5,127 results match your criteria probenecid

Development of a fluorescence-based assay for screening of urate transporter 1 inhibitors using 6-carboxyfluorescein.

Anal Biochem 2021 May 6:114246. Epub 2021 May 6.

MOE International Joint Research Laboratory on Synthetic Biology and Medicines, School of Biology and Biological Engineering, South China University of Technology, Guangzhou, 510006, P. R. China. Electronic address:

The urate transporter 1 (URAT1) inhibitors were considered a very promising class of uricosuric agents for the treatment of hyperuricemia and gout. In vitro activity testing of these compounds has been conducted by radio-labeling uric acid for a long time. However, relatively few offer the convenience and speed of fluorescence-based assays. Read More

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Population pharmacokinetics of free flucloxacillin in patients treated with oral flucloxacillin plus probenecid.

Br J Clin Pharmacol 2021 May 7. Epub 2021 May 7.

Department of Infectious Diseases, Christchurch Hospital, Christchurch, New Zealand.

Aim: Oral flucloxacillin may be co-administered with probenecid to reduce flucloxacillin clearance and increase attainment of pharmacokinetic-pharmacodynamic (PK/PD) targets. The aims of this study were to develop a population PK model of free flucloxacillin when administered orally with probenecid, and to identify optimal dosing regimens for this combination.

Methods: We performed a prospective observational study of adults (45 participants) treated with oral flucloxacillin 1000 mg and probenecid 500 mg 8-hourly for proven or probable staphylococcal infections. Read More

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Efflux at the Blood-Brain Barrier Reduces the Cerebral Exposure to Ochratoxin A, Ochratoxin α, Citrinin and Dihydrocitrinone.

Toxins (Basel) 2021 04 30;13(5). Epub 2021 Apr 30.

Institute of Food Chemistry, Westfälische Wilhelms-Universität Münster, 48149 Münster, Germany.

Recent studies have implied that environmental toxins, such as mycotoxins, are risk factors for neurodegenerative diseases. To act directly as neurotoxins, mycotoxins need to penetrate or affect the integrity of the blood-brain barrier, which protects the mammalian brain from potentially harmful substances. As common food and feed contaminants of fungal origin, the interest in the potential neurotoxicity of ochratoxin A, citrinin and their metabolites has recently increased. Read More

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Pleiotropic effects of probenecid on three-dimensional cultures of prostate cancer cells.

Life Sci 2021 Apr 28;278:119554. Epub 2021 Apr 28.

Department of Biochemistry, Asahikawa Medical University, Asahikawa 078-8510, Japan.

Aims: Chemoresistance remains a persistent challenge in advanced prostate cancer therapy. Probenecid reportedly inhibits multiple drug-efflux transporters; hence, it can be employed as a potential sensitizer for chemotherapy. In the present study, we evaluated the effects of probenecid on three-dimensional (3D)-cultures of prostate cancer cells. Read More

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Stability-Indicating Chromatographic Methods for the Simultaneous Determination of Probenecid and Colchicine in Their Combined Tablet.

J Chromatogr Sci 2021 Apr 20. Epub 2021 Apr 20.

Analytical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr el Aini Street, 11562, Cairo, Egypt.

Two stability-indicating chromatographic methods have been established and validated for concurrent determination of probenecid (PRO), colchicine (COL) along with the degradation product of colchicine (COL deg). PRO and COL were exposed to a stress stability study, which includes acidic, alkaline, oxidative, photolytic and thermal degradations. Chromatographic methods included the use of thin layer chromatography (TLC-densitometry) and high performance liquid chromatography (HPLC). Read More

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Clinical Investigation on Endogenous Biomarkers to Predict Strong OAT-Mediated Drug-Drug Interactions.

Clin Pharmacokinet 2021 Apr 10. Epub 2021 Apr 10.

Drug Metabolism and Pharmacokinetics, Janssen Pharmaceutical Companies of Johnson & Johnson, Turnhoutseweg 30, 2340, Beerse, Belgium.

Background: Endogenous biomarkers are promising tools to assess transporter-mediated drug-drug interactions early in humans.

