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Showing "Study Assess Effect Ketoconazole Metabolism Navitoclax" PubMed Articles 1–25 of 78,000+

A novel role for ketoconazole in hepatocellular carcinoma treatment: linking PTGS2 to mitophagy machinery.

Ketoconazole is a broad-spectrum antifungal agent, which has recently been characterized as a potential anticancer agent in several cancer types. However, the molecular mechanism underlying the anticancer effect of ketoconazole is not clearly defined. Our recent findings demonstrate that ketoconazole suppresses the growth of hepatocellular carcinoma (HCC) cells by exacerbating mitophagy in vitro and in vivo. Mechanistically, PINK1-PRKN-mediated mitophagy are led by ketoconazole-induced suppression of PTGS2 ...

Evaluation of ketoconazole formulations for topical use in cutaneous leishmaniasis caused by Leishmania (Viannia).

The effectiveness of various pharmaceutical formulations of ketoconazole was evaluated in experimental models of cutaneous leishmaniasis (LC) in BALB C mice. Topical gel, lipogel, and cream formulations containing permeation enhancers and different concentrations of ketoconazole were prepared. Stability, toxicity and anti-Leishmania activity were determined in vitro. In addition, the effectiveness of topically applied formulations in LC-infected mice infected with Leishmania (Viannia) braziliensis was evalu...

Automated small-scale in vitro transfer model as screening tool for the prediction of in vivo-dissolution and precipitation of poorly solubles.

Precipitation testing, especially for weakly basic APIs, represents a key parameter in drug substance characterization during early development stages, where the amount of API available is limited. Therefore, it was the aim of this study to develop an automated small-scale in vitro transfer model to characterize the supersaturation and precipitation behavior of two poorly water-soluble drugs. Following automation and scale-down of the standard transfer model, the developed small-scale model was used to asse...

Revisiting the Warburg Effect: Some Tumors Hold Their Breath.

Studies have shown that tumors commonly exhibit normal or enhanced respiration in addition to glycolytic metabolism. In this issue, Courtney et al. (2018) report a reduction in mitochondrial function in kidney cancer patients and thus a classic "Warburg Effect" that further illustrates the heterogeneity of human cancer metabolism.

CYP2C9 and OATP1B1 genetic polymorphisms affect the metabolism and transport of glimepiride and gliclazide.

The therapeutic use of glimepiride and gliclazide shows substantial inter-individual variation in pharmacokinetics and pharmacodynamics in human populations, which might be caused by genetic differences among individuals. The aim of this study was to assess the effect of CYP2C9 and OATP1B1 genetic polymorphisms on the metabolism and transport of glimepiride and gliclazide. The uptake of glimepiride and gliclazide was measured in OATP1B1*1a, *5 and *15-HEK293T cells, and their metabolism was measured using C...

The effect of red blood cell transfusion on iron metabolism in critically ill patients.

Anemia of inflammation (AI) has a high prevalence in critically ill patients. In AI, iron metabolism is altered, as high levels of inflammation-induced hepcidin reduce the amount of iron available for erythropoiesis. AI is treated with red blood cell (RBC) transfusions. The effect of RBC transfusion on iron metabolism during inflammatory processes in adults is unknown. We investigated the effect of RBC transfusion on iron metabolism in critically ill patients.

Liver damage indices as a tool for modifying methadone maintenance treatment: a cross-sectional study.

To assess the effect of liver damage on methadone metabolism in opiate addicts undergoing methadone maintenance treatment (MMT).

Effect of organic acids on molecular mobility, physical stability and dissolution of ternary ketoconazole spray dried dispersions.

In an earlier investigation, ketoconazole (KTZ) - organic acid coamorphous systems were prepared, wherein, in the solid-state, there was ionic and/or hydrogen bonding interactions between the drug and the acid (Fung et al, Mol. Pharmaceutics, 2018, 15 (5), 1862-1869). While the coamorphous systems accelerated KTZ dissolution, the organic acids were not effective in maintaining supersaturation and drug precipitation was observed. Ternary drug-polymer-acid amorphous solid dispersions (ASDs) were prepared with...

In vivo confirmation of altered hepatic glucose metabolism in patients with liver fibrosis/cirrhosis by F-FDG PET/CT.

