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https://www.readbyqxmd.com/read/28722112/in-silico-and-in-vitro-prediction-of-gastrointestinal-absorption-from-potential-drug-eremantholide-c
#1
Tamires G Caldeira, Dênia A Saúde-Guimarães, André B Dezani, Cristina Helena Dos Reis Serra, Jacqueline de Souza
OBJECTIVES: Analysis of the biopharmaceutical properties of eremantholide C, sesquiterpene lactone with proven pharmacological activity and low toxicity, is required to evaluate its potential to become a drug. METHODS: Preliminary analysis of the physicochemical characteristics of eremantholide C was performed in silico. Equilibrium solubility was evaluated using the shake-flask method, at 37.0 °C, 100 rpm during 72 h in biorelevant media. The permeability was analysed using parallel artificial membrane permeability assay, at 37...
July 19, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28720958/aroma-composition-of-shalgam-a-traditional-turkish-lactic-acid-fermented-beverage
#2
Hasan Tanguler, Serkan Selli, Kemal Sen, Turgut Cabaroglu, Huseyin Erten
Shalgam, a traditional red, cloudy and sour soft beverage, is produced by lactic acid fermentation of black carrot, sourdough, salt, bulgur flour, turnip and adequate water. The present study was designed to characterize the volatile compounds of shalgam obtained from different methods. The aroma compounds of shalgams produced by traditional and direct methods, and addition of Lactic acid bateria (LAB) cultures were examined. Volatile components of shalgam samples were extracted by liquid-liquid extraction technique with pentane/dichloromethane and analyzed by gas chromatography-mass spectrometry (GC-MS)...
June 2017: Journal of Food Science and Technology
https://www.readbyqxmd.com/read/28720125/profiling-of-the-perturbed-metabolomic-state-of-mouse-spleen-during-acute-and-chronic-toxoplasmosis
#3
Xiao-Qing Chen, Chun-Xue Zhou, Hany M Elsheikha, Shuai He, Gui-Xue Hu, Xing-Quan Zhu
BACKGROUND: Toxoplasma gondii, a common opportunistic protozoan, is a leading cause of illness and mortality among immunosuppressed individuals and during congenital infections. Current therapeutic strategies for toxoplasmosis are not fully effective at curtailing disease progression in these cases. Given the parasite ability to influence host immunity and metabolism, understanding of the metabolic alterations in the host's immune organs during T. gondii infection may enhance the understanding of the molecular mechanisms that define the pathophysiology of T...
July 18, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/28717205/genome-reconstruction-in-cynara-cardunculus-taxa-gains-access-to-chromosome-scale-dna-variation
#4
Alberto Acquadro, Lorenzo Barchi, Ezio Portis, Giulio Mangino, Danila Valentino, Giovanni Mauromicale, Sergio Lanteri
The genome sequence of globe artichoke (Cynara cardunculus L. var. scolymus, 2n = 2x = 34) is now available for use. A survey of C. cardunculus genetic resources is essential for understanding the evolution of the species, carrying out genetic studies and for application of breeding strategies. We report on the resequencing analyses (~35×) of four globe artichoke genotypes, representative of the core varietal types, as well as a genotype of the related taxa cultivated cardoon. The genomes were reconstructed at a chromosomal scale and structurally/functionally annotated...
July 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28715477/the-rhlr-quorum-sensing-receptor-controls-pseudomonas-aeruginosa-pathogenesis-and-biofilm-development-independently-of-its-canonical-homoserine-lactone-autoinducer
#5
Sampriti Mukherjee, Dina Moustafa, Chari D Smith, Joanna B Goldberg, Bonnie L Bassler
Quorum sensing (QS) is a bacterial cell-to-cell communication process that relies on the production, release, and response to extracellular signaling molecules called autoinducers. QS controls virulence and biofilm formation in the human pathogen Pseudomonas aeruginosa. P. aeruginosa possesses two canonical LuxI/R-type QS systems, LasI/R and RhlI/R, which produce and detect 3OC12-homoserine lactone and C4-homoserine lactone, respectively. Here, we use biofilm analyses, reporter assays, RNA-seq studies, and animal infection assays to show that RhlR directs both RhlI-dependent and RhlI-independent regulons...
