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https://www.readbyqxmd.com/read/29245089/metabolic-analysis-of-panax-notoginseng-saponins-with-gut-microbiota-mediated-biotransformation-by-hplc-dad-q-tof-ms-ms
#1
Man-Yun Chen, Li Shao, Wei Zhang, Chong-Zhi Wang, Hong-Hao Zhou, Wei-Hua Huang, Chun-Su Yuan
Saponins such as notoginsenosides and ginsenosides from Panax notoginseng are responsible for the herb's clinical applications. Unfortunately, there is poor oral bioavailability of saponins. However, gut microbiota can transform saponins to yield the metabolites that are potential bioactive substances. In this study, we aimed to characterize the metabolic profiles of P. notoginseng saponins (PNS) by incubating them with human gut microbiota. The notoginsenosides, ginsenosides and related metabolites were separated and identified using a highly sensitive and selective high-performance liquid chromatography coupled with diode array detection/quadrupole tandem time-of-flight mass spectrometry (HPLC-DAD-Q-TOF-MS/MS)...
December 7, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29245085/excretion-of-metabolites-of-the-synthetic-cannabinoid-jwh-018-in-urine-after-controlled-inhalation
#2
Stefan W Toennes, Anna Geraths, Werner Pogoda, Alexander Paulke, Cora Wunder, Eef L Theunissen, Johannes G Ramaekers
Each year, synthetic cannabinoids are occurring in high numbers on the illicit drug market but data obtained after controlled application are rare. The present study on pharmacokinetics in urine is part of a pilot study on adverse effects of JWH-018, which is one of the oldest and best known synthetic cannabinoids. Six subjects inhaled smoke from 2 and 3mg JWH-018. The drug and ten potential metabolites were analyzed in urine samples collected during 12h after inhalation by liquid chromatography-mass spectrometry (LC-MS/MS) without and with conjugate cleavage...
December 9, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29244856/in-vitro-anthelmintic-effects-of-spigelia-anthelmia-protein-fractions-against-haemonchus-contortus
#3
Sandra Alves Araújo, Alexandra Martins Dos Santos Soares, Carolina Rocha Silva, Eduardo Bezerra Almeida Júnior, Cláudia Quintino Rocha, André Teixeira da Silva Ferreira, Jonas Perales, Livio M Costa-Júnior
Gastrointestinal nematodes are a significant concern for animal health and well-being, and anthelmintic treatment is mainly performed through the use of chemical products. However, bioactive compounds produced by plants have shown promise for development as novel anthelmintics. The aim of this study is to assess the anthelmintic activity of protein fractions from Spigelia anthelmia on the gastrointestinal nematode Haemonchus contortus. Plant parts were separated into leaves, stems and roots, washed with distilled water, freeze-dried and ground into a fine powder...
2017: PloS One
https://www.readbyqxmd.com/read/29244711/flavonoids-and-ellagitannins-characterization-antioxidant-and-cytotoxic-activities-of-phyllanthus-acuminatus-vahl
#4
Mirtha Navarro, Ileana Moreira, Elizabeth Arnaez, Silvia Quesada, Gabriela Azofeifa, Felipe Vargas, Diego Alvarado, Pei Chen
The phenolic composition of leaves from Phyllanthus acuminatus L., a plant commonly used in Costa Rica as traditional medicine, was studied using UPLC-ESI-MS on an enriched phenolic extract. A total of 20 phenolic compounds were identified, comprising eight flavonoids (two flavanones-pinocembrin isomers and six derivatives from apigenin, chrysin, quercetin, and kaempferol); seven ellagitannins, two flavan-3-ols (prodelphinidin B dimer and (epi)gallocatechin); and three phenolic acids (ellagic acid, trimethylellagic acid, and ferulic acid)...
December 15, 2017: Plants (Basel, Switzerland)
https://www.readbyqxmd.com/read/29244172/human-in-vitro-spermatogenesis-from-pluripotent-stem-cells-in-need-of-a-stepwise-differentiation-protocol
#5
C Rombaut, H Mertes, B Heindryckx, E Goossens
Recently, complete in-vitro generation of male gametes starting from pluripotent stem cells was obtained in a mouse model with live offspring as a result. This breakthrough was probably due to the use of a stepwise differentiation protocol taking the tightly regulated in-vivo situation into account. As shown previously, factors of the TGFβ superfamily, metabolites of vitamin A, growth hormones, sex steroids and, most importantly, somatic cell support are major regulators of the development, survival, proliferation and differentiation of male gametes...
