3-[1-(3,4-Dichloro­phen­yl)eth­yl]-1,3-thia­zinane-2-thione

In the title compound, C12H13Cl2NS2, the thia­zinane ring adopts a half-boat conformation. An intra­molecular C—H⋯S hydrogen bond is observed. In the crystal structure, centrosymmetrically related mol­ecules inter­act through an aromatic π–π stacking inter­actions, with a centroid–centroid separation of 3.790 (2) Å

3-(1-Phenyl­ethyl)-1,3-thia­zinane-2-thione

In the title mol­ecule, C12H15NS2, the 1,3-thia­zinane ring has a half-boat conformation; the C atom at position 5 deviates by 0.715 (2) Å from the mean plane (P) of the remaining five atoms. Plane P and the phenyl ring form a dihedral angle of 83.62 (3)°. In the crystal structure, weak inter­molecular C—H⋯S hydrogen bonds link mol­ecules related by translation along the axis a into chains

Hypoglycemic and Hypolipidemic Effects of Malonyl Ginsenosides from American Ginseng (<i>Panax quinquefolius</i> L.) on Type 2 Diabetic Mice

American ginseng (Panax quinquefolius L.) is popularly consumed as traditional herbal medicine and health food for the treatment of type 2 diabetes mellitus (T2DM). Malonyl ginsenosides (MGR) are the main natural ginsenosides in American ginseng. However, whether the malonyl ginsenosides in P. quinquefolius (PQ-MGR) possess antidiabetic effects has not been explored yet. In this study, the antidiabetic effects and the underlying mechanism of PQ-MGR in high-fat diet/streptozotocin (HFD/STZ)-induced T2DM mice were investigated. The chemical composition was analyzed by high-performance liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MS/MS). Our results showed that 14 malonyl ginsenosides were identified in the PQ-MGR. Among them, the content of m-Rb1 represented about 77.4% of the total malonyl ginsenosides. After a 5-week experiment, the PQ-MGR significantly reduced the fasting blood glucose (FBG), triglyceride (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), nonesterified fatty acid (NEFA), alanine transaminase (ALT), and aspartate transaminase (AST) levels and improved glucose tolerance and insulin resistance. Furthermore, Western blot analysis demonstrated that the protein expressions of p-PI3K, p-AKT, p-AMPK, p-ACC, PPARγ, and GLUT4 in the liver and skeletal muscle were significantly upregulated after PQ-MGR treatment. In contrast, the protein expressions of p-IRS1 and p-JNK were significantly downregulated. Our results revealed that PQ-MGR could ameliorate glucose and lipid metabolism and insulin resistance in T2DM via regulation of the insulin receptor substrate-1/phosphoinositide3-kinase/protein-kinase B (IRS1/PI3K/Akt) and AMP-activated protein kinase/acetyl-CoA carboxylase (AMPK/ACC) pathways. These findings suggest that PQ-MGR may be used as an antidiabetic candidate drug for T2DM treatment

Circulating microRNAs as novel biomarkers for dilated cardiomyopathy

Background: Circulating microRNAs (miRNAs) potentially carry disease-specific information. In the current study, we aim to characterize the miRNA signature in plasma from dilated cardiomyopathy (DCM) patients and assess the possible correlation between expression levels of circulating miRNAs and symptom severity in DCM patients. Methods: Using microarray-based miRNA expression profiling, we compared the miRNA expression levels in plasma samples from 4 DCM patients and 3 healthy controls. The expression levels of selected differentially expressed, upregulated miRNAs (miR-3135b, miR-3908 and miR-5571-5p) were validated independently in plasma samples from 19 DCM patients and 20 controls. Results: We observed that plasma miR-3135b (p &lt; 0.001), miR-3908 (p &lt; 0.001) and miR-5571-5p (p &lt; 0.001) were significantly upregulated in DCM patients. The area under receiver operating characteristic (ROC) curves for the 3 miRNAs ranged from 0.83 to 1.00. Moreover, miR-5571-5p levels in plasma were significantly upregulated with severe New York Heart Association (NYHA) classification (p &lt; 0.05). Conclusions: The circulating miRNAs (miR-3135b, miR-3908 and miR-5571-5p) have potential as diagnostic biomarkers for DCM. Additionally, miR-5571-5p correlated with NYHA classification.

