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https://www.readbyqxmd.com/read/28945033/-preparation-and-evaluation-of-gastric-adhesive-floating-pellets-for-bolo-leaf-phenols
#1
Ya-Li He, Ying Li, Dan-Dan Yang, Chun-Yan Zhu
Gastric adhesive-floating pellets for Bolo leaf phenols (BLP) were prepared by extrusion-spheronization method, with chitosan as skeleton bioadhesive material, and stearyl alcohol as help-bleaching agent to evaluate its in vitro adhesivity, floatability and in vivo retention situation, and investigate its in vitro release characteristics. The in vitro adhesivity and floatability were evaluated respectively by in vitro tissue retention method and visual observation method. The retention of pellets in rats was investigated by in vivo tissue retention method and in vivo imaging of small animals...
January 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28944086/development-of-spinal-deformities-in-the-tight-skin-mouse
#2
Bing Li, Jill Pg Urban, Jing Yu
Tight-skin (TSK) mice are commonly used as an animal model to study the pathogenesis of Marfan syndrome (MFS), but little is known of their skeletal phenotype and in particular of the development of the spinal deformities, common in MFS. Here we examined growth of the axial skeletons of TSK and wild-type(B6) mice during their period of rapid growth. The whole bodies of mice, 4-12 weeks of age, were scanned after sacrifice, by micro-computed tomography (microCT). We reconstructed three-dimensional models of the spine and ribs, and measured vertebral body heights and rib lengths using the Mac-based image-processing software "OsiriX"...
2017: Bone Research
https://www.readbyqxmd.com/read/28942966/haploinsufficiency-of-the-chromatin-remodeler-bptf-causes-syndromic-developmental-and-speech-delay-postnatal-microcephaly-and-dysmorphic-features
#3
Paweł Stankiewicz, Tahir N Khan, Przemyslaw Szafranski, Leah Slattery, Haley Streff, Francesco Vetrini, Jonathan A Bernstein, Chester W Brown, Jill A Rosenfeld, Surya Rednam, Sarah Scollon, Katie L Bergstrom, Donald W Parsons, Sharon E Plon, Marta W Vieira, Caio R D C Quaio, Wagner A R Baratela, Johanna C Acosta Guio, Ruth Armstrong, Sarju G Mehta, Patrick Rump, Rolph Pfundt, Raymond Lewandowski, Erica M Fernandes, Deepali N Shinde, Sha Tang, Juliane Hoyer, Christiane Zweier, André Reis, Carlos A Bacino, Rui Xiao, Amy M Breman, Janice L Smith, Nicholas Katsanis, Bret Bostwick, Bernt Popp, Erica E Davis, Yaping Yang
Bromodomain PHD finger transcription factor (BPTF) is the largest subunit of nucleosome remodeling factor (NURF), a member of the ISWI chromatin-remodeling complex. However, the clinical consequences of disruption of this complex remain largely uncharacterized. BPTF is required for anterior-posterior axis formation of the mouse embryo and was shown to promote posterior neuroectodermal fate by enhancing Smad2-activated wnt8 expression in zebrafish. Here, we report eight loss-of-function and two missense variants (eight de novo and two of unknown origin) in BPTF on 17q24...
September 19, 2017: American Journal of Human Genetics
https://www.readbyqxmd.com/read/28942679/highly-oxygenated-antioxidative-2h-chromen-derivative-from-the-red-seaweed-gracilaria-opuntia-with-pro-inflammatory-cyclooxygenase-and-lipoxygenase-inhibitory-properties
#4
Fasina Makkar, Kajal Chakraborty
Phytochemical investigation of the thalli of ethyl acetate-methanol extract of the red seaweed Gracilaria opuntia led to isolation of a substituted 2H-chromen derivative of unusual structure possessing highly oxygenated carbon skeleton, characterised as 2-acetoxy-2-(5-acetoxy-4-methyl-2-oxotetrahydro-2H-pyran-4-yl)ethyl 4-(3-methoxy-2-(methoxymethyl)-7-methyl-3,4,4a,7,8,8a-hexahydro-2H-chromen-4-yloxy)-5-methylheptanoate, which have not been reported in nature. The chemical structure was resolved by detailed spectroscopic analysis...
