Background The aim of this study was to evaluate the clinical efficacy of Xuanfei Baidu Decoction (XBD) combined with conventional drug therapy compared with conventional medicine alone in patients with coronavirus disease 2019 (COVID-19). Methods Forty-two patients with COVID-19 were randomly assigned to XBD plus conventional medicine (n = 22) and conventional medicine alone (n = 20). Both groups were treated for 1 week. The primary endpoint was the disappearance rate of main symptoms (fever, cough, and fatigue). Results Compared with the conventional medicine, the disappearance rate of clinical symptoms such as fever, cough, fatigue and loss of appetite in the experimental group were significantly reduced (P < 0.05). The number of white blood cells and lymphocytes in the experimental group increased significantly (P < 0.05), which all returned to normal parameters. Meanwhile, the C-reactive protein and erythrocyte sedimentation rate in the experimental group were significantly reduced (P < 0.05). Conclusion XBD combined with conventional medicine may significantly improve patient's clinical symptoms, increase the number of white blood cells and lymphocytes to improve immunity, and also significantly reduce C-reactive protein and erythrocyte sedimentation rate to play an anti-inflammatory effect. However, it needs to be confirmed by a large sample study. Clinical trial registration China Clinical Trial Registry (ChiCTR2000034795).

A strategy for the NHC-catalyzed asymmetric synthesis of spirobenzazepinones, spiro-1,2-diazepinones, and spiro-1,2-oxazepinones has been developed via [3+4]-cycloaddition reactions of isatin-derived enals (3C component) with in-situ-generated aza-o-quinone methides, azoalkenes, and nitrosoalkenes (4atom components). The [3+4] annulation strategy leads to the seven-membered target spiro heterocycles bearing an oxindole moiety in high yields and excellent enantioselectivities with a wide variety of substrates. Notably, the benzazepinone synthesis is atroposelective and an all-carbon spiro stereocenter is generated.

In chemical crystallography, the thermal motion of scattering centres is commonly described by anisotropic displacement parameters (ADPs). Very recently, it has been shown that ADPs are not only accessible by diffraction experiments but also via theory: this emerging approach seems promising but must be thoroughly tested. In this study, we have performed specifically tailored X-ray diffraction (XRD) experiments in fine steps between 100 and 300 K which allow detailed comparison to ab initio data from dispersion-corrected density functional theory (DFT) combined with periodic lattice-dynamics. The compound chosen for this study, crystalline pentachloropyridine IJC 5 NCl 5 ), is well suited for this purpose: it represents a molecular crystal without H atoms, thus posing no challenge to XRD; its solid-state structure is controlled by dispersion and halogen-bonding interactions; and the ADPs associated with the peripheral Cl atoms show strong temperature dependence. Quality criteria in direct and in reciprocal space prove that ADPs are predicted with high confidence for the temperature range between 100 and 200 K, and that several economic dispersion corrections to DFT can be reliably employed for this purpose. Within the limits we have explored here, the ab initio prediction of ADPs appears to be a facile and complementary tool, especially in those cases where diffraction data cannot provide a straightforward model for thermal motion.7414 | CrystEngComm, 2015, 17, 7414-7422This journal is

A manganese-catalyzed regio- and stereoselective hydroarylation of allenes is reported. The C-H functionalization method provides access to various alkenylated indoles in excellent yields. Moreover, a hydroarylation/cyclization cascade involving an unexpected C-N bond cleavage and aryl shift has been developed, which provides a new synthetic approach to substituted pyrroloindolones.

