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Yao Qi et al.
Molecular bioSystems, 10(10), 2617-2625 (2014-07-22)
Rheumatoid arthritis (RA) is a chronic systemic inflammatory and autoimmune disease accompanied by the destruction and deformities of joints. Adjuvant-induced arthritis (AIA) is one of the excellent animal models of RA used to understand disease pathogenesis and screen potential drugs.
Roberto Pellicciari et al.
Journal of medicinal chemistry, 52(24), 7958-7961 (2009-12-18)
In the framework of the design and development of TGR5 agonists, we reported that the introduction of a C(23)(S)-methyl group in the side chain of bile acids such as chenodeoxycholic acid (CDCA) and 6-ethylchenodeoxycholic acid (6-ECDCA, INT-747) affords selectivity for
Nevzat Kazgan et al.
Gastroenterology, 146(4), 1006-1016 (2014-01-07)
Sirtuin 1 (SIRT1), the most conserved mammalian oxidized nicotinamide adenine dinucleotide-dependent protein deacetylase, is an important metabolic sensor in many tissues. However, little is known about its role in the small intestine, which absorbs and senses nutrients. We investigated the
Spyridon Theofilopoulos et al.
Nature chemical biology, 9(2), 126-133 (2013-01-08)
Liver X receptors (Lxrα and Lxrβ) are ligand-dependent nuclear receptors critical for ventral midbrain neurogenesis in vivo. However, no endogenous midbrain Lxr ligand has so far been identified. Here we used LC/MS and functional assays to identify cholic acid as
Manish Singh et al.
Biochimica et biophysica acta, 1828(8), 1926-1937 (2013-04-18)
We synthesized four cationic bile acid based facial amphiphiles featuring trimethyl ammonium head groups. We evaluated the role of these amphiphiles for cytotoxic activities against colon cancer cells and their membrane interactions by varying charge, hydration and hydrophobicity. The singly
Chunyan Zhao et al.
European journal of drug metabolism and pharmacokinetics, 39(2), 129-137 (2013-06-12)
For orally administered drugs, the metabolism of a drug by the gut flora plays an important role in the bioavailability, activation and disposition of the drug in vivo. However, no in vitro system is currently available to evaluate the metabolism
Dominique Brossard et al.
European journal of medicinal chemistry, 45(7), 2912-2918 (2010-04-13)
The novelty of this work derives from the use of nitrogenous heterocycles as building block in the synthesis of conjugate bile acid derivatives. New piperazinyl bile acid derivatives were synthesized and tested in vitro against various human cancer cells (GBM
Rebecca C Flanagan et al.
Infection and immunity, 77(6), 2399-2407 (2009-04-08)
Campylobacter jejuni colonization of chickens is presumably dependent upon multiple surface-exposed proteins termed adhesins. Putative C. jejuni adhesins include CadF, CapA, JlpA, major outer membrane protein, PEB1, Cj1279c, and Cj1349c. We examined the genetic relatedness of 97 C. jejuni isolates
Christopher A Elkins et al.
Antimicrobial agents and chemotherapy, 54(3), 1007-1015 (2009-12-30)
AcrAB-TolC imparts a strong intrinsic resistance phenotype to many clinically significant molecules in Escherichia coli. This complex is composed of a pump, AcrB, and a periplasmic protein, AcrA, that exports substrates through a common outer membrane porin, TolC. A sequence
Armanda Szücs et al.
PloS one, 15(5), e0233736-e0233736 (2020-05-30)
The liver is well known for its enormous regenerative capacity. If the hepatocytes are compromised the reserve stem cells can regrow the lost tissue by means of oval cells differentiating into hepatocytes. We were curious whether this standby system was
F J Reen et al.
European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology, 33(10), 1763-1771 (2014-05-13)
Chronic respiratory infections are a leading global cause of morbidity and mortality. However, the molecular triggers that cause respiratory pathogens to adopt persistent and often untreatable lifestyles during infection remain largely uncharacterised. Recently, bile aspiration caused by gastro-oesophageal reflux (GOR)
Ryan D Jones et al.
American journal of physiology. Gastrointestinal and liver physiology, 303(2), G263-G274 (2012-05-26)
Cholesterol 7α-hydroxylase (CYP7A1) is the initiating and rate-limiting enzyme in the neutral pathway that converts cholesterol to primary bile acids (BA). CYP7A1-deficient (Cyp7a1(-/-)) mice have a depleted BA pool, diminished intestinal cholesterol absorption, accelerated fecal sterol loss, and increased intestinal
Florence Janvier et al.
Journal of the mechanical behavior of biomedical materials, 18, 100-107 (2012-12-25)
Elevated red blood cell (RBC) aggregation increases low-shear blood viscosity and is closely related to several pathophysiological diseases such as atherosclerosis, thrombosis, diabetes, hypertension, cancer, and hereditary chronic hemolytic conditions. Non-ionic linear polymers such as poly(ethylene glycol) (PEG) and Pluronic
Wim F P M Van den Hof et al.
Toxicology in vitro : an international journal published in association with BIBRA, 29(3), 489-501 (2015-01-07)
In order to improve attrition rates of candidate-drugs there is a need for a better understanding of the mechanisms underlying drug-induced hepatotoxicity. We aim to further unravel the toxicological response of hepatocytes to a prototypical cholestatic compound by integrating transcriptomic
Bethany P Cummings et al.
Disease models & mechanisms, 6(2), 443-456 (2012-12-25)
Post-operative increases in circulating bile acids have been suggested to contribute to the metabolic benefits of bariatric surgery; however, their mechanistic contributions remain undefined. We have previously reported that ileal interposition (IT) surgery delays the onset of type 2 diabetes
Hiroyuki Sato et al.
