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54826

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Dany Spaggiari et al.
Analytical and bioanalytical chemistry, 406(20), 4875-4887 (2014-06-05)
The cocktail approach is an advantageous strategy used to monitor the activities of several cytochromes P450 (CYPs) in a single test to increase the throughput of in vitro phenotyping studies. In this study, a cocktail mixture was developed with eight...
Niina Tani et al.
Bioorganic & medicinal chemistry, 22(23), 6655-6664 (2014-12-03)
Inhibition of CYP2A6-mediated nicotine metabolism can reduce cigarette smoking. We sought potent and selective CYP2A6 inhibitors to be used as leads for drugs useful in smoking reduction therapy, by evaluating CYP2A6 inhibitory effect of novel formyl, alkyl amine or carbonitrile...
Juri M Timonen et al.
European journal of medicinal chemistry, 46(9), 3845-3850 (2011-06-18)
A number of 7-hydroxycoumarins have been synthesised by Pechmann cyclisation using differently substituted resorcinols employing perchloric acid as the condensing agent. All the compounds have been characterised by analytical and spectroscopic methods. The anti-inflammatory properties were tested with LPS-induced inflammation...
Tao Yi et al.
Journal of ethnopharmacology, 153(3), 701-713 (2014-03-26)
Saussurea laniceps Hand.-Mazz. (SL) has long been used under the herbal name Tibetan "Snow Lotus" for the treatment of rheumatoid arthritis, stomachache and dysmenorrhea in Tibetan folk medicine. Since herbal medicine (HM) is a synergistical system with multiple components, both...
Ju-ying Zou et al.
Zhong yao cai = Zhongyaocai = Journal of Chinese medicinal materials, 35(5), 724-725 (2012-12-12)
To study the chemical constituents of Pileostegia viburnoides var. glabrescens. The compounds were isolated and purified by various techniques. Their structures were determined by physicochemical properties and spectral analysis. Five compounds were isolated and identified as friedelin (1), beta-sitosterol (2)...
S Huber et al.
Journal of pharmaceutical and biomedical analysis, 104, 137-143 (2014-12-17)
Esters of the cytostatic bendamustine (1), previously demonstrated to be much more potent than the parent compound as antiproliferative agents in vitro, were investigated for stability in buffer and plasma, as well as against porcine liver esterase in the presence...
Yoshihiko Shimokawa et al.
Biological & pharmaceutical bulletin, 37(11), 1727-1735 (2014-11-05)
Delamanid is a new drug for the treatment of multidrug-resistant tuberculosis. Individuals who are co-infected with human immunodeficiency virus and Mycobacterium tuberculosis may require treatment with a number of medications that might interact significantly with the CYP enzyme system as...
Alexander H Penn et al.
Journal of pediatric gastroenterology and nutrition, 59(3), 365-373 (2014-05-21)
Fat is digested in the intestine into free fatty acids (FFAs), which are detergents and therefore toxic to cells at micromolar concentration. The mucosal barrier protects cells in the adult intestine, but this barrier may not be fully developed in...
Dany Spaggiari et al.
Journal of chromatography. A, 1371, 244-256 (2014-12-03)
The goal of this study was to evaluate the combination of powerful chromatographic methods and compact single quadrupole MS device for simple in vitro cytochrome P450 (CYP) inhibition assay, instead of more expensive triple quadrupole MS/MS detectors. For this purpose...
Ana C A X De-Oliveira et al.
PloS one, 10(1), e0117842-e0117842 (2015-01-31)
Mouse cytochrome P450 (CYP) 2A5 is induced by inflammatory conditions and infectious diseases that down-regulate the expression and activity of most other CYP isoforms. Enhanced oxidative stress and nuclear factor (erythroid 2-related factor) 2 (Nrf2) transcription factor activation have been...
Y Abe et al.
