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1.
Theriogenology ; 159: 77-86, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-33113448

RESUMO

Coenzyme Q10 (CoQ10) is essential to many fundamental biological processes. However, the effect of CoQ10 on meiotic maturation of pig oocytes still remains elusive. In the present study we aimed to understand the effects of CoQ10 on porcine oocyte maturation, by supplementing different concentrations of CoQ10 (25, 50 and 100 µM) into the maturation medium. We showed that CoQ10 at 50 µM had better capacity to promote the nuclear maturation of pig oocytes derived from both small and large antral follicles. Though the cleavage and blastocyst rates of parthenotes stayed stable, 50 µM CoQ10 treatment could accelerate the development of parthenotes to blastocyst stage, and increase the average cell number of blastocyst. For cumulus-oocyte complexes from large antral follicles categorized by the brilliant cresyl blue (BCB) test, 50 µM CoQ10 treatment could specifically promote the nuclear maturation of poor-quality oocytes in the BCB-negative group. Mitochondrial function of oocytes treated by 50 µM CoQ10 could be boosted, through increasing the levels of mitochondrial membrane potential, ATP production and CoQ6, and changing the pattern of mitochondrial distribution as well. Moreover, 50 µM CoQ10 treatment suppressed the level of reactive oxygen species and reduced the percentage of oocytes with early apoptosis signal. Taken together, CoQ10 could improve the meiotic maturation of pig oocytes, especially for poor-quality oocytes, mainly through enhancing mitochondrial function and suppressing oxidative stress to reduce apoptosis.

2.
Ann Palliat Med ; 2020 Oct 29.
Artigo em Inglês | MEDLINE | ID: mdl-33183037

RESUMO

BACKGROUND: This study aimed to investigate the dynamic changes of serum HBV DNA and hepatitis B surface antigen (HBsAg) titers apportioned by the same hepatic parenchyma cell volume (HPCV) at different liver histological inflammation grades in the natural history of chronic hepatitis B (CHB). METHODS: The serum HBV DNA and HBsAg titers were detected by real-time polymerase chain reaction and electrochemiluminescence, separately, in CHB patients without any treatment. The serum HBV DNA levels and HBsAg titers apportioned by the same HPCV were figured out based on sphere geometry theory. In addition, the differences of HBV DNA levels and HBsAg titers apportioned by the same HPCV in different liver inflammation grades were further assessed based on statistical analysis. RESULTS: There was no difference of serum HBV DNA levels or HBsAg titers before apportioned by the same HPCV in liver inflammation grades 1-4, but significant differences were observed after apportion in CHB patients (HBV DNA: P=0.101; HBsAg: P=0.211 & HBV DNA apportioned by HPCV: P<0.001; HBsAg apportioned by HPCV: P<0.001). No correlation was observed between HBV DNA levels and liver inflammation grades (r=0.083, P=0.186), or between HBsAg titers and liver inflammation grades (r=0.083, P=0.078). A significant correlation was observed between HBV DNA levels apportioned by HPCV and liver inflammation grades (r=0.249, P<0.001), and obvious correlation of HBsAg titers apportioned by HPCV and liver inflammation grades was also found in CHB patients (r=0.554, P<0.001). CONCLUSIONS: These results suggest that the levels of serum HBV DNA and HBsAg apportioned by the same HPCV are correlated with the severity of liver histological inflammation grade in the natural history of CHB.

3.
Int J Med Sci ; 17(17): 2635-2643, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33162791

RESUMO

Histone deacetylase 6 (HDAC6) controls many cellular processes via its catalyzing deacetylation of downstream substrates or interacting with its partner proteins. Dysregulation of HDAC6 signaling links to many diseases. Our previous study has been reported peptidyl-prolyl cis/trans isomerase, and NIMA-interacting 1 (Pin1) involving in HDAC6-mediated cell motility. To gain insight into precisely coordination of HDAC6 and Pin1 in cell migration, shRNA-mediated gene silencing and ectopic expression were applied to manipulate protein expression level to evaluate relationship between HDAC6 and Pin1 expression. Quantitative RT-PCR and the cycloheximide (CHX) chase assay resulted in HDAC6 expression is correlated with Pin1 level in H1299 cells. It hints that the Pin1 increases HDAC6 expression through increased transcripts and posttranslational stabilization. Furthermore, wound healing assay and transwell invasion assay evidenced the contribution of Pin1 on cell motility in H1299 cells. Our data suggest that Pin1 acts as an important regulator to manage HDAC6 expression for cell motility in lung cancer cells.

