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Thomas Cavalier-Smith, Ema E Chao, Rhodri Lewis
Infrakingdom Rhizaria is one of four major subgroups with distinct cell body plans that comprise eukaryotic kingdom Chromista. Unlike other chromists, Rhizaria are mostly heterotrophic flagellates, amoebae or amoeboflagellates, commonly with reticulose (net-like) or filose (thread-like) feeding pseudopodia; uniquely for eukaryotes, cilia have proximal ciliary transition-zone hub-lattices. They comprise predominantly flagellate phylum Cercozoa and reticulopodial phylum Retaria, whose exact phylogenetic relationship has been uncertain...
April 17, 2018: Protoplasma
Ling Ni, Xiu-Hong Zhong, Xiao-Jiao Chen, Bing-Jie Zhang, Mei-Fen Bao, Xiang-Hai Cai
Twenty-eight naturally occurring Cephalotaxus tropone analogues, including 19 previously undescribed ones, were identified from Cephalotaxus fortunei Hook. var. alpina H. L. Li and C. lanceolata K. M. Feng. The presence of the C20 cephinoids A-E revealed that these tropones were assigned to the norditerpenoids and were perhaps derived from labdane-type diterpenoids. These norditerpenoids showed excellent cytotoxicity against human cancer cells (IC50 , 20-0.1 μM) in vitro. The SAR (structure-activity relationship) analysis disclosed that the tropone moiety and the lactone ring were crucial structural features for the observed activities...
April 14, 2018: Phytochemistry
Andrew Fox-Lewis, Junko Takata, Thyl Miliya, Yoel Lubell, Sona Soeng, Poda Sar, Kolthida Rith, Gregor McKellar, Vanaporn Wuthiekanun, Erin McGonagle, Nicole Stoesser, Catrin E Moore, Christopher M Parry, Claudia Turner, Nicholas P J Day, Ben S Cooper, Paul Turner
To determine trends, mortality rates, and costs of antimicrobial resistance in invasive bacterial infections in hospitalized children, we analyzed data from Angkor Hospital for Children, Siem Reap, Cambodia, for 2007-2016. A total of 39,050 cultures yielded 1,341 target pathogens. Resistance rates were high; 82% each of Escherichia coli and Klebsiella pneumoniae isolates were multidrug resistant. Hospital-acquired isolates were more often resistant than community-acquired isolates; resistance trends over time were heterogeneous...
May 2018: Emerging Infectious Diseases
Prayasee Baruah, Grace Basumatary, Semen O Yesylevskyy, Kripamoy Aguan, Ghanashyam Bez, Sivaprasad Mitra
The inhibitory efficacy of two substituted coumarin derivatives on the activity of neurodegenerative enzyme acetylcholinesterase (AChE) was assessed in aqueous buffer as well as in the presence of human serum albumin (HSA) and compared against standard cholinergic AD drug, Donepezil (DON). The experimental data revealed the inhibition to be of non-competitive type with both the systems showing substantial inhibitory activity on AChE. In fact, one of the tested compounds Chromenyl Coumarate (CC) was found to be better inhibitor (IC50 = 48...
April 17, 2018: Journal of Biomolecular Structure & Dynamics
Sara E Martin, Catherine M Nguyen, Randall J Basaraba, Christian Melander
Biofilm formation is one of the many mechanisms bacteria utilize to survive antibiotic treatment. It has been demonstrated that when Mycobacterium tuberculosis exists in a biofilm in vitro it expresses phenotypic resistance to antimicrobial drugs. Since the in vivo survival of M. tuberculosis following drug treatment is potentially linked to a biofilm-like expression of drug tolerance, it is hypothesized that biofilm dispersion should increase antibiotic susceptibility and reduce the duration of the current antibiotic treatment regimen...
April 16, 2018: Chemical Biology & Drug Design
Piotr F J Lipiński, Piotr Garnuszek, Michał Maurin, Raphael Stoll, Nils Metzler-Nolte, Artur Wodyński, Jan Cz Dobrowolski, Marta K Dudek, Monika Orzełowska, Renata Mikołajczak
BACKGROUND: The cholecystokinin receptor subtype 2 (CCK-2R) is an important target for diagnostic imaging and targeted radionuclide therapy (TRNT) due to its overexpression in certain cancers (e.g., medullary thyroid carcinoma (MTC)), thus matching with a theranostic principle. Several peptide conjugates suitable for the TRNT of MTC have been synthesized, including a very promising minigastrin analogue DOTA-(DGlu)6 -Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 (CP04). In this contribution, we wanted to see whether CP04 binding affinity for CCK-2R is sensitive to the type of the complexed radiometal, as well as to get insights into the structure of CP04-CCK2R complex by molecular modeling...
