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Bile salts

Kristin Forner, Carl Roos, David Dahlgren, Filippos Kesisoglou, Moritz A Konerding, Johanna Mazur, Hans Lennernäs, Peter Langguth
CONTEXT: Prediction of the in vivo absorption of poorly soluble drugs may require simultaneous dissolution/permeation experiments. In vivo predictive media have been modified for permeation experiments with Caco-2 cells, but not for excised rat intestinal segments. OBJECTIVE: The present study aimed to improve the setup of dissolution/permeation experiments with excised rat intestinal segments by assessing suitable donor and receiver media. METHODS: The regional compatibility of rat intestine in Ussing chambers with modified Fasted and Fed State Simulated Intestinal Fluids (Fa/FeSSIFmod) as donor media was evaluated via several parameters that reflect the viability of the excised intestinal segments...
October 20, 2016: Drug Development and Industrial Pharmacy
Alice Strohmeier, Gesche Först, Philipp Tauber, Rolf Schubert
The interaction of liposomal membranes composed of soybean phosphatidylcholine with the bile salts (BSs) cholate (Ch), glycocholate (GC), chenodeoxycholate (CDC), and glycochenodeoxycholate (GCDC) was studied. The BSs differed with regard to their lipophilicity, pKa values, and the size of their hydrophilic moiety. Their membrane interactions were investigated using Laurdan as a membrane-anchored fluorescent dye. The apparent membrane/water partition coefficient, D, at pH 7.4 was calculated from binding plots and compared with direct binding measurements using ultracentrifugation as a reference...
October 18, 2016: Biophysical Journal
Delilah F G Hendriks, Lisa Fredriksson Puigvert, Simon Messner, Wolfgang Mortiz, Magnus Ingelman-Sundberg
Drug-induced cholestasis (DIC) is poorly understood and its preclinical prediction is mainly limited to assessing the compound's potential to inhibit the bile salt export pump (BSEP). Here, we evaluated two 3D spheroid models, one from primary human hepatocytes (PHH) and one from HepaRG cells, for the detection of compounds with cholestatic liability. By repeatedly co-exposing both models to a set of compounds with different mechanisms of hepatotoxicity and a non-toxic concentrated bile acid (BA) mixture for 8 days we observed a selective synergistic toxicity of compounds known to cause cholestatic or mixed cholestatic/hepatocellular toxicity and the BA mixture compared to exposure to the compounds alone, a phenomenon that was more pronounced after extending the exposure time to 14 days...
October 19, 2016: Scientific Reports
Giovanni Vitale, Giulia Simonetti, Martina Pirillo, Gianfranco Taruschio, Pietro Andreone
Bile Salt Export Pump (BSEP) Deficiency disease, including Progressive Familial Intrahepatic Cholestasis type 2 (PFIC2), is a rare disease, usually leading within the first ten years to portal hypertension, liver failure, hepatocellular carcinoma. Often liver transplantation is needed. Sodium 4-phenylbutyrate (4-PB) seems to be a potential therapeutic compound for PFIC2. Psychiatric side effects in the adolescent population are little known and little studied since the drug used to treat children and infants...
September 2016: Psychiatry Investigation
Vishnubhotla Venkata Ravikanth, Guduru Venkat Rao, Bale Govardhan, Mitnala Sasikala, Chivukula Subramanyam, H V Vivekananda Murthy, Siddapuram Siva Prasad, G Deepika, Rebala Pradeep, Duvvuru Nageshwar Reddy
BACKGROUND/OBJECTIVES: Pigmentous gallstones occur in South Indians despite significant higher levels of circulating cholesterol. This study was conducted to identify the biochemical and/or genetic causes for the formation of pigmentous gallstones in this ethnic group. METHODS: Plasma lipid profile, bile cholesterol, acids, and phospholipid levels were estimated in patients with gall stone disease and age, sex matched controls using standard protocols. Twenty-seven SNPs related to cholesterol and bilirubin metabolism pathway genes were genotyped in the study population using the Sequenom platform...
