- Efficacy and safety of urate-lowering agents in asymptomatic hyperuricemia: systematic review and network meta-analysis of randomized controlled trials. [Meta-Analysis]
- CONCLUSIONS: Evidence suggests that allopurinol and febuxostat are the ULTs of choice in reducing composite renal events and improving renal function.
- PMC Free PDF
- The induction and inhibition of UDP-glycosyltransferases in Haemonchus contortus and their role in the metabolism of albendazole. [Journal Article]
- Albendazole (ABZ) is an anthelmintic frequently used to treat haemonchosis, a common parasitosis of ruminants caused by the gastrointestinal nematode Haemonchus contortus. This parasite is able to protect itself against ABZ via the formation of inactive ABZ-glycosides. The present study was designed to deepen the knowledge about the role of UDP-glycosyltransferases (UGTs) in ABZ glycosylation in …
- PMC Free PDF
- Usefulness of Optimized Human Fecal Material in Simulating the Bacterial Degradation of Sulindac and Sulfinpyrazone in the Lower Intestine. [Journal Article]Mol Pharm. 2022 07 04; 19(7):2542-2548.MP
- The first aim of this study was to evaluate the usefulness of optimized human fecal material in simulating sulforeductase activity in the lower intestine by assessing bacterial degradation of sulindac and sulfinpyrazone, two sulforeductase substrates. The second aim was to evaluate the usefulness of drug degradation half-life generated in simulated colonic bacteria (SCoB) in informing PBPK models…
- Publisher Full Text (DOI)
- Exploration of Potential Ewing Sarcoma Drugs from FDA-Approved Pharmaceuticals through Computational Drug Repositioning, Pharmacogenomics, Molecular Docking, and MD Simulation Studies. [Journal Article]
- Novel drug development is a time-consuming process with relatively high debilitating costs. To overcome this problem, computational drug repositioning approaches are being used to predict the possible therapeutic scaffolds against different diseases. In the current study, computational drug repositioning approaches were employed to fetch the promising drugs from the pool of FDA-approved drugs aga…
- PMC Free PDF
- Medical Adjuvant Therapy in Reducing Thrombosis With Arteriovenous Grafts and Fistulae Use: A Meta-Analysis of Randomized Controlled Trials. [Meta-Analysis]
- Hemodialysis is required for patients with end-stage renal disease (ESRD) that require arteriovenous (AV) grafts or fistulas for vascular access. These access points are prone to thrombosis. To determine the effect of medical adjuvant therapy on AV graft/fistula patency among patients with ESRD on hemodialysis. Adhering to the PRISMA 2020 statement, a systematic search was conducted until August …
- PMC Free PDF
- Computational Insights on the Potential of Some NSAIDs for Treating COVID-19: Priority Set and Lead Optimization. [Journal Article]
- The discovery of drugs capable of inhibiting SARS-CoV-2 is a priority for human beings due to the severity of the global health pandemic caused by COVID-19. To this end, repurposing of FDA-approved drugs such as NSAIDs against COVID-19 can provide therapeutic alternatives that could be utilized as an effective safe treatment for COVID-19. The anti-inflammatory activity of NSAIDs is also advantage…
- PMC Free PDF
- Enhanced abatement of pharmaceuticals by permanganate via the addition of Co3O4 nanoparticles. [Journal Article]
- Pharmaceuticals may pose serious potential risks, such as biological responses and chronic health effects, due to their ubiquitous in natural aquatic water bodies. In this study, we proposed an effective, feasible, and low-cost strategy for the abatement of pharmaceuticals (i.e., phenylbutazone (PBZ) and sulfinpyrazone (SPZ)) via Co3O4 nanoparticles (NPs) as heterogeneous catalyst in permanganate…
- Publisher Full Text (DOI)
