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https://www.readbyqxmd.com/read/28506585/c21-steroidal-pregnane-sapogenins-and-their-derivatives-as-anti-inflammatory-agents
#1
Lie-Jun Huang, Shao-Ru Chen, Chun-Mao Yuan, Wei Gu, Bao-Jian Guo, Yi-Tao Wang, Ying Wang, Xiao-Jiang Hao
During the screening of natural anti-inflammatory agent, we identified some C21-steroidal pregnane sapogenins or the derivatives to inhibit TLR2, TLR3, and TLR4-initiatedinflammatory responses respectively. Treatment with active compounds 10, 2j and 3p failed to impact tumor necrosis factor-α (TNF-α) induced nucleus translocation of NF-κB p65 subunit. However, these compounds regulated distinct canonical or non-canonical NF-κB family members. Ectopic expression of TNF receptor associated factor 6 (TRAF6) abrogated the inhibitory activity of the compounds on production of pro-inflammatory cytokines downstream of TLR4...
May 2, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28501193/immunoaffinity-chromatography-combined-with-tandem-mass-spectrometry-a-new-tool-for-the-selective-capture-and-analysis-of-brassinosteroid-plant-hormones
#2
Jana Oklestkova, Danuše Tarkowská, Luděk Eyer, Tomáš Elbert, Aleš Marek, Zora Smržová, Ondřej Novák, Milan Fránek, Vladimir N Zhabinskii, Miroslav Strnad
Brassinosteroids (BRs) are plant-specific steroid hormones that play essential roles in the regulation of many important physiological processes in plant life. Their extremely low concentrations (~pmoles/g FW) in plant tissue and huge differences in polarity of individual members within the BR family hamper their detection and quantification. To address this problem, an immunoaffinity sorbent with broad specificity and high capacity for different BR metabolites containing a monoclonal antibody (mAb) against a BR spacer (20S)-2α,3α-dihydroxy-7-oxa-7α-homo-5α-pregnane-6-one-20 carboxylic acid (BR4812) was used for the rapid and highly selective isolation of endogenous BRs containing a 2α,3α-diol in ring A from minute plant samples...
August 1, 2017: Talanta
https://www.readbyqxmd.com/read/28496040/induction-of-human-cytochrome-p450-3a-enzymes-in-cultured-placental-cells-by-thalidomide-and-relevance-to-bioactivation-and-toxicity
#3
Norie Murayama, Yasuhiro Kazuki, Daisuke Satoh, Kazuya Arata, Tasuku Harada, Norio Shibata, F Peter Guengerich, Hiroshi Yamazaki
Evidence has been presented for auto-induced human cytochrome P450 3A enzyme involvement in the teratogenicity and clinical outcome of thalidomide due to oxidation to 5-hydroxythalidomide and subsequent metabolic activation in livers. In this study, more relevant human placenta preparations and placental BeWo cells showed low but detectable P450 3A4/5 mRNA expression and drug oxidation activities. Human placental microsomal fractions from three subjects showed detectable midazolam 1´- and 4-hydroxylation and thalidomide 5-hydroxylation activities...
2017: Journal of Toxicological Sciences
https://www.readbyqxmd.com/read/28480737/pregnane-steroids-from-the-vietnamese-octocoral-carijoa-riisei
#4
Nam Nguyen Hoai, Huong Nguyen Thi, Hanh Tran Thi Hong, Thanh Nguyen Van, Cuong Nguyen Xuan, Thung Do Cong, Kiem Phan Van, Minh Chau Van
Six pregnane steroids including one new compound namely 15β-hydroxypregna-4,20-dien-3-one (1), were isolated and structurally elucidated from the octocoral Carijoa riisei. The cytotoxic activity against a panel of eight human cancer cell lines of isolated compounds was also evaluated by SRB method. As the results, 18-acetoxypregna-1,4,20-trien-3-one (5) showed significant cytotoxicity against all the tested cell lines with the IC50 values from 22.29 ± 1.47 to 48.73 ± 3.93 μM, whereas 15β-acetoxypregna-1,4,20-trien-3-one (3) and 20R-acetoxypregna-1,4-dien-3-one (6) only exhibited weak effect on KB cell line with IC50 values of 93...