September 25, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28942113/novel-serms-based-on-3-aryl-4-aryloxy-2h-chromen-2-one-skeleton-a-possible-way-to-dual-er%C3%AE-vegfr-2-ligands-for-treatment-of-breast-cancer
#5
Guoshun Luo, Xinyu Li, Guoqing Zhang, Chengzhe Wu, Zhengpu Tang, Linyi Liu, Qidong You, Hua Xiang
There is considerable interest in developing new SERMs as multifunctional agents in women's health. Development of dual selective estrogen receptor modulators/VEGFR-2 inhibitors (SERMs/V-2I) has been an attractive strategy for the discovery of new breast cancer therapeutic agents. Our previous efforts led to the preparation of a series of 3-aryl-4-anilino-2H-chromen-2-ones endowed with potent estrogen receptor binding affinity and anti-proliferative efficacy. In this study, various structurally related 3-aryl-4-anilino/aryloxy-2H-chromen-2-one analogues were rationally designed, synthesized and evaluated as a new chemo-type of dual ERα and VEGFR-2 inhibitors...
September 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28941059/gold-i-catalyzed-synthesis-of-indenes-and-cyclopentadienes-access-to-%C3%A2-laurokamurene-b-and-the-skeletons-of-cycloaurenones-and-dysiherbols
#6
Antonio M Echavarren, Xiang Yin, Mauro Mato
The formal (3 + 2) cycloaddition between terminal allenes with aryl or styryl gold(I) carbenes generated by retro-Buchner reaction of 7-substituted 1,3,5-cycloheptatrienes leads to indenes and cyclopentadienes, respectively. These cycloadditions have been applied to the construction of the carbon skeleton of the cycloaurenones and the dysiherbols as well as to the total synthesis of ()-laurokamurene B.
September 20, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28940131/nitrogen-nutrition-in-cotton-and-control-strategies-for-greenhouse-gas-emissions-a-review
#7
Aziz Khan, Daniel Kean Yuen Tan, Fazal Munsif, Muhammad Zahir Afridi, Farooq Shah, Fan Wei, Shah Fahad, Ruiyang Zhou
Cotton (Gossypium hirustum L.) is grown globally as a major source of natural fiber. Nitrogen (N) management is cumbersome in cotton production systems; it has more impacts on yield, maturity, and lint quality of a cotton crop than other primary plant nutrient. Application and production of N fertilizers consume large amounts of energy, and excess application can cause environmental concerns, i.e., nitrate in ground water, and the production of nitrous oxide a highly potent greenhouse gas (GHG) to the atmosphere, which is a global concern...
September 22, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28939863/total-synthesis-of-avenaol
#8
Motohiro Yasui, Rina Ota, Chihiro Tsukano, Yoshiji Takemoto
Avenaol, isolated from the allelopathic plant black oat, was the first C20 germination stimulant related to strigolactones. Structurally, it consisted of a bicyclo[4.1.0]heptanone skeleton containing a cyclopropane ring bearing three main chains projecting in the same direction (i.e. all-cis-substituted cyclopropane). Herein, we report the total synthesis of avenaol using a robust strategy involving the formation of an all-cis-substituted cyclopropane via an alkylidenecyclopropane. The key factors in the success of this total synthesis include the Rh-catalysed intramolecular cyclopropanation of an allene, an Ir-catalysed stereoselective double-bond isomerisation, and the differentiation of two hydroxymethyl groups via the regioselective formation and oxidation of a tetrahydropyran based on the reactivity of a cyclopropyl group...
September 22, 2017: Nature Communications
https://www.readbyqxmd.com/read/28939560/plastic-responses-of-bryozoans-to-ocean-acidification
#9
Daniel S Swezey, Jessica R Bean, Tessa M Hill, Brian Gaylord, Aaron T Ninokawa, Eric Sanford
Phenotypic plasticity has the potential to allow organisms to respond rapidly to global environmental change, but the range and effectiveness of these responses are poorly understood across taxa and growth strategies. Colonial organisms might be particularly resilient to environmental stressors, as organizational modularity and successive asexual generations can allow for distinctively flexible responses in the aggregate form. We performed laboratory experiments to examine the effects of increasing dissolved carbon dioxide (i...
September 22, 2017: Journal of Experimental Biology
https://www.readbyqxmd.com/read/28938619/anti-cancer-efficacy-of-biotinylated-chitosan-nanoparticles-in-liver-cancer
#10
Mingrong Cheng, Weiping Zhu, Qing Li, Dejian Dai, Yiming Hou
The present study investigated the synthesis of biotinylated chitosan (Bio-CS) from chitosan using a nanomaterial skeleton with biotin and the successful targeting of the formulation in liver cancer cells. Bio-CS was validated by fourier transformed infrared spectroscopy and hydrogen(-1) nuclear magnetic resonance spectroscopy. Bio-CS and plasmid DNA were used to construct Bio-CS/plasmid DNA nanoparticles according to the optimal molar ratio of 1:1 and the optimal pH-value of 5.5. Under these conditions, the parameters mean particle size, potential, encapsulation rate and drug loading, were 82...
