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Bao-Jun Zhang, Wen-Wei Fu, Rong Wu, Jin-Ling Yang, Cai-Yun Yao, Bing-Xiong Yan, Hong-Sheng Tan, Chang-Wu Zheng, Zhi-Jun Song, Hong-Xi Xu
Six new prenylated xanthones (1: -6: ) and seventeen known xanthones were isolated from extracts of Garcinia bracteata leaves. Their structures were determined by extensive NMR and MS spectroscopic data analysis. The inhibitory activities of the isolates were assayed on HeLa, A549, PC-3, HT-29, and WPMY-1 cell lines. Compounds 1: and 15: -17: showed moderate inhibitory effects on tumor cell growth, with IC50 s ranging from 3.7 to 14.7 µM.
January 16, 2019: Planta Medica
Abraham Giacoman-Martínez, Francisco J Alarcón-Aguilar, Alejandro Zamilpa, Sergio Hidalgo-Figueroa, Gabriel Navarrete-Vázquez, Rebeca García-Macedo, Rubén Román-Ramos, Julio C Almanza-Pérez
Hibiscus sabdariffa is a medicinal plant consumed as a diuretic and anti-obesity remedy. Several pharmacological studies have shown its beneficial effects in metabolism. Peroxisome proliferator-activated receptors δ and γ may play a role in the actions of H. sabdariffa. These nuclear receptors regulate lipid and glucose metabolism and are therapeutic targets for type 2 diabetes. This research aimed to perform a phytochemical study guided by a bioassay from H. sabdariffa to identify compounds with peroxisome proliferator-activated receptor δ and peroxisome proliferator-activated receptor γ agonist activity, supported by messenger ribonucleic acid expression, molecular docking, lipid accumulation, and an antihyperglycemic effect...
January 16, 2019: Planta Medica
Yahui Lan, Heng Pan, Cheng Li, Kelly M Banks, Jessica Sam, Bo Ding, Olivier Elemento, Mary G Goll, Todd Evans
Ten-eleven translocation (Tet) enzymes (Tet1/2/3) mediate 5-methylcytosine (5mC) hydroxylation, which can facilitate DNA demethylation and thereby impact gene expression. Studied mostly for how mutant isoforms impact cancer, the normal roles for Tet enzymes during organogenesis are largely unknown. By analyzing compound mutant zebrafish, we discovered a requirement for Tet2/3 activity in the embryonic heart for recruitment of epicardial progenitors, associated with development of the atrial-ventricular canal (AVC)...
January 15, 2019: Cell Reports
Patrick S Fier, Kevin M Maloney
Herein we describe the development and application of a method for the mild, late-stage conversion of primary sulfonamides to several other other functional groups. These reactions occur via initial reductive deamination of sulfonamides to sulfinates via an NHC-catalyzed reaction of transiently formed N-sulfonylimines. The method described here is tolerant of nearly all common functional groups, as exemplified by the late-stage derivatization of several complex pharmaceutical compounds. Based on the prevalence of sulfonamide-containing drugs and building blocks, we have developed a method to enable sulfonamides to be applied as versatile synthetic handles for synthetic chemsitry...
January 16, 2019: Journal of the American Chemical Society
Andi Leubitz, Anat Frydman-Marom, Neal Sharpe, John van Duzer, Kathleen C M Campbell, Frédéric Vanhoutte
ELX-02 is an investigational synthetic eukaryotic ribosome-selective glycoside optimized as a translational read-through molecule that induces read through of nonsense mutations, resulting in normally localized full-length functional proteins. ELX-02 is being developed as a therapy for genetic diseases caused by nonsense mutations. Two phase 1a, randomized, double-blind placebo-controlled, single-ascending-dose studies were conducted in healthy human subjects to evaluate the safety and pharmacokinetics of ELX-02...
January 16, 2019: Clinical Pharmacology in Drug Development
Carlos Aydillo, Nuria Mazo, Claudio D Navo, Gonzalo Jiménez-Osés
For the first time, a simple methodology for the chemical synthesis and utilization of highly reactive 4-methylen-oxazol-5(4H)-ones from serine is presented. These dehydroalanine derivatives, which resemble the natural 4-methylideneimidazole-5-one (MIO) cofactor present in lyases and aminomutases, undergo rapid reaction with carbon nucleophiles such as silyl enol ethers, and cycloaddition reactions with diazo compounds and reactive dienes under very mild conditions and in the absence of metal catalysts and ring-strain activation, offering potential for bioconjugation...
January 16, 2019: Chembiochem: a European Journal of Chemical Biology
Yuan-Bo Tong, Zheng-Fang Tian, Hai-Bao Duan, Zhong-Peng Zhu, Tian-Yu Hong, Shun-Ping Zhao, Jing-Kui Yang
A cyclen-based hybrid supermolecule crystal, [(FeCl2)(cyclen)]Cl (1), where cyclen=1,4,7,10-Tetraazacyclododecane, was prepared using a liquid-liquid diffusion approach. The variable crystal structures exhibit that compound 1 belongs to orthorhombic crystal system, Pna21 space group (point group C2V) in the temperature range of 150-400 K. This hybrid supermolecule shows a dielectric relaxation behavior around the room temperature, and the ferroelectric nature of 1 has been directly verified by hysteresis measurements...
