keyword
https://read.qxmd.com/read/37258948/unravelling-the-hepatic-elimination-mechanisms-of-colistin
#21
JOURNAL ARTICLE
Bing Qi, Matthias Gijsen, Tom De Vocht, Neel Deferm, Pieter Van Brantegem, Getahun B Abza, Nina Nauwelaerts, Joost Wauters, Isabel Spriet, Pieter Annaert
PURPOSE: Colistin is an antibiotic which is increasingly used as a last-resort therapy in critically-ill patients with multidrug resistant Gram-negative infections. The purpose of this study was to evaluate the mechanisms underlying colistin's pharmacokinetic (PK) behavior and to characterize its hepatic metabolism. METHODS: In vitro incubations were performed using colistin sulfate with rat liver microsomes (RLM) and with rat and human hepatocytes (RH and HH) in suspension...
May 31, 2023: Pharmaceutical Research
https://read.qxmd.com/read/37193181/the-potential-of-chinese-medicines-in-the-treatment-of-hyperuricemia
#22
REVIEW
Jiaqi Tang, Hongyan Gao, Yanqiu Xu, Jingru Chen, Bin Wu
The annual incidence of gout is increasing along with lifestyle and dietary changes. Accumulation of urate crystals in joints and tissues when the amount of uric acid exceeds its saturation concentration causes acute inflammation that leads to gout. Reducing the serum uric acid concentration is the key to treating gout. Allopurinol, febuxostat, benzbromarone, and other drugs are effective, but side effects of treatment such as toxicity and recurrence after drug withdrawal cannot be ignored. Recent studies have found that many Chinese medicines are effective and safe, provide durable efficacy, and are associated with low recurrence rates...
2023: American Journal of Translational Research
https://read.qxmd.com/read/37127506/comparison-of-benzbromarone-and-allopurinol-on-the-risk-of-chronic-kidney-disease-in-people-with-asymptomatic-hyperuricemia
#23
JOURNAL ARTICLE
Shih-Wei Lai, Kuan-Fu Liao, Yu-Hung Kuo, Bing-Fang Hwang, Chiu-Shong Liu
OBJECTIVE: The objective of the study was to compare the relative effects of benzbromarone and allopurinol on the risk of developing chronic kidney disease in persons with asymptomatic hyperuricemia. METHODS: A retrospective cohort study was conducted to analyze a 2003-2015 national database including all claims data of 2 million beneficiaries in Taiwan. Asymptomatic hyperuricemia was defined as follows: persons using urate-lowering drugs who never developed gout flares...
April 29, 2023: European Journal of Internal Medicine
https://read.qxmd.com/read/37105395/a-functional-genomics-approach-reveals-suggestive-quantitative-trait-loci-associated-with-combined-tlr4-and-bcp-crystal-induced-inflammation-and-osteoarthritis
#24
JOURNAL ARTICLE
Viola Klück, Collins K Boahen, Brenda Kischkel, Jéssica C Dos Santos, Vasiliki Matzaraki, Cindy G Boer, Joyce B J van Meurs, Kiki Schraa, Heidi Lemmers, Helga Dijkstra, Megan P Leask, Tony R Merriman, Tania O Crişan, Geraldine M McCarthy, Vinod Kumar, Leo A B Joosten
OBJECTIVE: Basic calcium phosphate (BCP) crystals can activate the NLRP3 inflammasome and are potentially involved in the pathogenesis of osteoarthritis (OA). In order to elucidate relevant inflammatory mechanisms in OA, we used a functional genomics approach to assess genetic variation influencing BCP crystal-induced cytokine production. METHOD: Peripheral blood mononuclear cells (PBMCs) were isolated from healthy volunteers who were previously genotyped and stimulated with BCP crystals and/or lipopolysaccharide (LPS) after which cytokines release was assessed...