Die Pharmazie, 70(1), 38-46 (2015-05-16)
Ritobegron, a selective β3-adrenoceptor agonist, is the prodrug of the active compound, KUC-7322. We investigated species differences in its metabolism in vitro and the potential for drug-drug interactions with ritobegron. In rat, dog, monkey, and human liver microsomes, ritobegron was...
Behrooz M Parast et al.
Plant physiology and biochemistry : PPB, 49(10), 1138-1146 (2011-04-29)
Psoralen, an important furanocoumarin occurring abundantly in seeds of Psoralea corylifolia is used as an anticancerous compound against leukemia and other cancer cell lines. Evaluation and isolation of psoralen from the calluses derived from different plant parts, viz. cotyledons, nodes...
Tsvetanka Stefanova et al.
Immunological investigations, 41(2), 199-213 (2011-10-20)
Coumarin and its derivatives have potent immunomodulatory activities. Here we describe the parameters of the protective effect of 7-hydroxycoumarin (7-OHC) in experimental Salmonella enterica Serovar Typhimurium infection in mice. The protective effect depended on the duration of treatment reaching its...
S Sebastian et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 101, 370-381 (2012-11-06)
In this work, we report harmonic vibrational frequencies, molecular structure, NBO and HOMO, LUMO analysis of Umbelliferone also known as 7-hydroxycoumarin (7HC). The optimized geometric bond lengths and bond angles obtained by computation (monomer and dimmer) shows good agreement with...
Hemakesh Mohapatra et al.
Angewandte Chemie (International ed. in English), 51(44), 11145-11148 (2012-10-06)
Smell of success: Reagent 1 provides the dual readouts of odor (ethanethiol) and fluorescence (derivative of 7-hydroxycoumarin) and can be used in down-selection assays based on smell and quantitative fluorescence assays of the samples that give a positive result. An...
Amira S El Senousy et al.
Phytochemistry, 108, 67-76 (2014-10-11)
The metabolomic differences in phenolics from leaves derived from 3 artichoke cultivars (Cynara scolymus): American Green Globe, French Hyrious and Egyptian Baladi, collected at different developmental stages, were assessed using UHPLC-MS coupled to chemometrics. Ontogenic changes were considered as leaves...
Hiromu Kashida et al.
Bioorganic & medicinal chemistry, 20(14), 4310-4315 (2012-06-19)
In this study, we synthesized a simple but efficient quencher-free molecular beacon tethering 7-hydroxycoumarin on D-threoninol based on its pK(a) change. The pK(a) of 7-hydroxycoumarin in a single strand was determined as 8.8, whereas that intercalated in the duplex was...
Tao Lin et al.
Zygote (Cambridge, England), 23(2), 297-306 (2014-01-05)
In the present study, a porcine system was supplemented with sorbitol during in vitro maturation (IVM) or in vitro culture (IVC), and the effects of sorbitol on oocyte maturation and embryonic development following parthenogenetic activation were assessed. Porcine immature oocytes...
Li Sun et al.
Brain research, 1415, 103-108 (2011-08-30)
Oxygen therapy (OT) with hyperbaric oxygen (HBO) or normobaric hyperoxia (NBO) improves the oxygenation of penumbral tissue in experimental ischemic stroke. However, whether this results in the improvement of energy metabolism is unclear. We investigated the effect of both OTs...
Siti Nur Fadzilah Muhsain et al.
Toxicology and applied pharmacology, 282(1), 77-89 (2014-12-06)
The intracellular level of bilirubin (BR), an endogenous antioxidant that is cytotoxic at high concentrations, is tightly controlled within the optimal therapeutic range. We have recently described a concerted intracellular BR regulation by two microsomal enzymes: heme oxygenase 1 (HMOX1)...
Soo Hyeon Bae et al.
Antimicrobial agents and chemotherapy, 58(9), 5036-5046 (2014-06-04)
Macrolactin A (MA) and 7-O-succinyl macrolactin A (SMA), polyene macrolides containing a 24-membered lactone ring, show antibiotic effects superior to those of teicoplanin against vancomycin-resistant enterococci and methicillin-resistant Staphylococcus aureus. MA and SMA are currently being evaluated as antitumor agents...