January 16, 2019: Chemistry, An Asian Journal
Ryota Chijimatsu, Fumiko Yano, Taku Saito, Masato Kobayashi, Shuichi Hamamoto, Takashi Kaito, Junichi Kushioka, David A Hart, Ung-Il Chung, Sakae Tanaka, Hideki Yoshikawa, Norimasa Nakamura
As an alternative to chondrocytes-based cartilage repair, stem cell-based therapies have been investigated. Specifically, human synovium-derived stem cells (hSSCs) are a promising cell source based on their highly capacities for chondrogenesis, but some methodological improvements are still required towards optimal cartilage regeneration. Recently, a small compound, TD-198946, was reported to promote chondrogenesis of several stem cells, but the effect on hSSCs is still unknown. This study aimed to examine the effects of TD-198946 on chondrocyte differentiation and cartilaginous tissue formation with hSSCs...
January 16, 2019: Journal of Tissue Engineering and Regenerative Medicine
Volodymyr Gvozdetskyi, Michael P Hanrahan, Raquel A Ribeiro, Tae-Hoon Kim, Lin Zhou, Aaron J Rossini, Paul C Canfield, Julia V Zaikina
Ternary lithium nickel borides LiNi3B1.8 and Li2.8Ni16B8 have been synthesized by using reactive LiH as a precursor. This synthetic route allows for the better mixing of the precursor powders, thus facilitating fast preparation of the alkali metal containing ternary borides. This method is suitable for "fast screening" of multicomponent systems comprised of elements with drastically different reactivities. Crystal structures of the compounds LiNi3B1.8 and Li2.8Ni16B8 were reinvestigated by combination of X-ray single crystal/synchrotron powder diffraction data, solid state 7Li and 11B NMR, and scanning transmission electron microscopy which allow determination of fine structural details including split position of Ni sites and ordering of B vacancies...
January 16, 2019: Chemistry: a European Journal
Felix Schroeter, Johannes Soellner, Thomas Strassner
We present a new class of tunable aryl alkyl ionic liquids (TAAILs) containing different palladate counter ions. Solid-state structures for representative compounds have been obtained. Their properties are presented in comparison to those of newly synthesized and reported palladate ionic liquids with conventional counter ions. It was found that the aryl substitution pattern and the type of anion have a profound influence on the melting point. The speciation of the different anions in solution has been rationalized by DFT calculations...
January 16, 2019: Chemistry: a European Journal
Dorota Latek, Ewelina Rutkowska, Szymon Niewieczerzal, Judyta Cielecka-Piontek
A disturbance of glucose homeostasis leading to type 2 diabetes mellitus (T2DM) is one of the severe side effects that may occur during a prolonged use of many drugs currently available on the market. In this manuscript we describe the most common cases of drug-induced T2DM, discuss available pharmacotherapies and propose new ones. Among various pharmacotherapies of T2DM, incretin therapies have recently focused attention due to the newly determined crystal structure of incretin hormone receptor GLP1R. Incretin hormone receptors: GLP1R and GIPR together with the glucagon receptor GCGR regulate food intake and insulin and glucose secretion...
2019: PloS One
Juliane Ollinger, Anuradha Kumar, David M Roberts, Mai A Bailey, Allen Casey, Tanya Parish
Tuberculosis is a disease of global importance for which novel drugs are urgently required. We developed a whole-cell phenotypic screen which can be used to identify inhibitors of Mycobacterium tuberculosis growth. We used recombinant strains of virulent M. tuberculosis which express far-red fluorescent reporters and used fluorescence to monitor growth in vitro. We optimized our high throughput assays using both 96-well and 384-well plates; both formats gave assays which met stringent reproducibility and robustness tests...
2019: PloS One
Nesrin Özsaraç, Nuray Kolsarici, Eda Demirok Soncu, Güliz Haskaraca
This study was designed to determine the formation of heterocyclic aromatic amines (HCAs) in two different types of doner kebab (yaprak doner-YD or mix doner-MD) cooked with different cooking methods (gas or electric) at varying degrees of doneness (rare, medium, well-done). In doner samples, nine common HCAs (IQ, IQx, MeIQ, MeIQx, PhIP, 4,8-DiMeIQx, 7,8-DiMeIQx, AαC, MeAαC) were detected. Additionally, the changes in the HCA precursors were evaluated. The initial concentration of precursors gradually decreased with the increase in doneness degree due to degradation or possible contribution in the Maillard reaction to form HCA compounds as a result of heat treatment (p < 0...