4.
J Agric Food Chem ; 68(45): 12558-12568, 2020 Nov 11.
Artigo em Inglês | MEDLINE | ID: mdl-33140649

RESUMO

In recent years, naturally occurring tetrahydro-ß-carboline (THC) alkaloids and their derivatives have been of biological interest. However, few studies and developments have reported the use of such structures in managing plant bacterial diseases. Herein, an array of novel THC derivatives containing an attractive 1,3-diaminopropan-2-ol pattern were prepared to evaluate the antiphytopathogen activity in vitro and in vivo and explore innovative antibacterial frameworks. Notably, target compounds exhibited excellent activities against three rebellious phytopathogens, namely, Pseudomonas syringae pv. actinidiae (Psa), Xanthomonas axonopodis pv. citri, and Xanthomonas oryzae pv. oryzae, at related optimal EC50 values of 2.39 (II9), 2.06 (I23), and 1.69 (II9) µg/mL, respectively. These effects were superior to those of the parent structure 1,2,3,4-THC and positive controls. In vivo assays showed that II9 exhibited excellent control efficiencies of 51.89 and 65.45% at 200 µg/mL against rice bacterial blight and kiwifruit bacterial canker, respectively, and I23 substantially relieved the citrus canker on the leaves. Antibacterial mechanisms indicated that these THC compounds could induce the increment of reactive oxygen species and subsequently endow the tested bacteria with distinct apoptotic behavior. In addition, II9 could alleviate the hypersensitive response and pathogenicity of Psa. Overall, these simple THC derivatives can be further developed as versatile antibacterial agents.

6.
J Oleo Sci ; 69(11): 1481-1486, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33132280

RESUMO

Via utilizing the mixed-ligand method, a novel coordination polymer (CP) containing Cu(II) has been prepared by self-assembly at the ambient temperature, and its chemical formula is {[Cu(BINDI)0.5 (bpe)]·3H2O} n (1, bpe = 1,2-bis(4-pyridyl)ethylene and H4BINDI = N,N'-bis(5-isophthalic acid) naphthalenediimide). For the treatment of the tuberculosis, its biological function was evaluated as well. The CFU assay was performed to determine the bacterial numbers of the Mycobacterium in alveolar macrophages. In addition to this, the ropA gene of the Mycobacterium in alveolar macrophages was also detected through the real time RT-PCR method. Only the oxygen atoms on the metal complex are identified to be able to interact with the probe protein by molecular docking simulation.


Assuntos
Cobre/farmacologia , Macrófagos Alveolares/microbiologia , Mycobacterium tuberculosis/efeitos dos fármacos , Polímeros/farmacologia , Proteínas de Bactérias/análise , Proteínas de Bactérias/genética , Contagem de Colônia Microbiana , Cobre/química , Cobre/uso terapêutico , Expressão Gênica/efeitos dos fármacos , Ligantes , Conformação Molecular , Simulação de Acoplamento Molecular , Mycobacterium tuberculosis/genética , Oxigênio , Polímeros/química , Polímeros/uso terapêutico , Reação em Cadeia da Polimerase em Tempo Real , Tuberculose/tratamento farmacológico , Tuberculose/microbiologia
7.
Artigo em Inglês | MEDLINE | ID: mdl-33165141