July 17, 2017: PLoS Pathogens
https://www.readbyqxmd.com/read/28714386/nitroisoxazolones-showing-diverse-chemical-behavior-a-useful-building-block-for-polyfunctionalized-systems
#6
Nagatoshi Nishiwaki
4-Nitroisoxazolin-5(2H)-one (nitroisoxazolone) has multiple functionalities embedded as the partial structures that include a nitroalkene, an enamine, a lactone, a N-O bond, and an α, β-unsaturated carbonyl moiety. These structural features facilitate versatile chemical transformations that lead to polyfunctionalized heterocycles that are not easily available by alternative methods. Anionic nitroisoxazolone readily undergoes ring opening to afford dianionic cyano-aci-nitroacetate. This dianionic reagent serves as a safe cyano(nitro)methylating agent to afford glutaronitriles and α-nitro-δ-keto nitriles that are precursors of polyfunctionalized isoxazolines, pyridines, and diazabicycliccompounds...
July 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28714256/a1s_2811-a-chea-y-like-hybrid-two-component-regulator-from-acinetobacter%C3%A2-baumannii-atcc17978-is-involved-in-surface-motility-and-biofilm-formation-in-this-bacterium
#7
Rong Chen, Ruichen Lv, Lisheng Xiao, Min Wang, Zongmin Du, Yafang Tan, Yujun Cui, Yanfeng Yan, Yanping Luo, Ruifu Yang, Yajun Song
Two-component systems in Acinetobacter baumannii are associated with its virulence, drug resistance, motility, biofilm formation, and other characteristics. In this study, we used RecAb , a genetic engineering method, to investigate the function of A1S_2811 in A. baumannii strain ATCC17978. A1S_2811, a hypothetical hybrid sensor histidine kinase/response regulator, has four histidine-containing phosphotransfer domains, a CheA-like regulatory domain, and a CheY-like receiver domain at its C terminus. Compared with the ATCC17978 strain, both surface motility and biofilm formation at the gas-liquid interface decreased significantly in the A1S_2811 knock-out strain...
July 17, 2017: MicrobiologyOpen
https://www.readbyqxmd.com/read/28712049/ginkgolide-b-suppresses-methamphetamine-induced-microglial-activation-through-tlr4-nf-%C3%AE%C2%BAb-signaling-pathway-in-bv2-cells
#8
Fen Wan, Songsong Zang, Guoqing Yu, Hang Xiao, Jun Wang, Jinrong Tang
Accumulating evidence suggests that microglial cells have altered morphology and proliferation in different brain regions of methamphetamine (Meth) abusers and Meth-abusing animal models. However, the possible mechanisms underlying Meth-induced microglial activation remain poorly understood. Meanwhile, Toll-like receptor4 (TLR4) is closely associated with inflammation. Therefore the aim of the present study was to assess whether Meth treatment affects TLR4 expression; in addition, we evaluated the effects of ginkgolide B (GB), a diterpene lactone extracted from Ginkgo biloba, on Meth-mediated inflammation...
July 15, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28708672/artemisinin-disrupts-androgen-responsiveness-of-human-prostate-cancer-cells-by-stimulating-the-26s-proteasome-mediated-degradation-of-the-androgen-receptor-protein
#9
Andrea M Steely, Jamin A Willoughby, Shyam N Sundar, Vasiliki I Aivaliotis, Gary L Firestone
Androgen receptor (AR) expression and activity is highly linked to the development and progression of prostate cancer and is a target of therapeutic strategies for this disease. We investigated whether the antimalarial drug artemisinin, which is a sesquiterpene lactone isolated from the sweet wormwood plant Artemisia annua, could alter AR expression and responsiveness in cultured human prostate cancer cell lines. Artemisinin treatment induced the 26S proteasome-mediated degradation of the receptor protein, without altering AR transcript levels, in androgen-responsive LNCaP prostate cancer cells or PC-3 prostate cancer cells expressing exogenous wild-type AR...