May 7, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28470937/endothelial-cell-derived-matrix-promotes-the-metabolic-functional-maturation-of-hepatocyte-via-integrin-src-signalling
#5
Xinyue Guo, Weihong Li, Minghui Ma, Xin Lu, Haiyan Zhang
The extracellular matrix (ECM) microenvironment is involved in the regulation of hepatocyte phenotype and function. Recently, the cell-derived extracellular matrix has been proposed to represent the bioactive and biocompatible materials of the native ECM. Here, we show that the endothelial cell-derived matrix (EC matrix) promotes the metabolic maturation of human adipose stem cell-derived hepatocyte-like cells (hASC-HLCs) through the activation of the transcription factor forkhead box protein A2 (FOXA2) and the nuclear receptors hepatocyte nuclear factor 4 alpha (HNF4α) and pregnane X receptor (PXR)...
May 4, 2017: Journal of Cellular and Molecular Medicine
https://www.readbyqxmd.com/read/28467654/sterol-regulatory-element-binding-protein-1c-knockout-mice-show-altered-neuroactive-steroid-levels-in-sciatic-nerve
#6
Nico Mitro, Gaia Cermenati, Matteo Audano, Silvia Giatti, Marzia Pesaresi, Silvia Pedretti, Roberto Spezzano, Donatella Caruso, Roberto Cosimo Melcangi
Neuroactive steroid levels are altered in several experimental models of peripheral neuropathy, and on this basis, they have been proposed as protective agents. For the first time, the levels of these molecules were here assessed in sterol regulatory-binding protein-1c (SREBP-1c) knock-out (KO) male mice (i.e., an experimental model of peripheral neuropathy) and compared with observations in wild type animals. The levels of neuroactive steroids have been evaluated by liquid chromatography tandem mass spectrometry in plasma and sciatic nerve at two and ten months of age and these analyses were implemented analyzing the gene expression of crucial steroidogenic enzymes in sciatic nerve...
May 3, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/28456553/an-unusual-spinaceamine-bearing-pregnane-from-a-soft-coral-scleronephthya-sp-inhibits-the-migration-of-tumor-cells
#7
Wei Cheng, Zhen Liu, Yang Yu, Leen van Ofwegen, Peter Proksch, Siwang Yu, Wenhan Lin
An unprecedented spinaceamine-bearing pregnane namely scleronine (1) was isolated from a Chinese soft coral Scleronephthya sp. Its structure was determined on the basis of 1D and 2D NMR spectroscopic analyses in association with the HRESIMS data, while the absolute configurations were deduced by the single-crystal X-ray diffraction analysis. In addition, a dehydrogenated analogue (3) was synthesized through six steps with pregna-1,20-dien-3-one (2) as a precursor. The significantly inhibitory effects of 1 and 3 against the migration of tumor cells A549 and B16 accompanying the down-regulation of key genes (TGFβ, TNFα, IL-1β, and IL-6) were observed...
April 20, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28454188/metabolic-profiling-of-hoodia-chamomile-terminalia-species-and-evaluation-of-commercial-preparations-using-ultrahigh-performance-liquid-chromatography-quadrupole-time-of-flight-mass-spectrometry
#8
Bharathi Avula, Yan-Hong Wang, Giorgis Isaac, Jimmy Yuk, Mark Wrona, Kate Yu, Ikhlas A Khan
Ultrahigh-performance liquid chromatography quadrupole-time-of-flight mass spectrometry (UHPLC-QToF-MS) profiling was used for the identification of marker compounds and generation of metabolic patterns that could be interrogated using chemometric modeling software. UHPLC-QToF-MS was used to generate comprehensive fingerprints of three botanicals (Hoodia, Terminalia, and chamomile), each having different classes of compounds. Detection of a broad range of ions was carried out in full scan mode in both positive and negative modes over the range m/z 100-1700 using high-resolution mass spectrometry...
