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  • Oxford University Press (OUP)  (23)
  • Pharmacy  (23)
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  • Oxford University Press (OUP)  (23)
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  • Pharmacy  (23)
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  • 1
    In: Journal of Antimicrobial Chemotherapy, Oxford University Press (OUP), Vol. 75, No. 10 ( 2020-10-01), p. 2986-2993
    Abstract: Real-world experience regarding the effectiveness of co-formulated elvitegravir, cobicistat, emtricitabine and tenofovir alafenamide (EVG/C/FTC/TAF) as a switch regimen is sparse among people living with HIV (PLWH) harbouring the M184V/I mutation with or without thymidine analogue-associated mutations (TAMs). Methods In this retrospective multicentre study, PLWH who were switched to EVG/C/FTC/TAF after having achieved viral suppression (plasma HIV RNA & lt;200 copies/mL) for 6 months or longer were included. Patients with archived M184V/I mutation (case patients) were matched to controls without M184V/I mutation at a 1:4 ratio. Patients with a history of virological failure or resistance to elvitegravir were excluded. The primary endpoint was virological non-success (plasma HIV RNA ≥50 copies/mL) at Week 48 of switch using a modified FDA snapshot analysis. Results Overall, 100 case patients with the M184V/I mutation were identified, including 6 (6.0%) with K65R and 13 (13.0%) with at least one TAM, and were matched to 400 controls in terms of gender, age (mean = 40.3 versus 39.7 years) and cumulative exposure duration to tenofovir disoproxil fumarate (median = 146 versus 143 weeks). At Week 48, the rate of virological non-success for the case patients and controls was 5.0% (5/100) and 3.3% (13/400), respectively (difference = 1.7%; 95% CI = −2.9%–6.3%), while the rate of virological success was 88.0% and 89.5% for the case patients and controls, respectively. The presence of the K65R mutation or TAMs was not associated with virological non-response. Conclusions Among virally suppressed PLWH, EVG/C/FTC/TAF is effective in maintaining viral suppression at Week 48 despite archived M184V/I mutation with or without TAMs.
    Type of Medium: Online Resource
    ISSN: 0305-7453 , 1460-2091
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2020
    detail.hit.zdb_id: 1467478-6
    SSG: 15,3
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  • 2
    In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 68, No. 4 ( 2016-04-25), p. 494-502
    Abstract: This study investigated the effect of tannic acid (TA), a plant-derived hydrolyzable polyphenol, on Kv7.4 and Kv7.5 K+ channels and rat mesenteric artery. Methods Whole-cell patch clamp experiments were used to record the Kv7.4 and Kv7.3/7.5 K+ currents expressed in HEK293 cells; and the tension changes of mesenteric arteries isolated from rats were recorded using small vessel myography apparatus. Key findings Tannic acid increases the Kv7.4 and Kv7.3/7.5 K+ currents in a concentration-dependent manner (median effective concentration (EC50) = 27.3 ± 3.6 μm and EC50 = 23.1 ± 3.9 μm, respectively). In addition, 30 μm TA shifts the G–V curve of Kv7.4 and Kv7.3/7.5 K+ currents to the left by 14.18 and 25.24 mV, respectively, and prolongs the deactivation time constants by 184.44 and 154.77 ms, respectively. Moreover, TA relaxes the vascular tension of rat mesenteric arteries in a concentration-dependent manner (half inhibitory concentration (IC50) = 148.7 ± 13.4 μm). Conclusion These results confirms the vasodilatory effects of TA on rat mesenteric artery and the activating effects on the Kv7.4 and Kv7.3/7.5 K+ channels, which may be a mechanism to explain the vasodilatory effect and this mechanism can be used in the research of antihypertension.