- Functional validation of key cytochrome P450 monooxygenase and UDP-glycosyltransferase genes conferring cyantraniliprole resistance in Aphis gossypii Glover. [Journal Article]
- Cytochrome P450 monooxygenases (P450s) and UDP-glycosyltransferases (UGTs) are major detoxifying enzymes that metabolize plant toxins and insecticides. In the present study, the synergists of piperonyl butoxide, sulfinpyrazone and 5-nitrouracil significantly increased cyantraniliprole and α-cypermethrin toxicity against the resistant strain. The transcripts of UGT341A4, UGT344B4, UGT344D6, UGT344…
- Publisher Full Text (DOI)
- UDP-Glycosyltransferases from the UGT344 Family Are Involved in Sulfoxaflor Resistance in Aphis gossypii Glover. [Journal Article]
- UDP-glycosyltransferases (UGTs) are major phase II detoxification enzymes that catalyze the transfer of glycosyl residues from activated nucleotide sugars to acceptor hydrophobic molecules and play very important roles in the biotransformation of various endogenous and exogenous compounds. Our previous studies demonstrated that UGTs participated in the detoxification of insecticides in Aphis goss…
- PMC Free PDF
- Overexpression of Multiple UDP-Glycosyltransferase Genes Involved in Sulfoxaflor Resistance in Aphis gossypii Glover. [Journal Article]
- UDP-glycosyltransferases (UGTs) are major phase II enzymes involved in the metabolic detoxification of xenobiotics. In this study, two UGT-inhibitors, 5-nitrouracil and sulfinpyrazone, significantly increased sulfoxaflor toxicity against sulfoxaflor-resistant (Sul-R) Aphis gossypii, whereas there were no synergistic effects in susceptible (Sus) A. gossypii. The activity of UGTs in the Sul-R strai…
- Publisher Full Text (DOI)
- Association Between Use of Anti-gout Preparations and Dementia: Nested Case-Control Nationwide Population-Based Cohort Study. [Journal Article]
- Objectives: Gout is the most common form of inflammatory arthritis and was found to be independently associated with incident dementia in the elderly. However, the associations between anti-gout preparations and dementia were not well-studied. Methods: Data were collected from Taiwan's National Health Insurance Research Database (NHIRD). A 2005-2013 retrospective cohort study was conducted, and a…
- PMC Free PDF
- UDP-glycosyltransferases contribute to spirotetramat resistance in Aphis gossypii Glover. [Review]
- Uridine diphosphate (UDP)-glycosyltransferases (UGTs) catalyze the conjugation of small lipophilic endogenous and exogenous compounds with sugars to produce water-soluble glycosides, playing an important role in insect endobiotic regulation and xenobiotic detoxification. In this study, two UGT-inhibitors, sulfinpyrazone and 5-nitrouracil, significantly increased spirotetramat toxicity against thi…
- Publisher Full Text (DOI)
- Intestinal UDP-glucuronosyltransferase as a potential target for the treatment and prevention of lymphatic filariasis. [Journal Article]
- Lymphatic filariasis (LF), a morbid disease caused by the tissue-invasive nematodes Wuchereria bancrofti, Brugia malayi, and Brugia timori, affects millions of people worldwide. Global eradication efforts have significantly reduced worldwide prevalence, but complete elimination has been hampered by limitations of current anti-filarial drugs and the lack of a vaccine. The goal of this study was to…
- PMC Free PDF
- The impact of adoption of a new urate-lowering agent on trends in utilization and cost in practice. [Journal Article]
- CONCLUSIONS: ULT use moved to favor benzbromarone and febuxostat; greater expensive uptake for febuxostat led to a rapid rise in ULT cost. Marginal values of increasing access to febuxostat for asymptomatic hyperuricemia should be focus on future studies to facilitate drug prices negotiation and ensure appropriate ULT use.
