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https://www.readbyqxmd.com/read/29031222/apolipoproteins-adsorption-and-brain-targeting-evaluation-of-baicalin-nanocrystals-modified-by-combination-of-tween80-and-tpgs
#1
Yang Liu, Yueqin Ma, Junnan Xu, Yingchong Chen, Jin Xie, Pengfei Yue, Qin Zheng, Ming Yang
To help baicalin pass across BBB and improve its targeting in brain, we designed a novel formulation strategy of baicalin nanocrystals that preferentially adsorbing apolipoprotein E (ApoE) and repelling protein adsorption of opsonins. Intravenous baicalin nanocrystals suspensions (BCL-NS) modified by different surfactant were prepared by high-pressure homogenization. The targeting potential of surface-modified BCL-NS with mean particles size of about 250nm was assessed by in vitro protein adsorption studies using two-dimensional polyacrylamide gel electrophoresis (2-D PAGE), and further evaluated in vivo pharmacokinetics...
October 5, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29031077/4-quinolone-hybrids-and-their-antibacterial-activities
#2
Yuan-Qiang Hu, Shu Zhang, Zhi Xu, Zao-Sheng Lv, Ming-Liang Liu, Lian-Shun Feng
The emergence and wide-spread of drug-resistant bacteria including multi-drug resistant and pan-drug resistant pathogens which are associated with considerable mortality, represent a significant global health threat. 4-Quinolones which are exemplified by fluoroquinolones are the second largest chemotherapy agents used in clinical practice for the treatment of various bacterial infections. However, the resistance of bacteria to 4-quinolones develops rapidly and spreads widely throughout the world due to the long-term, inappropriate use and even abuse...
September 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031066/serendipitous-discovery-of-potent-human-head-and-neck-squamous-cell-carcinoma-anti-cancer-molecules-a-fortunate-failure-of-a-rational-molecular-design
#3
Chiara Zagni, Venerando Pistarà, Luciana A Oliveira, Rogerio M Castilho, Giovanni Romeo, Ugo Chiacchio, Antonio Rescifina
Histone deacetylase inhibitors (HDACis) play an important role as valuable drugs targeted to cancer therapy: several HDACis are currently being tested in clinical trials. Two new potential HDACis 1a and 1d, characterized by the presence of a biphenyl-4-sulfonamide group as a connection unit between the N-{4-[(E)-(2-formylhydrazinylidene)methyl]-3-hydroxyphenyl} and the 2-hydroxy-N-(trifluoroacetyl)benzamide moiety, respectively, as two zinc-binding group (ZBG), have been designed, synthesized and tested for their biological activity...
October 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29028366/synthesis-modeling-and-biological-evaluation-of-hybrids-from-pyrazolo-1-5c-pyrimidine-as-antileishmanial-agents
#4
Kamal Fahmy Mohamed Atta, Tamer Mohamed Ibrahim, Omaima Osman Mahmoud Farahat, Tareq Qasem Al-Shargabi, Mohamed Gaber Marei, Adnan Ahmed Bekhit, El Sayed Helmy El Ashry
AIM: A new series of pyrazolo[1,5-c]pyrimidines were synthesized by different hybridization strategies. METHODOLOGY: All structures were confirmed by IR, (1)H, (13)C, (1)H-(13)C heteronuclear multiple-quantum correlation (HMQC) spectra and microanalysis. They were evaluated for their in vitro antileishmanial activity against miltefosine and amphotericin B deoxycholate as reference drugs. RESULTS: The most active compounds 2a and 9a demonstrated superior potencies to miltefosine by ten- and six-fold, respectively, for the promastigote form, and by 5...
October 13, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29028335/metallo-supramolecular-complexes-enantioselectively-eradicate-cancer-stem-cells-in-vivo
#5
Hongshuang Qin, Chuanqi Zhao, Yuhuan Sun, Jinsong Ren, Xiaogang Qu
Cancer stem cells (CSCs) are responsible for drug resistance, metastasis and recurrence of cancers. However, there is still no clinically approved drug that can effectively eradicate CSCs. Thus, it is crucial and important to develop specific CSC-targeting agents. Chiral molecular recognition of DNA plays an important role in rational drug design. Among them, poly-morphic telomeric G-quadruplex DNA has received much attention due to its significant roles in telomerase activity and chromosome stability. Herein, we find that one enantiomer of zinc-finger-like chiral metallohelices, [Ni2L3]4+-P, a telomeric G-quadruplex-targeting ligand, can preferentially reduce cell growth in breast CSCs compared to the bulk cancer cells...