August 2023: Osteoarthritis and Cartilage
https://read.qxmd.com/read/36967511/effects-of-different-doses-glimepiride-intake-on-the-pharmacokinetics-of-benzbromarone-in-rats
#25
JOURNAL ARTICLE
Yuxian Lin, Xuejing Gu, Jiali Liu, Qinghua Weng, Jianhua Xiong, Zhifang Chen, Yingcong Yu, Hui Xu, Yu Wang
Benzbromarone (BNR) is prescribed for the management of hyperuricemia, whereas glimepiride (GLM) for the treatment of Type 2 Diabetes Mellitus. Both drugs are certified to be mainly metabolized via cytochrome P450 (CYP) 2C9 in vivo and may have the potential drug-drug interactions. This study aims to investigate the possible influence of orally administered low- and high-dose glimepiride (GLM) on pharmacokinetic characteristics (PK) of benzbromarone (BNR) in rats. Fifteen rats were randomly assigned to group A, B and C (n=5) and administered 0...
January 2023: Pakistan Journal of Pharmaceutical Sciences
https://read.qxmd.com/read/36967079/the-tmem16a-blockers-benzbromarone-and-monna-cause-intracellular-ca-2-release-in-mouse-bronchial-smooth-muscle-cells
#26
JOURNAL ARTICLE
Ritu Dwivedi, Bernard T Drumm, Tuleen Alkawadri, S Lorraine Martin, Gerard P Sergeant, Mark A Hollywood, Keith D Thornbury
We investigated effects of TMEM16A blockers benzbromarone, MONNA, CaCCinh A01 and Ani9 on isometric contractions in mouse bronchial rings and on intracellular calcium in isolated bronchial myocytes. Separate concentrations of carbachol (0.1-10 μM) were applied for 10 min periods to bronchial rings, producing concentration-dependent contractions that were well maintained throughout each application period. Benzbromarone (1 μM) markedly reduced the contractions with a more pronounced effect on their sustained component (at 10 min) compared to their initial component (at 2 min)...
March 24, 2023: European Journal of Pharmacology
https://read.qxmd.com/read/36951953/tmem16e-regulates-endothelial-cell-procoagulant-activity-and-thrombosis
#27
JOURNAL ARTICLE
Alec A Schmaier, Papa F Anderson, Siyu M Chen, Emale El-Darzi, Ivan Aivasovsky, Milan P Kaushik, Kelsey D Sack, H Criss Hartzell, Samir M Parikh, Robert Flaumenhaft, Sol Schulman
Endothelial cells (ECs) normally form an anticoagulant surface under physiological conditions, but switch to support coagulation following pathogenic stimuli. This switch promotes thrombotic cardiovascular disease. To generate thrombin at physiologic rates, coagulation proteins assemble on a membrane containing anionic phospholipid, most notably phosphatidylserine (PS). PS can be rapidly externalized to the outer cell membrane leaflet by phospholipid "scramblases," such as TMEM16F. TMEM16F-dependent PS externalization is well characterized in platelets...
June 1, 2023: Journal of Clinical Investigation
https://read.qxmd.com/read/36950016/niclosamide-does-not-modulate-airway-epithelial-function-through-blocking-of-the-calcium-activated-chloride-channel-tmem16a
#28
JOURNAL ARTICLE
Henry Danahay, Sarah Lilley, Kathryn Adley, Holly Charlton, Roy Fox, Martin Gosling
Niclosamide and benzbromarone have been described as inhibitors of the calcium activated chloride channel, TMEM16A, and on this basis have been considered and tested as clinical candidates for the treatment of airway diseases. However, both compounds have previously demonstrated activity on a range of additional biological targets and it is unclear from the literature to what extent any activity on TMEM16A may contribute to efficacy in these models of airway disease. The aim of the present study was therefore to examine the pharmacology and selectivity of these clinical candidates together with a structurally unrelated TMEM16A blocker, Ani9, in a range of functional assays to better appreciate the putative role of TMEM16A in the regulation of both epithelial ion transport and the development of an airway epithelial mucus secretory phenoptype...