April 28, 2017: Planta Medica
https://www.readbyqxmd.com/read/28446029/sugar-free-pregnane-type-steroids-from-the-roots-of-cynanchum-stauntonii
#9
An-Jun Deng, Dan Zhang, Qian Li, Zhi-Hui Zhang, Zhi-Hong Li, Hai-Lin Qin
Two new sugar-free 14,15-secopregnane-type steroids, 14-O-methyl-3-epi-hirundigenin (1) and 2-deoxyamplexicogenin A (2), along with two known sugar-free pregnane-type steroids, were isolated from the 95% ethanol extract of the roots of Cynanchum stauntonii. The structures of the new compounds were characterized on the basis of extensive spectroscopic analyses, mainly 1D and 2D NMR methods, albeit the MS experiments did not display the molecular ion peaks. Compound 2 was the aglycones of stauntosides J and K, etc...
April 27, 2017: Journal of Asian Natural Products Research
https://www.readbyqxmd.com/read/28442602/molecular-basis-of-metabolism-mediated-conversion-of-pk11195-from-an-antagonist-to-an-agonist-of-the-constitutive-androstane-receptor
#10
Bryan Mackowiak, Linhao Li, Matthew A Welch, Daochuan Li, Jace W Jones, Scott Heyward, Maureen A Kane, Peter W Swaan, Hongbing Wang
The constitutive androstane receptor (CAR) plays an important role in xenobiotic metabolism, energy homeostasis, and cell proliferation. Antagonism of CAR represents a key strategy for studying its function and may have potential clinical applications. However, specific human CAR (hCAR) antagonists are limited and conflicting data on the activity of these compounds have been reported. PK11195, a typical peripheral benzodiazepine receptor ligand, has been established as a potent hCAR deactivator in immortalized cells; whether it inhibits hCAR activity under physiologically-relevant conditions remains unclear...
April 25, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28436464/glucose-dependent-regulation-of-pregnane-x-receptor-is-modulated-by-amp-activated-protein-kinase
#11
Peter O Oladimeji, Wenwei Lin, C Trent Brewer, Taosheng Chen
Pregnane X receptor (PXR) is a xenobiotic receptor that regulates the detoxification and clearance of drugs and foreign compounds from the liver. There has been mounting evidence of crosstalk between the drug metabolism pathway and the energy metabolism pathway, but little is known about this cross-regulation. To further delineate the energy metabolism and drug metabolism crosstalk in this study, we exposed HepG2 cells to varying glucose concentrations. We observed that PXR activity was induced under high-glucose conditions...
April 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28432535/exploring-the-carbamazepine-interaction-with-human-pregnane-x-receptor-and-effect-on-abcc2-using-in-vitro-and-in-silico-approach
#12
Gurpreet K Grewal, Khuraijam D Singh, Neha Kanojia, Chitra Rawat, Samiksha Kukal, Ajay Jajodia, Anshika Singhal, Richa Misra, Selvaraman Nagamani, Karthikeyan Muthusamy, Ritushree Kukreti
PURPOSE: Over expression of ATP-binding cassette transporters is considered one of the major reasons for non-responsiveness to antiepileptic drugs. Carbamazepine (CBZ), one of first line antiepileptic drug is known to influence ABCC2 expression but its exact molecular mechanism is unknown. METHODS: We investigated the effect of CBZ on expression of ABCC2 and pregnane X receptor (PXR) in HepG2 cell line and compared with hyperforin (agonist of PXR) and ketoconazole (antagonist of PXR) through realtime PCR and western blot assay...
