Synthesis of 1,1-Diarylvinylsulfides via Visible-Light-Promoted Cascade Reaction of Alkynoates with Phenyl Disulfides.

Without any additives and photocatalysts, the visible-light-promoted radical cascade reaction between alkynoates and phenyl disulfides has been developed at room temperature. Through S-S bond photolysis and homolytic cleavage, addition of a sulfur radical, aryl migration, decarboxylation, and H atom abstraction, the cascade reaction provides an efficient and practical route to trisubstituted 1,1-diarylvinylsulfides with a wide scope of substrates and good to excellent yields.

Huaju Xiaoji Formula Regulates ERS-lncMGC/miRNA to Enhance the Renal Function of Hypertensive Diabetic Mice with Nephropathy.

Background: Better therapeutic drugs are required for treating hypertensive diabetic nephropathy. In our previous study, the Huaju Xiaoji (HJXJ) formula promoted the renal function of patients with diabetes and hypertensive nephropathy. In this study, we investigated the therapeutic effect and regulation mechanism of HJXJ in hypertensive diabetic mice with nephropathy. Methods: We constructed a mouse hypertensive diabetic nephropathy (HDN) model by treating mice with streptozotocin (STZ) and nomega-nitro-L-arginine methyl ester (LNAME). We also constructed a human glomerular mesangial cell (HGMC) model that was induced by high doses of sugar (30 mmol/mL) and TGFß1 (5 ng/mL). Pathological changes were evaluated by hematoxylin and eosin (H&E) staining, periodic acid Schiff (PAS) staining, and Masson staining. The fibrosis-related molecules (TGFß1, fibronectin, laminin, COL I, COL IV, α-SMA, and p-smad2/3) were detected by enzyme-linked immunosorbent assay (ELISA). The mRNA levels and protein expression of endoplasmic reticulum stress, fibrosis molecules, and their downstream molecules were assessed using qPCR and Western blotting assays. Results: Administering HJXJ promoted the renal function of HDN mice. HJXJ reduced the expression of ER stress makers (CHOP and GRP78) and lncMGC, miR379, miR494, miR495, miR377, CUGBP2, CPEB4, EDEM3, and ATF3 in HDN mice and model HGMCs. The positive control drugs (dapagliflozin and valsartan) also showed similar effects after treatment with HJXJ. Additionally, in model HGMCs, the overexpression of CHOP or lncMGC decreased the effects of HJXJ-M on the level of fibrosis molecules and downstream target molecules. Conclusion: In this study, we showed that the HJXJ formula may regulate ERS-lncMGC/miRNA to enhance renal function in hypertensive diabetic mice with nephropathy. This study may act as a reference for further investigating whether combining HJXJ with other drugs can enhance its therapeutic effect. The findings of this study might provide new insights into the clinical treatment of hypertensive diabetic nephropathy with HJXJ.

Quantitative analysis and simulation of anti-inflammatory effects from the active components of Paino Powder () in rats.

OBJECTIVE: To explore different combinations of the active ingredients of Paino Powder ()), including paeoniflorln, naringin, neohesperidln and platyeodin-D, which are responsible for the inhibition of carrageenin-induced edema in rats, and to evaluate the performance of the orthogonal simulation method in quantitative analysis and the simulation of the combinations. METHODS: A 1-level (used) and 2-level (unused) orthogonal design was applied to assign 7 combinations of active components. Aspirin and saline were set as the two controls. The carrageen In-Induced edema in the right hind paws of rats was established as the acute inflammation model The efficacy indices were expressed by the area under the curve (AUC) and the peak value of the swelling change (%) over time in rats. RESULTS: Compared with the saline group, the rats in active component combinations showed a significant reduction of AUG and peak value in the swelling (P<0.05). The maximum anti-inflammatory effect was from the whole four-ingredient combination. Among the four ingredients, naringin showed a dominant contribution to the combination, while paeoniflorin > platycodin-D > naringin contributed in succession. These results are consistent with the results of computer simulation. CONCLUSIONS: A single component from Paino Powder does not exhibit any anti-inflammatory effect, but some combinations show such effect. The strongest inhibition to edema comes from the full 4-ingredient combination. The orthogonal simulation method is feasible in the research on decomposed formulas of Chinese medicine.

[Anti-inflammatory effects and quantitative study of the combinations of active ingredients of Painong powder in mice].

OBJECTIVE: To study the anti-inflammatory effects of the combinations of active components of Painong powder, a compound traditional Chinese herbal medicine, and the quantitative analysis of their interactions. METHODS: The mouse model of acute inflammation with increase of capillary permeability was induced by intraperitoneal injection of acetic acid. An orthogonal design with 2 levels (used and unused) was applied to assign the combinations groups of active ingredients including naringin and neohesperidin, peoniflorin, and platycodin. Aspirin and normal saline were administered as control. The pharmacodynamic interactions were analyzed by the optical density (OD) of infiltrated Evans blue. RESULTS: The different combinations of active ingredients showed anti-inflammatory effect with different degree, and the predicted values of OD varied from 0.115 to 0.170. The maximum anti-inflammatory effect was from the combination of naringin, neohesperidin, paeoniflorin and platycodin, better than that of the saline group (P < 0.01). However, there was no significant difference as compared with the aspirin group (P > 0.05). Paeoniflorin showed a dominant contribution to the formula, and platycodin the least. The combination of all active components exhibited synergism. CONCLUSION: The results suggest that all the ingredients are efficacious constituents of the formula, and paeoniflorin shows a dominant contribution to the formula. More information about prescription compatibility can be obtained by the orthogonal simulation method.

Synthesis of bioactive ceramic on the titanium substrate by micro-arc oxidation.

Bioactive ceramic films on titanium substrate are prepared successfully by micro-arc oxidation in electrolyte solution containing NaOH only. The coatings are prepared by micro-arc oxidation at various applied current densities (200-400 mA/cm2) and in NaOH electrolyte with different concentrations. The XRD shows that they are composed of rutile, anatase, Na2Ti6O13, and Na2Ti4O9 phases. The composition and surface morphologies are strongly dependent on the applied current density and electrolyte concentration. For example, at high current density, the phase is mainly composed of rutile and Na2Ti6O13, and at high electrolyte concentration, it is Na2Ti6O13 phase. The morphologies of the samples vary with the increase of current and electrolyte concentration. The apatite-inducing ability of bioactive ceramic films is evaluated in biological model fluids. After soaking in biological model fluids, the titania-based coatings containing Na2Ti6O13 phase have excellent capability of inducing bone-like apatite.

Direct preparation of CaTi4 (PO4)6 coatings on the surface of titanium substrate by micro arc oxidation.

CaTi(4) (PO(4))(6) coatings was prepared on the surface of CP (commercially pure) Titanium substrate via micro arc oxidation in a newly designed electrolyte system. The preparation method -micro arc oxidation, as well as its discharge characterization was described and studied. The phases, morphology, chemical composition of the coatings were characterized by XRD, EDX and SEM analysis respectively. The results show: the main phase of the prepared coating was CaTi(4) (PO(4))(6) which is a bioactive coating material, the morphology of the coating was rather coarse and not like that of traditional MAO coating which was full of pores. Also the samples prepared in different electrolyte systems were studied and compared.