    Type of Medium: Online Resource
    ISSN: 2042-7158 , 0022-3573
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2016
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    detail.hit.zdb_id: 2050532-2
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  • 3
    Online Resource
    Online Resource
    Oxford University Press (OUP) ; 2023
    In:  Alcohol and Alcoholism Vol. 58, No. 5 ( 2023-09-09), p. 485-496
    In: Alcohol and Alcoholism, Oxford University Press (OUP), Vol. 58, No. 5 ( 2023-09-09), p. 485-496
    Abstract: Alcohol use is a major risk factor for the burden of mortality and morbidity. Alcoholic cirrhosis (AC) and alcoholic liver cancer (ALC) are most important and severe liver disease outcomes caused by alcohol use. The objectives of the current study were to investigate the global prevalence and burden of disease in disability-adjusted life years (DALYs) for AC and ALC, based on data from the Global Burden of Disease (GBD). Incidence, prevalence, death, and DALYs for GBDs in different locations, years, sex, and age groups were estimated using DisMod-MR 2.1 and a generic Cause of Death Ensemble Modeling approach. The correlations between the age-standardized incidence rate or age-standardized death rate and gender, sociodemographic index (SDI), and alcohol usage were conducted by Generalized Linear Models. Globally, the changes of age-standardized rates of indicators were not much significant over the 30-year period. However, the changes varied widely across regions. Central Asia and East Europe contributed the highest age-standardized incidence, prevalence, death, and DALYs and increased sharply by past 30 years. Generalized Linear Models (GLMs) showed male gender as a risk factor of AC, with the relative risk of incidence of 1.521 and relative risk of death of 1.503. Globally, there were improvements in overall health with regard to GBDs over the 30 years. However, the prevention of AC and ALC should be promoted in middle and middle-high SDI regions, especially Central Asia and East Europe, whereas more medical resources should be provided to improve treatment levels in low SDI region.
    Type of Medium: Online Resource
    ISSN: 0735-0414 , 1464-3502
    RVK:
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2023
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  • 4
    In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 73, No. 9 ( 2021-08-12), p. 1218-1229
    Abstract: Diabetic nephropathy (DN) is a severe diabetic complication. Dioscorea zingiberensis (DZ) possesses excellent pharmacological properties with lower toxicity. The purpose of this study was to investigate the efficacy and mechanism of DZ in DN. Methods DN was established by the high-fat diet combining intraperitoneal injection of streptozotocin in mice. The DZ (125 and 250 mg/kg/day) were intragastrical administered for 8 consecutive weeks. After treatment, blood, urine and kidney tissue were collected for biological detection, renal morphology, fibrosis and molecular mechanism research, respectively. Key findings This study has shown that DZ significantly ameliorated kidney hypertrophy, renal structural damage and abnormal function of the kidney indicators (creatinine, urinary protein and blood urea nitrogen). Further molecular mechanism data suggested that the NLRP3/Cleaved-caspase-1 signal pathway was remarkably activated in DN, and DZ treatment reversed these changes, which indicated that it effectively attenuated inflammatory response caused by hyperglycaemia. In addition, DN inhibits hyperglycaemia-induced activation of oxidative stress by suppressing the expression of p66Shc proteins. Conclusions DZ could efficiently suppress oxidative stress and inflammatory responses to postpone the development of DN, and its mechanism might be related to inhibition of NLRP3 and p66Shc activities. Thus, DZ could be developed into a new therapeutic agent for DN.
    Type of Medium: Online Resource
    ISSN: 0022-3573 , 2042-7158
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2021
    detail.hit.zdb_id: 2041988-0
    detail.hit.zdb_id: 2050532-2
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  • 5
    Online Resource
    Online Resource
    Oxford University Press (OUP) ; 2018
    In:  Journal of Pharmacy and Pharmacology Vol. 70, No. 12 ( 2018-11-08), p. 1596-1605
    In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 70, No. 12 ( 2018-11-08), p. 1596-1605
    Abstract: Pethidine hydrochloride (PH) and fentanyl citrate (FC) are opioid receptor agonists commonly used to treat pain clinically. PH and FC have been reported to have a high potential for pseudoallergic effects, but the underlying mechanism has not been well studied. MRGPRX2 is a novel atypical opioid receptor that is mainly expressed in human mast cells and considered to mediate drug-induced pseudoallergic reactions. This study aimed to investigate the allergy effect of these two opioid receptor agonists and the possible association of MRGPRX2 with this response. Methods HEK293-MRGPRX2/CMC assay, molecular docking assay, calcium mobilization assay, the test of β-hexosaminidase, histamine and cytokine release assay were performed in this article. Key findings PH but not FC induced LAD2 cell activation and degranulation dose-dependently. Histamine, tumour necrosis factor (TNF)-α, interleukin (IL)-8, monocyte chemotactic protein 1 (MCP-1) and macrophage inflammatory protein (MIP-1β) levels were upregulated by PH, but not FC. The PH-induced activation of mast cell was MRGPRX2-dependent. Conclusions PH but not FC activated mast cells, leading to degranulation mediated via MRGPRX2 receptors, which could be greatly significant in future clinical applications of opioid receptor drugs.