August 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28938315/proteus-syndrome-with-a-cranial-intraosseous-lipoma
#11
Erik M Wolfswinkel, Thomas A Imahiyerobo, J Gordon McComb, Pedro A Sanchez-Lara, Mark M Urata
Intraosseous lipomas are almost exclusively seen in the long bones. Presence in the craniofacial skeleton is extremely rare. A 7-year-old male is presented with a marked craniofacial deformation from a bony tumor containing an intraosseous lipoma. This finding established a clinical diagnosis of Proteus syndrome. Given the size of the tumor, producing an extensive deformity, three-dimensional modeling was used to generate a three-dimensional printed implant. The process to achieve a successful outcome is herein described...
September 21, 2017: Journal of Craniofacial Surgery
https://www.readbyqxmd.com/read/28938189/the-potent-suppressive-effect-of-%C3%AE-d-mannuronic-acid-m2000-on-molecular-expression-of-the-tlr-nf-kb-signaling-pathway-in-ankylosing-spondylitis-patients
#12
Maryam Roozbehkia, Mahdi Mahmoudi, Somaye Aletaha, Nima Rezaei, Mohammad Javad Fattahi, Fahimeh Jafarnezhad-Ansariha, Anis Barati, Abbas Mirshafiey
Ankylosing spondylitis (AS) is a chronic inflammatory rheumatic disease characterized by the inflammation of sacroiliac joints and axial skeleton. A combination of genetic, environmental and immunological factors are involved in AS's pathogenesis. TLRs are type I transmembrane glycoproteins that play a crucial role in the innate immune responses against invading pathogens. Observational studies have demonstrated a possible association between TLR dysregulation and AS. The β-d-mannuronic acid (M2000), as a novel NSAID with immunosuppressive property, has shown an inhibitory effect on Toll-like receptor (TLR) 2, 4 signaling in HEK293 cells...
September 19, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28936605/sex-determination-of-a-tunisian-population-by-ct-scan-analysis-of-the-skull
#13
Malek Zaafrane, Mehdi Ben Khelil, Ines Naccache, Ekbel Ezzedine, Frédéric Savall, Norbert Telmon, Najla Mnif, Moncef Hamdoun
It is widely accepted that the estimation of biological attributes in the human skeleton is more accurate when population-specific standards are applied. With the shortage of such data for contemporary North African populations, it is duly required to establish population-specific standards. We present here the first craniometric standards for sex determination of a contemporary Tunisian population. The aim of this study was to analyze the correlation between sex and metric parameters of the skull in this population using CT scan analysis and to generate proper reliable standards for sex determination of a complete or fragmented skull...
September 21, 2017: International Journal of Legal Medicine
https://www.readbyqxmd.com/read/28935804/the-growth-pattern-of-neandertals-reconstructed-from-a-juvenile-skeleton-from-el-sidr%C3%A3-n-spain
#14
Antonio Rosas, Luis Ríos, Almudena Estalrrich, Helen Liversidge, Antonio García-Tabernero, Rosa Huguet, Hugo Cardoso, Markus Bastir, Carles Lalueza-Fox, Marco de la Rasilla, Christopher Dean
Ontogenetic studies help us understand the processes of evolutionary change. Previous studies on Neandertals have focused mainly on dental development and inferred an accelerated pace of general growth. We report on a juvenile partial skeleton (El Sidrón J1) preserving cranio-dental and postcranial remains. We used dental histology to estimate the age at death to be 7.7 years. Maturation of most elements fell within the expected range of modern humans at this age. The exceptions were the atlas and mid-thoracic vertebrae, which remained at the 5- to 6-year stage of development...
September 22, 2017: Science
https://www.readbyqxmd.com/read/28934646/clerodane-diterpenoids-from-scutellaria-formosana-with-inhibitory-effects-on-no-production-and-interactions-with-inos-protein
#15
Peixia Wang, Feng Liu, Xueyuan Yang, Yue Liang, Shen Li, Guochen Su, Da-Qing Jin, Yasushi Ohizumi, Jing Xu, Yuanqiang Guo
A phytochemical study on Scutellaria formosana afforded five previously undescribed spiro-diterpenoids, scutellapenes A-E. The structures were elucidated on the basis of extensive 1D and 2D NMR spectroscopic data analysis, and the absolute configurations of these compounds were established by the time-dependent density functional theory (TDDFT) electronic circular dichroism (ECD) calculations. Scutellapenes B-E possess a spiro-diterpenoid skeleton. All of the compounds showed inhibitory effects on LPS-induced nitric oxide (NO) production in murine microglial BV-2 cells...