April 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28430654/alpha-ketoglutarate-suppresses-the-nf-%C3%AE%C2%BAb-mediated-inflammatory-pathway-and-enhances-the-pxr-regulated-detoxification-pathway
#13
Liuqin He, Huan Li, Niu Huang, Xihong Zhou, Junquan Tian, Tiejun Li, Jing Wu, Yanan Tian, Yulong Yin, Kang Yao
Alpha-ketoglutarate (AKG) is a critical nutritional factor in the maintenance of intestinal homeostasis. However, the relative mechanism of AKG has not been well understood. It was recently shown that the interaction between nuclear factor kappa B (NF-κB)-mediated inflammatory pathway and pregnane X receptor (PXR)-regulated detoxification pathway is a check and balance mechanism for keeping the homeostatic state of the intestine, preventing the onset of intestinal inflammation which may lead to cancer. In the current study we used lipopolysaccharide (LPS)-challenged piglet and intestinal porcine epithelial cells-J2 models to investigate the effects of dietary AKG supplementation on the intestinal immune system and PXR regulated target expression...
April 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28428226/rapid-throughput-analysis-of-gabaa-receptor-subtype-modulators-and-blockers-using-disbac1-3-membrane-potential-red-dye
#14
Atefeh Mousavi Nik, Brandon Pressly, Vikrant Singh, Shane Antrobus, Susan Hulsizer, Michael A Rogawski, Heike Wulff, Isaac N Pessah
Fluorometric Imaging Plate Reader (FLIPR®) membrane potential dye (FMP-Red-Dye) is a proprietary tool for basic discovery and high throughput drug screening for G-protein coupled receptors and ion channels. We optimized and validated this potentiometric probe to assay functional modulators of heterologous expressed GABAA receptor (GABAAR) isoforms (synaptic α1β3γ2, extrasynaptic α4β3δ, and β3 homopentomers). High-resolution mass spectrometry identified FMP-Red-dye as DisSBAC1(3). GABAAR expressing cells equilibrated with FMP-Red-Dye exhibited depolarized equilibrium membrane (Em) potentials compared to GABAAR-null cells...
April 20, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28428138/pregnane-x-receptor-regulates-the-ahr-cyp1a1-pathway-and-protects-liver-cells-from-benzo-%C3%AE-pyrene-induced-dna-damage
#15
Hongmei Cui, Xinsheng Gu, Jingshu Chen, Ying Xie, Sui Ke, Jing Wu, Andrei Golovko, Benjamin Morpurgo, Chunhong Yan, Timothy D Phillips, Wen Xie, Jianyuan Luo, Zhijun Zhou, Yanan Tian
Pregnane X receptor (PXR) plays an important role in protecting cells from mutagenic DNA damages induced by endogenous and exogenous toxicants. This protective function is often attributed to the PXR-regulated metabolic detoxification. Here we report a novel potential mechanism that PXR reduces benzo-[α]-pyrene(BaP)-induced DNA damage through inhibiting the transcriptional activity of aryl hydrocarbon receptor (AhR) which plays a pivotal role in the bioactivation of BaP. We have utilized three well-characterized cell lines, i...
April 18, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28420184/metajapogenins-a-c-pregnane-steroids-from-shells-of-metaplexis-japonica
#16
Hui-Li Yao, Yang Liu, Xiao-Hong Liu, Hua Gao, Kun Liu, Yan-Lin Shao, Xin-Yu Fang, Wei Wang
Phytochemical investigation of the shells of Metaplexis japonica (Thunb.) Makino, belonging to the family of Apocynaceae, afforded three new pregnane steroids, metajapogenins A-C, along with three known compounds. The structures of the new compounds were elucidated as 12β,14β,17β-trihydroxypregna-3,5-dien-7,20-dione, 12β,14β,17β,20β-tetrahydroxypregna-3,5-dien-7-one; 3β,12β,14β,17β-tetrahydroxypregn-5-ene-7,20-dione on the basis of extensive spectroscopic evidence derived from 1D; 2D-NMR experiments and mass spectrometry...