Methods: We evaluated on a common and validated in vitro system the selectivity of 4-pyridoxic acid (PDA), homovanillic acid (HVA), glycochenodeoxycholate-3-sulphate (GCDCA-S) and taurine towards different renal transporters, including multidrug resistance-associated protein, and assessed the in vivo biomarker sensitivity towards the strong organic anion transporter (OAT) inhibitor probenecid at 500 mg every 6 h to reach close to complete OAT inhibition.

Results: PDA and HVA were substrates of the OAT1/2/3, OAT4 (PDA only) and multidrug resistance-associated protein 4; GCDCA-S was more selective, having affinity only towards OAT3 and multidrug resistance-associated protein 2. Read More

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Transcranial Ultrasound Stimulation Suppresses Neuroinflammation in a Chronic Mouse Model of Parkinson's Disease.

IEEE Trans Biomed Eng 2021 Apr 8;PP. Epub 2021 Apr 8.

Objective: Neuroinflammation contributes to the development and progression of Parkinson's disease (PD). The aim of this study was to examine whether ultrasound (US) stimulation of the subthalamic nucleus (STN) could suppress the neuroinflammation in a chronic PD mouse model induced by 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP).

Methods: Chronic PD mouse model was built by injection of 20mg/kg MPTP and 250 mg/kg probenecid at 3. Read More

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Perfluoroalkyl substance excretion: Effects of organic anion-inhibiting and resin-binding drugs in a community setting.

Environ Toxicol Pharmacol 2021 Apr 2;85:103650. Epub 2021 Apr 2.

Department of Public Health, Environments, and Society, London School of Hygiene and Tropical Medicine, London, WCIH 9SH, United Kingdom; Centre for Radiation, Chemical and Environmental Hazards, Public Health England (PHE), Chilton, Oxfordshire, OX11 0RQ, United Kingdom.

Background: Longer serum half-lives of perfluoroalkyl substances (PFAS) in humans compared to other species has been attributed to differences in the activity of organic anion transporters (OAT).

Methods: Among 56,175 adult participants in the community-based C8 Health Project, 23 subjects were taking the uricosuric OAT-inhibitor probenecid, and 36 subjects were taking the bile acid sequestrant cholestyramine. In regression models of log transformed serum PFAS, medication effects were estimated in terms of mean ratios, adjusting for age, gender, BMI, estimated glomerular filtration rate (eGFR) and water-district of residence. Read More

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Endurance exercise training suppresses Parkinson disease-induced overexpression of apoptotic mediators in the heart.

NeuroRehabilitation 2021 ;48(3):315-320

Department of Anatomy. Faculty of Medicine, Jordan University of Science and Technology, Irbid, Jordan.

BACKGROUNDWe have shown elevated levels of p53 and active caspase-3 in the heart with Parkinson disease (PD). The main aim of this study is to examine the effect of treadmill training on the cardiac expression of p53 and active caspase-3 in the mouse with induced Parkinsonism.

Methods: Thirty randomly selected normal albino mice were equally divided into the following 3 groups: sedentary control (SC), sedentary Parkinson diseased (SPD), and exercised Parkinson diseased (EPD). Read More

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January 2021

Structural and Functional Characterization of the ABCC6 Transporter in Hepatic Cells: Role on PXE, Cancer Therapy and Drug Resistance.

Int J Mol Sci 2021 Mar 11;22(6). Epub 2021 Mar 11.

Department of Sciences, University of Basilicata, 85100 Potenza, Italy.

Pseudoxanthoma elasticum (PXE) is a complex autosomal recessive disease caused by mutations of ABCC6 transporter and characterized by ectopic mineralization of soft connective tissues. Compared to the other ABC transporters, very few studies are available to explain the structural components and working of a full ABCC6 transporter, which may provide some idea about its physiological role in humans. Some studies suggest that mutations of in the liver lead to a decrease in some circulating factor and indicate that PXE is a metabolic disease. Read More

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Treatment of pseudoxanthoma elasticum with probenecid.

Australas J Dermatol 2021 Apr 1. Epub 2021 Apr 1.

Department of Dermatology, The Royal Melbourne Hospital, Parkville, Victoria, Australia.

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Hypouricemic agents reduce indoxyl sulfate excretion by inhibiting the renal transporters OAT1/3 and ABCG2.