September 2016: Journal of Clinical and Experimental Hepatology
Yura Jang, Young Tae Je, Cheol-Won Yun, Hesson Chung
This study was designed to investigate the oil entrapment and systemic oil absorption-reducing activities of chitosan. High-molecular-weight chitosan formed gel aggregates with oil and bile salts in vitro. The oil/chitosan ratio and the molecular weight of chitosan were optimized for the in vivo study, and a molecular weight >100,000 was effective in reducing the oil contamination of mouse fur. The oil/chitosan weight ratio required for effective oil entrapment was less than 13 and 5 in the in vitro and in vivo experiments, respectively...
October 13, 2016: International Journal of Biological Macromolecules
Pauline D Scanlan, Anna M Bischofberger, Alex R Hall
Although experiments indicate that the abiotic environment plays an important role in bacterial interactions with their parasitic viruses (bacteriophages or phages), it is not yet clear how exposure to compounds present in nature alters the impact of phages on bacterial growth and evolution. To address this question we exposed Escherichia coli K12 MG1655, in combination with three lytic phages, to various substances that natural and clinical microbial populations are likely to encounter: bile salts (present in mammalian gastrointestinal tracts), sodium dodecyl sulfate (SDS, a common surfactant in cleaning and hygiene products), and four antibiotics (present at variable concentrations in natural and clinical environments)...
October 12, 2016: FEMS Microbiology Ecology
Marie-Agnès Travers, Cissé Sow, Séverine Zirah, Christiane Deregnaucourt, Soraya Chaouch, Rayner M L Queiroz, Sébastien Charneau, Thibault Allain, Isabelle Florent, Philippe Grellier
Giardiasis, currently considered a neglected disease, is caused by the intestinal protozoan parasite Giardia duodenalis and is widely spread in human as well as domestic and wild animals. The lack of appropriate medications and the spread of resistant parasite strains urgently call for the development of novel therapeutic strategies. Host microbiota or certain probiotic strains have the capacity to provide some protection against giardiasis. By combining biological and biochemical approaches, we have been able to decipher a molecular mechanism used by the probiotic strain Lactobacillus johnsonii La1 to prevent Giardia growth in vitro...
2016: Frontiers in Microbiology
Aly A Abdelbary, Wessam H Abd-Elsalam, Abdulaziz M Al-Mahallawi
The objective of this work was to encapsulate terconazole (TCZ), a water insoluble antifungal drug, into novel ultradeformable bilosomes (UBs) for achieving enhanced ocular delivery. In addition to the constituents of the conventional bilosomes; namely, Span 60, cholesterol, and the bile salts, UBs contain an edge activator which imparts extra elasticity to the vesicles and consequently hypothesized to result in improved corneal permeation. In this study, TCZ loaded UBs were prepared utilizing ethanol injection method according to 2(3) full factorial design...
October 4, 2016: International Journal of Pharmaceutics
Guadalupe Barrera-Escorcia, Irma Wong-Chang, Carlos Leopoldo Fernández-Rendón, Alfonso Vázquez Botello, Bruno Gómez-Gil, Marcial Leonardo Lizárraga-Partida
Oysters can accumulate potentially pathogenic water bacteria. The objective of this study was to compare two procedures to quantify Vibrio species present in oysters to determine the most sensitive method. We analyzed oyster samples from the Gulf of Mexico, commercialized in Mexico City. The samples were inoculated in tubes with alkaline peptone water (APW), based on three tubes and four dilutions (10(-1) to 10(-4)). From these tubes, the first quantification of Vibrio species was performed (most probable number (MPN) from tubes) and bacteria were inoculated by streaking on thiosulfate-citrate-bile salts-sucrose (TCBS) petri dishes...