July 13, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28706484/alantolactone-improves-prolonged-exposure-of-interleukin-6-induced-skeletal-muscle-inflammation-associated-glucose-intolerance-and-insulin-resistance
#10
Minjee Kim, Kwangho Song, Yeong Shik Kim
The pro-inflammatory cytokine, Interleukin-6 (IL-6), has been proposed to be one of the mediators that link chronic inflammation to glucose intolerance and insulin resistance. Many studies have demonstrated the effects of IL-6 on insulin action in the skeletal muscle. However, few studies have investigated the effect of long-term treatment of IL-6, leading to glucose intolerance and insulin resistance. In the present study, we observed protective effects of alantolactone, a sesquiterpene lactone isolated from Inula helenium against glucose intolerance and insulin resistance induced by prolonged exposure of IL-6...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28706483/phytoagent-deoxyelephantopin-and-its-derivative-inhibit-triple-negative-breast-cancer-cell-activity-through-ros-mediated-exosomal-activity-and-protein-functions
#11
Jeng-Yuan Shiau, Yong-Qun Chang, Kyoko Nakagawa-Goto, Kuo-Hsiung Lee, Lie-Fen Shyur
A novel plant sesquiterpene lactone derivative, DET derivative (DETD)-35, originating from parental deoxyelephantopin (DET) was previously observed to effectively suppress human triple negative breast cancer (TNBC) MDA-MB-231 cell activity and tumor growth in mice. In this study, the mechanisms underlying the activity of DETD-35 were elucidated. DET and DETD-35 induced reactive oxygen species (ROS) which caused structural damage and dysfunction of mitochondria and increased cytosolic calcium level, subsequently evoking exosome release from the cancer cells...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28705432/identification-of-galiellalactone-based-novel-stat3-selective-inhibitors-with-cytotoxic-activities-against-triple-negative-breast-cancer-cell-lines
#12
Hyun Su Kim, Taewoo Kim, Hyejin Ko, Jeeyeon Lee, Yeong Shik Kim, Young-Ger Suh
Signal transducer and activator of transcription 3 (STAT3) is phosphorylated in breast cancer cells, particularly triple-negative breast cancers (TNBCs). Therefore, the inhibition of constitutive phosphorylated STAT3 is a promising therapeutic for TNBC treatment. Recently, a series of novel STAT3 inhibitors based on natural (-)-galiellalactone have been identified to inhibit STAT3 phosphorylation at the Tyr705 residue. Interestingly, the truncation of the cyclohexene moiety of (-)-galiellalactone to [3.3] bicyclic lactone as a pharmacophoric core produced improved cytotoxic effects against TNBCs...
June 23, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28702662/chiral-squaramide-catalysed-enantioselective-michael-cyclization-cascade-reaction-of-3-hydroxyoxindoles-with-%C3%AE-%C3%AE-unsaturated-n-acylated-succinimides
#13
Sheng Ming, Bo-Liang Zhao, Da-Ming Du
A bifunctional squaramide-catalysed asymmetric Michael/cyclization cascade reaction of 3-hydroxyoxindoles with α,β-unsaturated N-acylated succinimides is disclosed. With quinine-derived squaramide as the catalyst, a broad range of the desired spirooxindole lactone derivatives bearing two contiguous stereocenters were obtained in good yields (up to 89%) with high diastereoselectivities (up to >95 : 5 dr) and excellent enantioselectivities (up to 99% ee).
July 12, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28702008/hypersensitive-response-of-plasmid-encoded-ahl-synthase-gene-to-lifestyle-and-nutrient-by-ensifer-adhaerens-x097
#14
Yanhua Zeng, Yanli Wang, Zhiliang Yu, Yili Huang
It is known that some bacteria, especially members of the family Rhizobiaceae, have multiple N-acyl homoserine lactones (AHL) synthase genes and produce multiple AHL signals. However, how bacteria selectively utilize these multiple genes and signals to cope with changing environments is poorly understood. Ensifer adhaerens is an important microorganism in terms of biotechnology, ecology and evolutionary. In this study, we investigated the AHL-based QS system of E. adhaerens X097 and its response to different lifestyles or nutrients...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28701209/alantolactone-a-natural-sesquiterpene-lactone-has-potent-antitumor-activity-against-glioblastoma-by-targeting-ikk%C3%AE-kinase-activity-and-interrupting-nf-%C3%AE%C2%BAb-cox-2-mediated-signaling-cascades
#15
Xun Wang, Zhenlong Yu, Chao Wang, Wei Cheng, Xiangge Tian, Xiaokui Huo, Yan Wang, Chengpeng Sun, Lei Feng, Jinshan Xing, Yulong Lan, Dongdong Sun, Qingjuan Hou, Baojing Zhang, Xiaochi Ma, Bo Zhang
BACKGROUND: Glioblastoma multiforme (GBM) is one of the most refractory and palindromic central nervous system (CNS) neoplasms, and current treatments have poor effects in GBM patients. Hence, the identification of novel therapeutic targets and the development of effective treatment strategies are essential. Alantolactone (ATL) has a wide range of pharmacological activities, and its anti-tumor effect is receiving increasing attention. However, the molecular mechanism underlying the anti-GBM activity of ATL remains poorly understood...
