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https://www.readbyqxmd.com/read/28087627/inhibition-of-cell-polarity-establishment-in-stomatal-asymmetric-cell-division-using-the-chemical-compound-bubblin
#1
Yumiko Sakai, Shigeo S Sugano, Takashi Kawase, Makoto Shirakawa, Yu Imai, Yusuke Kawamoto, Hiroshi Sugiyama, Tsuyoshi Nakagawa, Ikuko Hara-Nishimura, Tomoo Shimada
Stem-cell polarization is a crucial step in asymmetric cell division, which is a universal system for generating cellular diversity in multicellular organisms. Several conventional genetics studies have attempted to elucidate the mechanisms underlying cell polarization in plants, but it remains largely unknown. In plants, stomata, which are valves for gas exchange, are generated through several rounds of asymmetric divisions. In this study, we identified and characterized a chemical compound that affects stomatal stem-cell polarity...
January 13, 2017: Development
https://www.readbyqxmd.com/read/28086774/androgenic-effects-of-aqueous-and-methanolic-extracts-of-ficus-asperifolia-in-male-wistar-rats
#2
Pierre Watcho, Hermine Meli Watio, Modeste Wankeu-Nya, Esther Ngadjui, Patrick Deeh Defo, Pepin Alango Nkeng-Efouet, Telesphore Benoit Nguelefack, Albert Kamanyi
BACKGROUND: Androgen deficiency is a clinical syndrome resulting from the inability of the testes to produce physiological levels of testosterone due to a disturbance occurring at one or more levels of the hypothalamic-pituitary-testicular axis. The present study was undertaken to evaluate the androgenic properties of aqueous and methanolic extracts of Ficus asperifolia on normal and castrated immature rats. METHODS: Normal rats were treated either per os with aqueous or methanolic extract of Ficus asperifolia (100 mg/kg or 500 mg/kg b...
January 13, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28081499/screening-active-compounds-from-corydalis-yanhusuo-by-combining-high-expression-vegf-receptor-hek293-cell-membrane-chromatography-with-hplc-esi-it-tof-msn-method
#3
Fen Wei, Qi Hu, Jing Huang, Shengli Han, Sicen Wang
Corydalis Thizoma,or Yuanhu in China, is a common herbal drug used for thousands of years as analgesic in Chinese medicine that has been reported to have potential anti-angiogenic effects. In this study, a VEGFR/cell membrane chromatography (VEGFR/CMC) coupled with HPLC- ESI-IT-TOF-MSn system was developed and successfully applied for identifying active components from YuanHu extract acting on VEGFR. We identified tetrahydropalmatine and corydaline as bioactive components with VEGFR activity, thus confirming their inhibitory activity on VEGFR engineered HEK293 cell growth by MTT assay...
January 4, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28078991/vegetable-organosulfur-compounds-and-their-health-promoting-effects
#4
Spyridon A Petropoulos, Francesco Di Gioia, Georgia Ntatsi
BACKGROUND: Trends in modern pharmaceutical science show an increase in demand for new drugs and diet supplements derived from natural products, while during the last decades, great research is conducted regarding the natural compounds and their medicinal and bioactive properties. Organosulfur compounds are present in many plants and their bioactive properties have been used in folk and traditional medicine throughout the centuries. Not until recently, modern science confirmed and revealed the chemical compounds that are responsible for these properties, the chemistry involved in their biosynthesis and the main mechanisms of action...
January 10, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28078539/unfolding-of-the-myosin-head-by-purealin-in-glycerol
#5
Jiro Takito, Jun'ichi Kobayashi, Masanori Nakamura, Yasushi Ohizumi, Yoshiaki Nonomura
Purealin is a small bioactive compound obtained from the marine sponge. The compound modulates various types of ATPase activity of myosin from skeletal muscle, cardiac muscle, and smooth muscle. To elucidate the structural basis of these effects of purealin on myosin ATPases, we examined the effect of purealin on the conformation of skeletal muscle myosin in aqueous solution and in glycerol. Analysis of the circular dichroism spectrum of subfragment 1, a single-headed fragment of myosin, revealed that in 10% glycerol purealin decreased the β-sheet content of S1, but in aqueous solution it had little effect on the secondary structure of S1...