    Type of Medium: Online Resource
    ISSN: 0022-3573 , 2042-7158
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2018
    detail.hit.zdb_id: 2041988-0
    detail.hit.zdb_id: 2050532-2
    SSG: 15,3
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  • 6
    In: Journal of Antimicrobial Chemotherapy, Oxford University Press (OUP), Vol. 76, No. 11 ( 2021-10-11), p. 2875-2883
    Abstract: Ceftazidime/avibactam is not active against MBL-producing bacteria. Combining ceftazidime/avibactam or avibactam with aztreonam can counter the resistance of MBL-producing Enterobacterales. The aim of this study was to evaluate whether the addition of avibactam could reduce or close the mutant selection window (MSW) of aztreonam in Escherichia coli and Klebsiella pneumoniae harbouring MBLs; MSW is a pharmacodynamic (PD) parameter for the selection of emergent resistant mutants. Methods In vitro susceptibility of 19 clinical isolates to ceftazidime/avibactam, aztreonam alone, and in co-administration (aztreonam/ceftazidime/avibactam and aztreonam/avibactam) was determined, as well as the mutant prevention concentration (MPC). The fraction of time within 24 h that the free drug concentration was within the MSW (fTMSW) and the fraction of time that the free drug concentration was above the MPC (fT & gt;MPC) in both plasma and epithelial lining fluid (ELF) were determined from simulations of 10 000 profiles. The joint PTA was used to derive a joint cumulative fraction of response (CFR). Results All isolates were resistant to ceftazidime/avibactam or aztreonam. Combining aztreonam and avibactam or ceftazidime/avibactam resulted in synergistic bactericidal activities against all isolates. Synergism was primarily due to the aztreonam/avibactam combination. For aztreonam/avibactam dosing regimens evaluated in clinical trials, fT & gt;MPC values were & gt;90% and & gt;80%, whereas fTMSW measures were & lt;10% and & lt;20% in plasma and ELF, respectively. The CFR was 100% for aztreonam/avibactam against the collection of clinical isolates. Conclusions Effective antimicrobial combination optimized the PD parameters measuring selection for emergent mutants by increasing fT & gt;MPC and reducing fTMSW.
    Type of Medium: Online Resource
    ISSN: 0305-7453 , 1460-2091
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2021
    detail.hit.zdb_id: 1467478-6
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  • 7
    In: Journal of Antimicrobial Chemotherapy, Oxford University Press (OUP), Vol. 68, No. 5 ( 2013-5), p. 1089-1096
    Type of Medium: Online Resource
    ISSN: 1460-2091 , 0305-7453
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2013
    detail.hit.zdb_id: 1467478-6
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  • 8
    Online Resource
    Online Resource
    Oxford University Press (OUP) ; 2023
    In:  Journal of Pharmacy and Pharmacology Vol. 75, No. 4 ( 2023-04-07), p. 502-514
    In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 75, No. 4 ( 2023-04-07), p. 502-514
    Abstract: Reactive oxygen species (ROS) are involved in the structural remodelling of vascular segments and vascular beds. We identified a new imperatorin derivative, OW1, which has significant effects on vasodilation and inhibits vascular remodelling in hypertensive rats. In this study, we investigated whether OW1 inhibits vascular cell proliferation and migration by attenuating Nox1-ROS signalling. Methods Vascular smooth muscle cells (VSMCs) were treated with OW1 (1, 3 and 10 µmol/L) for 24 h incubation, and it has been analysed for proliferation and peroxidation levels. Moreover, the mRNA and protein levels of nicotinamide adenine dinucleotide phosphate oxidase (Noxs) were measured by RT-PCR and western blot. Furthermore, Nox1-ROS-MAPK/MMP mediated cell proliferation was detected by western blot. Key findings Ang II-induced increases in the levels of peroxidation and Noxs in VSMCs were also inhibited by OW1. OW1 attenuates cell proliferation and migration through the MAPK pathway and MMPs. OW1 treatment had no significant effects on cell migration, ROS levels, or the expression of phosphorylated MAPKs in VSMCs when Nox1 was knocked down. OW1 reduced ROS levels and expression of phosphorylated MAPKs in NIH3T3 cells with a Nox1 overexpression plasmid. Conclusion OW1 may inhibit vascular remodelling by downregulating the Nox1-ROS-MAPK/MMP signalling pathway.