October 13, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29028301/metallic-cobalt-nitrogen-doped-carbon-nanocomposites-carbon-shell-regulation-toward-efficient-bi-functional-electrocatalysis
#6
Qijie Mo, Nana Chen, Mengdie Deng, Lichun Yang, Qingsheng Gao
To advance hydrogen economy, noble-metal-free electrocatalysts with good efficiency are urgently demanded. They can be developed from metal-organic frameworks (MOFs) with abundant structure-variety, in which a controlled pyrolysis is desired to rationalize nanostructure and maximize catalytic activity. Herein, the efficient regulation is proposed for the first time on the carbon-shell of MOFs-derived Co@NC nanocomposites via varying temperature and flow-rate during pyrolysis, enabling the good accessibility and the electronic optimization of active Co cores...
October 13, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29028138/2d-ruddlesden-popper-perovskites-for-optoelectronics
#7
REVIEW
Yani Chen, Yong Sun, Jiajun Peng, Junhui Tang, Kaibo Zheng, Ziqi Liang
Conventional 3D organic-inorganic halide perovskites have recently undergone unprecedented rapid development. Yet, their inherent instabilities over moisture, light, and heat remain a crucial challenge prior to the realization of commercialization. By contrast, the emerging 2D Ruddlesden-Popper-type perovskites have recently attracted increasing attention owing to their great environmental stability. However, the research of 2D perovskites is just in their infancy. In comparison to 3D analogues, they are natural quantum wells with a much larger exciton binding energy...
October 13, 2017: Advanced Materials
https://www.readbyqxmd.com/read/29028116/effect-of-%C3%AE-mannanase-domain-from-trichoderma-reesei-on-its-biochemical-characters-and-synergistic-hydrolysis-of-sugarcane-bagasse
#8
Lijuan Ma, Qing Ma, Rui Cai, Zhiyou Zong, Liping Du, Gaojie Guo, Yingying Zhang, Dongguang Xiao
BACKGROUND: β-mannanase is a key enzyme for hydrolyzing mannan, a major composition of hemicellulose which is the second most abundant polysaccharides in nature. Different structural domains greatly affect its biochemical characters and catalytic efficiency. But the effects of linker and CBM on β-mannanase from Trichoderma reesei (Man1) have not yet been fully described. This study aimed to elucidate the influence of different domains on expression efficiency, biochemical characteristics and hemicellulosic deconstruction of Man1...
October 13, 2017: Journal of the Science of Food and Agriculture
https://www.readbyqxmd.com/read/29027991/n6-isopentenyladenosine-dual-targeting-of-ampk-and-rab7-prenylation-inhibits-melanoma-growth-through-the-impairment-of-autophagic-flux
#9
Roberta Ranieri, Elena Ciaglia, Giuseppina Amodio, Paola Picardi, Maria Chiara Proto, Patrizia Gazzerro, Chiara Laezza, Paolo Remondelli, Maurizio Bifulco, Simona Pisanti
Targeting the autophagic process is considered a promising therapeutic strategy in cancer since a great number of tumors, including melanoma, show high basal levels of protective autophagy that contributes to tumor progression and chemoresistance. Here, exploiting both in vitro and in vivo approaches, we identified N6-isopentenyladenosine (iPA), an end product of the mevalonate pathway, as a novel autophagy inhibitor with an interesting anti-melanoma activity. iPA, after being phosphorylated by adenosine kinase into 5'-iPA-monophosphate, induces autophagosome accumulation through AMPK activation, measured by increased fluorescent GFP-LC3 puncta and enhanced conversion into the lipidated autophagosome-associated LC3-II...
October 13, 2017: Cell Death and Differentiation
https://www.readbyqxmd.com/read/29027774/rational-approach-to-transfusion-in-liver-transplantation
#10
Fuat H Saner, Lasitha Abeysundara, Matthias Hartmann, Susan V Mallett
For over 50 years patients with liver cirrhosis were considered to be at markedly increased risk of bleeding. This dogma was seemingly supported by abnormalities in standard laboratory tests (SLTs), such as the prothrombin time, that were interpreted as indicating a bleeding diathesis. However, publications from the last decade have revealed SLTs to be poor predictors of bleeding and it is now understood that stable patients with cirrhosis have a rebalanced haemostatic system and preserved thrombin generation...