RESUMO

Hydrogen sulfide (H2S), generally known as a new gas signal molecule after nitric oxide (NO) and carbon monoxide (CO), in the last few decades has been found as an important endogenous gasotransmitter, playing a significant role in the cardiovascular system both pathologically and physiologically. In recent years, there is growing evidence that H2S provides myocardial protection against myocardial ischemia-reperfusion injury (MIRI), which resulted in an ongoing focus on the possible mechanisms of action accounting for the H2S cardioprotective effect. At present, lots of mechanisms of action have been verified through in vitro and in vivo models of ischemia-reperfusion (I/R) injury, such as S-sulfhydrated modification, anti-apoptosis, effects on miRNA, bidirectional effect on autophagy, anti-oxidant stress, or interaction with NO and CO. With advances in understanding of the molecular pathogenesis of MIRI and pharmacology studies, the design, the development and the pharmacological characterization of H2S-donor drugs have been made great important progress. This review summarizes the latest research progress on the role of H2S in MIRI, systematically explains the molecular mechanism of H2S affecting MIRI, and provides a new idea for the formulation of a myocardial protection strategy in the future.

8.
J Affect Disord ; 2020 Nov 13.
Artigo em Inglês | MEDLINE | ID: mdl-33229018

RESUMO

OBJECTIVES: Convergent evidence has demonstrated that trait impulsivity, a key feature in obsessive-compulsive disorder (OCD), involves dysregulated frontal-striatal circuits. The present study aims to explore relationships between frontal-striatal circuits, trait impulsivity, and obsessive-compulsive symptoms. METHODS: Thirty-six unmedicated patients with OCD and 50 healthy controls (HCs) matched for age, sex, and years of education underwent a magnetic resonance imaging (MRI) procedure. Voxel-wise statistical parametric analysis was used to investigate the differences in resting-state functional connectivity between brain regions functionally connected to six pairs of a-priori defined striatal seed regions, between patients with OCD and HCs. Associations between frontal-striatal connectivity and both trait impulsivity and symptom severity of OCD were analyzed. RESULTS: The results showed altered striatal functional connectivity in OCD group compared to HCs, including increased connectivity of dorsal caudate (DC)-orbitofrontal cortex (OFC), ventral striatum (VS)-OFC, VS-medial prefrontal cortex, and putamen-sensorimotor area, and decreased functional connectivity of DC-anterior cingulate cortex (ACC), putamen-ACC, and putamen-dorsolateral prefrontal cortex (DLPFC). Furthermore, the putamen-DLPFC connectivity was negatively correlated with attentional impulsivity in the OCD group, but showed a positive correlation in HCs. CONCLUSIONS: The present findings suggested that dorsal cognitive circuits could reflect the level of inhibitory control, which is balanced with the impulsive drive in healthy controls, but breakdown in OCD. Our findings supported that DLPFC-putamen connectivity underlying trait impulsivity, which were involved in the pathophysiology of OCD. The findings have provided new insights into the neurobiological mechanisms of OCD.

9.
Artigo em Inglês | MEDLINE | ID: mdl-33160878

RESUMO

INTRODUCTION: The incidence of distal radius fractures (DRFs) is increasing as the number of people in recreational or sporting activities rises, due to a combination of increased leisure time and greater public awareness of the health-related benefits of sports. Despite the increases in sports-related distal radius fractures (SR-DRFs), there are limited studies regarding the characteristics of treatment and recovery. HYPOTHESIS: There are characteristics specific to SR-DRF treated with conservative or operative management. MATERIAL AND METHODS: Retrospective review was carried out between January 2010 and December 2017. Overall, 1706 patients were included in the study analysis. Among them, 317 patients were injured during sports activity (18.6%) and 1389 were injured during non-sports activity (81.4%). Demographic data were compared between the two groups. The type of sports was investigated in SR-DRF. Also, we compared surgically treated DRF patients to describe differences in patient characteristics, fracture characteristics, and postoperative complications. RESULTS: The mean age of patients with SR-DRFs was significantly younger (28 vs. 52 years). The proportion of men was also significantly higher in SR-DRF group compared to NSR-DRF group (62.8 vs. 33.8%). We identified 27 kinds of sports associated with DRFs and the 5 sports topping the list associated were soccer (22.7%), cycling (17.7%), snowboarding (11.0%), ice-skating (9.1%), and mountain hiking (9.1%). There was no difference in terms of the treatment method. However, SR-DRF group had higher proportion of AO/OTA type A fracture (32.6 vs. 13.7%), and NSR-DRF group had higher proportion of type C fracture (79.5 vs. 64.2%). Postoperative complications showed no significant differences, except higher implant removal rate in SR-DRF. DISCUSSION: Patients with SR-DRF were significantly younger and had higher proportion of men. Proportion of AO/OTA type A was higher in SR-DRF group and proportion of AO/OTA type C was higher in NSR-DRF group. Proportion of surgical treatment was similar in two groups. Given the growing population participating in sports activity worldwide, SR-DRFs are predicted to increase and further study is required. LEVEL OF EVIDENCE: III; retrospective, epidemiological study.