April 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28414139/ligand-dependent-and-independent-regulation-of-human-hepatic-sphingomyelin-phosphodiesterase-acid-like-3a-expression-by-pregnane-x-receptor-and-crosstalk-with-liver-x-receptor
#17
Judith Jeske, Andreas Bitter, Wolfgang E Thasler, Thomas S Weiss, Matthias Schwab, Oliver Burk
Pregnane X receptor (PXR) mainly regulates xenobiotic metabolism and detoxification. Additionally, it exerts pleiotropic effects on liver physiology, which in large parts depend on transrepression of other liver-enriched transcription factors. Based on the hypothesis that lower expression levels of PXR may reduce the extent of this inhibition, an exploratory genome-wide transcriptomic profiling was performed using HepG2 cell clones with different expression levels of PXR. This screen and confirmatory real-time RT-PCR identified sphingomyelin phosphodiesterase acid-like (SMPDL) 3A, a novel nucleotide phosphodiesterase and phosphoramidase, as being up-regulated by PXR-deficiency...
April 13, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28408657/negative-regulation-of-human-pregnane-x-receptor-by-microrna-18a-5p-evidence-for-suppression-of-microrna-18a-5p-expression-by-rifampin-and-rilpivirine
#18
Devinder Sharma, Abdullah A Turkistani, Wenjun Chang, Catherine Hu, Zhaoming Xu, Thomas K H Chang
Small non-coding microRNAs act as post-transcriptional regulators of gene expression involved in diverse biological functions. Pregnane X receptor (PXR, NR1I2), which is a member of the superfamily of nuclear receptors, is a transcription factor governing the transport and biotransformation of various endobiotics and xenobiotics. In the present study, we identified a specific microRNA involved in regulating the expression and functionality of human PXR (hPXR). According to bioinformatics analysis employing three commonly used algorithms (TargetScan, miRanda, and DIANA-microT-CDS), miR-18a-5p was predicted to be the top candidate microRNA regulator of hPXR...
April 13, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28390928/itraconazole-cis-diastereoisomers-activate-aryl-hydrocarbon-receptor-ahr-and-pregnane-x-receptor-pxr-and-induce-cyp1a1-in-human-cell-lines-and-human-hepatocytes
#19
Martina Stepankova, Barbora Pastorkova, Petr Bachleda, Zdenek Dvorak
Triazole antimycotic itraconazole contains in its structure three chiral centres; therefore, it forms eight stereoisomers. Commercial preparations of itraconazole are a mixture of four cis-diastereoisomers. There is much evidence that efficacy, adverse effects, and toxicity of chiral drugs may be stereospecific. Therefore, we have prepared 4 pure cis-diastereoisomers of itraconazole and investigated their effects on transcriptional activities of xenoreceptors aryl hydrocarbon receptor AhR and pregnane X receptor PXR...
April 5, 2017: Toxicology
https://www.readbyqxmd.com/read/28361559/a-new-immunosuppressive-pregnane-glycoside-from-aqueous-fraction-of-epigynum-cochinchinensis
#20
Zong Wan, Yuan-Cheng Yao, Fei Gao, Sheng-Bao Cai, Afsar Khan, Tian-Rui Zhao, Xiao-Yan Yang, Jian Fan, Sheng-Yan Qian, Jian-Xin Cao, Gui-Guang Cheng
Chemical investigation on the aqueous fraction of the stems of Epigynum cochinchinensis led to the isolation of a new pregnane glycoside named as epigycoside A (1) along with three known analogues (2-4). The structure of compound 1 was elucidated by means of spectroscopic techniques, including HRESIMS, and 1D and 2D NMR experiments. The immunosuppressive activity of 1 was evaluated by an in vitro model of concanavalin A-induced mice splenocytes proliferation. Compound 1 showed significant inhibitory activity in a dose-dependent manner, closer to the efficacy of positive control, dexamethasone, at a concentration of 50 μM...
March 31, 2017: Natural Product Research
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