LC/MS-guided isolation and GNPS procedures to identify flavonoid of HCoV-OC43 inhibitors.

The screening of based target compounds supported by LC/MS, MS/MS and Global Natural Products Social (GNPS) used to identify the compounds 1-10 of Butea monsperma. They were evaluated in human malignant embryonic rhabdomyoma cells (RD cells) infected with Human coronavirus OC43 (HCoV-OC43) and showed significant inhibitory activity. Target inhibition tests showed that compounds 6 and 8 inhibited the proteolytic enzyme 3CLpro, which is widely present in coronavirus and plays an important role in the replication process, with an effective IC50 value. The study confirmed that dioxymethylene of compound 8 may be a key active fragment in inhibiting coronavirus (EC50 7.2 µM, SI > 139.1). The results have led to identifying natural bioactive compounds for possible inhibiting HCoV-OC43 and developing drug for Traditional Chinese Medicine (TCM).

CRHR1 mediates the transcriptional expression of pituitary hormones and their receptors under hypoxia.

Hypothalamus-pituitary-adrenal (HPA) axis plays critical roles in stress responses under challenging conditions such as hypoxia, via regulating gene expression and integrating activities of hypothalamus-pituitary-targets cells. However, the transcriptional regulatory mechanisms and signaling pathways of hypoxic stress in the pituitary remain to be defined. Here, we report that hypoxia induced dynamic changes in the transcription factors, hormones, and their receptors in the adult rat pituitary. Hypoxia-inducible factors (HIFs), oxidative phosphorylation, and cAMP signaling pathways were all differentially enriched in genes induced by hypoxic stress. In the pituitary gene network, hypoxia activated c-Fos and HIFs with specific pituitary transcription factors (Prop1), targeting the promoters of hormones and their receptors. HIF and its related signaling pathways can be a promising biomarker during acute or constant hypoxia. Hypoxia stimulated the transcription of marker genes for microglia, chemokines, and cytokine receptors of the inflammatory response. Corticotropin-releasing hormone receptor 1 (CRHR1) mediated the transcription of Pomc, Sstr2, and Hif2a, and regulated the function of HPA axis. Together with HIF, c-Fos initiated and modulated dynamic changes in the transcription of hormones and their receptors. The receptors were also implicated in the regulation of functions of target cells in the pituitary network under hypoxic stress. CRHR1 played an integrative role in the hypothalamus-pituitary-target axes. This study provides new evidence for CRHR1 involved changes of hormones, receptors, signaling molecules and pathways in the pituitary induced by hypoxia.

The influence of heat treatment on acid-tolerant emulsions prepared from acid soluble soy protein and soy soluble polysaccharide complexes.

This research presents a green procedure to prepare oil in water (O/W) emulsion from acid soluble soy protein (ASSP) and soy soluble polysaccharide (SSPS), a long-term stable nanoscale system for delivering the lipophilic components. The emulsion technique involved the preparation complexion using ASSP and SSPS by electrostatic and hydrophobic interactions as well as high pressure homogenization. The average diameter of the droplet of emulsions (fresh and heated) is 263±2nm. Such emulsions resulted in heating stable dispersions containing corn oil at the concentration of 20.0%, even at the pH around the isoelectric points of ASSP. After 90days storage at 4°C, the mean diameter of emulsions after heating at 80°C for 60min is 314±1nm compared with 341±3nm of emulsions unheated. The heat-stability of dispersions were affected by emulsion conditions, so the present research demonstrates the emulsion stability against heat treatment, ionic strength and pH change.

Fabrication and Characterization of Stable Soy ß-Conglycinin-Dextran Core-Shell Nanogels Prepared via a Self-Assembly Approach at the Isoelectric Point.

The preparation of soy ß-conglycinin-dextran nanogels (∼90 nm) went through two stages, which are safe, facile, and green. First, amphiphilic graft copolymers were formed by dextran covalently attaching to ß-conglycinin via Maillard dry-heating reaction. Second, the synthesized conjugates were heated above the denaturation temperature at the isoelectric point (pH4.8) so as to assemble nanogels. The effects of pH, concentration, heating temperature, and time on the fabrication of nanogels were examined. The morphology study displayed that the nanogels exhibited spherical shape with core-shell structures, which was reconfirmed by zeta-potential investigation. Both circular dichroism spectra and surface hydrophobicity analyses indicated that the conformations of ß-conglycinin in the core of nanogels were changed, and the latter experiment further revealed that the hydrophobic groups of ß-conglycinin were exposed to the surface of protein. The nanogels were stable against various conditions and might be useful to deliver hydrophobic bioactive compounds.