January 11, 2017: Anatomical Science International
https://www.readbyqxmd.com/read/28077256/montivipera-bornmuelleri-venom-selectively-exhibits-high-cytotoxic-effects-on-keratinocytes-cancer-cell-lines
#6
Saly Sawan, Tania Yaacoub, Souad Hraoui-Bloquet, Riyad Sadek, Walid Hleihel, Ziad Fajloun, Marc Karam
CONTEXT: The Viperidae family venom is a rich source of bioactive compounds such as many proteases, which cause tissue necrosis and affect mostly the vascular system. However, the venom exhibits therapeutic potentials and has contributed to the development of some medical drugs. Specifically, the Montivipera bornmuelleri venom has shown to exhibit antibacterial, pro-inflammatory and antifungal activities. OBJECTIVE: This work evaluates the cytotoxic effect of the M...
January 8, 2017: Experimental and Toxicologic Pathology: Official Journal of the Gesellschaft Für Toxikologische Pathologie
https://www.readbyqxmd.com/read/28076651/controlled-release-of-chlorhexidine-from-a-mesoporous-silica-containing-macroporous-titanium-dental-implant-prevents-microbial-biofilm-formation
#7
K De Cremer, A Braem, E Gerits, K De Brucker, K Vandamme, J A Martens, J Michiels, J Vleugels, B P Cammue, K Thevissen
Roughened surfaces are increasingly being used for dental implant applications as the enlarged contact area improves bone cell anchorage, thereby facilitating osseointegration. However, the additional surface area also entails a higher risk for the development of biofilm associated infections, an etiologic factor for many dental ailments, including peri-implantitis. To overcome this problem, we designed a dental implant composed of a porous titanium-silica (Ti/SiO2) composite material and containing an internal reservoir that can be loaded with antimicrobial compounds...
January 11, 2017: European Cells & Materials
https://www.readbyqxmd.com/read/28075447/anti-metastatic-effect-of-rhodomyrtone-from-rhodomyrtus-tomentosa-on-human-skin-cancer-cells
#8
Malatee Tayeh, Sirinun Nilwarangoon, Wilawan Mahabusarakum, Ramida Watanapokasin
This study focused on the inhibitory effect of rhodomyrtone, a bioactive compound isolated from the leaves of Rhodomyrtus tomentosa (Aiton) Hassk., on cancer metastasis in epidermoid carcinoma A431 cells and on the verification of the underlying related molecular mechanisms of this event. We demonstrated that rhodomyrtone at the subcytotoxic concentration (0.5 and 1.5 µg/ml) exhibited pronounced inhibition of cancer metastasis by reducing cell migration, cell adhesive ability and cell invasion of A431 cells in a dose-dependent manner...
January 9, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28075411/tamaractam-a-new-bioactive-lactam-from-tamarix-ramosissima-induces-apoptosis-in-rheumatoid-arthritis-fibroblast-like-synoviocytes
#9
Yao Yao, Cheng-Shuai Jiang, Na Sun, Wei-Qi Li, Yang Niu, Huai-Qin Han, Zhen-Hua Miao, Xun-Xia Zhao, Jing Zhao, Juan Li
Chemical investigation of Tamarix ramosissima Ledeb, a traditional herbal medicine used for rheumatoid arthritis (RA) treatment in northwest China, led to the discovery of a new phenolic aromatic rings substituted lactam, tamaractam (1), together with the previously reported compounds cis-N-feruloyl-3-O-methyldopamine (2) and trans-N-feruloyl-3-O-methyldopamine (3). The structures of the compounds were determined by high resolution electrospray ionization mass spectroscopy (HRESIMS) and 1D and 2D-NMR experiments, as well as comparison with the literature data...
January 10, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28075408/time-course-exo-metabolomic-profiling-in-the-green-marine-macroalga-ulva-chlorophyta-for-identification-of-growth-phase-dependent-biomarkers
#10
Taghreed Alsufyani, Anne Weiss, Thomas Wichard
The marine green macroalga Ulva (Chlorophyta) lives in a mutualistic symbiosis with bacteria that influence growth, development, and morphogenesis. We surveyed changes in Ulva's chemosphere, which was defined as a space where organisms interact with each other via compounds, such as infochemicals, nutrients, morphogens, and defense compounds. Thereby, Ulva mutabilis cooperates with bacteria, in particular, Roseovarius sp. strain MS2 and Maribacter sp. strain MS6 (formerly identified as Roseobacter sp. strain MS2 and Cytophaga sp...