10.
Artigo em Inglês | MEDLINE | ID: mdl-33158888

RESUMO

Under anoxic conditions, many bacteria including Shewanella loihica PV-4 strain could use nitrate as electron acceptors for dissimilatory nitrate reduction to ammonium (DNRA) and/or denitrification. Previous and current studies have shown that DNRA is favored under higher ambient carbon-to-nitrogen (C/N) ratios while denitrification is upregulated under lower C/N ratios, which is consistent with our bioenergetics calculations. Interestingly, computational analyses indicate that the common cyclic AMP receptor protein (designated CRP1) and its paralogue CRP2 might be both involved in the regulation of two competing dissimilatory nitrate reduction pathways, DNRA and denitrification, in S. loihica PV-4 and several other denitrifying Shewanella species. To explore the regulatory mechanism underlying the DNR pathways, nitrate reduction of a series of in-frame deletion mutants was analyzed and compared under different C/N ratios. Deletion of crp1 could accelerate reduction of nitrite to NO under both low and high C/N ratios. CRP1 is not required for denitrification and actually suppresses production of NO and N2O gases. Deletion of either NO-forming nitrite reductase gene nirK or crp2 blocked production of NO gas. Furthermore, real-time PCR and electrophoretic mobility shift assays (EMSAs) demonstrated that the transcription of DNRA-relevant genes such as nap-beta (napDABGH), nrfA and cymA genes were upregulated by CRP1, while nirK transcription was dependent on CRP2. There are tradeoffs between the different physiological roles of nitrate/lactate as nitrogen nutrient/carbon source and electron acceptor/donor and CRPs may leverage dissimilatory nitrate reduction pathways for maximizing energy yield and bacterial survival under ambient environments.Importance Some microbes utilize different dissimilatory nitrate reduction (DNR) pathways, including DNR to ammonia (DNRA) and denitrification, for anaerobic respiration in response to ambient carbon/nitrogen ratio changes. Large-scale industrial nitrogen fixation and fertilizer application raise the concern of emission of N2O, a stable gas with a potent global warming potential, as consequence of microbial respiration, hereby aggravating global warming and climate change. However, little is known about the molecular mechanism underlying the choice of two competing DNR pathways. We demonstrate that the global regulator CRP1 widely encoded in bacteria is required for DNRA in S. loihica PV-4 strain while the CRP2 paralogue is required for transcription of nitrite reductase gene nirK for denitrification. Sufficient carbon source leads to the predominance of DNRA, while carbon source/electron donor deficiency may result in an incomplete denitrification process, raising the concern of high levels of N2O emission from nitrate-rich and carbon source-poor waters and soils.