November 2016: Environmental Monitoring and Assessment
Mohamed Sellami, Hanen Louati, Jannet Kamoun, Ali Kchaou, Mohamed Damak, Youssef Gargouri
The aim of this study is to search new anti-obesity and anti-diabetic agents from plant and spices crude extracts as alternative to synthetic drugs. The inhibitory effect of 72 extracts was evaluated, in vitro, on lipase and amylase activities. Aqueous extracts of cinnamon and black tea exhibited an appreciable inhibitory effect on pancreatic amylase with IC50 values of 18 and 87 μg, respectively. Aqueous extracts of cinnamon and mint showed strong inhibitory effects against pancreatic lipase with IC50 of 45 and 62 μg, respectively...
October 6, 2016: International Journal of Food Sciences and Nutrition
Serge J Zweers, Elisabeth M de Vries, Martin Lenicek, Dagmar Tolenaars, D Rudi de Waart, Kiran V K Koelfat, Albert K Groen, Steven W M Olde Damink, Ulrich Beuers, Cyriel Ponsioen, Peter L M Jansen, Frank G Schaap
BACKGROUND: Bile salts likely contribute to liver injury in patients with primary sclerosing cholangitis (PSC) and primary biliary cholangitis (PBC). Fibroblast growth factor 19 (FGF19) is a bile salt-induced enterokine with hepatoprotective potential as it suppresses de novo bile salt synthesis. Here, we evaluated the bile salt receptor FXR/FGF19 gut-liver axis in PSC and PBC patients. METHODS: Fasted patients with PSC (n = 12) and PBC (n = 10), and healthy controls (HC; n = 10) were orally challenged with the natural FXR agonist chenodeoxycholic acid (CDCA 15 mg/kg)...
September 30, 2016: Hepatology International
Xiaofang Huo, Agoston T Agoston, Kerry B Dunbar, Daisha J Cipher, Xi Zhang, Chunhua Yu, Edaire Cheng, Qiuyang Zhang, Thai H Pham, Uttam K Tambar, Richard K Bruick, David H Wang, Robert D Odze, Stuart J Spechler, Rhonda F Souza
OBJECTIVE: In an earlier study wherein we induced acute reflux by interrupting proton pump inhibitor (PPI) therapy in patients with reflux oesophagitis (RO) healed by PPIs, we refuted the traditional concept that RO develops as an acid burn. The present study explored our alternative hypothesis that RO results from reflux-stimulated production of pro-inflammatory molecules mediated by hypoxia-inducible factors (HIFs). DESIGN: Using oesophageal biopsies taken from patients in our earlier study at baseline and at 1 and 2 weeks off PPIs, we immunostained for HIF-1α, HIF-2α and phospho-p65, and measured pro-inflammatory molecule mRNAs...
September 30, 2016: Gut
Romy E Verbeek, Peter D Siersema, Frank P Vleggaar, Fiebo J Ten Kate, George Posthuma, Rhonda F Souza, Judith de Haan, Jantine W P M van Baal
BACKGROUND AND AIMS: Inflammation plays an important role in the development of esophageal adenocarcinoma and its metaplastic precursor lesion, Barrett's esophagus. Toll-like receptor (TLR) 2 signalling and lysosomal function have been linked to inflammation-associated carcinogenesis. We examined the expression of TLR2 in the esophagus and the effect of long-term TLR2 activation on morphological changes and expression of factors involved in lysosomal function in a Barrett's esophagus epithelium cell line...
September 2016: Journal of Gastrointestinal and Liver Diseases: JGLD
Mosab Arafat, Cathrin Kirchhoefer, Momir Mikov
BACKGROUND AND OBJECTIVES: Cefotaxime is a class III drug according to the Biopharmaceutical Classification System due to low intestinal permeability based on poor oral bioavailability. Bile salt compounds have been shown to be effective additive for drug permeation through several biological membranes. The main purpose of this study was to investigate the ability of a mixed micelles made of phosphatidylcholine, sodium deoxycholate, and loaded with a cefotaxime-3α,7α-dihydroxy-12-keto-5β-cholanate complex to enhance the oral bioavailability of cefotaxime in rats...
