Uncarboxylated osteocalcin promotes osteogenesis and inhibits adipogenesis of mouse bone marrow-derived mesenchymal stem cells via the PKA-AMPK-SIRT1 axis.

Osteoporosis is a bone disease characterized by reduced bone density, thin cortical bone and large gaps in the bone's honeycomb structure, which increases the risk of bone fragility. Uncarboxylated osteocalcin (unOC), a vitamin K-dependent bone protein, is known to regulate carbohydrate and energy metabolism. A previous study demonstrated that unOC promotes the differentiation of mouse bone marrow-derived mesenchymal stem cells (BMSCs) into osteoblasts, but inhibits their differentiation into adipocytes.

A Single-Center Experience of Endovascular Treatment in Subtypes of Basilar Artery Occlusion: Embolization Caused by Tandem Vertebral Artery Stenosis May Be Associated with Better Outcomes.

Objective: Basilar artery occlusion (BAO) is a severe condition with high mortality. However, surgical procedures and outcomes of BAO with different pathologic subtypes have not been fully clarified. This study compared the surgical procedures and clinical outcomes of mechanical thrombectomy in different subtypes of BAO.

Synthesis and evaluation of new compounds bearing 3-(4-aminopiperidin-1-yl)methyl magnolol scaffold as anticancer agents for the treatment of non-small cell lung cancer via targeting autophagy.

Magnolol and honokiol are the two major active ingredients with similar structure and anticancer activity from traditional Chinese medicine Magnolia officinalis, and honokiol is now in a phase I clinical trial (CTR20170822) for advanced non-small cell lung cancer (NSCLC). In search of potent lead compounds with better activity, our previous study has demonstrated that magnolol derivative C2, 3-(4-aminopiperidin-1-yl)methyl magnolol, has better activity than honokiol. Here, based on the core of 3-(4-aminopiperidin-1-yl)methyl magnolol, we synthesized fifty-one magnolol derivatives.

Flavonoids with Inhibitory Effects on NLRP3 Inflammasome Activation from .

Eight new flavonoids, including two β-hydroxy/methoxychalcones, velutones A and B ( and ), two 1,3-diarylpropan-1-ols, velutols C and D ( and ), a dihydroxychalcone, velutone E (), a chalcone, velutone F (), a furanoflavanone, velutone G (), and a furanoflavonol, velutone H (), and 14 known compounds were isolated from . Their structures were determined by high-resolution electrospray ionisation mass spectrometry (HR-ESIMS) and spectroscopic data analyses and time-dependent density functional theory electronic circular dichroism (TD-DFT-ECD) calculations. Among the isolated constituents, compound exhibited the most potent inhibitory effect (IC: 1.

Uncarboxylated osteocalcin ameliorates hepatic glucose and lipid metabolism in KKAy mice via activating insulin signaling pathway.

Osteocalcin, expressed in osteoblasts of the bone marrow, undergoes post-translational carboxylation and deposits in mineralized bone matrix. A portion of osteocalcin remains uncarboxylated (uncarboxylated osteocalcin, GluOC) that is released into blood where it functions as a hormone to regulate insulin secretion and insulin sensitivity. As insulin resistance is closely associated with metabolic syndrome, this study is aimed to elucidate how GluOC regulates glucose and lipid metabolism in KKAy mice, an animal model displaying obese, hyperglycemia, hyperinsulinemia, insulin resistance, and hepatic steatosis.

An arc fault diagnosis algorithm using multiinformation fusion and support vector machines.

Arc faults in low-voltage electrical circuits are the main hidden cause of electric fires. Accurate identification of arc faults is essential for safe power consumption. In this paper, a detection algorithm for arc faults is tested in a low-voltage circuit.

The efficacy and safety of aripiprazole for tic disorders in children and adolescents: A systematic review and meta-analysis.

The aims are to evaluate the efficacy and safety of aripiprazole for tic disorders (TDs) in children and adolescents. We searched PubMed, Embase, PsychINFO, Cochrane database as well as Chinese databases of CNKI, VIP, CBM and Wanfang from the database inception to October 2016, and 17 full-text studies (N=1305) were included in our article. The meta-analysis of 10 studies (N=817) showed that there was no significant difference in the reduction of total YGTSS score between aripiprazole and other drugs, and meta-analysis of 7 studies (n=324) which used tic symptom control ≧30% as outcome measure showed that there was no significant difference between aripiprazole and other treatments.

