Search results for "bile acids"
showing 10 items of 68 documents
Micellar electrokinetic chromatography with bile salts for predicting ecotoxicity of aromatic compounds.
2004
The retention factors of several aromatic compounds were obtained by micellar electrokinetic chromatography (MEKC) using cholate, taurocholate, deoxycholate and deoxytaurocholate as micellar systems. The possibility of using these retention factors to describe and predict several ecotoxicological activities of different aromatic compounds was evaluated. Adequate correlations retention–ecotoxicity (log LC50 in fish and daphnia, log EC50 in green algae and daphnia, chronic values in fish and green algae, bioconcentration factor, and soil sorption coefficient) were obtained for the micellar systems studied. The predictive ability of the models obtained for these micellar systems was compared. …
Bisphosphonate prodrugs utilizing endogenous carriers
2016
Targeting of therapeutic agents to a specific site, as well as controlling the rate and time of release, has been intensively investigated and established over the last decades. These studies concerning drug delivery systems led to the formulation of several products that can improve the diffusion across the barriers after drug administration. For this purpose, the development of strategies of novel drug delivery systems for bisphosphonates had taken hold to improve both the bioavailability and safety. Firstly, they have been used for over a century in the branch of industry and later, in the 1960s, in medicine. Bisphosphonates are synthetic compound analogs to the naturally occurring pyrop…
CLA-Enriched Diet Containing t10,c12-CLA Alters Bile Acid Homeostasis and Increases the Risk of Cholelithiasis in Mice
2011
International audience; Mice fed a mixture of CLA containing t10,c12-CLA lose fat mass and develop hyperinsulinemia and hepatic steatosis due to an accumulation of TG and cholesterol. Because cholesterol is the precursor in bile acid (BA) synthesis, we investigated whether t10,c12-CLA alters BA metabolism. In Expt. 1, female C57Bl/6J mice were fed a standard diet for 28 d supplemented with a CLA mixture (1 g/100 g) or not (controls). In Expt. 2, the feeding period was reduced to 4, 6, and 10 d. In Expt. 3, mice were fed a diet supplemented with linoleic acid, c9,t11-CLA, or t10,c12-CLA (0.4 g/100 g) for 28 d. In Expt. 1, the BA pool size was greater in CLA-fed mice than in controls and the …
Synthesis and Structure-Activity Relationships of Amino Acid Conjugates of Cholanic Acid as Antagonists of the EphA2 Receptor
2013
The Eph–ephrin system plays a critical role in tumor growth and vascular functions during carcinogenesis. We had previously identified cholanic acid as a competitive and reversible EphA2 antagonist able to disrupt EphA2-ephrinA1 interaction and to inhibit EphA2 activation in prostate cancer cells. Herein, we report the synthesis and biological evaluation of a set of cholanic acid derivatives obtained by conjugation of its carboxyl group with a panel of naturally occurring amino acids with the aim to improve EphA2 receptor inhibition. Structure-activity relationships indicate that conjugation of cholanic acid with linear amino acids of small size leads to effective EphA2 antagonists whereas …
Metabolite Sensing GPCRs: Promising Therapeutic Targets for Cancer Treatment?
2020
G-protein-coupled receptors constitute the most diverse and largest receptor family in the human genome, with approximately 800 different members identified. Given the well-known metabolic alterations in cancer development, we will focus specifically in the 19 G-protein-coupled receptors (GPCRs), which can be selectively activated by metabolites. These metabolite sensing GPCRs control crucial processes, such as cell proliferation, differentiation, migration, and survival after their activation. In the present review, we will describe the main functions of these metabolite sensing GPCRs and shed light on the benefits of their potential use as possible pharmacological targets for cancer treat…
Porphyrin-bile acid conjugates: from saccharide recognition in the solution to the selective cancer cell fluorescence detection.
2008
This paper describes the preparation and use of conjugates of porphyrins and bile acids as ligands to bind to tumor expressed saccharides. Bile acid-porphyrin conjugates were tested for recognition of saccharides that are typically present on malignant tumor cells. Fluorescence microscopy, in vitro PDT cell killing, and PDT of subcutaneous 4T1 mouse tumors is reported. High selectivity for saccharide cancer markers and cancer cells was observed. This in vivo and in vitro study demonstrated high potential use for these compounds in targeted photodynamic therapy.
Metabolomics discloses donor liver biomarkers associated with early allograft dysfunction
2014
Background & Aims Early allograft dysfunction (EAD) dramatically influences graft and patient outcome after orthotopic liver transplantation and its incidence is strongly determined by donor liver quality. Nevertheless, objective biomarkers, which can assess graft quality and anticipate organ function, are still lacking. This study aims to investigate whether there is a preoperative donor liver metabolomic biosignature associated with EAD. Methods A comprehensive metabolomic profiling of 124 donor liver biopsies collected before transplantation was performed by mass spectrometry coupled to liquid chromatography. Donor liver grafts were classified into two groups: showing EAD and immediate g…
Specific tyrosine phosphorylation in response to bile in Fasciola hepatica and Echinostoma friedi
2003
Protein tyrosine phosphorylation (PY) is a well-known signalling mechanism which is also involved in host-parasite interactions. Despite its transcendence, PY has been poorly studied in parasitic helminths. The aim of this study is to examine the effect of bile salts on the PY pattern in parasitic trematodes. Two distinct adult models were analysed: Echinostoma friedi, of intestinal habitat, and Fasciola hepatica, naturally inhabitant of host biliary channels. Our results show that bile salts induce specific and distinct protein PY in both trematode species, indicating that this signalling process seems to be also involved in host-trematode relationships.
Liposome Formation from Bile Salt–Lipid Micelles in the Digestion and Drug Delivery Model FaSSIFmod Estimated by Combined Time-Resolved Neutron and D…
2011
The flow of bile secretion into the human digestive system was simulated by the dilution of a bile salt-lipid micellar solution. The structural development upon the dilution of the fed state bile model FeSSIF(mod6.5) to the fasted state bile model FaSSIF(mod) was investigated by small-angle neutron scattering (SANS) and dynamic light scattering (DLS) in crossed beam experiments to observe small and large structures in a size range of 1 nm to 50 μm in parallel. Because of the physiologically low lipid and surfactant concentrations of 2.625 mM egg-phosphatidylcholine and 10.5 mM taurocholate the sensitivity of the neutron-structural investigations was improved by partial solvent deuteration w…
Bile acid amidoalcohols: simple organogelators.
2003
Simple bile acid amide synthesis of lithocholic and deoxycholic acids with 2-aminoethanol and 3-aminopropanol are reported. The structural properties of these amides were examined by NMR spectroscopic, ESI-TOF mass spectral, and X-ray crystallographic methods. The gelation properties of these amides in common organic solvents and in three different water solutions were also investigated using Tyndall effect, SEM, TEM, and optical microscopy. 2-Hydroxyethylamides were found to be effective gelators in chlorinated organic solvents and 3-hydroxypropylamides in aromatic solvents. Both derivatives thicken neutral and acidic water solutions.