11.
J Phys Chem Lett ; : 10144-10149, 2020 Nov 16.
Artigo em Inglês | MEDLINE | ID: mdl-33191751

RESUMO

In further advancing display technologies, especially for improved blue emitters, to engineer the bandgap of promising semiconductors such as hybrid perovskites is important. Present-day methods for tuning the bandgaps of perovskites, such as the incorporation of mixed halide anions, suffer drawbacks such as phase separation and difficulty in synthesis. Here we report a new 2D lead iodide perovskite that emits in the blue spectral region. We exploit an increased angular distortion of PbI42- octahedra to widen the bandgap of 2D metal halide perovskites. We synthesized 2D lead iodide perovskites based on (4-Y-C6H4CH2NH3)2PbI4 (Y = H, F, Cl, Br, I) and substituted the halogen atoms with a -CF3 group to create (4-CF3-C6H4CH2NH3)2PbI4 compounds. We observed that the CF3-substituted material exhibited a ∼0.16 eV larger bandgap than did the halogen-substituted materials. We used X-ray diffraction and density functional theory simulations and found that the blue shift can be assigned to the angular distortion of the PbI42- lattice, a distortion traceable to repulsive intermolecular interactions between the trifluoromethyl groups on oppositely-arranged spacers. These results add a degree of freedom in tuning 2D perovskites to selected bandgaps for optoelectronic applications.

12.
Curr Mol Med ; 2020 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-33191885

RESUMO

BACKGROUND: Cellular senescence is a state of stable growth arrest triggered by mitogenic and metabolic stressors. Ageing and a high-fat diet (HFD) are proven inducers of senescence in various organs, presenting a challenge for ageing populations worldwide. Our previous study demonstrated that ROS scavenger N-acetylcysteine (NAC) can improve insulin resistance(IR) and chronic inflammation in diet-induced obesity mice, an effect better achieved through early intervention. We herein investigate whether NAC can improve cellular senescence in a diet-induced obesity mouse model, and whether a legacy effect is presented with early intervention. MATERIALS AND METHODS: For a twelve-month treatment course, all C57B/L6 mice were fed a chow diet (CD), high-fat high sucrose diet (HFD), CD+NAC1-12 (NAC intervention 1st-12th month), HFD+NAC1-12, and HFD+NAC1-6 (NAC intervention 1st-6th month). Statical analysis was used to analyze the different of markers of cellular senescence and inflammation. RESULTS: Throughout the study, the HFD group exhibited significantly increased body weight (BW) and body fat, markers of senescence, decreased motor activity (MA) and impaired glucose tolerance. Compared to the HFD group, the HFD+NAC1-12 group exhibited increased MA, decreased BW and body fat, improved glucose tolerance, and decreased senescence markers. The HFD+NAC1-6 group showed similar effects to the HFD+NAC1-12 group, despite discontinuing NAC for6 months. Our study showed that NAC significantly increased MA in the both HFD+NAC1-12 and HFD+NAC1-6 groups, and improved HFD-induced mitochondrial and intracellular ROS expression, DNA and protein oxidative damage, and adipose tissue inflammation. CONCLUSION: Legacy effect was indeed presented in HFD-induced cellular senescence with NAC intervention, with possible mechanisms being persistently increased motor activity and anti-oxidative stress effects.

13.
Psychol Med ; : 1-10, 2020 Nov 20.
Artigo em Inglês | MEDLINE | ID: mdl-33213536

RESUMO

BACKGROUND: Childhood trauma is a vulnerability factor for the development of obsessive-compulsive disorder (OCD). Empirical findings suggest that trauma-related alterations in brain networks, especially in thalamus-related regions, have been observed in OCD patients. However, the relationship between childhood trauma and thalamic connectivity in patients with OCD remains unclear. The present study aimed to examine the impact of childhood trauma on thalamic functional connectivity in OCD patients. METHODS: Magnetic resonance imaging resting-state scans were acquired in 79 patients with OCD, including 22 patients with a high level of childhood trauma (OCD_HCT), 57 patients with a low level of childhood trauma (OCD_LCT) and 47 healthy controls. Seven thalamic subdivisions were chosen as regions of interest (ROIs) to examine the group difference in thalamic ROIs and whole-brain resting-state functional connectivity (rsFC). RESULTS: We found significantly decreased caudate-thalamic rsFC in OCD patients as a whole group and also in OCD_LCT patients, compared with healthy controls. However, OCD_HCT patients exhibited increased thalamic rsFC with the prefrontal cortex when compared with both OCD_LCT patients and healthy controls. CONCLUSIONS: Taken together, OCD patients with high and low levels of childhood trauma exhibit different pathological alterations in thalamic rsFC, suggesting that childhood trauma may be a predisposing factor for some OCD patients.

