The transient-chelating-group-controlled stereoselective Rh(i)-catalyzed silylative aminocarbonylation of 2-alkynylanilines: access to (Z)-3-(silylmethylene)indolin-2-ones.

A new method involving mild acryl transient-chelating-group-controlled stereoselective Rh(i)-catalyzed silylative aminocarbonylation of 2-alkynylanilines with CO and silanes is presented for producing (Z)-3-(silylmethylene)indolin-2-ones. Upon using an acryl transient chelating group, 2-alkynylanilines undergo an unprecedented alkyne cis-silylrhodation followed by aminocarbonylation to assemble (Z)-3-(silylmethylene)indolin-2-ones. Mechanistic studies show that acryl transient chelating effects result in the key alkyne cis-silylrhodation process.

Formation and Antioxidant Activity of Maillard Reaction Products Derived from Different Sugar-amino Acid Aqueous Model Systems of Sesame Roasting.

This investigation was carried out to offer insight into the formation and antioxidant activity of Maillard reaction products (MRPs) derived from various sugar-amino acid model systems active in the roasting of sesame seeds. Reducing sugars (glucose, fructose, and xylose) and amino acids (serine, cystine, arginine, and lysine) present in sesame seeds were used to prepare the MRPs at various reaction times, and then the effect of reaction time on the MRPs derived from the various model systems was investigated. Within the first 15 min, the amounts of free amino groups decreased around 40% remaining amino groups of Lys-sugar model and around 75% remaining amino groups of Arg-sugar model. Results indicated that reducing sugar and free amino groups decreased obviously in Lys- and Arg-model systems. Based on correlation coefficient of antioxidant activities assessment and MRP formation in the Lys- and Arg-model systems above 0.978 and an extremely significant correlation in Pearson test exists, a conclusion could be made that these model systems are critical contributing factors in MRP formation during the roasting of sesame seeds. These findings offer insight into the formation and antioxidation of MRPs during the sesame seeds roasting.

Investigation on glucocorticoid receptors within platelets from adult patients with immune thrombocytopenia.

Objective: The expression of glucocorticoid receptors within platelets from newly diagnosed Immune Thrombocytopenia (ITP) patients in the adult was investigated.Methods: GR expression in platelets from newly diagnosed ITP patients and healthy controls was measured using flow cytometry. Subsequently, platelets RNA and proteins were isolated and used for confirming the flow cytometry results by using RT-qPCR and ELISA.Results: Flow cytometry showed that the percentages of platelets expressing GRα and GRß from ITP patients were significantly higher than those from healthy controls (P < 0.05). qPCR and ELISA confirmed that GRα and GRß were increased at both RNA transcription and protein expression levels within platelets from ITP patients compared with healthy controls.Conclusion: We speculated that the up-regulation of glucocorticoid receptor within platelets may be an important biological feature of platelets in patients with ITP, and may also play an important role in the treatment of ITP, which is worthy of further study.

Improvement of the oxidative stability of cold-pressed sesame oil using products from the Maillard reaction of sesame enzymatically hydrolyzed protein and reducing sugars.

BACKGROUND: In recent years, cold-pressed oils have become more and more popular with consumers. However, their oxidative stability is low. Improving the oxidative stability of cold-pressed oils will increase their shelf life. Maillard reaction products (MRPs) have been shown to promote the oxidative stability of lipids. In this study, products from the Maillard reaction of reducing sugars and sesame enzymatically hydrolyzed protein (SEHP) were added to cold-pressed sesame oils to improve their oxidative stability. RESULTS: Three types of MRPs from reducing sugars (xylose, fructose, and glucose) and SEHP were prepared. Xylose-SEHP MRPs prepared under optimum conditions had the highest antioxidant activities among the three. The optimum conditions for xylose-SEHP were as follows: reaction temperature, 130 °C; reaction time, 180 min; pH, 6.5; and sugar/protein ratio, 10:1. The addition of xylose-SEHP MRPs at a level of 20 g kg-1 could significantly improve the oxidative stability of cold-pressed sesame oil. Besides, the addition of MRPs reduced the loss of tocopherol. The interaction of MRPs with endogenous antioxidants in the sesame oil (sesamol and tocopherol) was proved by comparison with lard. There was a synergistic increase in antioxidant activity for the combination of MRPs and sesamol and the combination of MRPs and tocopherol. CONCLUSIONS: The results provide evidence that adding certain MRPs can improve the oxidative stability of cold-pressed sesame oil. © 2019 Society of Chemical Industry.

The photoredox alkylarylation of styrenes with alkyl N-hydroxyphthalimide esters and arenes involving C-H functionalization.

The In(OTf)3-promoted three-component photoredox alkylarylation of styrenes with alkyl NHP esters and arenes to access alkylated arene derivatives through C-C bond cleavage and C-H functionalization is reported. By utilizing visible-light photoredox catalysis, alkyl N-hydroxyphthalimide esters serving as alkyl carbon-centered radicals and a wide range of arenes (e.g., indoles, pyrrole, and electron-rich arenes) as nucleophiles were used to enable the introduction of various alkyl groups and aryl groups across the C[double bond, length as m-dash]C bonds with excellent selectivity and functional group tolerance.