April 16, 2018: EJNMMI Research
Prateek Pathak, Parjanya Kumar Shukla, Vikas Kumar, Ankit Kumar, Amita Verma
A series of quinazoline clubbed 1,3,5-triazine derivatives (QCT) were synthesized and evaluated for their in vitro anticancer activity against HeLa (human cervical cancer), MCF-7 (human breast cancer cell), HL-60 (human promyelocytic leukemia cell), HepG2 (human Hepatocellular carcinoma cell), and one normal cell line HFF (human foreskin fibroblasts). In vitro assay result encouraged to further move towards in ovo anticancer evaluation using chick embryo. The series of QCT derivatives showed higher anticancer and antiangiogenic activity against HeLa and MCF-7 cell lines...
April 16, 2018: Inflammopharmacology
Nuria Galiana, Miguel Lurgi, Bernat Claramunt-López, Marie-Josée Fortin, Shawn Leroux, Kevin Cazelles, Dominique Gravel, José M Montoya
Species-area relationships (SARs) are pivotal to understand the distribution of biodiversity across spatial scales. We know little, however, about how the network of biotic interactions in which biodiversity is embedded changes with spatial extent. Here we develop a new theoretical framework that enables us to explore how different assembly mechanisms and theoretical models affect multiple properties of ecological networks across space. We present a number of testable predictions on network-area relationships (NARs) for multi-trophic communities...
April 16, 2018: Nature Ecology & Evolution
Guillaume Bacques, Marcello de Michele, Daniel Raucoules, Hideo Aochi, Frédérique Rolandone
This study focuses on the shallow deformation that occurred during the 5 years following the Parkfield earthquake (28/09/2004, Mw 6, San Andreas Fault, California). We use Synthetic Aperture Radar interferometry (InSAR) to provide precise measurements of transient deformations after the Parkfield earthquake between 2005 and 2010. We propose a method to combine both ERS2 and ENVISAT interferograms to increase the temporal data sampling. Firstly, we combine 5 years of available Synthetic Aperture Radar (SAR) acquisitions including both ERS-2 and Envisat...
April 16, 2018: Scientific Reports
Chengcheng Fei, Yanfei Chen, Zhiyan Jiang, Dingxin Jiang
Owing to thioether diverse physicochemical properties by non-covalent interactions with bio-macromolecules, thioether derivatives containing heterocyclic moiety are known for their interesting insecticidal bioactivities and attracting considerable attention as neuroactive insecticides. Here we synthesis a series of novel thioether bridged N-phenylpyrazole derivatives incorporating various (hetero)aromatic substituents into 4-position of the pyrazole ring. Structure-activity relationship (SAR) studies resulted in compounds 6d and 7d with the most potent insecticidal activity among the series containing various substituted benzene substituents (LC50  = 13...
April 12, 2018: Bioorganic & Medicinal Chemistry Letters
María José Ojeda-Montes, Aleix Gimeno, Sarah Tomas-Hernández, Adrià Cereto-Massagué, Raúl Beltrán-Debón, Cristina Valls, Miquel Mulero, Gerard Pujadas, Santiago Garcia-Vallvé
The inhibition of dipeptidyl peptidase-IV (DPP-IV) has emerged over the last decade as one of the most effective treatments for type 2 diabetes mellitus, and consequently (a) 11 DPP-IV inhibitors have been on the market since 2006 (three in 2015), and (b) 74 noncovalent complexes involving human DPP-IV and drug-like inhibitors are available at the Protein Data Bank (PDB). The present review aims to (a) explain the most important activity cliffs for DPP-IV noncovalent inhibition according to the binding site structure of DPP-IV, (b) explain the most important selectivity cliffs for DPP-IV noncovalent inhibition in comparison with other related enzymes (i...
April 16, 2018: Medicinal Research Reviews
Katrin Gruner, Tatyana Zeier, Christina Aretz, Jürgen Zeier
Members of the MILDEW RESISTANCE LOCUS O (MLO) gene family confer susceptibility to powdery mildews in different plant species, and their existence therefore seems to be disadvantageous for the plant. We recognized that expression of the Arabidopsis MLO2 gene is induced after inoculation with the bacterial pathogen Pseudomonas syringae, promoted by salicylic acid (SA) signaling, and systemically enhanced in the foliage of plants exhibiting systemic acquired resistance (SAR). Importantly, distinct mlo2 mutant lines were unable to systemically increase resistance to bacterial infection after inoculation with P...
April 16, 2018: Plant Journal: for Cell and Molecular Biology
Hao Zhu, Chunfa Wu, Jun Wang, Xumei Zhang
Stabilization technology is one of widely used remediation technologies for cadmium (Cd)-contaminated agricultural soils, but stabilized Cd in soil may be activated again when external conditions such as acid rain occurred. Therefore, it is necessary to study the effect of acid rain on the performance of different stabilizing agents on Cd-polluted agriculture soils. In this study, Cd-contaminated soils were treated with mono-calcium phosphate (MCP), mono-ammonium phosphate (MAP), and artificial zeolite (AZ) respectively and incubated 3 months...