Moumita Chakraborty et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 97, 722-727 (2012-08-14)
Absorption and emission spectroscopic studies, in combination with FTIR measurements, were carried out for 7-hydroxycoumarin (7HC) and nanocolloidal dispersion of silica. Attempt has been made to identify the characteristics of excited state H-bond formed between colloidal silica and 7HC in...
Jing Dai et al.
Drug development and industrial pharmacy, 39(9), 1457-1463 (2013-08-02)
Photo-responsive monoolein (MO) cubic phase was developed by incorporating coumarin-Tween 20 conjugate in the cubic phase. 7-chlorocarbonylmethoxycoumarin was obtained from 7-hydroxycoumarin through three-step reactions with the yield of 19.8% and it was conjugated to the head group of Tween 20....
C Preston Pugh et al.
Archives of biochemistry and biophysics, 564, 244-253 (2014-12-03)
The widely used anticoagulant Coumadin (R/S-warfarin) undergoes oxidation by cytochromes P450 into hydroxywarfarins that subsequently become conjugated for excretion in urine. Hydroxywarfarins may modulate warfarin metabolism transcriptionally or through direct inhibition of cytochromes P450 and thus, UGT action toward hydroxywarfarin...
In-Hwan Baek et al.
Xenobiotica; the fate of foreign compounds in biological systems, 44(11), 975-987 (2014-05-31)
1. JHL45, a novel immune modulator against atopic dermatitis (AD), was synthesized from decursin isolated from Angelica gigas. The goal is to evaluate the lead compound using quantitative modeling approaches to novel anti-AD drug development. 2. We tested the anti-inflammatory effect of...
Yuki Kondo et al.
PloS one, 9(8), e104010-e104010 (2014-08-02)
In this study, we aimed to elucidate the effects and mechanism of action of valproic acid on hepatic differentiation from human induced pluripotent stem cell-derived hepatic progenitor cells. Human induced pluripotent stem cells were differentiated into endodermal cells in the...
Victor M Navarro-García et al.
Mycoses, 54(5), e569-e571 (2011-05-25)
The bis-coumarin daphnoretin and its monomeric precursors scopoletin and umbelliferone were isolated for the first time from the aerial part of Loeselia mexicana Brand (a vegetal species used in Mexican traditional medicine) using chromatographic techniques. The structures of these compounds...
Sang Yoon Lee et al.
Xenobiotica; the fate of foreign compounds in biological systems, 45(2), 131-138 (2014-08-26)
1. The herb-drug interaction potential of Hwang-Ryun-Hae-Dok-Tang (HR) extracts mediated by cytochrome P450 (CYP) inhibition was determined using human liver microsomes. 2. HR strongly inhibited CYP1A2 and moderately inhibited CYP2C19, CYP2D6, and CYP3A4 (testosterone) but not CYP2A6, CYP2B6, CYP2C8, CYP2C9, and CYP3A4...
Jagadeesha K Dammanahalli et al.
Drug metabolism and disposition: the biological fate of chemicals, 40(2), 298-303 (2011-11-02)
Mammalian cytosolic sulfotransferases (SULTs) catalyze the sulfation of xenobiotics as well as numerous endogenous molecules. The major aryl (phenol) SULT in rat liver, rSULT1A1, has been used extensively as a model enzyme for understanding the catalytic function of SULTs. Previous...
Jan Kočí et al.
Chemical communications (Cambridge, England), 47(23), 6713-6715 (2011-05-17)
Synthesis and chemiluminescent properties of a new 1,2-dioxetane chemiluminophore bearing a 7-hydroxycoumarin moiety are presented. The 1,2-dioxetane decomposition ended up with strong and long-lived emission of light. This new structure opens way to the development of a new generation of...
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