Sci Rep 2021 Mar 31;11(1):7232. Epub 2021 Mar 31.

Research Laboratories 2, Fuji Yakuhin Co., Ltd., 636-1, Iida-Shinden, Nishi-ku, Saitama, Japan.

Indoxyl sulfate (IS) accumulates in the body in chronic kidney disease (CKD). In the renal proximal tubules, IS excretion is mediated by OAT1/3 and ABCG2. These transporters are inhibited by some hypouricemic agents; OATs by probenecid and benzbromarone, ABCG2 by febuxostat and benzbromarone. Read More

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A key role for the transporter OAT1 in systemic lipid metabolism.

J Biol Chem 2021 Mar 27:100603. Epub 2021 Mar 27.

Department of Pediatrics, University of California San Diego, La Jolla, California 92093-0693; Department of Medicine, University of California San Diego, La Jolla, California 92093-0693.

Organic anion transporter 1 (OAT1/SLC22A6) is a drug transporter with numerous xenobiotic and endogenous substrates. The Remote Sensing and Signaling Theory suggests that drug transporters with compatible ligand preferences can play a role in "organ crosstalk," mediating overall organismal communication. Other drug transporters are well known to transport lipids, but surprisingly little is known about the role of OAT1 in lipid metabolism. Read More

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Clinical efficacy and tolerability of 1.5 g/day oral amoxicillin therapy without probenecid for the treatment of syphilis.

Sex Transm Infect 2021 Mar 29. Epub 2021 Mar 29.

Department of Infectious Diseases, Tokyo Metropolitan Cancer and Infectious Diseases Center Komagome Hospital, Bunkyo-ku, Japan.

Objectives: Intramuscular benzathine penicillin G is not available in certain countries. In a previous report, 3 g/day amoxicillin with probenecid was shown to be effective in treating syphilis in patients with HIV; however, 7.3% of patients changed their therapy owing to adverse events. Read More

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Transient receptor potential vanilloid 2 mediates the inhibitory effect of far-infrared irradiation on adipogenic differentiation of tonsil-derived mesenchymal stem cells.

Stem Cell Res 2021 Mar 17;53:102291. Epub 2021 Mar 17.

Department of Molecular Medicine, College of Medicine, 25 Magokdong-ro-2-gil, Gangseo-gu, Seoul 07804, Republic of Korea; Graduate Program in System Health Science and Engineering, Ewha Womans University, 25 Magokdong-ro-2-gil, Gangseo-gu, Seoul 07804, Republic of Korea. Electronic address:

Aims: Far-infrared (FIR) irradiation inhibits adipogenic differentiation of tonsil-derived mesenchymal stem cells (TMSCs) by activating Ca-dependent protein phosphatase 2B (PP2B), but it stimulates osteogenic differentiation in a PP2B-independent pathway. We investigated the potential involvement of transient receptor potential vanilloid (TRPV) channels, a well-known Ca-permeable channel, in the effects of FIR irradiation on adipogenic or osteogenic differentiation of TMSCs.

Methods: TMSCs, in the absence or presence of activators or inhibitors, were exposed to FIR irradiation followed by adipogenic or osteogenic differentiation, which was assessed using Oil red O or Alizarin red S staining, respectively. Read More

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Coordinate regulation of systemic and kidney tryptophan metabolism by the drug transporters OAT1 and OAT3.

J Biol Chem 2021 Mar 21:100575. Epub 2021 Mar 21.

Department of Pediatrics; Department of Medicine, University of California San Diego, La Jolla, 92093. Electronic address:

How organs sense circulating metabolites is a key question. Here, we show that the multi-specific organic anion transporters of drugs, OAT1 (SLC22A6 or NKT) and OAT3 (SLC22A8), play a role in organ sensing. Metabolomics analyses of the serum of Oat1 and Oat3 knockout mice revealed changes in tryptophan derivatives involved in metabolism and signaling. Read More

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Role of organic anion transporter 3 in the renal excretion of biapenem and potential drug-drug interactions.

Eur J Pharm Sci 2021 Mar 19;162:105814. Epub 2021 Mar 19.