14.
Mol Immunol ; 128: 249-257, 2020 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-33176179

RESUMO

Germinal center (GC) formation is a critical step during T-dependent humoral immune responses. We report Death Associated Protein Kinase 2, a serine/threonine kinase, is rapidly induced in T cells following activation and plays an inhibitory role in T cell-mediated help for the GC formation. Specifically, T cells deficient in Dapk2 have an increased ability to physically conjugate with antigen-presenting B cells and to promote GC formation. However, Dapk2 does not regulate T cell receptor signaling strength and does not influence cytokine-driven T-cell subset polarization. Instead, Dapk2 dampens mTORC1 activities by associating with Raptor. Silencing of Raptor rescues defects observed with the Dapk2 insufficiency. Our study thus identifies Dapk2 as a new kinase likely involved in negative regulation of contact-dependent help delivery to B cells and GC formation.

15.
Artigo em Inglês | MEDLINE | ID: mdl-33051888

RESUMO

Glucose homeostasis is tightly controlled by balance between glucose production and uptake in liver tissue upon energy shortage condition. Altered glucose homeostasis contributes to the pathophysiology of metabolic disorders including diabetes and obesity. Here, we aimed to analyze the change of proteomic profile upon prolonged fasting in mice with isobaric tag for relative and absolute quantification (iTRAQ) labelling followed by liquid chromatography-mass spectrometry (LC/MS) technology. Adult male mice were fed or fasted for 16 hours and liver tissues were collected for iTRAQ labelling followed by LC/MS analysis. A total of 322 differentially expressed proteins were identified, including 189 upregulated and 133 downregulated proteins. Bioinformatics analyses, including Gene Ontology analysis (GO), Kyoto encyclopaedia of genes and genomes analysis (KEGG) and protein-protein interaction analysis (PPI) were conducted to understand biological process, cell component, and molecular function of the 322 differentially expressed proteins. Among the 322 hepatic proteins differentially expressed between fasting and fed mice, we validated three upregulated proteins (Pqlc2, Ehhadh and Apoa4) and two downregulated proteins (Uba52 and Rpl37) by western blotting analysis. In cultured HepG2 hepatocellular cells, we found that depletion of Pqlc2 by siRNA-mediated knockdown impaired the insulin-induced glucose uptake, inhibited GLUT2 mRNA level and suppressed the insulin-induced Akt phosphorylation. By contrast, knockdown of Pqlc2 did not affect the cAMP/dexamethasone-induced gluconeogenesis. In conclusion, our study provides important information on protein profile change during prolonged fasting with iTRAQ- and LC-MS/MS-based quantitative proteomics, and identifies Pqlc2 as a potential regulator of hepatic glucose metabolism and insulin signalling pathway in this process.