Journal of medicinal chemistry, 51(6), 1831-1841 (2008-03-01)
TGR5, a metabotropic receptor that is G-protein-coupled to the induction of adenylate cyclase, has been recognized as the molecular link connecting bile acids to the control of energy and glucose homeostasis. With the aim of disclosing novel selective modulators of
Kejun Zhou et al.
Journal of proteome research, 14(11), 4844-4850 (2015-10-10)
Biliary atresia (BA) is a severe chronic cholestasis disorder of infants that leads to death if not treated on time. Neonatal hepatitis syndrome (NHS) is another leading cause of neonatal cholestasis confounding the diagnosis of BA. Recent studies indicate that
Biao Nie et al.
Hepatology (Baltimore, Md.), 56(4), 1300-1310 (2012-04-26)
Bile acids are known to play important roles as detergents in the absorption of hydrophobic nutrients and as signaling molecules in the regulation of metabolism. We tested the novel hypothesis that naturally occurring bile acids interfere with protein-mediated hepatic long
Yubing Xiong et al.
Macromolecular bioscience, 12(4), 515-524 (2012-05-19)
A novel amphiphilic and biodegradable polyelectrolyte DS-CA is prepared by the esterification of DS with CA. DS-CA can self-assemble into stable nanoparticles in water. SOD can effectively associate with DS-CA at pH = 5.0 by virtue of electrostatic and hydrophobic
Roberto Pellicciari et al.
Journal of medicinal chemistry, 50(18), 4265-4268 (2007-08-10)
23-Alkyl-substituted and 6,23-alkyl-disubstituted derivatives of chenodeoxycholic acid are identified as potent and selective agonists of TGR5, a G-protein coupled receptor for bile acids (BAs). In particular, we show that methylation at the C-23(S) position of natural BAs confers a marked
Sylwia Mildner-Szkudlarz et al.
Journal of the science of food and agriculture, 93(13), 3271-3278 (2013-04-16)
New breads fortified with two different forms of grape by-products, namely dried powdered skins (PGP) and freeze-dried extract therefrom (EGP), were characterised and their protective effect against hypercholesterolaemia in rats was studied. The phenolic compound profiles of supplemented breads were
Liliya Vinarova et al.
Food & function, 6(4), 1319-1330 (2015-03-17)
Quillaja saponin extracts are known to reduce plasma cholesterol levels in humans. Here we study the mechanism of this effect with Quillaja Dry saponin extract (QD). In vitro model of triglyceride lipolysis is used to quantify the effect of QD
Yu Shao et al.
ACS applied materials & interfaces, 6(13), 10381-10392 (2014-06-13)
To develop a feasible and efficient nanocarrier for potential clinical application, a series of photo and redox dual responsive reversibly cross-linked micelles have been developed for the targeted anticancer drug delivery. The nanocarrier can be cross-linked efficiently via a clean
Yinying Chen et al.
Naunyn-Schmiedeberg's archives of pharmacology, 385(8), 797-806 (2012-05-25)
In order to elucidate the overlapping and diverse pharmacological protective mechanisms of different Chinese medicinal compounds, we investigated the alteration of gene expression and activation of signaling pathways in the mouse hippocampus after treatment of cerebral ischemia-reperfusion injury with various
Jilite Wang et al.
Bioscience, biotechnology, and biochemistry, 79(3), 456-461 (2014-11-07)
Dietary plant protein is well known to reduce serum cholesterol levels. Rice bran is a by-product of rice milling and is a good source of protein. The present study examined whether feeding rats a high-cholesterol diet containing 10% rice bran
Justin D Schumacher et al.
Hepatology (Baltimore, Md.), 71(2), 670-685 (2019-06-18)
Farnesoid X receptor (FXR) induces fibroblast growth factor 15 (FGF15; human ortholog FGF19) in the gut to potently inhibit bile acid (BA) synthesis in the liver. FXR activation in hepatic stellate cells (HSCs) reduces liver fibrosis (LF). Fgf15-/- mice develop
Sindy Escobar-Alvarez et al.
Molecular and cellular biology, 30(21), 5099-5109 (2010-09-02)
Deformylases are metalloproteases in bacteria, plants, and humans that remove the N-formyl-methionine off peptides in vitro. The human homolog of peptide deformylase (HsPDF) resides in the mitochondria, along with its putative formylated substrates; however, the cellular function of HsPDF remains
Chiara Gabbi et al.
Digestive and liver disease : official journal of the Italian Society of Gastroenterology and the Italian Association for the Study of the Liver, 44(12), 1018-1026 (2012-08-14)
Non-alcoholic fatty liver disease, one of the most prevalent liver disorders in Western countries, is characterized by hepatic accumulation of triglycerides. Bile acids have long been known to affect triglyceride homeostasis through a not completely understood mechanism. To analyse the
Clara John et al.
Journal of chromatography. A, 1371, 184-195 (2014-12-03)
Recently, hydroxy sterols and bile acids have gained growing interest as they are important regulators of energy homoeostasis and inflammation. The high number of different hydroxy sterols and bile acid species requires powerful analytical tools to quantify these structurally and
Edurne Nuin et al.
Organic letters, 15(2), 298-301 (2013-01-01)
New photoactive dyads have been synthesized by derivatization of cholic acid (CA) or cholesterol (Ch). These compounds have proven to be efficient tools to monitor incorporation of CA and Ch to mixed micelles (MM) and to probe the microenvironment experienced
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