Inflammation has been shown to play an important role in the mechanisms involved in the pathogenesis of hypertension. Connexins (Cxs)-based gap junction channels (GJCs) or hemichannels (HCs) are involved in the maintenance of homeostasis in the immune system. However, the role of Cx43-based channels in T-lymphocytes in mediating the immune response in essential hypertension is not fully understand. The present study was designed to investigate the role of Cxs-based channels in T lymphocytes in the regulation of hypertension-mediated inflammation. The surface expressions of T lymphocyte subtypes, Cx40/Cx43, and inflammatory cytokines (IFN-γ (interferon-gamma) and TNF-ɑ (tumor necrosis factor alpha)) in T cells, as well as gap junction communication of peripheral blood lymphocytes from essential hypertensive patients (EHs) and normotensive healthy subjects (NTs) were detected by flow cytometry. Expression levels and phosphorylation of Cx43 protein in peripheral blood lymphocytes of EHs and NTs were analyzed by Western blot. The proliferation rate of peripheral blood mononuclear cells (PBMCs) after treatment with a Cxs inhibitor was examined by a CCK-8 assay. The levels of inflammatory cytokines were detected using ELISA. Within the CD3+ T cell subsets, we found a significant trend toward an increase in the percentage of CD4+ T cells and CD4+/CD8+ ratio as well as in serum levels of IFN-γ and TNF-ɑ in the peripheral blood of EHs compared with those in NTs. Moreover, the peripheral blood lymphocytes of EH patients exhibited enhanced GJCs formation, increased Cx43 protein level and Cx43 phosphorylation at Ser368, and a significant increase in Cx40/Cx43 surface expressions levels in CD4+ or CD8+ T lymphocytes. Cx43-based channel inhibition by a mimetic peptide greatly reduced the exchange of dye between lymphocytes, proliferation of stimulated lymphocytes and the pro-inflammatory cytokine levels of EHs and NTs. Our data suggest that Cx40/Cx43-based channels in lymphocytes may be involved in the regulation of T lymphocyte proliferation and the production of pro-inflammatory cytokines, which contribute to the hypertensive inflammatory response.

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Abstract:The enantioselective organocatalytic nucleophilic addition of thiols to isatin-derived ketimines has been developed utilizing only 1 mol% of an enantiopure BINOL-derived phosphoric acid.The new protocol provides a series of isatin-derived N,S-acetals in high yields (up to 98%) and high enantioselectivities (up to 93% ee).

BackgroundImbalances in circulating T lymphocytes play critical roles in the pathogenesis of hypertension-mediated inflammation. Connexins (Cxs) in immune cells are involved in the maintenance of homeostasis of T lymphocytes. However, the association between Cxs in peripheral blood T lymphocytes and hypertension-mediated inflammation remains unknown. This study was designed to investigate the role of Cxs in T lymphocytes in hypertension-mediated inflammation in spontaneously hypertensive rats (SHRs).MethodsThe systolic blood pressure (SBP) in Wistar-Kyoto (WKY) rats and SHRs was monitored using the tail-cuff method. The serum cytokine level was determined using ELISA. The proportions of different T-lymphocyte subtypes in the peripheral blood, the expressions of Cx40/Cx43 in the T-cell subtypes, and the gap junctional intracellular communication (GJIC) of peripheral blood lymphocytes were measured using flow cytometry (FC). The accumulations of Cx40/Cx43 at the plasma membrane and/or in the cytoplasm were determined using immunofluorescence staining. The in vitro mRNA levels of cytokines and GJIC in the peripheral blood lymphocytes were respectively examined using real-time PCR and FC after treatment with Gap27 and/or concanavalin A (Con A).ResultsThe percentage of CD4+ T cells and the CD4+/CD8+ ratio were high, and the accumulation or expressions of Cx40/Cx43 in the peripheral blood lymphocytes in SHRs were higher than in those of WKY rats. The percentage of CD8+ and CD4+CD25+ T cells was lower in SHRs. The serum levels of IL-2, IL-4 and IL-6 from SHRs were higher than those from WKY rats, and the serum levels of IL-2 and IL-6 positively correlated with the expression of Cx40/Cx43 in the peripheral blood T lymphocytes from SHRs. The peripheral blood lymphocytes of SHRs exhibited enhanced GJIC. Cx43-based channel inhibition, which was mediated by Gap27, remarkably reduced GJIC in lymphocytes, and suppressed IL-2 and IL-6 mRNA expressions in Con A stimulated peripheral blood lymphocytes.ConclusionsOur data suggest that Cxs may be involved in the regulation of T-lymphocyte homeostasis and the production of cytokines. A clear association was found between alterations in Cxs expression or in Cx43-based GJIC and hypertension-mediated inflammation.