- The efficacy and safety comparison between tenofovir and entecavir in treatment of chronic hepatitis B and HBV related cirrhosis: A systematic review and Meta-analysis. [Journal Article]
- IIInt Immunopharmacol 2016 Dec 01; 42:168-175
- CONCLUSIONS: TDF has a better efficacy than ETV in 3months treatment duration, but intriguingly, TDF might not better than ETV during the 6months treatment period in the viral suppression and liver function improvement. There's no significant difference between TDF and ETV in the long-term treatment duration and in the treatment of HBV related liver cirrhosis. Both TDF and ETV could influence renal function but patients under TDF therapy may have more risk to suffer from renal damage and hypophosphatemia.
- Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia. [Journal Article]
- BMBioorg Med Chem 2016 Nov 14
- Triazolopyridine ethers with mGlu2 positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The ...
Triazolopyridine ethers with mGlu2 positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The effort resulted in the discovery of a potent, selective, and brain penetrant lead molecule BMT-133218 ((+)-7m). After oral administration at 10mg/kg, BMT-133218 demonstrated full reversal of PCP-stimulated locomotor activity and prevented MK-801-induced working memory deficits in separate mouse models. Also, reversal of impairments in executive function were observed in rat set-shifting studies at 3 and 10mg/kg (p.o.). Extensive plasma protein binding as the result of high lipophilicity likely limited activity at lower doses. Optimized triazolopyridine ethers offer utility as mGlu2 PAMs for the treatment of schizophrenia and merit further preclinical investigation.
- Oleuropein protects L-02 cells against H2O2-induced oxidative stress by increasing SOD1, GPx1 and CAT expression. [Journal Article]
- BPBiomed Pharmacother 2016 Nov 30
- Oleuropein (OL), a natural phenolic compound, comprises the major constituent of Olea europea leaves and unprocessed olives, and OL is considered to be the principal components that confer the charac...
Oleuropein (OL), a natural phenolic compound, comprises the major constituent of Olea europea leaves and unprocessed olives, and OL is considered to be the principal components that confer the characteristic taste and stability of olive oil. Oxidative damage induced by H2O2 treatment can irreversibly damage the L-02 cells, resulting in cell death and apoptosis. Whether the effects of oxidative stress could be attenuated in cultured human L-02 cells by incubation with OL is still unknown. In this research, the function of OL in protecting human L-02 cells against H2O2 induced cell death and cell apoptosis was investigated, and the mechanism by which OL underlies the effect was also examed. L-02 cells were exposed to 100μM H2O2 with or without OL pretreatment at different concentrations. Cell viabilities were monitored by WST-1 assay. ALT, AST and LDH production in culture medium were also determined. ROS levels were detected by L-012 chemiluminescence, and OL increased SOD1, CAT and GPx1 expression in a concentration-dependent manner. Further studies showed that OL also inhibited H2O2-induced P38 and JNK phosphorylation but enhanced ERK1/2 phosphorylation in a dose-dependent manner. These findings suggested that OL as a potent antioxidant agent and a natural compound found in several plants, may be exploited as a potentially useful method for hepatopathy prevention.
- Under-prescription of statins in patients with non-alcoholic fatty liver disease. [Journal Article]
- NMNutr Metab Cardiovasc Dis 2016 Sep 28
- CONCLUSIONS: Our findings show that about 50% of patients with indication to statin treatment do not receive any cholesterol-lowering medication. Statin under-use was particularly high in subjects with NAFLD. Use of statin treatment should be encouraged in the context of NAFLD, as it may improve lipid profile and reduce the cardiovascular risk in this setting.
- Ammonothermal Synthesis of Novel Nitrides: Case Study on CaGaSiN3. [Journal Article]
- CChemistry 2016 Dec 03
- The first gallium-containing nitridosilicate CaGaSiN3 was synthesized in newly developed high-pressure autoclaves using supercritical ammonia as solvent and nitriding agent. The reaction was conducte...