The aim of this study was to assess the value of F-FDG PET/CT for quantitative assessment of hepatic metabolism in patients with different stages of liver fibrosis/cirrhosis.

Effect of liraglutide on physical performance in type 2 diabetes: Results of a randomized, double-blind, controlled trial (LIPER2).

-: To assess the effect of the GLP-1 analogue liraglutide on measures of cardiac function and physical performance in patients with type 2 diabetes (T2D).

The misery-is-not-miserly effect revisited: Replication despite opportunities for compensatory consumption.

Sadness increases how much decision makers pay to acquire goods, even when decision makers are unaware of it. This effect is coined the "misery-is-not-miserly effect". The paper that first established this effect is the second most-cited article appearing in Psychological Science in 2004. In light of its impact, the present study sought to assess whether the misery-is-not-miserly effect would replicate (a) in a novel context and (b) even when another way of alleviating a sense of loss (i.e., compensatory co...

The effects of plasma chromium on lipid profile, glucose metabolism and cardiovascular risk in type 2 diabetes mellitus. A case - control study.

The study was aimed at determining the effect of plasma chromium concentration on the metabolism of glucose, and lipids and their subsequent cardiovascular risk in patients with type 2 diabetes in the Bolgatanga district of Ghana.

An integrative urinary metabolomic study of the therapeutic effect of Guizhi Fuling capsule on primary dysmenorrheal rats based H NMR and UPLC-MS.

Guizhi Fuling capsule (GFC) was an important traditional Chinese herbal medicine used for the treatment of primary dysmenorrheal (PD). The aim of this study was to evaluate the anti-dysmenorrheal effect of GFC on dysmenorrheal rats induced by oxytocin and to investigate its mechanism of action. An integrative urinary metabolomic study based on H NMR and UPLC-MS was used to investigate the therapeutic effect of GFC on PD rats. In addition, in order to obtain more potential biomarkers and to investigate the g...

Effect sizes of BOLD CVR, resting-state signal fluctuations and time delay measures for the assessment of hemodynamic impairment in carotid occlusion patients.

The BOLD signal amplitude as a response to a hypercapnia stimulus is commonly used to assess cerebrovascular reserve. Despite recent advances, the implementation remains cumbersome and alternative ways to assess hemodynamic impairment are desirable. Resting-state BOLD signal fluctuations (rsBOLD) have been proposed however data on its sensitivity and dependence on baseline venous cerebral blood volume (vCBV) is limited. The primary aim of this study was to compare the effect sizes of resting-state and hyper...

Mannose receptor C type 2 mediates 1,25(OH)D/vitamin D receptor-regulated collagen metabolism through collagen type 5, alpha 2 chain and matrix metalloproteinase 13 in murine MC3T3-E1 cells.

Vitamin D plays an important role in maintaining skeletal development and bone homeostasis. Although vitamin D has been extensively researched, the direct effect of 1,25(OH)D on osteoblasts is unclear. To explore the 1,25(OH)D action on murine osteoblasts, we performed tandem mass tag experiments on MC3T3-E1 cells treated with and without 1,25(OH)D. Three up-regulated proteins (MRC2, WWTR1 and RASSF2) related to bone metabolism were confirmed in this study. 1,25(OH)D up-regulated the expression of MRC2 thro...

Pharmacokinetics of a Lobeglitazone/Metformin Fixed-Dose Combination Tablet (CKD-395 0.5/1000 mg) Versus Concomitant Administration of Single Agents and the Effect of Food on the Metabolism of CKD-395 in Healthy Male Subjects.

This study aimed to compare the pharmacokinetic profile of combined CKD-395 0.5/1000 mg treatment with that of the coadministration of lobeglitazone sulfate 0.5 mg and metformin hydrochloride (HCl) extended-release (XR) 1000 mg and assess the effect of food on the pharmacokinetics of CKD-395 0.5/1000 mg. Two clinical trials were conducted as part of an open-label, single-dose, randomized, 2-period, 2-sequence crossover study. In study 1, a total of 26 subjects received either CKD-395 0.5/1000 mg as a t...

Intervention effect of Qi-Yu-San-Long Decoction on Lewis lung carcinoma in C57BL/6 mice: Insights from UPLC-QTOF/MS-based metabolic profiling.