- PMC Free PDF
- Characterization of UDP-Glucuronosyltransferases and the Potential Contribution to Nicotine Tolerance in Myzus persicae. [Journal Article]
- Uridine diphosphate (UDP)-glycosyltransferases (UGTs) are major phase II detoxification enzymes involved in glycosylation of lipophilic endobiotics and xenobiotics, including phytoalexins. Nicotine, one of the most abundant secondary plant metabolites in tobacco, is highly toxic to herbivorous insects. Plant-herbivore competition is the major impetus for the evolution of large superfamilies of UG…
- PMC Free PDF
- Safety and tolerability of available urate-lowering drugs: a critical review. [Review]
- Urate-lowering therapy (ULT) is the cornerstone of gout management, which is a widespread chronic illness characterized by hyperuricemia, arthropathy, tophus development, and urolithiasis. Since asymptomatic increased serum urate levels are associated with a higher risk of cardiovascular, renal and metabolic disorders, a larger use of ULTs in the general population is expected in the near future.
- Publisher Full Text (DOI)
- 2-O-β-d-glucopyranosyl-l-ascorbic acid, a novel vitamin C derivative from Lycium barbarum, prevents oxidative stress. [Journal Article]
- Reducing agents are crucial for the management of maladaptive inflammation-induced macrophage death and hematopoietic toxicity of chemotherapy. 2-O-β-d-glucopyranosyl-l-ascorbic acid (AA-2βG), a unique AA (or vitamin C) derivative identified in Lycium barbarum, exhibited enhanced free radical scavenging activity compared with AA and its synthetic derivative AA-2αG. AA-2βG protected hydrogen perox…
- PMC Free PDF
- UDP-Glycosyltransferases are involved in imidacloprid resistance in the Asian citrus psyllid, Diaphorina citri (Hemiptera: Lividae). [Journal Article]
- UDP-glycosyltransferases (UGTs), as phase II detoxification enzymes, are widely distributed within living organisms and play vital roles in the biotransformation of endobiotics and xenobiotics in insects. Insects increase the expression of detoxification enzymes to cope with the stress of xenobiotics, including insecticides. However, the roles of UGTs in insecticide resistance are still seldom re…
- Publisher Full Text (DOI)
- Characterization of tick organic anion transporting polypeptides (OATPs) upon bacterial and viral infections. [Journal Article]
- CONCLUSIONS: This study provides additional evidence on the role of arthropod OATPs in vector-intracellular pathogen interactions.
- PMC Free PDF
- An Ex Vivo Fermentation Screening Platform to Study Drug Metabolism by Human Gut Microbiota. [Journal Article]
- Colon microbiota-based drug metabolism has received little attention thus far in the process of drug development, whereas the role of gut microbiota in clinical safety and efficacy of drugs has become more clear. Many of these studies have been performed using animal studies, but the translational value of these data with respect to drug pharmacokinetics, efficacy, and safety is largely unknown. …
- Publisher Full Text (DOI)
- Thiamethoxam Resistance in Aphis gossypii Glover Relies on Multiple UDP-Glucuronosyltransferases. [Journal Article]
- Uridine diphosphate (UDP)-glycosyltransferases (UGTs) are major phase II enzymes that conjugate a variety of small lipophilic molecules with UDP sugars and alter them into more water-soluble metabolites. Therefore, glucosidation plays a major role in the inactivation and excretion of a great variety of both endogenous and exogenous compounds. In this study, two inhibitors of UGT enzymes, sulfinpy…
- PMC Free PDF
- Effects of Discontinuation of Urate-Lowering Therapy: A Systematic Review. [Journal Article]
- Urate-lowering therapy (ULT) is associated with low rates of adherence, leading to a potential risk of relapse of gouty arthritis, tophi, or urolithiasis. Our main aim was to identify the recurrence of gouty arthritis, tophi, or urolithiasis after discontinuation of ULT. Secondary aims included an assessment of ULT reintroduction rates and factors associated with relapse.