    Type of Medium: Online Resource
    ISSN: 0022-3573 , 2042-7158
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2023
    detail.hit.zdb_id: 2041988-0
    detail.hit.zdb_id: 2050532-2
    SSG: 15,3
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  • 9
    In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 72, No. 6 ( 2020-05-05), p. 852-862
    Abstract: Screen and identify the anti-pseudo-allergic activity components of Perilla frutescens leaves that interacted with MRGPRX2 (a new reported pseudo-allergic reaction-related receptor). Methods An overexpressed MRGPRX2 cell membrane chromatography (CMC) coupled with HPLC-ESI-IT-TOF system has been established to screen and identify the effective components from P. frutescens leaves. A frontal analysis method was performed to investigate the binding affinity between ligands and MRGPRX2. Their activity of relieving pseudo-allergic reaction was evaluated in vitro by histamine release assay, β-hexosaminidase release assay and intracellular Ca2+ mobilization assay. Key findings Extract of P. frutescens leaves was proved to be effective in anti-pseudo-allergic reaction by inhibiting MRGPRX2. Apigenin (API) and rosmarinic acid (ROS) were confirmed to be the potential anti-allergy compounds that could bind with MRGPRX2. The binding affinity (KD) of ROS and API with MRGPRX2 was (8.79 ± 0.13) × 10−8  m and (6.54 ± 1.69) × 10−8  m, respectively. The IC50 of API inhibiting laboratory of allergic disease 2 cells degranulation was also determined to be (51.96 ± 0.18) μm. Conclusions A MRGPRX2/CMC coupled with HPLC-ESI-IT-TOF system was successfully established and applied to discover the effective components from P. frutescens leaves.
    Type of Medium: Online Resource
    ISSN: 0022-3573 , 2042-7158
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2020
    detail.hit.zdb_id: 2041988-0
    detail.hit.zdb_id: 2050532-2
    SSG: 15,3
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  • 10
    In: Journal of Pharmacy and Pharmacology, Oxford University Press (OUP), Vol. 70, No. 3 ( 2018-02-14), p. 393-403
    Abstract: In alcoholic liver disease, alcohol and lipopolysaccharide (LPS) are major stimulation factors of hepatic lipogenesis. Our objective was to determine the protective mechanism of acanthoic acid (AA) in EtOH- and LPS-induced hepatic lipogenesis. Methods HSC-T6 cells were treated with ethanol (200 mm) plus LPS (1 μg/ml) for 1 h, followed by AA (10 or 20 μm) for another 6 h. C57BL/6 mice were pretreated with of AA (20 and 40 mg/kg) or equal volume of saline and then exposed to three doses of ethanol (5 g/kg body weight) within 24 h. The mice were sacrificed at 6 h after the last ethanol dosing. Key findings Acanthoic acid significantly decreased the expressions of α-SMA, collagen-I, SREBP-1, and lipin1/2 induced, also decreased fat droplets caused by EtOH/LPS. AA treatment decreased the protein expressions of TLR4, CD14, IRAK4, TRAF3, p-TAK1 and NF-κB increased by EtOH/LPS on HSC cells. Results in vivo were consistent with results in vitro. Conclusions Our data demonstrated that AA might modulate hepatic fibrosis and lipid deposition in HSC-T6 cell stimulated with ethanol combined with LPS by decreasing lipin1/2 via TLR4 and IRAK4 signalling pathways, and AA might be considered as a potential therapeutic candidate for alcoholic liver disease.
    Type of Medium: Online Resource
    ISSN: 2042-7158 , 0022-3573
    Language: English
    Publisher: Oxford University Press (OUP)
    Publication Date: 2018
    detail.hit.zdb_id: 2041988-0
    detail.hit.zdb_id: 2050532-2
    SSG: 15,3
    Location Call Number Limitation Availability
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