Department of Pharmacy, Shanghai Pudong New Area Gongli Hospital, The Second Military Medical University, 219 Miaopu Road, Shanghai 200135, PR China. Electronic address:

Biapenem is a carbapenem antibiotic. It is excreted predominantly through the kidney as unchanged forms. However, the molecular mechanism of renal excretion of biapenem and potential drug-drug interactions (DDIs) were still unknown. Read More

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Hemorrhagic cystitis: A successful outcome for a challenging complication in stem cell transplant.

Hematol Rep 2021 Mar 12;13(1):8574. Epub 2021 Mar 12.

Department of Hematology and Hemotherapy.

Hemorrhagic cystitis (HC) secondary to BK polyomavirus (BKPyV) is a frequent complication related to allogenic stem cell transplantation. With an important morbidity and mortality, this disease doesn't have a stablished standard treatment or prophylaxis strategies. At this moment, the supportive therapies approved to treat included hyperhydration, forced diuresis and transfusion support. Read More

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Quantitative high-throughput assay to measure MC4R-induced intracellular calcium.

J Mol Endocrinol 2021 Apr 26;66(4):285-297. Epub 2021 Apr 26.

Department of Physiology, Faculty of Medical and Health Sciences, University of Auckland, Auckland, New Zealand.

The melanocortin-4 receptor (MC4R), a critical G-protein-coupled receptor (GPCR) regulating energy homeostasis, activates multiple signalling pathways, including mobilisation of intracellular calcium ([Ca2+]i). However, very little is known about the physiological significance of MC4R-induced [Ca2+]i since few studies measure MC4R-induced [Ca2+]i. High-throughput, read-out assays for [Ca2+]i have proven unreliable for overexpressed GPCRs like MC4R, which exhibit low sensitivity mobilising [Ca2+]i. Read More

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Population pharmacokinetic modeling and simulation to support qualification of pyridoxic acid as endogenous biomarker of OAT1/3 renal transporters.

CPT Pharmacometrics Syst Pharmacol 2021 Mar 11. Epub 2021 Mar 11.

Centre for Applied Pharmacokinetic Research, School of Health Sciences, The University of Manchester, Manchester, UK.

Renal clearance of many drugs is mediated by renal organic anion transporters OAT1/3 and inhibition of these transporters may lead to drug-drug interactions (DDIs). Pyridoxic acid (PDA) and homovanillic acid (HVA) were indicated as potential biomarkers of OAT1/3. The objective of this study was to develop a population pharmacokinetic model for PDA and HVA to support biomarker qualification. Read More

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Novel Pannexin-1-Coupled Signaling Cascade Involved in the Control of Endothelial Cell Function and NO-Dependent Relaxation.

Oxid Med Cell Longev 2021 20;2021:2678134. Epub 2021 Feb 20.

Departamento de Fisiología, Facultad de Ciencias Biológicas, Pontificia Universidad Católica de Chile, Santiago 8330025, Chile.

Deletion of pannexin-1 (Panx-1) leads not only to a reduction in endothelium-derived hyperpolarization but also to an increase in NO-mediated vasodilation. Therefore, we evaluated the participation of Panx-1-formed channels in the control of membrane potential and [Ca] of endothelial cells. Changes in NO-mediated vasodilation, membrane potential, superoxide anion (O) formation, and endothelial cell [Ca] were analyzed in rat isolated mesenteric arterial beds and primary cultures of mesenteric endothelial cells. Read More

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February 2021

Pannexin 1 binds β-catenin to modulate melanoma cell growth and metabolism.

J Biol Chem 2021 Feb 26:100478. Epub 2021 Feb 26.

Department of Anatomy and Cell Biology, Schulich School of Medicine and Dentistry, University of Western Ontario, London, Ontario, Canada, N6A 5C1; Department of Oncology, Division of Experimental Oncology, Schulich School of Medicine and Dentistry, University of Western Ontario, London, Ontario, Canada, N6A 5C1. Electronic address:

Melanoma is the most aggressive skin malignancy with increasing incidence worldwide. Pannexin1 (PANX1), a member of the pannexin family of channel-forming glycoproteins, regulates cellular processes in melanoma cells including proliferation, migration, and invasion/metastasis. However, the mechanisms responsible for coordinating and regulating PANX1 function remain unclear. Read More

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February 2021

Clinical Investigation of Metabolic and Renal Clearance Pathways Contributing to the Elimination of Fevipiprant Using Probenecid as Perpetrator.

