New Publications
Scientific studies, scholarly articles, and patent information to Nuclear Receptors and Nuclear Receptor research.
In Vitro Metabolism and CYP-Modulating Activity of Lavender Oil and Its Major Constituents
ABSTRACT The application of essential oils has historically been limited to topical (massage therapy) and inhalational (aromatherapy) routes of administration. More recently, however, evaluation of the therapeutic effects of essential oils has expanded to include the oral route of administration, which increases the herb-drug interaction potential. The purpose of this study was to evaluate theRead More
Assessment of the mode of action underlying development of liver lesions in mice following oral exposure to HFPO-DA and relevance to humans
ABSTRACT HFPO-DA (ammonium, 2,3,3,3-tetrafluoro-2-(heptafluoropropoxy)propanoate) is a short-chain polyfluorinated alkyl substance (PFAS) used in the manufacture of some types of fluorinated polymers. Like many PFAS, toxicity studies with HFPO-DA indicate the liver is the primary target of toxicity in rodents following oral exposure. Due to the structural diversity of PFAS, the mode of action (MOA) canRead More
Alfaxalone anaesthesia increases brain derived neurotrophic factor levels and preserves postoperative cognition by activating pregnane-X receptors: an in vitro study and a double blind randomised controlled trial
ABSTRACT Background: Alfaxalone is a fast acting intravenous anaesthetic with high therapeutic index. It is an analogue of the naturally-occurring neurosteroid allopregnanolone responsible for maintenance of cognition and neuroprotection by activation of brain pregnane X receptors and consequent increased production of mature brain-derived neurotrophic factor (m-BDNF). Two studies are reported here: an in vitro studyRead More
Human CYP2B6 produces oxylipins from polyunsaturated fatty acids and reduces diet-induced obesity
ABSTRACT Multiple factors in addition to over consumption lead to obesity and non-alcoholic fatty liver disease (NAFLD) in the United States and worldwide. CYP2B6 is the only human detoxification CYP whose loss is associated with obesity, and Cyp2b-null mice show greater diet-induced obesity with increased steatosis than wildtype mice. However, a putative mechanism has notRead More
Tris(1,3-dichloro-2-propyl) phosphate is a metabolism-disrupting chemical in male mice
ABSTRACT Tris(1,3-dichloro-2-propyl) phosphate (TDCPP) is an organophosphate flame retardant. The primary TDCPP metabolite, bis(1,3-dichloro-2-propyl) phosphate (BDCPP), is detectable in the urine of over 90 % of Americans. Epidemiological studies show sex-specific associations between urinary BDCPP levels and metabolic syndrome, which is an established risk factor for type 2 diabetes, heart disease, and stroke. We usedRead More
Design, synthesis, and properties of des-D-ring interphenylene derivatives of 1α,25-Dihydroxyvitamin D3
ABSTRACT Novel des-D-ring interphenylene analogs of vitamin D3 were designed on the basis of their conformational analysis and affinity to vitamin D receptor (VDR) estimated using ligand-protein docking simulation. According to this design, a series of the des-D-ring interphenylene analogs were synthesized via Suzuki-Miyaura coupling reactions of des-D, C-ring and A-ring intermediates. A fluorescence polarizationRead More
Defining the Chemical Additives Driving In Vitro Toxicities of Plastics
ABSTRACT Increases in the global use of plastics have caused concerns regarding potential adverse effects on human health. Plastic products contain hundreds of potentially toxic chemical additives, yet the exact chemicals which drive toxicity currently remain unknown. In this study, we employed nontargeted analysis and in vitro bioassays to identify the toxicity drivers in plastics.Read More
Bile Acids Are Substrates for Amine N-Acyl Transferase Activity by Bile Salt Hydrolase
Summary Bacteria in the gastrointestinal tract (GI) produce a variety of amino acid bile acid amidates that impact host-mediated metabolic processes; however, the bacterial gene(s) responsible for their production remain unknown. Herein, we report that bile salt hydrolase (BSH) possesses dual functions, including a new role in bile acid metabolism by functioning as an amineRead More
Inhibition of Borrelia Burgdorferi-Induced TLR2-NFκB Canonical Signaling by Gallic Acid through Targeting the CD14+ Adaptor Protein and p65 Molecule
ABSTRACT The cases of Lyme disease caused by Borrelia burgdorferi infection have been increasing throughout Northern America and Europe. This pathogen, if not treated in a timely manner with antibiotics, can cause persisting and debilitating health outcomes. In the search for novel agents against B. burgdorferi, we investigated a phenolic compound-gallic acid-for its anti-Borrelia andRead More
In vitro activity of a panel of per- and polyfluoroalkyl substances (PFAS), fatty acids, and pharmaceuticals in peroxisome proliferator-activated receptor (PPAR) alpha, PPAR gamma, and estrogen receptor assays
ABSTRACT Data demonstrate numerous per- and polyfluoroalkyl substances (PFAS) activate peroxisome proliferator-activated receptor alpha (PPARα), however, additional work is needed to characterize PFAS activity on PPAR gamma (PPARγ) and other nuclear receptors. We utilized in vitro assays with either human or rat PPARα or PPARγ ligand binding domains to evaluate 16 PFAS (HFPO-DA, HFPO-DA-AS, NBP2,Read More