2023: Frontiers in Pharmacology
https://read.qxmd.com/read/36831103/urate-transporter-1-can-be-a-therapeutic-target-molecule-for-chronic-kidney-disease-and-diabetic-kidney-disease-a-retrospective-longitudinal-study
#29
JOURNAL ARTICLE
Hidekatsu Yanai, Hisayuki Katsuyama, Mariko Hakoshima, Hiroki Adachi
Chronic kidney disease (CKD) is a major global health problem for which there are no curative drug treatments. Hyperuricemia is one of risk factors for CKD. The evidence on effects of uric acid (UA)-lowering treatments on the progression of CKD was very limited and previous meta-analyses used only trials which primarily used xanthin oxidase (XO) inhibitors because the reports on fulminant hepatitis due to benzbromarone kept us from using uricosuric agents for hyperuricemia patients. Dotinurad, a novel selective urate reabsorption inhibitor for the treatment of hyperuricemia, reduces serum UA levels by selectively inhibiting urate transporter 1 (URAT1)...
February 15, 2023: Biomedicines
https://read.qxmd.com/read/36749254/the-risk-of-ischemic-cerebrovascular-disease-associated-with-benzbromarone-use-in-gout-people-a-retrospective-cohort-study-in-taiwan
#30
JOURNAL ARTICLE
Shih-Wei Lai, Kuan-Fu Liao, Yu-Hung Kuo, Bing-Fang Hwang, Chiu-Shong Liu
Epidemiological studies have shown that people having hyperuricemia are at increased risk of ischemic cerebrovascular disease. This research aimed to study the relation of ischemic cerebrovascular disease with benzbromarone use among persons with gout-related disorders. This was a retrospective cohort design utilizing a 2003 to 2015 national health insurance database in Taiwan. Subjects aged 20 to 99 years who already had suffered from gout-related disorders were included as eligible subjects. Eligible persons who had the benzbromarone prescription alone were selected into the benzbromarone group...
February 3, 2023: Medicine (Baltimore)
https://read.qxmd.com/read/36724945/uricosuric-agents-affect-plasma-and-kidney-concentration-of-adefovir-via-inhibition-of-oat1-and-mrp2-in-rats
#31
JOURNAL ARTICLE
Keisuke Motoki, Tetsuya Taniguchi, Naoki Ashizawa, Miku Sakai, Noriko Chikamatsu, Katsuhiro Yamano, Takashi Iwanaga
Uricosuric agents lower serum uric acid levels by increasing urinary excretion via inhibition of urate transporter 1 (URAT1), urate reabsorption transporter in the renal proximal tubules. Probenecid and benzbromarone have been used as uricosurics, but these drugs inhibit organic anion transporters (OATs) in addition to URAT1. In this study, we investigated whether uricosuric agents interacted with adefovir, known as a substrate for OAT1, using Sprague-Dawley (SD) rats. Furthermore, involvement of other transporters, multi-drug resistance protein 2 (MRP2) in this interaction was examined using Mrp2-deficient rats...
2023: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/36672567/atrial-fibrillation-risk-and-urate-lowering-therapy-in-patients-with-gout-a-cohort-study-using-a-clinical-database
#32
JOURNAL ARTICLE
Ching-Han Liu, Shih-Chung Huang, Chun-Hao Yin, Wei-Chun Huang, Jin-Shuen Chen, Yao-Shen Chen, Su-Ting Gan, Shiow-Jyu Tzou, Ching-Tsai Hsu, Hao-Ming Wu, Wen-Hwa Wang
Individuals of Asian descent are at higher risk for developing hyperuricemia and gout as compared to Western populations. Urate-lowering therapy (ULT) is an effective treatment for hyperuricemia and gout. It was reported that febuxostat, one of the ULTs, raises the risk of atrial fibrillation (AF) in elderly populations. Nevertheless, this association has not been properly investigated in Asian populations. We aimed to investigate the development of AF after ULT with different drugs in an Asian population. We conducted a retrospective cohort study using the clinical database at Kaohsiung Veterans General Hospital...