16.
Gut ; 2020 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-33028669

RESUMO

OBJECTIVE: Intraductal papillary mucinous neoplasms (IPMNs) are non-invasive precursor lesions that can progress to invasive pancreatic cancer and are classified as low-grade or high-grade based on the morphology of the neoplastic epithelium. We aimed to compare genetic alterations in low-grade and high-grade regions of the same IPMN in order to identify molecular alterations underlying neoplastic progression. DESIGN: We performed multiregion whole exome sequencing on tissue samples from 17 IPMNs with both low-grade and high-grade dysplasia (76 IPMN regions, including 49 from low-grade dysplasia and 27 from high-grade dysplasia). We reconstructed the phylogeny for each case, and we assessed mutations in a novel driver gene in an independent cohort of 63 IPMN cyst fluid samples. RESULTS: Our multiregion whole exome sequencing identified KLF4, a previously unreported genetic driver of IPMN tumorigenesis, with hotspot mutations in one of two codons identified in >50% of the analyzed IPMNs. Mutations in KLF4 were significantly more prevalent in low-grade regions in our sequenced cases. Phylogenetic analyses of whole exome sequencing data demonstrated diverse patterns of IPMN initiation and progression. Hotspot mutations in KLF4 were also identified in an independent cohort of IPMN cyst fluid samples, again with a significantly higher prevalence in low-grade IPMNs. CONCLUSION: Hotspot mutations in KLF4 occur at high prevalence in IPMNs. Unique among pancreatic driver genes, KLF4 mutations are enriched in low-grade IPMNs. These data highlight distinct molecular features of low-grade and high-grade dysplasia and suggest diverse pathways to high-grade dysplasia via the IPMN pathway.

17.
Chem Asian J ; 15(22): 3825-3828, 2020 Nov 16.
Artigo em Inglês | MEDLINE | ID: mdl-33047472

RESUMO

A Rh(III)-catalyzed C-H arylation reaction of N-nitrosoanilines has been developed in which arylboronic acids were used as arylation reagents. It provides an efficient strategy for the synthesis of N-nitroso-[1,1'-biphenyl]-2-amine, which is an important starting material for the synthesis of N-hetero biaryl compounds, such as 2-amine-1,1'-biphenyl, carbazole, phenanthridone. This protocol can be applied to various N-alkyl substituted N-nitrosoanilines and N-nitrosoanilines with substituents on the phenyl ring. Arylboronic acids with both electron-donating and electron-withdrawing groups are tolerated.

18.
Curr Eye Res ; : 1-6, 2020 Oct 13.
Artigo em Inglês | MEDLINE | ID: mdl-33026255

RESUMO

PURPOSE: To evaluate the associations between medical check-up items (MCI) for fundus and intraocular pressure abnormality (FIPA) diseases in the Department of Health Management Centre, the Fifth Affiliated Hospital of Sun Yat-sen University (DHMC-FHS). PATIENTS AND METHODS: Individuals who visited DHMC-FHS and underwent MCI between June 2017 to May 2019 were included, 3237 subjects. A total of 356 participants were diagnosed as FIPA and enrolled. The general clinical characteristics were collected. Diseases for FIPA diagnosed included five cohort, high intraocular pressure, diabetic retinopathy, hypertension fundus arteriosclerosis, large eye cup, and high myopia fundus changes. Possible impact factors of MCI included blood routine, B-ultrasound, heart rate, hypertension, hyperlipidemia, standard vision, cerebral arteriosclerosis, body mass, arterial/carotid arteriosclerosis, etc. Further, the Pearson's correlation coefficients and logistic regression analyses were used to examine associations between MCI and FIPA. RESULTS: The weighted study population who belonged to FIPA included 356 subjects. There were significant differences in age, IOP, habitual exercise, smoking, sleep duration (P˂0.05) between FIPA and without FIPA. And RBC, Hemoglobin, B-ultrasound abnormal event, heart rate, systolic pressure, diastolic pressure, TC, LDL-C, standard vision, cerebral arteriosclerosis, body mass index, carotid arteriosclerosis were positively correlated with high intraocular pressure, hypertension fundus arteriosclerosis and high myopia fundus changes (P < .05). Possible prognosis risk factors, higher IOP, habitual exercise and more frequent smoking affect FIPA prognosis significantly [Odds ratio (OR) = 0.53, P = .01; OR = 0.13, P = .03; OR = 0.83; P = .04, respectively]. CONCLUSION: Of FIPA participants, high intraocular pressure, hypertension fundus arteriosclerosis and high myopia fundus changes were shown a positive relationship with MCI. Control IOP, habitual exercise and less frequent smoking were regarded as positive associations with decreased FIPA. These findings could help us prevent and diagnose FIPA diseases in time via MCI.