PRODUCTION, DIELECTRIC PROPERTY AND MICROWAVE ABSORPTION PROPERTY OF SiC(Fe) SOLID SOLUTION POWDER BY SOL-GEL METHOD

SiC(Fe) solid solution powders were synthesized by sol–gel method under different reaction time, using methyltriethoxysilane as the silicon and carbon source and analytic ferric chloride as the dopant, respectively. The synthesized powders have been characterized by XRD, SEM and Raman spectra. Results show that the lattice constant decreases with increasing reaction time. The electric permittivities of SiC samples were determined in the frequency range of 8.2 ~ 12.4 GHz. Results show that the permittivity of SiC decreases with increasing reaction time. The SiC(Fe) solid solution powder with reaction time of 4 h with 2 mm thickness exhibit the best microwave absorption property in X-band range (8.2 - 12.4 GHz). The microwave absorption mechanism has been discussed

Metabolic Patterns and Biotransformation Activities of Resveratrol in Human Glioblastoma Cells: Relevance with Therapeutic Efficacies

-resveratrol rather than its biotransformed monosulfate metabolite exerts anti-medulloblastoma effects by suppressing STAT3 activation. Nevertheless, its effects on human glioblastoma cells are variable due to certain unknown reason(s).Citing resveratrol-sensitive UW228-3 medulloblastoma cell line and primarily cultured rat brain cells/PBCs as controls, the effect of resveratrol on LN-18 human glioblastoma cells and its relevance with metabolic pattern(s), brain-associated sulfotransferase/SULT expression and the statuses of STAT3 signaling and protein inhibitor of activated STAT3 (PIAS3) were elucidated by multiple experimental approaches. Meanwhile, the expression patterns of three SULTs (SULT1A1, 1C2 and 4A1) in human glioblastoma tumors were profiled immunohistochemically. The results revealed that 100 µM resveratrol-treated LN-18 generated the same metabolites as UW228-3 cells, while additional metabolite in molecular weight of 403.0992 in negative ion mode was found in PBCs. Neither growth arrest nor apoptosis was found in resveratrol-treated LN-18 and PBC cells. Upon resveratrol treatment, the levels of SULT1A1, 1C2 and 4A1 expression in LN-18 cells were more up-regulated than that expressed in UW228-3 cells and close to the levels in PBCs. Immunohistochemical staining showed that 42.0%, 27.1% and 19.6% of 149 glioblastoma cases produced similar SULT1A1, 1C2 and 4A1 levels as that of tumor-surrounding tissues. Unlike the situation in UW228-3 cells, STAT3 signaling remained activated and its protein inhibitor PIAS3 was restricted in the cytosol of resveratrol-treated LN-18 cells. No nuclear translocation of STAT3 and PIAS3 was observed in resveratrol-treated PBCs. Treatment with STAT3 chemical inhibitor, AG490, committed majority of LN-18 and UW228-3 cells but not PBCs to apoptosis within 48 hours.LN-18 glioblastoma cells are insensitive to resveratrol due to the more inducible brain-associated SULT expression, insufficiency of resveratrol to suppress activated STAT3 signaling and the lack of PIAS3 nuclear translocation. The findings from PBCs suggest that an effective anticancer dose of resveratrol exerts little side effect on normal brain cells

A Preclinical Systematic Review and Meta-Analysis of Astragaloside IV for Myocardial Ischemia/Reperfusion Injury

Astragaloside IV (AS-IV), the major pharmacological extract from Astragalus membranaceus Bunge, possesses a variety of biological activities in the cardiovascular systems. Here, we aimed to evaluate preclinical evidence and possible mechanism of AS-IV for animal models of myocardial ischemia/reperfusion (I/R) injury. Studies of AS-IV in animal models with myocardial I/R injury were identified from 6 databases from inception to May, 2018. The methodological quality was assessed by using CAMARADES 10-item checklist. All the data were analyzed using Rev-Man 5.3 software. As a result, 22 studies with 484 animals were identified. The quality score of studies ranged from 3 to 6 points. Meta-analyses showed AS-IV can significantly decrease the myocardial infarct size and left ventricular ejection fraction, and increase shortening fraction compared with control group (P &lt; 0.01). Significant decreasing of cardiac enzymes and cardiac troponin and increasing of decline degree in ST-segment were reported in one study each (P &lt; 0.05). Additionally, the possible mechanisms of AS-IV for myocardial I/R injury are promoting angiogenesis, improving the circulation, antioxidant, anti-inflammatory and anti-apoptosis. Thus, AS-IV is a potential cardioprotective candidate for further clinical trials of myocardial infarction