The first gallium-containing nitridosilicate CaGaSiN3 was synthesized in newly developed high-pressure autoclaves using supercritical ammonia as solvent and nitriding agent. The reaction was conducted in ammonobasic environment starting from intermetallic CaGaSi with NaN3 as mineralizer. At 770 K, intermediate compounds were obtained, which were subsequently converted to the crystalline nitride at temperatures up to 1070 K (70 - 150 MPa). The impact of other mineralizers (e. g. LiN3, KN3 and CsN3) on the product formation was investigated as well. The crystal structure of CaGaSiN3 was analyzed by powder X-ray diffraction and refined by the Rietveld method. The structural results were further corroborated by transmission electron microscopy, 29Si MAS-NMR and first-principle DFT calculations. CaGaSiN3 crystallizes in the orthorhombic space group Cmc21 (no. 36) with lattice parameters a = 9.8855(11), b = 5.6595(1), c = 5.0810(1) Å, Z = 4, Rwp = 0.0326) and is isostructural to CaAlSiN3 (CASN). Eu2+ doped samples exhibit red luminescence with an emission maximum of 620 nm and FWHM of 90 nm. Thus, CaGaSiN3:Eu2+ also represents an interesting candidate as red-emitting material in phosphor-converted light-emitting diodes (pc-LEDs). Besides the already known substitution of the alkaline earth metals in (Ca,Sr)AlSiN3:Eu2+, inclusion of Ga is a further and promising perspective for luminescence tuning of widely used red-emitting CASN type materials.
- Didymin ameliorates hepatic injury through inhibition of MAPK and NF-κB pathways by up-regulating RKIP expression. [Journal Article]
- IIInt Immunopharmacol 2016 Nov 29; 42:130-138
- A flavone was isolated from Origanum vulgare and identified as didymin (O. vulgare didymin, OVD). The protective effect and mechanism of OVD on acute liver injury was then assessed in vivo and in vit...
A flavone was isolated from Origanum vulgare and identified as didymin (O. vulgare didymin, OVD). The protective effect and mechanism of OVD on acute liver injury was then assessed in vivo and in vitro. Our results showed that OVD significantly alleviated CCl4-induced liver injury in mice and markedly decreased serum ALT and AST activities. OVD treatment significantly reduced CYP2E1 activity, lipid peroxidation level, ROS generation, NO production and pro-inflammatory cytokines (such as TNF-α, IL-6 and IL-1β) in liver tissues and RAW 264.7 cells, but enhanced the hepatic antioxidative enzymes activities. Further study showed that OVD significantly inhibited the NF-κB and MAPK pathways. Interestingly, OVD notably enhanced Raf kinase inhibitor protein (RKIP) expression, and the effects of OVD on histological changes, oxidative stress and inflammation was largely abolished by the RKIP specific inhibitor locostatin. Our findings indicate that OVD can ameliorate CCl4-induced liver injury, which may be ascribed to its radical scavenging action, antioxidant activity, and modulation of MAPK and NF-κB signaling pathways.
- Avalanche Accidents Causing Fatalities: Are They Any Different in the Summer? [Journal Article]
- HAHigh Alt Med Biol 2016 Dec 02
- CONCLUSIONS: Fatal summer avalanche accidents caused a higher mean number of fatalities per avalanche than winter avalanches, and those deaths resulted mostly from trauma. Rescue teams should anticipate managing polytrauma for victims in summer avalanche accidents rather than hypothermia or asphyxia; they should be trained in prehospital trauma life support and equipped accordingly to ensure efficient patient care.
- Oxidative Stress and Biochemical Markers of Endothelial Dysfunction and Organ Damage under Conditions of Experimental Nonferrous Metal Intoxication. [Journal Article]
- BEBull Exp Biol Med 2016 Dec 02
- Chronic nickel intoxication caused by parenteral nickel chloride administration (0.5 mg/kg of body weight) to Wistar rats led to ROS generation inducing LPO in erythrocyte membranes and homogenates o...
