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Allylboration of ketones and imines with a bifunctional allylboron reagent is reported. Addition of the bifunctional allylboronate to a broad scope of ketones gave tertiary alcohols in excellent yields at ambient temperature without any catalyst or additive. Allylboration of cyclic aldimines also proceeded to give allylated products in good yields under the same reaction conditions. The allylsilane moiety in the product underwent a second allylation with aldehydes or acetals. As such, the bifunctional allylboron reagent serves as a useful linchpin to join two distinct carbonyl compounds to provide synthetically useful intermediates.Influenza and dengue viruses present a growing global threat to public health. Both viruses depend on the host endoplasmic reticulum (ER) glycoprotein folding pathway. In 2014, Sadat et al. reported two siblings with a rare genetic defect in ER α-glucosidase I (ER Glu I) who showed resistance to viral infections, identifying ER Glu I as a key antiviral target. Here, we show that a single dose of UV-4B (the hydrochloride salt form of N-(9'-methoxynonyl)-1-deoxynojirimycin; MON-DNJ) capable of inhibiting Glu I in vivo is sufficient to prevent death in mice infected with lethal viral doses, even when treatment is started as late as 48 h post infection. The first crystal structure of mammalian ER Glu I will constitute the basis for the development of potent and selective inhibitors. Targeting ER Glu I with UV-4B-derived compounds may alter treatment paradigms for acute viral disease through development of a single-dose therapeutic regime.PEP 1b is a novel immunoregulatory protein isolated from Pleurotus eryngii, a popular edible mushroom. In this study, isobaric tags for relative and absolute quantitation (iTRAQ) approach and bioinformatics analysis were used to characterize the PEP-1b-induced proteome alterations in Raw 264.7 macrophage cells, to comprehensively excavate the molecular mechanisms involved in the immunoregulatory effects of PEP 1b. In comparison to the control group, PEP 1b treatment significantly changed the expression of 292 proteins, including 191 upregulated and 101 downregulated proteins. Bioinformatics analysis showed that PEP-1b-regulated proteins were involved in 437 biological process domains, 131 cellular component domains, and 90 molecular function domains. Moreover, PEP 1b played the role of immunomodulator by mainly modulating the Rap1 signaling pathway, Wnt signaling pathway, Ras signaling pathway, and PI3K-Akt signaling pathway. Interestingly, PEP 1b regulated the proteins involved in the immune system, signal transduction, and transport processes, which were related to the immunoregulatory effects of PEP 1b. The western blotting analysis confirmed that the immune-boosting activities of PEP 1b were associated with modulating the expression of Sqstm1, Cox2, Rap1b, and Pyk2. The current research provided a comprehensive understanding of the immunoregulatory effects and molecular mechanisms involved in the PEP 1b supplementation.Grapevine canes are an abundant by-product of wine industry. The stilbene contents of Vitis vinifera cultivars have been largely studied, but little is known about the stilbene contents of wild Vitis accessions. Moreover, there have only been few studies on the quantification of other phenolic compounds in just pruned grapevine canes. In our study, we investigated the polyphenol profile of 51 genotypes belonging to 15 Vitis spp. Thirty-six polyphenols (20 stilbenes, six flavanols, seven flavonols and three phenolic acids) were analyzed by High Performance Liquid Chromatography coupled with a Triple Quadrupole Mass Spectrometer. click here Our results suggest that some wild Vitis accessions could be of interest in terms of concentration of bioactive polyphenols and that flavanols contribute significantly to the antioxidant activity of grapevine cane extracts. To the best of our knowledge, this is the most exhaustive study of the polyphenolic composition of grapevine canes of wild Vitis spp.An extract of Galtonia regalis from the Natural Products Discovery Institute showed moderate antiplasmodial activity, with an IC50 value less than 1.25 μg/mL. The two known cholestane glycosides 1 and 2 and the five new cholestane glycosides galtonosides A-E (3-7) were isolated after bioassay-directed fractionation. The structures of the new compounds were determined by interpretation of their NMR and mass spectra. Among these compounds, galtonoside B (4) displayed the most potent antiplasmodial activity, with an IC50 value of 0.214 μM against the drug-resistant Dd2 strain of Plasmodium falciparum.Maltooligosyltrehalose synthase (MTSase) is a key enzyme for the production of trehalose from starch. Thermophilic MTSases offer advantages for trehalose production but suffer from low yield. In this study, directed evolution was used to increase the production of Sulfolobus acidocaldarius MTSase (SaMTSase) in Escherichia coli. Mutant libraries constructed using error-prone polymerase chain reaction were assessed using high-throughput activity assays. Three mutants with enhanced activities were obtained, the best of which (mutant D-4) exhibited 2.4 times greater activity than wild-type SaMTSase. The specific activity and catalytic efficiency of D-4 were also greater than those of wild-type SaMTSase. The D-4 activity (624.7 U·mL-1) produced in a 3 L fermenter was 2.0 times greater than that of wild-type SaMTSase. Because the same trehalose yield was obtained using an equal amount of either D-4 or wild-type SaMTSase activity, using D-4 will significantly lower the cost of trehalose production. The activities of the individual mutations present in the three SaMTSase mutants obtained using directed evolution were analyzed. Mutants F284V and T439A exhibited the greatest increases in enzyme activity. Homology models suggested that the decreased side-chain size, weakened hydrophobicity, and decreased interaction might enhance the flexibility of the loop containing catalytic residue Asp443, which was conducive to catalysis.While being considered as the building block of ice on a hydrophobic metal surface, the global minimum of the water hexamer is still elusive, which has impeded our understanding of water/metal interfaces. Herein, we comprehensively investigate water hexamer on Cu(111) theoretically and propose the boat configuration as the new in situ adsorption configuration from the scanning tunneling microscope experiments. All existing experimental measurements can therefore be well reproduced. Calculations in high-level theories reveal that the boat configuration is indeed the global minimum under experimental conditions, solving a long-standing discrepancy.