Drug Metab Dispos 2021 May 25;49(5):389-394. Epub 2021 Feb 25.

Novartis Institutes for Biomedical Research, Basel, Switzerland (H.M.W., T.L., G.R., and B.P.); Novartis Institutes for Biomedical Research, Cambridge, Massachusetts (M.C.); Novartis Institutes for Biomedical Research, East Hanover, New Jersey (S.K. and B.S.); and Novartis Healthcare Pvt. Ltd., Hyderabad, India (J.V.).

Fevipiprant, an oral, nonsteroidal, highly selective, reversible, and competitive prostaglandin D receptor 2 antagonist, is eliminated by glucuronidation and by direct renal excretion predominantly via organic anion transporter (OAT) 3. This study aimed to assess the effect of simultaneous UDP-glucuronosyltransferase (UGT) and OAT3 inhibition by probenecid on the pharmacokinetics of fevipiprant and its acyl glucuronide (AG) metabolite to support the dosing recommendation of fevipiprant in the presence of drugs inhibiting these pathways; however, phase III clinical trial results did not support its submission. This was a single-center, open-label, single-sequence, two-period crossover study in healthy subjects. Read More

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Assessment of drug transporters involved in the urinary secretion of [Tc]dimercaptosuccinic acid.

Nucl Med Biol 2021 Mar-Apr;94-95:92-97. Epub 2021 Feb 5.

School of Health Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, Japan; Biomedical Imaging Research Center, University of Fukui, Fukui, Japan.

Introduction: We clarified the renal uptake and urinary secretion mechanism of [Tc]dimercaptosuccinic acid ([Tc]DMSA) via drug transporters in renal proximal tubules.

Methods: [Tc]DMSA was added to human embryonic kidney 293 cells expressing human multidrug and toxin extrusion (MATE)1 and MATE2-K, carnitine/organic cation transporter (OCTN)1 and OCTN2, and organic cation transporter (OCT)2; to Flp293 cells expressing human organic anion transporter (OAT)1 and OAT3; and to vesicles expressing P-glycoprotein (P-gp), multidrug resistance associated protein (MRP)2, MRP4, or breast cancer resistance protein with and without probenecid (OAT inhibitor for both OATs and MRPs). Time activity curves of [Tc]DMSA with and without probenecid were established using LLC-PK cells. Read More

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February 2021

Effects of Probenecid on Hepatic and Renal Disposition of Hexadecanedioate, an Endogenous Substrate of Organic Anion Transporting Polypeptide 1B in Rats.

J Pharm Sci 2021 05 17;110(5):2274-2284. Epub 2021 Feb 17.

Faculty of Pharmacy, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, Japan. Electronic address:

The aim of the present study was to investigate changes in plasma concentrations and tissue distribution of endogenous substrates of organic anion transporting polypeptide (OATP) 1B, hexadecanedioate (HDA), octadecanedioate (ODA), tetradecanedioate (TDA), and coproporphyrin-III, induced by its weak inhibitor, probenecid (PBD), in rats. PBD increased the plasma concentrations of these four compounds regardless of bile duct cannulation, whereas liver-to-plasma (K) and kidney-to-plasma concentration ratios of HDA and TDA were reduced. Similar effects of PBD on plasma concentrations and K of HDA, ODA, and TDA were observed in kidney-ligated rats, suggesting a minor contribution of renal disposition to the overall distribution of these three compounds. Read More

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Increased kynurenine concentration attenuates serotonergic neurotoxicity induced by 3,4-methylenedioxymethamphetamine (MDMA) in rats through activation of aryl hydrocarbon receptor.

Neuropharmacology 2021 04 16;187:108490. Epub 2021 Feb 16.