December 26, 2022: Biomedicines
https://read.qxmd.com/read/36669879/-a-novel-role-of-uricosuric-agent-benzbromarone-in-bk-channel-activation-and-reduction-of-airway-smooth-muscle-contraction
#33
JOURNAL ARTICLE
Jian Gao, Hao Yin, Yanqun Dong, Xintong Wang, Yani Liu, KeWei Wang
A uricosuric drug benzbromarone, widely used for treatment of gout, hyperpolarizes the membrane potential of airway smooth muscle cells, but how it works remains unknown. Here we show a novel role of benzbromarone in activation of large conductance calcium-activated K+ channels. Benzbromarone results in dose-dependent activation of macroscopic BK currents about 1.7 to 14.5 folds with an EC50 of 111 μM and shifts the voltage-dependent channel activation to a more hyperpolarizing direction about 10 to 54 mV in whole-cell patch clamp recordings...
January 20, 2023: Molecular Pharmacology
https://read.qxmd.com/read/36578257/time-and-concentration-dependent-stimulation-of-oxidative-stress-in-chondrocytes-by-intracellular-soluble-urate
#34
JOURNAL ARTICLE
Bingqing Zhang, Hong Di, Yun Zhang, Xinxin Han, Yue Yin, Yingdong Han, Yu Cao, Xuejun Zeng
BACKGROUND: Gout could result in irreversible bone erosion, and chondrocyte might be involved in the process. Increased soluble urate is the early stage of gout and is strongly oxidative. OBJECTIVE: To explore the effect of intracellular urate on the oxidative status of chondrocytes Methods: A chondrocyte model was used. Serial concentrations of exogenous urate were incubated with chondrocytes for increasing amounts of time. Reactive oxygen species (ROS), oxidant, and anti-oxidant molecules were measured with biochemical assays, rt-PCR, and western blot...
December 27, 2022: Current Molecular Medicine
https://read.qxmd.com/read/36525382/naringenin-ameliorates-hyperuricemia-by-regulating-renal-uric-acid-excretion-via-the-pi3k-akt-signaling-pathway-and-renal-inflammation-through-the-nf-%C3%AE%C2%BAb-signaling-pathway
#35
JOURNAL ARTICLE
Bendong Yang, Meiling Xin, Shufei Liang, Yuhong Huang, Jingda Li, Chao Wang, Chao Liu, Xinhua Song, Jinyue Sun, Wenlong Sun
Hyperuricemia characterized by high serum levels of uric acid (UA, >6.8 mg/dL) is regarded as a common chronic metabolic disease. When used as a food supplement, naringenin might have various pharmacological activities, including antioxidant, free-radical-scavenging, and inflammation-suppressing activities. However, the effects of naringenin on hyperuricemia and renal inflammation and the underlying mechanisms remain to be elucidated. Here, we comprehensively examined the effects of naringenin on hyperuricemia and the attenuation of renal impairment...
December 16, 2022: Journal of Agricultural and Food Chemistry
https://read.qxmd.com/read/36482671/research-progress-of-natural-active-substances-with-uric-acid-reducing-activity
#36
REVIEW
Xin Zhang, Jie Cui, Junling Hou, Wenquan Wang
Hyperuricemia is a metabolic disease caused by the accumulation of uric acid in the body. Allopurinol, benzbromarone, and febuxostat, which are available in the market, have reduced the circulating urate levels; however, they exhibit serious side effects. Therefore, it is reasonable to develop a new active antihyperuricemia drug with few side effects. With the deepening of research, numerous kinds of literature have shown that natural active substances are effective in the treatment of hyperuricemia with a variety of sources and few side effects, which have become the focus of research in recent years...