Qi-Yu-San-Long Decoction (QYSLD) has been used to treat lung carcinoma for over twenty years in clinical practices, and its curative effect is considered credible. However, the therapeutic mechanism of this effect has not been thoroughly elucidated to date. In this study, a MTT dye reduction assay and DAPI staining were first used to evaluate the cell viability and apoptosis of A549 cells with and without QYSLD-treatment, respectively. The weight/volume of Lewis lung carcinoma (LLC) sarcoma was used to asse...

Global rewiring of cellular metabolism renders Saccharomyces cerevisiae Crabtree negative.

Saccharomyces cerevisiae is a Crabtree-positive eukaryal model organism. It is believed that the Crabtree effect has evolved as a competition mechanism by allowing for rapid growth and production of ethanol at aerobic glucose excess conditions. This inherent property of yeast metabolism and the multiple mechanisms underlying it require a global rewiring of the entire metabolic network to abolish the Crabtree effect. Through rational engineering of pyruvate metabolism combined with adaptive laboratory evolut...

Non-targeted metabolomic analysis on multidrug resistance hepatocellular carcinoma cell and reversal effect of annonaceous acetogenins.

Multidrug-resistance (MDR) has been shown to play a critical role in the development of many diseases. In this study, we used metabolomic method to evaluate the MDR in hepatocellular carcinoma, and investigate regulatory of annonaceous acetogenins on MDR of hepatocellular carcinoma. Multivariate statistical analysis revealed that the MDR of SMMC 7721 together with changes in glutathione metabolism, arginine and proline metabolism, sphingolipid metabolism. Annonaceous acetogenins impact these metabolism path...

Assessing tackle performance using a novel collision sport simulator in comparison to a "live" one-on-one tackling drill.

It is necessary to study the rugby tackle as it is associated with successful performance outcomes and is responsible for the majority of contact injuries. A novel collision sport simulator was developed to study tackle performance. The main aim of this validation study was to assess tackle technique performance between two different conditions: simulator versus a standardised one-on-one tackle drill previously used to assess technique. Tackling proficiency was assessed using a list of technical criteria. M...

Effect of sitagliptin on energy metabolism and brown adipose tissue in overweight individuals with prediabetes: a randomised placebo-controlled trial.

The aim of this study was to evaluate the effect of sitagliptin on glucose tolerance, plasma lipids, energy expenditure and metabolism of brown adipose tissue (BAT), white adipose tissue (WAT) and skeletal muscle in overweight individuals with prediabetes (impaired glucose tolerance and/or impaired fasting glucose).

No Clinical Impact of CYP3A5 Gene Polymorphisms on the Pharmacokinetics and/or Efficacy of Maraviroc in Healthy Volunteers and HIV-1-Infected Subjects.

Maraviroc is a C-C chemokine receptor type-5 antagonist approved for the treatment of HIV-1. Previous studies show that cytochrome P450 3A5 (CYP3A5) plays a role in maraviroc metabolism. CYP3A5 is subject to a genetic polymorphism. The presence of 2 functional alleles (CYP3A5*1/*1) confers the extensive metabolism phenotype, which is rare in whites but common in blacks. The effect of CYP3A5 genotype on maraviroc and/or metabolite pharmacokinetics was evaluated in 2 clinical studies: a post hoc analysis from...

Effect of liraglutide on ambulatory blood pressure in hypertensive patients with type 2 diabetes: randomized, double blind, placebo-controlled trial.

To assess the effect of liraglutide on 24-h ambulatory blood pressure and heart rate in patients with hypertension (pre- and stage 1 hypertension) and inadequately controlled type 2 diabetes (hemoglobin A 7-10%).

Female rats are more susceptible to metabolic effects of DHEA treatment.

Dehydroepiandrosterone (DHEA) is a steroid hormone that presents several effects on metabolism, however, most of the studies have been performed in male animals, while few authors have investigated possible sex differences regarding the metabolic effects of DHEA. Therefore, the aim of this study was to evaluate the effect of different doses of DHEA in metabolic parameters of male and ovariectomized female Wistar rats. Sex differences were found in the metabolism of distinct substrates and in relation to the...

Water supplementation reduces copeptin and plasma glucose in adults with high copeptin: the H2O Metabolism pilot study.

As elevated copeptin, a marker of vasopressin, is linked to low water intake and high diabetes risk, we tested the effect of water supplementation on copeptin and fasting glucose.

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