Peroxisome proliferator-activated receptor alpha (PPARα) controls lipid homeostasis through regulation of lipid transport and catabolism. PPARα activators are clinically used for hyperlipidemia treatment. The role of PPARα in bile acid (BA) homeostasis is beginning to emerge. Herein, Ppara-nu...

Apolipoprotein E (ApoE) plays a central role in lipid transport and cholesterol metabolism, with surplus cholesterol being removed from the liver through bile acid (BA) synthesis. Furthermore, BAs are of critical importance in fat absorption by forming intestinal lipid-bile salt mixed micelles. ...

Introduction: Taurohyodeoxycholic acid (THDC), a new natural hydrophilic bile salt, dissolves human cholesterol gallstones in vitro and may be effective as a litholytic agent in vivo. We thus, investigated in man the effects of short-term oral administration of THDC on lipid composition and phys...

A GC-MS (SIM) method has been developed which allows the measurement of tamoxifen and its metabolites in uterine cytosol and 0.5 M KCl-extracts of uterine nuclei from groups of immature rats. The method was shown to be specific, precise and accurate. Using this procedure tamoxifen and 4-hydroxyt...

The concentrations of tamoxifen and two of its metabolites, N-desmethyltamoxifen and 4′-hydroxytamoxifen (metabolite B), have been measured in rat plasma and DMBA-induced tumours using gas chromatography-mass spectrometry. At a dose of 100 μg/day all three compounds produced tumour regression ...

There is increasing evidence that the clinical efficacy of tamoxifen, the first and most widely used targeted therapy for estrogen-sensitive breast cancer, depends on the formation of the active metabolites 4-hydroxy-tamoxifen and 4-hydroxy-N-desmethyl-tamoxifen (endoxifen). Large inter-individu...

Fluorescence excitation and emission spectra, relative fluorescence quantum yield φr and fluorescence lifetime τ of methyl 8-(2-anthroyl)-octanoate have been studied in a set of organic solvents covering a large scale of polarity and in the presence of water. In this probe, the 2-anthroyl chro...

On increasing the amount of myristic acid in mixed multilayers of 7-(2-anthryl)-heptanoic acid (2A7) and myristic acid the emission of shallow traps emitting at 420 nm is favoured compared with that of deeper traps emitting at 455 nm. This change in the emission spectrum is accompanied by a chan...

The interaction of the tetramisole derivative (±)-5,6-dihydro-6-phenyl-imidazo[2,1-b]thiazole and a number of its 2-n-alkyl homologues (-ethyl through -n-pentyl and -n-neptyl) with large unilamellar phosphatidylethanolamine/dipalmitoylphosphatidic acid (2:1:0.06, w/w) vesicles was studied by me...

8-(2-Anthroyl)-octanoic acid is a chromophore whose fluorescence properties are strongly dependent on the polarity of the surrounding medium. Synthesis and phase properties of anthroylphosphatidylcholine molecules which were obtained by condensing this anthroyl fatty acid with egg lysophosphatid...

The novel water soluble antenna polyelectrolyte: poly[sodium styrene sulfonate-co-(4-acryolyloxyphenyl)-10,15,20-tritolylporphyrin] (PSSS-Po) was synthesised, and its photophysical and photochemical properties were studied. Solubilisation of the various molecular probes such as pyrene or perylen...

BK channels are dually regulated by voltage and Ca2 +, providing a cellular mechanism to couple electrical and chemical signalling. Intracellular Ca2 + concentration is sensed by a large cytoplasmic region in the channel known as “gating ring”, which is formed by four tandems of regulator of c...

Grafting of free maleimide and epoxide pendant groups onto the surface of ∼7-nm silica nanoparticles was investigated. Glycidyloxypropyl groups (3-glycidyloxypropyltrimethoxysilane and 3-aminopropyltrimethoxysilane) that carried epoxide groups and aminopropyl groups were grafted to the silica s...

Reaction of N-phenyl maleimide (NPM) with silica surfaces modified with a self-assembled monolayer of (aminopropyl)triethoxysilane (APTES) was investigated using infrared spectroscopy (FTIR), elemental analysis, and titration assays. This reaction is of interest as a test case for using amine–m...

Previous studies have shown that the nicotine-derived N-nitrosamine-4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) induces tracheal papillomas and lung carcinomas in Syrian golden hamsters: In this study, we showed that hamster tracheal and lung explants metabolize NNK by α-carbon hydroxy...

Dietary ellagic acid has been shown to reduce the incidence of methylbenzylnitrosamine-induced esophageal carcinoma in the rat. Methylbenzylnitrosamine (MBN) is a naturally occurring carcinogen which requires cytochrome P-450 dependent activation to be mutagenic. We examined whether the reductio...

This study was undertaken to determine the amount of ellagic acid, a naturally occurring inhibitor of carcinogenesis, in various fruits and nuts. Ellagic acid was extracted from freeze-dried berries, pears, peaches, plums, grapes, apples, kiwi, and several nuts using either acetone/water or meth...

The distribution and metabolism of ellagic acid (EA), a naturally occurring plant phenolic compound with reported antimutagenic and anticarcinogenic activity, was investigated in mice following intraperitoneal injection. Male Swiss-Webster mice were given a single i.p. injection of [3H] EA and s...

Ellagic acid (EA) is an inhibitor of the in vitro mutagenicity of N-nitrosodimethylamine (NDMA) in Salmonella typhimurium strain TA100 using pyrazole-induced rat liver 9000 × g supernatant (S-9). In order to understand this activity, the effect of EA on the metabolic hydroxylation of 4-nitrophe...

The ability of the plant phenol ellagic acid to inhibit the mutagenicity of the food mutagen IQ was evaluated using Salmonella typhimurium strain TA98 in the Ames mutagenicity test. Ellagic acid caused a concentration-dependent decrease in the S-9- and microsome-mediated mutagenicity of IQ. The ...