January 10, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28074962/crossed-flow-microfluidics-for-high-throughput-screening-of-bioactive-chemical-cell-interactions
#11
Ziqiu Tong, Angela Ivask, Keying Guo, Scott McCormick, Enzo Lombi, Craig Priest, Nicolas H Voelcker
This paper describes the use of crossed laminar flow microfluidics for the selective capture of multiple cell types on-chip aiming for high throughput screening of various cell treatment compounds. Parallel laminar streams containing different cell types were perfused and captured on a cell adhesion protein-functionalized reaction area. Thereafter, parallel streams containing cell treatment solutions were delivered orthogonally over the captured cells. Multiple cell types and a range of cell treatment conditions could therefore be assessed in a single experiment...
January 11, 2017: Lab on a Chip
https://www.readbyqxmd.com/read/28074893/understanding-the-molecular-mechanism-for-the-differential-inhibitory-activities-of-compounds-against-mth1
#12
Mian Wang, Shuilian Zhou, Qing Chen, Lisheng Wang, Zhiqun Liang, Jianyi Wang
MTH1 can hydrolyze oxidized nucleotides and is required for cancer survival. The IC50 values were 0.8 nM for TH287 with a methyl substitution, 5.0 nM for TH588 with a cyclopropyl substitution, and 2.1 μM for TH650 with an oxetanyl substitution. Thus, it is very significant to understand inhibitory mechanisms of these structurally similar compounds against MTH1 and influences of the substituent on the bioactivities. Our MD researches indicate that TH287 maintains significant hydrogen bonds with Asn33 and Asp119, stabilizes the binding site, and induces MTH1 adopt a closed motion, leading to a high inhibitory activity...
January 11, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28074489/a-novel-nf-%C3%AE%C2%BAb-inhibitor-edasalonexent-cat-1004-in-development-as-a-disease-modifying-treatment-for-patients-with-duchenne-muscular-dystrophy-phase-1-safety-pharmacokinetics-and-pharmacodynamics-in-adult-subjects
#13
Joanne M Donovan, Michael Zimmer, Elliot Offman, Toni Grant, Michael Jirousek
In Duchenne muscular dystrophy (DMD), NF-κB is activated in skeletal muscle from infancy regardless of the underlying dystrophin mutation and drives inflammation and muscle degeneration while inhibiting muscle regeneration. Edasalonexent (CAT-1004) is a bifunctional orally administered small molecule that covalently links 2 compounds known to inhibit NF-κB, salicylic acid and docosahexaenoic acid (DHA). Edasalonexent is designed to inhibit activated NF-κB upon intracellular cleavage to these bioactive components...
January 11, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28074433/partial-contribution-of-rho-kinase-inhibition-to-the-bioactivity-of-ganoderma-lingzhi-and-its-isolated-compounds-insights-on-discovery-of-natural-rho-kinase-inhibitors
#14
Yhiya Amen, Qinchang Zhu, Hai-Bang Tran, Mohamed S Afifi, Ahmed F Halim, Ahmed Ashour, Kuniyoshi Shimizu
Recent studies identified Rho-kinase enzymes (ROCK-I and ROCK-II) as important targets that are involved in a variety of diseases. Synthetic Rho-kinase inhibitors have emerged as potential therapeutic agents to treat disorders such as hypertension, stroke, cancer, diabetes, glaucoma, etc. Our study is the first to screen the total ethanol extract of the medicinal mushroom Ganoderma lingzhi with thirty-five compounds for Rho-kinase inhibitory activity. Moreover, a molecular binding experiment was designed to investigate the binding affinity of the compounds at the active sites of Rho-kinase enzymes...
January 10, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28073678/natural-potential-neuroinflammatory-inhibitors-from-alhagi-sparsifolia-shap
#15
Di Zhou, Hongyan Wei, Zhe Jiang, Xuezheng Li, Kun Jiao, Xiaoguang Jia, Yue Hou, Ning Li
Neuroinflammation is a key contributor to neuronal damage in neurodegenerative diseases. In our previous work on natural effective neuroinflammatory inhibitors, Alhagi sparsifolia Shap. (Leguminosae), a folk medicine widely distributed in Xinjiang, attracted our attention because of its significant anti-neuroinflammatory effect. Therefore, further investigation of the bioactive material basis was carried out. As a result, 33 major components were characterized and identified by chromatographic and spectral methods, respectively...