Chronic nickel intoxication caused by parenteral nickel chloride administration (0.5 mg/kg of body weight) to Wistar rats led to ROS generation inducing LPO in erythrocyte membranes and homogenates of renal, liver, and myocardial tissue. Superoxide dismutase (SOD) activity was inhibited, while catalase activity and ceruloplasmin concentration increased. LPO and its products disrupted nitric oxide production and reduced its bioavailability, which led to the development of endothelial dysfunction and impaired microcirculatory hemodynamics. At the same time, damage of cytoplasmic membranes of internal organs (kidney, liver, and myocardium) was revealed, which was seen from reduced Na(+), K(+)-ATPase activity in homogenates of these organs and increased serum activity of organ-specific (ALT, AST, and γ-glutamyl transpeptidase) and excretory (alkaline phosphatase) enzymes.
- Highly Sensitive Detection of Minimal Cardiac Ischemia using Positron Emission Tomography Imaging of Activated Platelets. [Journal Article]
- SRSci Rep 2016 Dec 02; 6:38161
- A reliable method for the diagnosis of minimal cardiac ischemia would meet a strong demand for the sensitive diagnosis of coronary artery disease in cardiac stress testing and risk stratification in ...
A reliable method for the diagnosis of minimal cardiac ischemia would meet a strong demand for the sensitive diagnosis of coronary artery disease in cardiac stress testing and risk stratification in patients with chest pain but unremarkable ECGs and biomarkers. We hypothesized that platelets accumulate early on in ischemic myocardium and a newly developed technology of non-invasive molecular PET imaging of activated platelets can thus detect minimal degrees of myocardial ischemia. To induce different degrees of minimal cardiac ischemia, the left anterior descending artery (LAD) was ligated for 10, 20 or 60 min. Mice were injected with a newly generated scFvanti-GPIIb/IIIa-(64)CuMeCOSar radiotracer, composed of a single-chain antibody that only binds to activated integrin GPIIb/IIIa (αIIbβIII) and thus to activated platelets, and a sarcophagine cage MeCOSar complexing the long half-life PET tracer copper-64. A single PET/CT scan was performed. Evans Blue/TTC staining to detect necrosis as well as classical serological biomarkers like Troponin I and heart-type fatty acid-binding protein (H-FABP) were negative, whereas PET imaging of activated platelets was able to detect small degrees of ischemia. Taken together, molecular PET imaging of activated platelets represents a unique and highly sensitive method to detect minimal cardiac ischemia.
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- Evaluation of tissue metal and trace element content in a rat model of non-alcoholic fatty liver disease using ICP-DRC-MS. [Journal Article]
- JTJ Trace Elem Med Biol 2017; 39:91-99
- The primary objective of the study was to assess the level of metals and trace elements in liver, serum, and hair of rats with diet-induced non-alcoholic fatty liver disease (NAFLD) using inductively...
The primary objective of the study was to assess the level of metals and trace elements in liver, serum, and hair of rats with diet-induced non-alcoholic fatty liver disease (NAFLD) using inductively coupled plasma dynamic reaction cell mass spectrometer (ICP-DRC-MS). 56 female 3-months-old Wistar rats divided into two equal groups were fed either standard (10% calories from fat) or high-fat high-carbohydrate diet (60% calories from fat in chow and 10% sucrose solution) for 6 weeks. Serum was examined for insulin resistance markers, lipid profile, and alanine aminotransferase (ALT) activity. Liver histology was assessed after hematoxylin and eosin staining. Metal and trace element concentrations were assessed by means of ICP-DRC-MS. Overfed animals were characterized by higher values of morphometric parameters. Liver examination revealed large and small droplet steatosis, hepatocyte ballooning and necrosis, being characteristic for NAFLD. Animals with NAFLD were characterized by insulin resistance, atherogenic changes of lipid profile and increased ALT activity. Significantly decreased hepatic Co, Cu, I, Li, Mn, Se, Zn levels were observed in rats with NAFLD. At the same time, only hepatic Mn and Se levels remained decreased after adjustment for total protein. Overfed animals were characterized by significantly lower I, Li, and Mn levels in blood serum, whereas concentration of Co, Se, V, and Sr exceeded the control values. In general, the results of the study demonstrate that NAFLD significantly affects metal and trace element status in experimental animals.