October 12, 2017: Minerva Anestesiologica
https://www.readbyqxmd.com/read/29027705/effects-of-dietary-supplementation-of-spices-on-forage-degradability-ruminal-fermentation-in-vivo-digestibility-growth-performance-and-nitrogen-balance-in-black-bengal-goat
#11
M R Chowdhury, M M H Khan, S U Mahfuz, M A Baset
The objective of the study was to evaluate the effects of spices on forage utilization and nitrogen (N) emission using in vitro and in vivo approach. A 6 × 5 factorial triplicate arrangement was used to assess the in vitro degradability of rice straw with control (without spices) and individual (40 mg/g rice straw) spices (cumin, coriander, clove, black cumin, turmeric) at five different incubation times. In vitro dry matter (DM) and organic matter (OM) degradability of rice straw were highest in presence of spices except for clove...
October 13, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/29027698/buffalo-heifers-selected-for-lower-residual-feed-intake-have-lower-feed-intake-better-dietary-nitrogen-utilisation-and-reduced-enteric-methane-production
#12
V K Sharma, S S Kundu, C Datt, S Prusty, M Kumar, U B Sontakke
This study was conducted to evaluate the utilisation of the residual feed intake (RFI) as a feed efficiency selection tool and its relationship with methane emissions. Eighteen Murrah buffalo (Bubalus bubalis) heifers were fed ad libitum with total mixed ration (TMR) for 120 days. Based on linear regression models involving dry matter intake (DMI), average daily gain (ADG) and mid-test metabolic body size (MBW(0.75) ), heifers were assigned into low and high RFI groups. The RFI varied from -0.09 to +0.12 kg DM/day with average RFI of -0...
October 13, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/29027555/formation-of-ordered-mesostructured-tio2-thin-films-a-soft-coarse-grained-simulation-study
#13
Qiyun Tang, Paula C Angelomé, Galo J A A Soler-Illia, Marcus Müller
Ordered mesostructured TiO2 thin films are employed in diverse applications ranging from catalysis and sensing, to photovoltaic and lithium-ion batteries. Experimentally these mesostructured thin films are fabricated via a sol-gel process coupled with evaporation-induced self-assembly of a supramolecular template, where the concentration of hydrogen chloride (HCl) and water play vital roles. We employ a soft, coarse-grained model of the amphiphilic template Brij58 and spherical particles, representing titanium-oxo clusters, to study the role of HCl and water in the formation of mesostructured TiO2 thin films...
October 13, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29027483/cdk4-6-blockade-in-breast-cancer-current-experience-and-future-perspectives
#14
Dimitrios Zardavas, Noam Pondé, Konstantinos Tryfonidis
Dysregulated cellular proliferation, one of the hallmarks of cancer, is mediated by aberrant activation of the cell cycle machinery through the biological effects of cyclin-dependent kinases (CDKs). The clinical development of non-selective CDK inhibitors failed due to combined lack of efficacy and excessive toxicity reported by clinical trials across different cancer types. The clinical development of second generation, CDK4/6-selective inhibitors, namely palbociclib, abemaciclib and ribociclib, led to practice-changing results in the setting of breast cancer...
October 13, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/29027409/-developing-traditional-chinese-medicine-injection-is-the-need-for-curing-sickness-to-save-patients
#15
Ping He, Feng-Jie Li, Lian-da Li, Yi-Kui Li
Safety issues of traditional Chinese medicine injections has been heated debate. There are two diametrically opposed views: it should be used reasonable and developed healthily or be forbidden to use. Some people have many misunderstandings and prejudices about the safety of traditional Chinese medicine injections. Compared with western medicine,traditional Chinese medicine has its own particularity. Traditional Chinese medicine has complex components. Its research and clinical application is different from western medicine...