19.
Int J Infect Dis ; 2020 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-33017697

RESUMO

OBJECTIVE: This study aims to present clinical characteristics of 30 hospitalized cases with epileptic seizure and coronavirus disease 2019(COVID-19).  METHODS: This is a retrospective observational research. Clinical data were extracted from electronic medical records in 1550 patients with laboratory-confirmed diagnosis of COVID-19 who hospitalized in Wuhan Central Hospital, China, from 1 January to 31 April, 2020. 30 COVID-19 patients with the diagnosis of epilepsy were enrolled. The clinical characteristics, complications, treatments,and clinical outcomes of 30 cases were collected. RESULT: Of 30 patients with diagnosis of epilepsy and COVID-19, 13 patients(43.4%) had new-onset epileptic seizure without epilepsy history(new-onset seizure group,NS group), 10 patients(33.3%) with epilepsy history had recurrent epileptic seizure(recurrent seizure group,RS group) and 7 patients(23.3%) with epilepsy history had no seizure during the course of COVID-19 (epilepsy history group,EH group). Patients in RS group had more other neurological disease history except for epilepsy than those in NS group and EH group(7/10[70%] VS 1/13 [7.7%]VS1/7[14.3%]), and the difference between RS group and NS group is significant (P < 0.05). Patients in NE group and RS group suffered more severe/critical COVID-19 infection than patients in EH group (10/13[76.9%] VS 6/10[60%] VS 1/7[14.3%]),and the difference between NS group and EH group is significant (P < 0.05). 36.7% of patients had 1 to 5 complications,and 46.4% of patients had 6-10 complications.The complications in patients with seizure(in RS group and NS group) seem to be more than those without seizure(in EH group), but it doesn't have statistic difference. The proportion of antiepileptic drugs (AEDs) treatment before admission was higher in EH group than in RE group(7/7 [100%] VS 2/10 [20%], P < 0.05). The mortality of 30 patients with epilepsy and COVID-19 was 36.67%. The mortality of NS group(38.5%) and RS group(50%) were a little higher than in EH group(14.3%). None of convalescent patients had recurrent seizure, and there was no more death in the 3 month follow-up after discharge. CONCLUSIONS: COVID-19 Patients with recurrent epileptic seizure had more underlying neurological diseases than patients who had epilepsy history but without seizure.Patients with new-onset and recurrent epileptic seizure suffered more sever/critical COVID-19, which may lead to a worse prognosis.If patients with epilepsy history continue using AEDs during COVID-19 pandemics, the risk of recurrent seizure may reduce, and a good prognosis for patients with epilepsy history could be expected.

20.
Artigo em Inglês | MEDLINE | ID: mdl-33012100

RESUMO

QF-036 is an HIV-1 maturation inhibitor in pre-clinical development, and its antiviral activity against a laboratory HIV-1 strain and two drug-resistant strains was determined in the C8166 line. QF-036 was also subjected to absorption, distribution and metabolism (ADM) assessment in vitro, and pharmacokinetic profiles were evaluated in rats and monkeys. The 50% effective concentrations (EC50 ) of QF-036 against the three strains were 20.36 nM, 0.39 µM and 2.11 nM, respectively, demonstrating better antiviral potential than the first-generation antiviral maturation inhibitor bevirimat. QF-036 demonstrated moderate cell permeability, high plasma protein binding ability and good metabolic stability in vitro. After oral QF-036 administration to rats and monkeys, both species exhibited moderate bioavailability, and the plasma drug exposure increased in an approximately dose-proportional manner. When administered orally (30 mg/kg) to monkeys, the QF-036 plasma concentration (Cmax ) peaked at 3671 ng/mL (4.82 µM), 12 to 2410 times higher than the EC50 of laboratory or resistant HIV-1 strains. Moreover, the plasma concentration of QF-036 at 12 hours after administration was 263 ng/mL (0.35 µM), which approximately matched the highest EC50 value of the three test strains. The favourable viral inhibitory activity and pharmacokinetic properties provide critical support for QF-036 as a promising anti-HIV therapeutic candidate.

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