fracture modes of various polymers will be presented.     

Platycodin D,a natural component of Platycodon grandiflorum,prevents both lysosome- and TMPRSS2-driven SARS-CoV-2 infection by hindering membrane fusion

An ongoing pandemic of coronavirus disease 2019 (COVID-19) is now the greatest threat to global public health. Herbal medicines and their derived natural products have drawn much attention in the treatment of COVID-19, but the detailed mechanisms by which natural products inhibit SARS-CoV-2 have not been elucidated. Here, we show that platycodin D (PD), a triterpenoid saponin abundant in Platycodon grandiflorum (PG), a dietary and medicinal herb commonly used in East Asia, effectively blocks the two main SARS-CoV-2 infection routes via lysosome- and transmembrane protease serine 2 (TMPRSS2)-driven entry. Mechanistically, PD prevents host entry of SARS-CoV-2 by redistributing membrane cholesterol to prevent membrane fusion, which can be reinstated by treatment with a PD-encapsulating agent. Furthermore, the inhibitory effects of PD are recapitulated by the pharmacological inhibition or gene silencing of NPC1, which is mutated in patients with Niemann–Pick type C (NPC) displaying disrupted membrane cholesterol distribution. Finally, readily available local foods or herbal medicines containing PG root show similar inhibitory effects against SARS-CoV-2 infection. Our study proposes that PD is a potent natural product for preventing or treating COVID-19 and that briefly disrupting the distribution of membrane cholesterol is a potential novel therapeutic strategy for SARS-CoV-2 infection.Subject terms: Viral infection, Lipid signalling     

Luminescence in the systems ZnS-CuAlS2 and ZnS-AgAlS2

ZnS-CuAlS₂ and ZnS-AgAlS₂ phosphors (denoted by CuAl and AgAl) have blue, green, and red emission bands. The excitation spectra of these bands have characteristic peaks. The effects of activator concentration on the parameters of the emission and excitation spectra are examined.