March 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29026788/trends-in-antimicrobial-prescription-for-inpatients-in-changsha-china-2003-to-2014
#16
Yinhua Zhang, Qun Yuan, Xia Yi, Honghua Liu, Xiaoyan Pan, Jingwei Liu, Yi Xu, Yang Chen, Guoping He
BACKGROUND: China had implemented policies to limit antimicrobials prescription since 2004; we conducted this study to reflect the effect of these national policies by analyzing antimicrobial prescription trends of medical insurance in patients from 2003 to 2014 in Changsha city, China. METHODS: The participants were inpatients of the medical insurance of urban workers (UEBMI). Data were extracted from medical insurance information system of Changsha Medical Insurance Institution, which directly connects with hospitals information systems...
September 2017: Iranian Journal of Public Health
https://www.readbyqxmd.com/read/29026441/modeling-the-architecture-of-the-regulatory-system-controlling-methylenomycin-production-in-streptomyces-coelicolor
#17
Jack E Bowyer, Emmanuel Lc de Los Santos, Kathryn M Styles, Alex Fullwood, Christophe Corre, Declan G Bates
BACKGROUND: The antibiotic methylenomycin A is produced naturally by Streptomyces coelicolor A3(2), a model organism for streptomycetes. This compound is of particular interest to synthetic biologists because all of the associated biosynthetic, regulatory and resistance genes are located on a single cluster on the SCP1 plasmid, making the entire module easily transferable between different bacterial strains. Understanding further the regulation and biosynthesis of the methylenomycin producing gene cluster could assist in the identification of motifs that can be exploited in synthetic regulatory systems for the rational engineering of novel natural products and antibiotics...
2017: Journal of Biological Engineering
https://www.readbyqxmd.com/read/29026301/rational-design-of-novel-fluorescent-tagged-glutamic-acid-dendrimers-with-different-terminal-groups-and-in-silico-analysis-of-their-properties
#18
Nuno Martinho, Liana C Silva, Helena F Florindo, Steve Brocchini, Mire Zloh, Teresa S Barata
Dendrimers are hyperbranched polymers with a multifunctional architecture that can be tailored for the use in various biomedical applications. Peptide dendrimers are particularly relevant for drug delivery applications due to their versatility and safety profile. The overall lack of knowledge of their three-dimensional structure, conformational behavior and structure-activity relationship has slowed down their development. Fluorophores are often conjugated to dendrimers to study their interaction with biomolecules and provide information about their mechanism of action at the molecular level...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29026201/dual-contribution-of-trpv4-antagonism-in-the-regulatory-effect-of-vasoinhibins-on-blood-retinal-barrier-permeability-diabetic-milieu-makes-a-difference
#19
David Arredondo Zamarripa, Ramsés Noguez Imm, Ana María Bautista Cortés, Osvaldo Vázquez Ruíz, Michela Bernardini, Alessandra Fiorio Pla, Dimitra Gkika, Natalia Prevarskaya, Fernando López-Casillas, Wolfgang Liedtke, Carmen Clapp, Stéphanie Thébault
Breakdown of the blood-retinal barrier (BRB), as occurs in diabetic retinopathy and other chronic retinal diseases, results in vasogenic edema and neural tissue damage, causing vision loss. Vasoinhibins are N-terminal fragments of prolactin that prevent BRB breakdown during diabetes. They modulate the expression of some transient receptor potential (TRP) family members, yet their role in regulating the TRP vanilloid subtype 4 (TRPV4) remains unknown. TRPV4 is a calcium-permeable channel involved in barrier permeability, which blockade has been shown to prevent and resolve pulmonary edema...
October 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29026180/ultraintense-uv-emission-from-zno-sheathed-zns-nanorods
#20
Jae Kyung Lee, Gun-Joo Sun, Woo Seok Lee, Soong Keun Hyun, Kyoung-Kook Kim, Seung-Bok Choi, Chongmu Lee
Short-wavelength luminescence is essential for high-performance optoelectronic device applications. There have been efforts to obtain intense ultraviolet (UV) emission by encapsulating ZnO one-dimensional (1D) nanostructures with materials such as ZnS. However, the encapsulation of ZnS 1D nanostructures with ZnO has not been reported. In this paper, we report ultraintense UV emission from ZnS nanorods coated with ZnO, i.e., ZnS-core/ZnO-shell nanorods. UV emission from the ZnS-core/ZnO-shell nanorods was much more intense than that obtained from the extensively studied ZnO-core/ZnS-shell nanorods...
October 12, 2017: Scientific Reports
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