December 13, 2017: Molecular Human Reproduction
https://www.readbyqxmd.com/read/29244082/quantitation-of-cocaine-and-metabolites-phencyclidine-butalbital-and-phenobarbital-in-meconium-by-liquid-chromatography-tandem-mass-spectrometry
#6
Triniti L Scroggin, Gwendolyn A McMillin
In this study, a quantitative polarity switching liquid chromatography coupled with a tandem mass spectrometer (LC-MS/MS) method was developed to detect and quantify cocaine and metabolites (cocaethylene, benzoylecgonine and meta-hydroxybenzoylecgonine), phencyclidine (PCP) and barbiturates (phenobarbital and butalbital) in meconium. Accuracy and precision samples at 0.0125% and 75% of the upper limit of quantitation (ULOQ) were analyzed in triplicate over 5 days with accuracy above 84% and average %CV values below 11%...
December 13, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29244080/quantification-of-methadone-and-main-metabolites-in-nails
#7
Teresa Patrícia Magalhães, Sara Cravo, Diana Dias da Silva, Ricardo Jorge Dinis-Oliveira, Carlos Afonso, Maria de Lourdes Bastos, Helena Carmo
The quantification of drugs of abuse in keratinized matrices is becoming of special relevance for monitoring consumption and for post-mortem investigations. We aimed to implement an analytical method for the simultaneous detection of morphine (MORF), 6-monoacetylmorphine (6-MAM), methadone (MET), 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP) and 2-ethyl-5-methyl-3,3-diphenylpyrrolidine (EMDP) in nails. After decontamination, the nail samples (30 mg) were submitted to an alkaline digestion followed by a two-step liquid-liquid and SPE extraction using mixed-mode cation exchange cartridges...
December 13, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29244059/the-mediterranean-diet-metabolic-and-molecular-mechanisms
#8
Valeria Tosti, Beatrice Bertozzi, Luigi Fontana
Consuming a Mediterranean diet rich in minimally processed plant foods has been associated with a reduced risk of developing multiple chronic diseases and increased life expectancy. Data from several randomized clinic trials have demonstrated a beneficial effect in the primary and secondary prevention of cardiovascular disease, type 2 diabetes, atrial fibrillation and breast cancer. The exact mechanism by which an increased adherence to the traditional Mediterranean diet exerts its favorable effects is not known...
December 13, 2017: Journals of Gerontology. Series A, Biological Sciences and Medical Sciences
https://www.readbyqxmd.com/read/29243909/optimization-of-coad-inhibitors-against-gram-negative-organisms-through-targeted-metabolomics
#9
Christopher M Rath, Bret M Benton, Javier De Vicente, Joseph E Drumm, Mei Geng, Cindy Li, Robert J Moreau, Xiaoyu Shen, Colin K Skepper, Micah Steffek, Kenneth Takeoka, Lisha Wang, Jun-Rong Wei, Wenjian Xu, Qiong Zhang, Brian Y Feng
Drug-resistant Gram-negative bacteria are of increasing concern worldwide. Novel antibiotics are needed, but their development is complicated by the requirement to simultaneously optimize molecules for target affinity and cellular potency, which can result in divergent structure-activity relationships (SARs). These challenges were exemplified during our attempts to optimize CoaD inhibitors identified through a biochemical screen. To facilitate lead optimization, we developed mass spectroscopy assays based on the hypothesis that levels of CoA metabolites would reflect the cellular enzymatic activity of CoaD...
December 15, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/29243439/-identification-of-saponins-from-panax-notoginseng-in-metabolites-of-rats
#10
Wen-Wen Shen, Yin Zhang, Shou-Bei Qiu, Fen-Xia Zhu, Xiao-Bin Jia, Dao-Quan Tang, Bin Chen
UPLC-QTOF-MS/MS was used to identify metabolites in rat blood, urine and feces after the administration of n-butanol extract derived from steamed notoginseng. The metabolic process of saponins came from steamed notoginseng was analyzed. The metabolites were processed by PeakView software, and identified according to the structural characteristics of prototype compounds and the accurate qualitative and quantitative changes of common metabolic pathways. Four saponins metabolites were identified based on MS/MS information of metabolites, namely ginsenoside Rh₄, Rk₃, Rk₁, Rg₅,and their 15 metabolites were verified...