December 21, 2022: Journal of Agricultural and Food Chemistry
https://read.qxmd.com/read/36386218/improved-effect-of-fresh-ginseng-paste-radix-ginseng-ziziphus-jujube-on-hyperuricemia-based-on-network-pharmacology-and-molecular-docking
#37
JOURNAL ARTICLE
Hao Zhang, Wei Liu, Si-Min Qi, Jian-Feng Chi, Qiang Gao, Xiang-Hui Lin, Shen Ren, Zi Wang, Xiu-Juan Lei, Wei Li
Background: Hyperuricemia (HUA) is a metabolic disease caused by reduced excretion or increased production of uric acid. This research aims to study the practical components, active targets, and potential mechanism of the "Radix ginseng (RG)-Ziziphus jujube (ZJ)" herb pair through molecular docking, network pharmacology, and animal experiments. Methods: The potential targets of "Radix ginseng (RG)-Ziziphus jujube (ZJ)" herb pair were obtained from the TCMSP database. The therapeutic targets of HUA were acquired from the GendCards, OMIM, PharmGkb, and TTD databases...
2022: Frontiers in Pharmacology
https://read.qxmd.com/read/36347120/design-synthesis-and-biological-studies-of-dual-urat1-inhibitor-and-fxr-agonist-based-on-benzbromarone
#38
JOURNAL ARTICLE
Wanqiu Huang, Shixuan Jiao, Siliang Chen, Ya Chen, Zhongcheng Yang, Wenxin Wang, Zhijun Cao, Zheng Li, Luyong Zhang
With increased unhealthy dietary patterns and a sedentary lifestyle, the prevalence of hyperuricemia is growing rapidly, placing a tremendous burden on the public health system. Persistent hyperuricemia in extreme cases induces gout, gouty arthritis, and other metabolic diseases. Benzbromarone is a potent human urate transporter 1 (URAT1) inhibitor that is widely used as a uric acid-lowering drug. Recent studies indicated that benzbromarone can also activate farnesoid X receptor (FXR), whereas its agonistic activity on FXR is rather poor...
November 2, 2022: Bioorganic & Medicinal Chemistry
https://read.qxmd.com/read/36317407/cardiovascular-risk-of-urate-lowering-drugs-a-study-using-the-national-database-of-health-insurance-claims-and-specific-health-checkups-of-japan
#39
JOURNAL ARTICLE
Sono Sawada, Kazuhiro Kajiyama, Haruka Shida, Ryota Kimura, Yuki Nakazato, Toyotaka Iguchi, Yukio Oniyama, Chieko Ishiguro, Yoshiaki Uyama
In the present study, we aimed to investigate the association between urate-lowering drugs and cardiovascular events, primarily focusing on the risk of febuxostat and topiroxostat when compared with allopurinol in Japan. We conducted an observational study with a cohort design using the National Database of Health Insurance Claims and Specific Health Checkups of Japan, including new urate-lowering drugs users between August 1, 2010, and March 31, 2018. Exposure and control groups were defined based on the first prescription of urate-lowering drugs as follows: febuxostat or topiroxostat for exposure groups, allopurinol for the control group, and benzbromarone for the secondary control group...
November 1, 2022: Clinical and Translational Science
https://read.qxmd.com/read/36273350/genotoxicity-of-pyrrolizidine-alkaloids-in-metabolically-inactive-human-cervical-cancer-hela-cells-co-cultured-with-human-hepatoma-hepg2-cells
#40
JOURNAL ARTICLE
Naji Said Aboud Hadi, Ezgi Eyluel Bankoglu, Helga Stopper
Pyrrolizidine alkaloids (PAs) are secondary plant metabolites, which can be found as contaminant in various foods and herbal products. Several PAs can cause hepatotoxicity and liver cancer via damaging hepatic sinusoidal endothelial cells (HSECs) after hepatic metabolization. HSECs themselves do not express the required metabolic enzymes for activation of PAs. Here we applied a co-culture model to mimic the in vivo hepatic environment and to study PA-induced effects on not metabolically active neighbour cells...
October 23, 2022: Archives of Toxicology
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