Flavonoids and biphenylneolignans with anti-inflammatory activity from the stems of Millettia griffithii.

Five new flavonoids, griffinones A-E (1-5), a new biphenylneolignan, griffilignan A (6) and ten known compounds were isolated from the n-hexane and EtOAc extracts of Millettia griffithii. The structures of the new compounds were determined by 1D and 2D NMR, and by HRMS. The anti-inflammatory activity of the isolated compounds was evaluated on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.

Guidelines and strategy of the International Conference of Harmonization (ICH) and its member states to overcome existing impurity control problems for antibiotics in China.

In the present report, we review the technical guidelines and principles on impurity research and control for antibiotics established by various agencies, including the International Conference of Harmonization (ICH), the US Food and Drug Administration (FDA), the European Medicines Agency (EMA) and the China Food and Drug Administration (CFDA). Progresses with the US Pharmacopoeia (USP), the European Pharmacopoeia (EP) and the Chinese Pharmacopoeia (ChP) to control impurities in antibiotics are also presented. Next, our discussion is focused on analyzing the CFDA's requirements on impurity research and control for antibiotics, and the implementation of ICH, FDA and other technical guidelines for generic drugs impurity control in China.

Caspase-8 Mediates Amyloid-β-induced Apoptosis in Differentiated PC12 Cells.

The pathogenesis of Alzheimer's disease (AD) is very complex and there are currently no significant treatments for the disease. Caspase-8 is known to be involved in neuronal apoptosis. To explore a possible molecular mechanisms involved in AD pathology, this study investigated the effect of caspase-8 knockdown on amyloid-β 1-40 (Aβ1-40)-induced apoptosis in PC12 cells.

Unusual cycloartane triterpenoids from Kadsura ananosma.

Five 3,4-seco-cycloartane triterpenoids were isolated from the stems of Kadsura ananosma, two of which had rearranged 5/6 consecutive carbocycle rings C/D (trivially named ananosins A (1) and B (2)), one had a migrated CH3-18 (named ananosins C (3)), and two were analogs, ananosins D (4) and E (5). Their structures were characterized by comprehensive spectroscopic analysis, especially using 2D NMR spectra. A biogenetic pathway to 1 was proposed.

Heterodimeric ent-kauranoids from Isodon tenuifolius.

Thirteen new heterodimeric ent-kauranoids, bistenuifolins A-M (1-13), were isolated from the aerial parts of Isodon tenuifolius. The constituent units of compounds 1-6 were linked by a six-membered dihydropyran ring, while those of compounds 7-11 were joined by a rare single carbon-carbon bond (C-16→C-17'). The constituent units of 12 and 13 were linked via an unusual cyclobutane moiety.

[Phenolic compounds in branches of Tamarix rasissima].

To study the chemical constituents of the branches of Tamarix rasissima, repeated silica gel column chromatography, Sephadex LH-20 chromatography and recrystallization were applied for chemical constituents isolation and purification. Ten phenolic compounds were isolated from the n-BuOH fraction and their structures were elucidated by physical properties and spectra analysis such as UV, ESI-MS and NMR as monodecarboxyellagic acid (1), ellagic acid (2), 3, 3'-di-O-methylellagic acid (3), 3, 3'-di-O-methylellagic acid-4-O-beta-D-glucopyranoside (4), 3, 3'-di-O-methylellagic acid-4'-O-alpha-D-arabinfuranoside (5), ferulic acid (6), isoferulic acid (7), caffeic acid (8), 4-O-acetyl-caffeic acid (9), and 4-methyl-1, 2-benzenediol (10). All compounds except for isoferulic acid were isolated firstly from this plant except for isoferulic acid, and compounds 5, 9 and 10 were obtained from Tamarix genus for the first time.

Serum Gamma-glutamyltransferase Levels Predict the Progression of Coronary Artery Calcification in Adults With Type 2 Diabetes Mellitus.

Progression of coronary artery calcification (CAC) may be more predictive of future coronary heart disease events than a baseline CAC score. We determined whether serum gamma-glutamyltransferase (GGT) activity can independently predict the progression of CAC in adults with type 2 diabetes mellitus (T2DM). Patients (n = 326) without symptomatic cardiovascular (CV) disease were evaluated by CAC imaging.

[Environmental geochemical baseline of heavy metals in soils of the Ili river basin and pollution evaluation].