October 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29243425/-overexpression-and-isolation-of-cyp76ah1-in-salvia-miltiorrhiza-hairy-roots
#11
Meng-Die Qi, Jian Wang, Xiao-Jing Ma, Quan Zhang, Fang-Fang Wang, Ying Kang, Yong Liu, Hui-Xin Lin
Protein complexes are involved in the synthesis of multiple secondary metabolites in plants, and their separation is essential to elucidate plant secondary metabolism and improve in vitro catalytic efficiency. In this study, the transgenic hairy roots of CYP76AH1, a key enzyme of tanshinone synthesis pathway, was constructed and the transgenic hairy roots of Danshen overexpressing CYP76AH1 protein were screened by Western blotting and used as a tissue culture material for the subsequent extraction of protein complex in tanshinone synthesis pathway...
October 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29243316/effect-of-lactic-acid-bacteria-treated-king-grass-silage-on-the-performance-traits-and-serum-metabolites-in-new-zealand-white-rabbits-oryctolagus-cuniculus
#12
A A Shah, X Yuan, R U Khan, T Shao
This study examined the effects of Lactobacillus plantarum and Pediococcus acidilactici-treated silage of King grass (Pennisetum purpureophoides) on the productive traits and blood biochemistry of New Zealand white (NZW) rabbits. King grass was ensiled without or with L. plantarum (T1), P. acidilactici (T2) and P. acidilactici + L. plantarum (T3). A total of 72 male NZW rabbits (6 weeks) of similar weight and appearance were housed in groups in metallic cages in a completely randomized design. The performance traits, daily feed intake, body weight gain and feed convention ratio were not affected by the silage treatment...
December 15, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/29243287/evaluation-of-the-effect-of-dabrafenib-and-metabolites-on-qtc-interval-in-patients-with-braf-v600-mutant-tumours
#13
Noelia Nebot, H T Arkenau, Jeffrey R Infante, Jason C Chandler, Andrew Weickhardt, Jason D Lickliter, John Sarantopoulos, Michael S Gordon, Gabriel Mak, Annie St-Pierre, Lihua Tang, Bijoyesh Mookerjee, Stanley W Carson, Siobhan Hayes, Kenneth F Grossmann
AIMS: The effect of repeat oral supratherapeutic dosing of the BRAF inhibitor dabrafenib on QTc interval was assessed in patients with BRAF V600-mutant tumours. METHODS: Part 1 of this phase 1, multicentre, 2-part study (BRF113773/NCT01738451) assessed safety/tolerability of dabrafenib 225 or 300 mg twice daily (BID) to inform part 2 dosing. Patients in part 2 received dabrafenib-matched placebo on day -1, single-dose dabrafenib 300 mg on day 1, 300 mg BID on days 2 to 7, and 300 mg on day 8 (morning), followed by 24-hour Holter electrocardiographic monitoring and pharmacokinetics sample collection each dose day...
December 15, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29243271/dynamic-modelling-of-limitations-on-improving-leaf-co2-assimilation-under-fluctuating-irradiance
#14
Alejandro Morales, Elias Kaiser, Xinyou Yin, Jeremy Harbinson, Jaap Molenaar, Steven M Driever, Paul C Struik
A dynamic model of leaf CO2 assimilation was developed as an extension of the canonical steady-state model, by adding the effects of energy-dependent non-photochemical quenching (qE), chloroplast movement, photoinhibition, regulation of enzyme activity in the Calvin cycle, metabolite concentrations, and dynamic CO2 diffusion. The model was calibrated and tested successfully using published measurements of gas exchange and chlorophyll fluorescence on Arabidopsis thaliana ecotype Col-0 and several photosynthetic mutants and transformants affecting the regulation of Rubisco activity (rca-2 and rwt43), NPQ (npq4-1 and npq1-2) and sucrose synthesis (spsa1)...
December 15, 2017: Plant, Cell & Environment
https://www.readbyqxmd.com/read/29243177/24-epibrassinolide-induced-alterations-in-the-root-cell-walls-of-cucumis-sativus-l-under-ca-no3-2-stress
#15
Ya-Hong An, Heng Zhou, Ying-Hui Yuan, Lin Li, Jin Sun, Sheng Shu, Shi-Rong Guo
Brassinosteroids (BRs) can effectively alleviate the oxidative stress caused by Ca(NO3)2 in cucumber seedlings. The root system is an essential organ in plants due to its roles in physical anchorage, water and nutrient uptake, and metabolite synthesis and storage. In this study, 24-epibrassinolide (EBL) was applied to the cucumber seedling roots under Ca(NO3)2 stress, and the resulting chemical and anatomical changes were characterized to investigate the roles of BRs in alleviating salinity stress. Ca(NO3)2 alone significantly induced changes in the components of cell wall, anatomical structure, and expression profiles of several lignin biosynthetic genes...