- PMC Free PDF
- Vitamin C modulates glutamate transport and NMDA receptor function in the retina. [Journal Article]
- Vitamin C (in the reduced form ascorbate or in the oxidized form dehydroascorbate) is implicated in signaling events throughout the central nervous system (CNS). In the retina, a high-affinity transport system for ascorbate has been described and glutamatergic signaling has been reported to control ascorbate release. Here, we investigated the modulatory role played by vitamin C upon glutamate upt…
- Publisher Full Text (DOI)
- Discovery and characterization of verinurad, a potent and specific inhibitor of URAT1 for the treatment of hyperuricemia and gout. [Journal Article]
- Gout is caused by elevated serum urate levels, which can be treated using inhibitors of the uric acid transporter, URAT1. Here, we characterize verinurad (RDEA3170), which is currently under evaluation for gout therapy. Verinurad specifically inhibits URAT1 with a potency of 25 nM. High affinity inhibition of uric acid transport requires URAT1 residues Cys-32, Ser-35, Phe-365 and Ile-481. Unlike …
- PMC Free Full TextPMC Free PDF
- The rising prevalence and incidence of gout in British Columbia, Canada: Population-based trends from 2000 to 2012. [Journal Article]
- CONCLUSIONS: The burden of gout in BC, Canada, is substantial, and both the prevalence and incidence have increased over the past decade, while prescription of ULT remains low. These data support the need to improve gout prevention and care.
- PMC Free PDF
- Over-expression of UDP-glycosyltransferase gene UGT2B17 is involved in chlorantraniliprole resistance in Plutella xylostella (L.). [Journal Article]
- CONCLUSIONS: UGT2B17 is involved in the detoxification of chlorantraniliprole, and its over-expression may play an important role in chlorantraniliprole resistance in P. xylostella. These results shed some light upon and further our understanding of the mechanisms of diamide insecticide resistance in insects. © 2016 Society of Chemical Industry.
- Publisher Full Text (DOI)
- Medical Adjuvant Treatment to Improve the Patency of Arteriovenous Fistulae and Grafts: A Systematic Review and Meta-analysis. [Review]
- CONCLUSIONS: This systematic review has not demonstrated a beneficial effect for any adjuvant treatment to increase the patency of AVF or grafts in the short term, except ticlopidine which has been taken off the market.
- Publisher Full Text (DOI)
- Vitamin C Facilitates Demethylation of the Foxp3 Enhancer in a Tet-Dependent Manner. [Journal Article]
- Demethylation of CpG motifs in the Foxp3 intronic element, conserved noncoding sequence 2 (CNS2), is indispensable for the stable expression of Foxp3 in regulatory T cells (Tregs). In this study, we found that vitamin C induces CNS2 demethylation in Tregs in a ten-eleven-translocation 2 (Tet2)-dependent manner. The CpG motifs of CNS2 in Tregs generated in vitro by TGF-β (iTregs), which were methy…
- Publisher Full Text (DOI)
- Triclinic and monoclinic polymorphs of meso-(E,E)-1,1'-[1,2-bis(4-chlorophenyl)ethane-1,2-diyl]bis(phenyldiazene): the high-yield synthesis of an unexpected product, concomitant polymorphism and configurational disorder. [Journal Article]
- Pyrazolidine-3,5-diones and their derivatives exhibit a wide range of biological activities. Seeking to explore the effect of combining a hydrocarbyl ring substituent, as present in sulfinpyrazone (used to treat gout), with a chlorinated aryl ring, as present in muzolimine (a diuretic), we explored the reaction between 1-phenylpyrazolidine-3,5-dione and 4-chlorobenzaldehyde under mildly basic con…
- Publisher Full Text (DOI)
- Ascorbic acid efflux from human brain microvascular pericytes: role of re-uptake. [Journal Article]
- Microvascular pericytes take up ascorbic acid on the ascorbate transporter SVCT2. Intracellular ascorbate then protects the cells against apoptosis induced by culture at diabetic glucose concentrations. To investigate whether pericytes might also provide ascorbate to the underlying endothelial cells, we studied ascorbate efflux from human pericytes. When loaded with ascorbate to intracellular con…
- PMC Free PDF