September 18, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28934336/the-oldest-record-of-aquatic-amniote-congenital-scoliosis
#16
Tomasz Szczygielski, Dawid Surmik, Agnieszka Kapuścińska, Bruce M Rothschild
We report the first occurrence of congenital scoliosis in an early Permian aquatic parareptile, Stereosternum tumidum from Paraná state, Brazil. The spine malformation is caused by a congenital hemivertebra. These observations give insight into the biomechanical aspects of underwater locomotion in an axial skeleton-compromised aquatic amniote. This is the oldest record of a hemivertebra in an aquatic animal.
2017: PloS One
https://www.readbyqxmd.com/read/28933833/total-synthesis-of-nahuoic-acid-ci-bii
#17
Qi Liu, Yifan Deng, Amos B Smith
A convergent total synthesis of (-)-nahuoic acid Ci(Bii) (3), a novel cis-decalin polyketide, has been achieved. Key synthetic transformations include Type II Anion Relay Chemistry (ARC) to construct the polyol chain, a Ti-catalyzed asymmetric Diels-Alder reaction to generate the cis-decalin skeleton, and a late-stage large fragment union exploiting a Micalizio alkoxide-directed alkyne-alkene coupling tactic.
September 21, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28933746/evaluation-of-novel-dual-acetyl-and-butyrylcholinesterase-inhibitors-as-potential-anti-alzheimer-s-disease-agents-using-pharmacophore-3d-qsar-and-molecular-docking-approaches
#18
Xiaocong Pang, Hui Fu, Shilun Yang, Lin Wang, Ai-Lin Liu, Song Wu, Guan-Hua Du
DL0410, containing biphenyl and piperidine skeletons, was identified as an acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitor through high-throughput screening assays, and further studies affirmed its efficacy and safety for Alzheimer's disease treatment. In our study, a series of novel DL0410 derivatives were evaluated for inhibitory activities towards AChE and BuChE. Among these derivatives, compounds 6-1 and 7-6 showed stronger AChE and BuChE inhibitory activities than DL0410. Then, pharmacophore modeling and three-dimensional quantitative structure activity relationship (3D-QSAR) models were performed...
July 26, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28933557/low-damage-reductive-patterning-of-oxidized-alkyl-self-assembled-monolayers-through-vacuum-ultraviolet-light-irradiation-in-an-evacuated-environment
#19
Ahmed Ibrahim Abdelhamid Soliman, Yudi Tu, Toru Utsunomiya, Takashi Ichii, Hiroyuki Sugimura
Through 172 nm vacuum ultraviolet light irradiation in a high vacuum condition (HV-VUV), well-defined micropatterns with varied periodic friction were fabricated at the surface of self-assembled monolayers (SAMs) terminated by oxygenated groups. No apparent height contrast between HV-VUV-irradiated and masked areas was observed, which indicated the stability of C-C skeleton of the assembled molecules. The trimming of oxygenated groups occurred through dissociating the C-O bonds and promoting the occurrence of α- and β-cleavages in the C=O containing components...
September 21, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28933481/bowl-shaped-deformation-in-a-planar-aromatic-polycycle-upon-reduction-li-and-na-separated-dianions-of-the-aromatic-polycycle-5-6-11-12-di-o-phenylene-tetracene
#20
T Wombacher, R Goddard, C W Lehmann, J J Schneider
Herein we report the synthesis and crystal structures of three light alkali metal salts of the dianion of the polycyclic aromatic hydrocarbon 5,6:11,12-di-o-phenylenetetracene (LDOPT). The compounds are obtained by reaction of LDOPT with an excess of lithium or sodium metal in different O-donor solvents (DME, diglyme) and crystallize as naked, solvated-cation separated dianions exhibiting no interaction between the alkali metal ion and the aromatic π-system of LDOPT. Depending on the aprotic etheral solvent and the hardness of the alkaline metal agent a significant structural perturbation of the conjugated carbon framework of LDOPT is observed resulting in a bowl shaped curvature of the anionic π-perimeter, in contrast to its fully planar neutral state...
September 21, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
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