July 12, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28697551/n-acyl-homoserine-lactone-dynamics-during-biofilm-formation-of-a-1-2-4-trichlorobenzene-mineralizing-community-on-clay
#16
Hongjie Sheng, Mourad Harir, Lisa A Boughner, Xin Jiang, Philippe Schmitt-Kopplin, Reiner Schroll, Fang Wang
In Gram-negative bacteria, quorum sensing systems are based on the N-acyl-homoserine lactone (AHL) molecule. The objective of this study was to investigate the role of quorum sensing systems during biofilm formation by a microbial community while degrading the pollutant. Our model system included 1,2,4-trichlorobenzene (1,2,4-TCB) and its mineralizing Gram-negative bacterial community to investigate the relationships between AHL dynamics, cell growth and pollutant degradation. Biomineralization of 1,2,4-TCB was monitored for both the planktonic bacterial community with and without sterile clay particles in liquid cultures...
July 6, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28695853/crystal-structure-of-the-n-terminal-domain-of-vqsr-from-pseudomonas-aeruginosa-at-2-1%C3%A2-%C3%A3-resolution
#17
Qing He, Kang Wang, Tiantian Su, Feng Wang, Lichuan Gu, Sujuan Xu
VqsR is a quorum-sensing (QS) transcriptional regulator which controls QS systems (las, rhl and pqs) by directly downregulating the expression of qscR in Pseudomonas aeruginosa. As a member of the LuxR family of proteins, VqsR shares the common motif of a helix-turn-helix (HTH)-type DNA-binding domain at the C-terminus, while the function of its N-terminal domain remains obscure. Here, the crystal structure of the N-terminal domain of VqsR (VqsR-N; residues 1-193) was determined at a resolution of 2.1 Å...
July 1, 2017: Acta Crystallographica. Section F, Structural Biology Communications
https://www.readbyqxmd.com/read/28695844/the-structure-of-a-complex-of-the-lactonohydrolase-zearalenone-hydrolase-with-the-hydrolysis-product-of-zearalenone-at-1-60%C3%A2-%C3%A3-resolution
#18
Qi Qi, Wen Jing Yang, Hu Jian Zhou, Deng Ming Ming, Kai Lei Sun, Tian Yu Xu, Xiao Jian Hu, Hong Lv
Zearalenone hydrolase (ZHD) is an α/β-hydrolase that detoxifies and degrades the lactone zearalenone (ZEN), a naturally occurring oestrogenic mycotoxin that contaminates crops. Several apoenzyme and enzyme-substrate complex structures have been reported in the resolution range 2.4-2.6 Å. However, the properties and mechanism of this enzyme are not yet fully understood. Here, a 1.60 Å resolution structure of a ZHD-product complex is reported which was determined from a C-terminally His6-tagged ZHD crystal soaked with 2 mM ZEN for 30 min...
July 1, 2017: Acta Crystallographica. Section F, Structural Biology Communications
https://www.readbyqxmd.com/read/28694686/molecular-docking-qsar-and-admet-studies-of-withanolide-analogs-against-breast-cancer
#19
Dharmendra K Yadav, Surendra Kumar, Saloni, Harpreet Singh, Mi-Hyun Kim, Praveen Sharma, Sanjeev Misra, Feroz Khan
Withanolides are a group of pharmacologically active compounds present in most prodigal amounts in roots and leaves of Withania somnifera (Indian ginseng), one of the most important medicinal plants of Indian traditional practice of medicine. Withanolides are steroidal lactones (highly oxygenated C-28 phytochemicals) and have been reported to exhibit immunomodulatory, anticancer and other activities. In the present study, a quantitative structure activity relationship (QSAR) model was developed by a forward stepwise multiple linear regression method to predict the activity of withanolide analogs against human breast cancer...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28693338/in-vitro-antiplasmodial-and-cytotoxic-activities-of-sesquiterpene-lactones-from-vernonia-fimbrillifera-less-asteraceae
#20
Annélise Bordignon, Michel Frédérich, Allison Ledoux, Pierre-Eric Campos, Patricia Clerc, Thomas Hermann, Joëlle Quetin-Leclercq, Ewa Cieckiewicz
Due to the in vitro antiplasmodial activity of leaf extracts from Vernonia fimbrillifera Less. (Asteraceae), a bioactivity-guided fractionation was carried out. Three sesquiterpene lactones were isolated, namely 8-(4'-hydroxymethacrylate)-dehydromelitensin (1), onopordopicrin (2) and 8α-[4'-hydroxymethacryloyloxy]-4-epi-sonchucarpolide (3). Their structures were elucidated by spectroscopic methods (1D and 2D NMR and MS analyses) and by comparison with published data. The isolated compounds exhibited antiplasmodial activity with IC50 values ≤ 5 μg/mL...
July 10, 2017: Natural Product Research
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