September 29, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Deepak Chand, Vellore Sunder Avinash, Yashpal Yadav, Archana Vishnu Pundle, Cheravakattu Gopalan Suresh, Sureshkumar Ramasamy
BACKGROUND: Bile salt hydrolase (BSH) enzyme is responsible for the de-conjugation of bile salts by commensal bacteria, thus playing a vital role in their colonization and survival in the mammalian intestine and determination of their probiotic potential. Further, bile deconjugation also leads to lowering of cholesterol and alterations in energy homeostasis, thus making BSH a clinically important enzyme. SCOPE OF THE REVIEW: Many recent observations have indicated that BSH may be involved in a multifaceted array of roles, directly or indirectly in the host and microbial physiology...
September 25, 2016: Biochimica et Biophysica Acta
Kimberly Lapham, Jonathan Novak, Lisa D Marroquin, Rachel Swiss, Shuzhen Qin, Christopher J Strock, Renato Scialis, Michael D Aleo, Thomas Schroeter, Heather Eng, A David Rodrigues, Amit S Kalgutkar
Conjugated hyperbilirubinemia accompanied by cholestasis is a frequent side effect during chronic treatment with the antimicrobial agent fusidic acid. Previous studies from our laboratory, addressing mechanisms of musculoskeletal toxicity arising from coadministration of fusidic acid with statins, demonstrated the ability of fusidic acid to potently inhibit human organic anion transporting polypeptides OATP1B1 (IC50 = 1.6 μM) and OATP1B3 (IC50 = 2.5 μM), which are responsible for the uptake-limited clearance of statins as well as bilirubin glucuronide conjugates...
October 4, 2016: Chemical Research in Toxicology
Xiao-Yan Liu, Xin Niu, Qian-Jin Feng, Xue-Zhi Yang, Dan-Wei Wang, Tong Zhao, Lei Li, Hong DU
The purpose of this study was to design and prepare a biocompatible microemulsion of Andrographis paniculata (BMAP) containing both fat-soluble and water-soluble constituents. We determined the contents of active constituents of BMAP and evaluated its bioavailability. The biocompatible microemulsion (BM), containing lecithin and bile salts, was optimized in the present study, showing a good physical stability. The mean droplet size was 19.12 nm, and the average polydispersity index (PDI) was 0.153. The contents of andrographolide and dehydroandrographolide in BMAP, as determined by high performance liquid chromatography (HPLC), were higher than that in ethanol extraction...
September 2016: Chinese Journal of Natural Medicines
Yaneisy García-Hernández, Tania Pérez-Sánchez, Ramón Boucourt, José L Balcázar, Jacques R Nicoli, João Moreira-Silva, Zoraya Rodríguez, Héctor Fuertes, Odalys Nuñez, Nereyda Albelo, Nabil Halaihel
In livestock production, lactic acid bacteria (LAB) are the most common microorganisms used as probiotics. For such use, these bacteria must be correctly identified and characterized to ensure their safety and efficiency. In the present study, LAB were isolated from broiler excreta, where a fermentation process was used. Nine among sixteen isolates were identified by biochemical and molecular (sequencing of the 16S rRNA gene) methods as Lactobacillus crispatus (n=1), Lactobacillus pentosus (n=1), Weissella cibaria (n=1), Pediococcus pentosaceus (n=2) and Enterococcus hirae (n=4)...
October 2016: Research in Veterinary Science
Mihalj Poša, Ana Pilipović, Mirjana Bećarević, Zita Farkaš
Due to a relatively small size of bile acid salts, their mixed micelles with nonionic surfactants are analysed. Of the special interests are real binary mixed micelles that are thermodynamically more stable than ideal mixed micelles. Thermodynamic stability is expressed with an excess Gibbs energy (G(E)) or over an interaction parameter (βij). In this paper sodium salts of cholic (C) and hiodeoxycholic acid (HD) in their mixed micelles with Tween 40 (T40) are analysed by potentiometric titration and their pKa values are determined...
September 17, 2016: Steroids
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