Departamento de Farmacología y Toxicología, Facultad de Medicina, Universidad Complutense, Pza. Ramón y Cajal s/n, 28040, Madrid, Spain; Instituto de Investigación Sanitaria Hospital 12 de Octubre, Madrid, Spain; Red de Trastornos Adictivos, Instituto de Salud Carlos III, Madrid, Spain; Instituto Universitario de Investigación Neuroquímica (IUIN), Universidad Complutense, Madrid, Spain. Electronic address:

3,4-Methylenedioxymethamphetamine (MDMA) is an amphetamine derivative that has been shown to produce serotonergic damage in the brains of primates, including humans, and of rats. Tryptophan, the precursor of serotonin, is primarily degraded through the kynurenine (KYN) pathway, producing among others KYN, the main metabolite of this route. KYN has been reported as an endogenous agonist of the aryl hydrocarbon receptor (AhR), a transcription factor involved in several neurological functions. Read More

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Capillaries communicate with the arteriolar microvascular network by a pannexin/purinergic-dependent pathway in hamster skeletal muscle.

Am J Physiol Heart Circ Physiol 2021 04 19;320(4):H1699-H1711. Epub 2021 Feb 19.

Department of Human Health and Nutritional Sciences, University of Guelph, Guelph, Ontario, Canada.

We sought to determine if a pannexin/purinergic-dependent intravascular communication pathway exists in skeletal muscle microvasculature that facilitates capillary communication with upstream arterioles that control their perfusion. Using the hamster cremaster muscle and intravital microscopy, we locally stimulated capillaries and observed the vasodilatory response in the associated upstream 4A arteriole. We stimulated capillaries with vasodilators relevant to muscle contraction: 10 M -nitroso--acetyl-dl-penicillamine (SNAP; nitric oxide donor), 10 M adenosine, 10 mM potassium chloride, 10 M pinacidil, as well as a known initiator of gap-junction-dependent intravascular communication, acetylcholine (10 M), in the absence and the presence of the purinergic membrane receptor blocker suramin (10 M), pannexin blocker mefloquine (2 × 10 M), or probenecid (5 × 10 M) and gap-junction inhibitor halothane (0. Read More

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Differential Action of Connexin Hemichannel and Pannexin Channel Therapeutics for Potential Treatment of Retinal Diseases.

Int J Mol Sci 2021 Feb 10;22(4). Epub 2021 Feb 10.

School of Optometry and Vision Science, New Zealand National Eye Centre, Centre for Brain Research, Brain Research New Zealand-Rangahau Roro Aotearoa, University of Auckland, Auckland 1142, New Zealand.

Dysregulation of retinal function in the early stages of light-induced retinal degeneration involves pannexins and connexins. These two types of proteins may contribute to channels that release ATP, leading to activation of the inflammasome pathway, spread of inflammation and retinal dysfunction. However, the effect of pannexin channel block alone or block of both pannexin channels and connexin hemichannels in parallel on retinal activity in vivo is unknown. Read More

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February 2021

[A case of early syphilitic hepatitis with jaundice cured by high-dose amoxicillin and probenecid].

Nihon Shokakibyo Gakkai Zasshi 2021 ;118(2):161-167

Division of Gastroenterology, Department of Medicine, Nagano Chuo Hospital.

A 44-year-old man was admitted because of general malaise, jaundice, and epigastric pain. The patient had no significant medical history. However, the patient visited a brothel 3 months ago and noticed initial induration on his penis 2 months ago. Read More

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February 2021

Bioaccessibility and Absorption of Flavonoid C-glycosides from Abrus mollis Using Simulated Digestion, Caco-2 Cell, and In Situ Single-pass Perfusion Models.

Planta Med 2021 Feb 5. Epub 2021 Feb 5.

State Key Laboratory of Natural Medicines, Department of TCMs Pharmaceuticals, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing, People's Republic of China.

is commonly used as a traditional Chinese medicine for the treatment of liver diseases due to its hepatoprotection and anti-inflammation, but the absorption properties of its main bioactive ingredients remain unclear. Our previous studies verified that the flavonoid -glycosides, including vicenin-2 (1: ), isoschaftoside (2: ), and schaftoside (3: ), were the major active components in for hepatic protection against nonalcoholic fatty liver disease, hepatitis, and hepatic fibrosis. This study investigated the bioaccessibility and transport mechanisms of total flavonoid -glycoside, as well as vicenin-2 (1: ), isoschaftoside (2: ), and schaftoside (3: ), in by simulated digestion and use of the Caco-2 cell model. Read More

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February 2021