January 16, 2019: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
Nirmish Singla, Rashed A Ghandour, Ganesh V Raj
The treatment and management of prostate cancer continues to evolve; newer classes of agents and combination therapies are being developed and some are being investigated in early phase clinical trials. Areas covered: We discuss investigational hormonal agents for the treatment of prostate cancer and focus primarily on luteinizing hormone releasing hormone (LHRH) agonists in early stage trials. We look at agents that target the hormonal axis, including anti-androgens, gonadotropins, estrogenic agents and progestogenic agents and other non-hormonal agents often used in combination with LHRH agonists...
January 16, 2019: Expert Opinion on Investigational Drugs
Elham Assadpour, Seid Mahdi Jafari
Many natural food bioactive ingredients are sensitive to processing and environmental conditions and thus it is necessary to improve their stability to create products with long shelf lives. Encapsulation by spray drying is a widely used economical strategy to tackle this issue, and many scientists and manufacturers are using it in their research, development, and production activities. In this review, the spray-drying process is described, as are recent trends in the encapsulation of fish oils, essential fatty acids, probiotics, phenolic compounds, and natural food colorants...
January 16, 2019: Annual Review of Food Science and Technology
Daniel J Clemens, David J Tester, John R Giudicessi, J Martijn Bos, Ram K Rohatgi, Dominic J Abrams, Seshadri Balaji, Lia Crotti, Julien Faure, Carlo Napolitano, Silvia G Priori, Vincent Probst, Caroline Rooryck-Thambo, Nathalie Roux-Buisson, Frederic Sacher, Peter J Schwartz, Michael J Silka, Mark A Walsh, Michael J Ackerman
BACKGROUND: Triadin knockout syndrome (TKOS) is a rare, inherited arrhythmia syndrome caused by recessive null mutations in TRDN-encoded cardiac triadin. Based previously on five TRDN null patients, TKOS has been characterized by extensive T-wave inversions, transient QT prolongation, and severe disease expression of exercise-induced cardiac arrest in early childhood refractory to conventional therapy. METHODS: We have established the International Triadin Knockout Syndrome Registry (ITKOSR) to include patients who have genetically proven homozygous/compound heterozygous TRDN null mutations...
January 16, 2019: Circulation. Genomic and precision medicine
Albert Th Thorhallsson, Ragnar Bjornsson
Molybdenum-dependent nitrogenase is the most active biological catalyst for dinitrogen reduction. This reaction is catalyzed by a [MoFe7 S9 C] cofactor (FeMoco). FeMoco can be described as a double-cubane, with [MoFe3 S3 ] and [Fe4 S3 ] parts, bound via an interstitial carbide and three bridging sulfides. Model compounds have been synthesized since early studies of the enzyme and Coucouvanis and co-workers demonstrated that [MoFe3 S4 ] cubanes are active catalysts for many substrates catalyzed by nitrogenase...
January 16, 2019: Inorganic Chemistry
Eun-Jung Park, Mayuramas Sang-Ngern, Leng Chee Chang, John M Pezzuto
In previous studies, withanolides isolated from Physalis peruviana were found to exhibit anti-inflammatory potential by suppressing nitrite production induced by lipopolysaccharide (LPS) treatment. Currently, we selected two of the most potent compounds, 4β-hydroxywithanolide E (1) and physalactone (2), to examine the underlying mechanism of action. With LPS-stimulated RAW 264.7 cells in culture, the compounds inhibited the mRNA and protein expression of iNOS and COX-2. To determine which upstream signaling proteins were involved in these effects, phosphorylation levels of three mitogen-activated protein kinases (MAPKs) including ERK1/2, JNK1/2, and p38, were examined, but found unaffected...
January 16, 2019: Journal of Natural Products
Juan Wei, Jiandong Wu, Yang Tang, Mark E Ridgeway, Melvin A Park, Catherine E Costello, Joseph Zaia, Cheng Lin
Glycosaminoglycans (GAGs) play vital roles in many biological processes, and are naturally present as complex mixtures of poly-saccharides with tremendous structural heterogeneity, including many structural isomers. Mass spectrometric analysis of GAG isomers, in particular highly sulfated heparin (Hep) and heparan sulfate (HS), is challenging because of their structural similarity and facile sulfo losses during analysis. Herein, we show that highly sulfated Hep/HS isomers may be resolved by gated-trapped ion mobility spectrometry (gated-TIMS) with negligible sulfo losses...
January 16, 2019: Analytical Chemistry
Dmitry A Grishanov, Andrei V Churakov, Alexander G Medvedev, Alexey A Mikhaylov, Ovadia Lev, Petr V Prikhodchenko
High, nearly 100%, yield synthesis of ammonium peroxogermanate (APG), (NH4 )6 [Ge6 (μ-OO)6 (μ-O)6 (OH)6 ]·6H2 O, is presented, and its crystal structure is determined by single crystal X-ray study. It comprises centrosymmetric hexanuclear peroxogermanate anions [Ge6 (μ-OO)6 (μ-O)6 (OH)6 ]6- with six μ-oxo- and six μ-peroxo groups forming negatively charged layers. The space between these layers is filled by ammonium cations and water molecules, forming a highly stable structure due to hydrogen bonding...
January 16, 2019: Inorganic Chemistry
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