The effect of Heweijiangni-decoction on esophageal morphology in a rat model of OVA-induced visceral hypersensitivity followed by acid exposure.

Heweijiangni decoction (HWJND) is an effective traditional Chinese medicine prescription in clinical treatment of nonerosive reflux disease (NERD). Esophageal hypersensitivity and acid contribute to the disease. However, the exact underlying mechanism of action remains unclear. In this study, we observed the effect of HWJND on esophageal morphology in a rat model of ovalbumin (OVA)-induced visceral hypersensitivity followed by acid exposure. Esophageal morphology was assessed by measuring the extent of dilated intercellular spaces (DIS), desmosome disruption, and mitochondrial fragmentation. HWJND in low, moderate, and high doses relieved DIS and desmosome disruption in esophageal epithelium compared with model group (P<0.05 for all doses). In addition, HWJND in high dose protected mitochondria from fragmentation (P<0.05). Other findings suggest that DIS and mitochondrial fragmentation are independent events, and that omeprazole protects mitochondria. Overall, HWJND significantly resists esophageal morphology changes in OVA-induced and acid exposure rat model.

Alkylarylation of styrenes via direct C(sp3)-Br/C(sp2)-H functionalization mediated by photoredox and copper cooperative catalysis.

For straightforward access to various substituted 1,1-diarylalkanes a photoredox-catalyzed and copper-promoted 1,2-alkylarylation reaction of styrenes has been developed, which uses α-carbonyl alkyl bromides and N,N-disubstituted anilines as functionalization reagents. In this radical difunctionalization reaction, α-carbonyl alkyl bromides, including primary-, secondary- and tertiary-α-bromoalkyl ketone esters, malonic esters and cycloalkane were transformed to the corresponding 1,1-diarylalkanes in moderate to good yields at room temperature. Notably, this transformation provided a new route for the C-H alkylation of N,N-disubstituted anilines with high para-selectivity beyond the typical Friedel-Crafts alkylation.

Yinchen Linggui Zhugan Decoction Ameliorates Nonalcoholic Fatty Liver Disease in Rats by Regulating the Nrf2/ARE Signaling Pathway.

Yinchen Linggui Zhugan Decoction (YCLGZGD) is the combination of Linggui Zhugan (LGZGD) and Yinchenhao (YCHD) decoctions, two famous traditional Chinese medicine prescriptions. In previous studies, we found that Yinchen Linggui Zhugan Decoction (YCLGZGD) could regulate lipid metabolism disorder and attenuate inflammation in pathological process of nonalcoholic fatty liver disease (NAFLD). However, the exact underlying mechanism remains unknown. The aim of this study was to explore the effect of Yinchen Linggui Zhugan Decoction on experimental NAFLD and its mechanism in rats with high-fat diet (HFD) which was established by 8-week administration of HFD. YCLGZGD, LGZGD, and YCHD were administered daily for 4 weeks, after which the rats were euthanized. The level of blood lipid, liver enzymes, H&E, and Oil Red O staining were determined to evaluate NAFLD severity. Western blotting and real-time polymerase chain reaction were, respectively, used to determine hepatic protein and gene expression of Keap1, Nrf2, NQO1, and HO-1. Oral YCLGZGD ameliorated HFD-induced NAFLD. Furthermore, YCLGZGD increased the protein and gene expression of Nrf2, NQO1, and HO-1 without changing Keap1. Overall, these results suggest that YCLGZGD ameliorates HFD-induced NAFLD in rats by upregulating the Nrf2/ARE signaling pathway.

An ErChen and YinChen Decoction Ameliorates High-Fat-Induced Nonalcoholic Steatohepatitis in Rats by Regulating JNK1 Signaling Pathway.

ErChen and YinChen decoction (ECYCD) is an effective traditional Chinese medicine and has been widely used in traditional Chinese medicine to treat nonalcoholic steatohepatitis (NASH), with good curative effects. However, the specific mechanisms underlying these effects are unclear. In this study, we determined the efficacy of ECYCD in a high-fat diet-induced NASH rat model, established by 8-week administration of a high-fat diet. ECYCD was administered daily for 4 weeks, after which the rats were euthanized. The results demonstrated that ECYCD ameliorated high-fat diet-induced NASH, as evidenced by decreased liver indexes, reduced hepatic lipid deposition and liver injury, lower serum biochemistry markers (including low-density lipoprotein), and reduced HOMA-IR scores. Moreover, levels of free fatty acids, tumor necrosis factor, and malondialdehyde were decreased, whereas glutathione was increased in the liver. Serum high-density lipoprotein was also increased in the liver, and ECYCD regulated the c-Jun N-terminal kinase 1 (JNK1) signaling pathway by decreasing the levels of JNK1 protein, JNK1 mRNA, activator protein- (AP-) 1 protein, AP-1 mRNA, and phospho-insulin receptor substrate- (IRS-) 1ser307 and increasing phopsho-PKBser473 levels. These results suggested that ECYCD could ameliorate high-fat diet-induced NASH in rats through JNK1 signaling. ECYCD may be a safe therapeutic option for the treatment of NASH.