Environmental geochemical baseline models of Cu, Zn, Pb, As, Hg were established by standardized method in the ehernozem, chestnut soil, sierozem and saline soil from the Ili river valley region. The theoretical baseline values were calculated. Baseline factor pollution index evaluation method, environmental background value evaluation method and heavy metal cleanliness evaluation method were used to compare soil pollution degrees.

The relationship between serum hypoxia-inducible factor 1α and coronary artery calcification in asymptomatic type 2 diabetic patients.

Background: Hypoxia-inducible factor 1 (HIF-1), a master regulator of oxygen homeostasis, is a heterodimer consisting of HIF-1α and HIF-1β subunits, and is implicated in calcification of cartilage and vasculature. The goal of this study was to determine the relationship between serum HIF-1α with coronary artery calcification (CAC) in patients with type 2 diabetes.

Methods: The subjects were 405 (262 males, 143 females, age 51.

Barbigerone inhibits tumor angiogenesis, growth and metastasis in melanoma.

Tumor angiogenesis, growth and metastasis are three closely related processes. We therefore investigated the effects of barbigerone on all three in the B16F10 tumor model established in both zebrafish and mouse models, and explored underlying molecular mechanisms. In vitro, barbigerone inhibited B16F10 cell proliferation, survival, migration and invasion and suppressed human umbilical vascular endothelial cell migration, invasion and tube formation in concentration-dependent manners.

Activation of the PI3K/Akt pathway by oxidative stress mediates high glucose-induced increase of adipogenic differentiation in primary rat osteoblasts.

Diabetes mellitus is associated with increased risk of osteopenia and bone fracture that may be related to hyperglycemia. However, the mechanisms accounting for diabetic bone disorder are unclear. Here, we showed that high glucose significantly promoted the production of reactive oxygen species (ROS) in rat primary osteoblasts.

Bioactive abietane and ent-kaurane diterpenoids from Isodon tenuifolius.

Three new abietane diterpenoids, isoabietenins A-C (1-3), and 13 new ent-kauranoids, tenuifolins A-M (4-16), along with four known compounds (17-20), were isolated from the aerial parts of Isodon tenuifolius. The structures of the new metabolites were established on the basis of detailed spectroscopic analysis. The absolute configurations of 1, 15, and 16 were confirmed by single-crystal X-ray diffraction.

New ent-abietane and ent-kaurane diterpenoids from Isodon rubescens.

Five new ent-abietane diterpenoids, ent-abierubesins A-E (1-5), and two new ent-kauranoids, hubeirubesins A and B (6, 7), together with three known diterpenoids (8-10), were isolated from the aerial parts of Isodon rubescens. Their structures were identified by means of extensive spectroscopic analysis, and the absolute stereochemistry of 1 was determined by single-crystal X-ray diffraction experiment.

[Effects of apolipoprotein E genetic polymorphism on susceptibility of depression and efficacy of antidepressants].

Objective: To assess the effects of apolipoprotein E (APOE) polymorphism on the susceptibility of depression and the efficacy of antidepressants.

Methods: A total of 275 patients with depression, who met the diagnostic criteria of both CCMD-3 and DSM-4, were randomly assigned into venlafaxine group (n=136)and paroxetine group(n=139). Another 202 healthy subjects were enrolled as the control group.

Detection of autoantibodies and increased concentrations of interleukins in plasma from patients with Tourette's syndrome.

The aim of this study was to assess levels of autoantibodies and cytokines in patients with Tourette's syndrome (TS, n = 40) and healthy control individuals (n = 40). Plasma interleukin (IL)-1β, IL-6, IL-17, and soluble gp130 concentrations were significantly higher in the TS group compared with the control group (P < 0.001); whereas the soluble IL-6 receptor concentration was significantly decreased in the TS group compared with the control group (P < 0.

[Dynamic level observation of brain-derived neurotrophic factor in patients with first-episode generalized anxiety disorder].

Objective: To examine the changing pattern of brain-derived neurotrophic factor (BDNF) in the patients with first-episode generalized anxiety disorder (GAD).

Methods: The levels of plasma BDNF and the Hamilton anxiety scale (HAMA) and Hamilton depression scale (HAMD) scores were measured in 34 patients with first-episode GAD recruited from our hospital between January and December 2007. At baseline and Week 6, they were treated by paroxetine and compared with 31 healthy participants in the control group.