April 16, 2018: Environmental Science and Pollution Research International
Jingru Liu, Ruxin Ma, Fangchao Bi, Fa Zhang, Chaoyu Hu, Henrietta Venter, Susan J Semple, Shutao Ma
A novel series of 5-methyl-2-phenylphenanthridium derivatives were displayed outstanding activity against a panel of antibiotic-sensitive and -resistant bacteria strains compared with their precursor sanguinarine, ciprofloxacin and oxacillin sodium. Compounds 7 l, 7m and 7n were found to display the most effective activity against five sensitive strains (0.06-2 μg/mL) and three resistant strains (0.25-4 μg/mL). The kinetic profiles indicated that compound 7l possessed the strongest bactericidal effect on S...
April 7, 2018: Bioorganic & Medicinal Chemistry Letters
Michael J Bennett, Yiqin Wu, Amogh Boloor, Jennifer Matuszkiewicz, Shawn M O'Connell, Lihong Shi, Ryan K Stansfield, Joselyn R Del Rosario, James M Veal, David J Hosfield, Jiangchun Xu, Stephen W Kaldor, Jeffrey A Stafford, Juan M Betancort
The bromodomain and extra-terminal (BET) family of epigenetic proteins has attracted considerable attention in drug discovery given its involvement in regulating gene transcription. Screening a focused small molecule library based on the bromodomain pharmacophore resulted in the identification of 2-methylisoquinoline-1-one as a novel BET bromodomain-binding motif. Structure guided SAR exploration resulted in >10,000-fold potency improvement for the BRD4-BD1 bromodomain. Lead compounds exhibited excellent potencies in both biochemical and cellular assays in MYC-dependent cell lines...
April 10, 2018: Bioorganic & Medicinal Chemistry Letters
John L Woodard, Andrew C Huntsman, Pratiq A Patel, Hee-Byung Chai, Ragu Kanagasabai, Soumendrakrishna Karmahapatra, Alexandria N Young, Yulin Ren, Malcolm S Cole, Denisse Herrera, Jack C Yalowich, A Douglas Kinghorn, Joanna E Burdette, James R Fuchs
A series of arylnaphthalene lignan lactones based on the structure of the phyllanthusmins, a class of potent natural products possessing diphyllin as the aglycone, has been synthesized and screened for activity against multiple cancer cell lines. SAR exploration was performed on both the carbohydrate and lactone moieties of this structural class. These studies have revealed the importance of functionalization of the carbohydrate hydroxy groups with both acetylated and methylated analogues showing increased potency relative to those with unsubstituted sugar moieties...
March 23, 2018: Bioorganic & Medicinal Chemistry
Martin Vogt
Activity landscapes (ALs) are representations and models of compound data sets annotated with a target-specific activity. In contrast to quantitative structure-activity relationship (QSAR) models, ALs aim at characterizing structure-activity relationships (SARs) on a large-scale level encompassing all active compounds for specific targets. The popularity of AL modeling has grown substantially with the public availability of large activity-annotated compound data sets. AL modeling crucially depends on molecular representations and similarity metrics used to assess structural similarity...
April 14, 2018: Expert Opinion on Drug Discovery
Maryam Saffari Aman, Mohammad Jafari, Majid Karimpour Reihan, Babak Motesharezadeh, Salman Zare
The main aim of this study is to investigate the physical and chemical properties, including soil salinity, acidity, concentrations of macro-nutrients (phosphorus, potassium, and Calcium-Magnesium) and sodium adsorption ratio to the soil, physiological and nutritional traits of three plant species including Caesalpinia gilliesii, Robinia pseudoacacia, and Cercis siliquastrum. First, some sample were taken from the agricultural soils irrigated with wastewater. The results of initial soil test revealed that the irrigation with wastewater significantly increased sodium adsorption ratio (SAR), electrical conductivity (ECe), cation exchange capacity (CEC) of the soil (p < 0...
April 12, 2018: Journal of Environmental Management
V Alagarsamy, K Chitra, G Saravanan, V Raja Solomon, M T Sulthana, B Narendhar
Most of the drugs and pharmacologically relevant molecules possess heterocyclic ring structures and presence of hetero atoms or groupings divulges privileged specificities in their pharmacological targets. Especially the heterocyclic systems, quinazoline is a biologically imperative scaffold known to be linked with several pharmacological activities. Some of the protuberant pharmacological responses attributed to this system are analgesic, anti-inflammatory, anti-convulsant, sedative-hypnotic, anti-histaminic, anti-hypertensive, anti-cancer, anti-microbial, anti-tubercular and anti-viral activities...
March 30, 2018: European Journal of Medicinal Chemistry
Long Yang, Yongchao Xu, Rui Zhang, Xiaotong Wang, Chao Yang
As a source of edible oil and protein, soybean is a major globally important economic crop; Improving its production has been an important objective of soybean breeding. Acid rain has been shown to influence soybean growth and productivity, with consequent adverse impacts on its production for use by human populations. In this study, RNA sequencing technology was utilized to examine changes in gene expression when soybean was exposed to simulated acid rain (SAR). We sampled soybean leaves at five time intervals (0, 6, 30, 54, 78, and 102 h), and built the cDNA library...
April 12, 2018: Ecotoxicology and Environmental Safety
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