December 30, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28073559/characterization-of-total-retinoid-like-activity-of-compounds-produced-by-three-common-phytoplankton-species
#16
Eliška Sychrová, Jana Priebojová, Marie Smutná, Kateřina Nováková, Jiří Kohoutek, Klára Hilscherová
Phytoplankton can produce various bioactive metabolites, which may affect other organisms in the aquatic environment. This study provides the first information on the total retinoid-like activity associated with both intracellular and extracellular metabolites produced by selected phytoplankton species that could play a role in teratogenic effects and developmental disruption in exposed organisms. The studied species included a coccoid cyanobacteria (Microcystis aeruginosa), a filamentous cyanobacteria (Aphanizomenon gracile) and a green alga (Desmodesmus quadricauda), all of which commonly occur in freshwater bodies in Europe...
December 2016: Harmful Algae
https://www.readbyqxmd.com/read/28073550/growth-and-bioactive-secondary-metabolites-of-arctic-protoceratium-reticulatum-dinophyceae
#17
Manuel Sala-Pérez, Tilman J Alpermann, Bernd Krock, Urban Tillmann
Harmful algal blooms are mainly caused by marine dinoflagellates and are known to produce potent toxins that may affect the ecosystem, human activities and health. Such events have increased in frequency and intensity worldwide in the past decades. Numerous processes involved in Global Change are amplified in the Arctic, but little is known about species specific responses of arctic dinoflagellates. The aim of this work was to perform an exhaustive morphological, phylogenetical and toxinological characterization of Greenland Protoceratium reticulatum and, in addition, to test the effect of temperature on growth and production of bioactive secondary metabolites...
May 2016: Harmful Algae
https://www.readbyqxmd.com/read/28073538/margalef-revisited-a-new-phytoplankton-mandala-incorporating-twelve-dimensions-including-nutritional-physiology
#18
Patricia M Glibert
Building on the classic depiction of the progression from a diatom to a dinoflagellate bloom as a function of nutrients and turbulence, known as the "Margalef mandala", a new conceptual model or mandala is presented here. The new mandala maps twelve response or effects traits, or environmental characteristics, related to different phytoplankton functional types: (1) relative preference for chemically reduced vs chemically oxidized forms of nitrogen; (2) relative availability of inorganic nitrogen and phosphorus; (3) adaptation to high vs low light and the tendency to be autotrophic vs mixotrophic; (4) cell motility; (5) environmental turbulence; (6) pigmentation quality; (7) temperature; (8) cell size; (9) relative growth rate; (10) relative production of bioactive compounds such as toxins or reactive oxygen species (ROS); (11) r vs K strategy; and (12) fate of the production in terms of grazing...
May 2016: Harmful Algae
https://www.readbyqxmd.com/read/28072544/why-can-unnatural-electron-acceptors-protect-photosynthesizing-organisms-but-kill-the-others
#19
Stanislav Anatolievich Pshenichnyuk, Alexei S Komolov
The polychlorinated compounds captafol (CPL) and 2,6-dichloroisonicotinic acid (INI) are able to protect plants acting as a fungicide or an inductor of plant resistance, respectively. At the same time, CPL and INI are dangerous for the respiratory organisms, i.e. mammalians, bacteria and fungi. The high electron-withdrawing ability of these compounds enables them to serve as unnatural electron acceptors in the cellular ambient near to electron transport pathways located in the thylakoid membrane of chloroplasts or in the mitochondrial respiratory chain...
January 10, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28071740/elucidating-the-modes-of-action-for-bioactive-compounds-in-a-cell-specific-manner-by-large-scale-chemically-induced-transcriptomics
#20
Michio Iwata, Ryusuke Sawada, Hiroaki Iwata, Masaaki Kotera, Yoshihiro Yamanishi
The identification of the modes of action of bioactive compounds is a major challenge in chemical systems biology of diseases. Genome-wide expression profiling of transcriptional responses to compound treatment for human cell lines is a promising unbiased approach for the mode-of-action analysis. Here we developed a novel approach to elucidate the modes of action of bioactive compounds in a cell-specific manner using large-scale chemically-induced transcriptome data acquired from the Library of Integrated Network-based Cellular Signatures (LINCS), and analyzed 16,268 compounds and 68 human cell lines...
January 10, 2017: Scientific Reports
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