December 14, 2017: Protoplasma
https://www.readbyqxmd.com/read/29243078/presence-of-bisphenol-s-and-surfactants-in-the-sediments-of-kongsfjorden-a-negative-impact-of-human-activities-in-arctic
#16
K K Nejumal, D Dineep, Mahesh Mohan, K P Krishnan, U K Aravind, C T Aravindakumar
Pollution and fate of pollutants in polar region are important topics of investigation in the last several decades. We have analysed sediment samples from Kongsfjorden and Krossfjorden, two sites from Arctic region, and detected a number of emerging contaminants (ECs) using high-resolution mass spectrometry connected to UPLC (LC-Q-ToF-MS). Out of the seven sampling sites selected, bisphenol S (BPS), an identified pollutant and plasticiser, was detected and quantified in three sediment samples from Kongsfjorden (≈ 0...
December 14, 2017: Environmental Monitoring and Assessment
https://www.readbyqxmd.com/read/29243069/identification-of-a-new-uncompetitive-inhibitor-of-adenosine-deaminase-from-endophyte-aspergillus-niger-sp
#17
Xin-Guo Zhang, Jin-Wen Liu, Peng Tang, Zi-Yu Liu, Guang-Jun Guo, Qiao-Yun Sun, Jian-Jun Yin
Adenosine deaminase (ADA) is an enzyme widely distributed from bacteria to humans. ADA is known as a potential therapeutic target for the treatment of lymphoproliferative disorders and cancer. Endophytes are endosymbionts, often bacteria or fungi, which live within plant tissues and internal organs or intercellular space. Endophytes have a broad variety of bioactive metabolites that are used for the identification of novel natural compounds. Here, 54 morphologically distinct endophyte strains were isolated from six plants such as Peganum harmala Linn...
December 14, 2017: Current Microbiology
https://www.readbyqxmd.com/read/29242837/the-human-gut-microbial-metabolome-modulates-fungal-growth-via-the-tor-signaling-pathway
#18
Carlos García, Faiza Tebbji, Michelle Daigneault, Ning-Ning Liu, Julia R Köhler, Emma Allen-Vercoe, Adnane Sellam
Candida albicans is well known as a major human fungal pathogen, but it is also a permanent resident of healthy gastrointestinal tracts. Recent studies have shown that the human gut microbial metabolome represents an interesting source of bioactive molecules with a significant degree of chemical diversity. Some of these bioactive molecules may have useful antivirulence activities. For instance, intestinal bacterial species belonging to the Lachnospiraceae family were found to secrete molecules that attenuate Salmonella pathogenicity and repress the expression of virulence genes...
November 2017: MSphere
https://www.readbyqxmd.com/read/29242644/parallelogram-based-approach-for-in-vivo-dose-estimation-of-genotoxic-metabolites-in-humans-with-relevance-to-reduction-of-animal-experiments
#19
Hitesh V Motwani, Cecilia Frostne, Margareta Törnqvist
When employing metabolism studies of genotoxic compounds/metabolites and cancer tests for risk estimation, low exposure doses in humans are roughly extrapolated from high exposure doses in animals. An improvement is to measure the in vivo dose, i.e. area under concentration-time curve (AUC), of the causative genotoxic agent. In the present work, we propose and evaluate a parallelogram based approach for estimation of the AUC of genotoxic metabolites that incorporates in vitro metabolic data and existing knowledge from published in vivo data on hemoglobin (Hb) adduct levels, using glycidamide (GA) as a case study compound that is the genotoxic metabolite of acrylamide (AA)...
December 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29242606/murine-stroma-adopts-a-human-like-metabolic-phenotype-in-the-pdx-model-of-colorectal-cancer-and-liver-metastases
#20
Arnaud Blomme, Gaetan Van Simaeys, Gilles Doumont, Brunella Costanza, Justine Bellier, Yukihiro Otaka, Félicie Sherer, Pierre Lovinfosse, Sébastien Boutry, Ana Perez Palacios, Edwin De Pauw, Touko Hirano, Takehiko Yokobori, Roland Hustinx, Akeila Bellahcène, Philippe Delvenne, Olivier Detry, Serge Goldman, Masahiko Nishiyama, Vincent Castronovo, Andrei Turtoi
Cancer research is increasingly dependent of patient-derived xenograft model (PDX). However, a major point of concern regarding the PDX model remains the replacement of the human stroma with murine counterpart. In the present work we aimed at clarifying the significance of the human-to-murine stromal replacement for the fidelity of colorectal cancer (CRC) and liver metastasis (CRC-LM) PDX model. We have conducted a comparative metabolic analysis between 6 patient tumors and corresponding PDX across 4 generations...
December 15, 2017: Oncogene
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