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Mostafa M Ghorab, Mansour S Alsaid, Ghada H Al-Ansary, Ghada A Abdel-Latif, Dalal A Abou El Ella
Twenty novel chromene derivatives carrying different sulfonamide moieties (3-22) were designed and synthesized. All the newly prepared compounds were evaluated for their in vitro anticancer activity against breast cancer cell line (T47D). Most of the synthesized compounds showed good to moderate activity (IC50 = 8.8-108.9 μM), where compound 16 (IC50 = 8.8 μM) exhibited higher activity compared to doxorubicin (IC50 = 9.8 μM). In order to determine the mechanism of the anticancer activity in T47D cells, the effect of the most potent compounds (5-8, 11-14, and 16-18) on the aromatase activity was tested...
October 13, 2016: European Journal of Medicinal Chemistry
Todd Blevins
Cells have evolved intricate RNA-directed mechanisms that destroy viruses, silence transposons, and regulate gene expression. These nucleic acid surveillance and gene silencing mechanisms rely upon the selective base-pairing of ~19-25 nt small RNAs to complementary RNA targets. This chapter describes northern blot hybridization techniques for the detection of such small RNAs. Blots spiked with synthetic standards are used to illustrate the detection specificity and sensitivity of DNA oligonucleotide probes...
2017: Methods in Molecular Biology
Norimitsu Shirai, Frank J Geoly, Walter F Bobrowski, Carlin Okerberg
Drug-induced phospholipidosis is characterized by intracellular accumulation of phospholipids with lamellar bodies in cells exposed to xenobiotics. Demonstration of the lamellar bodies by transmission electron microscopy (TEM) is the hallmark for a definitive diagnosis of phospholipidosis. However, the preparation of tissue samples for TEM and their ultrastructural evaluation are technically challenging and time consuming. Paraphenylenediamine (PPD) is essentially a fat stain, and the staining mechanism is based upon the osmication of unsaturated lipids...
October 21, 2016: Toxicologic Pathology
Eun-Young Nam, Sun Ah Kim, Heejung Kim, Su-Hyun Kim, Jae-Hyun Han, Ju-Hee Lee, Dong-Il Kim
ETHNOPHARMACOLOGICAL RELEVANCE: Evodiae Fructus (EF) is the dried, unripe fruit of Evodia rutaecarpa Benth., and one of the main components of traditional herbal prescriptions issued for the treatment of sterility caused by irregular menstruation in Korea. However, scientific evidence regarding the efficacy and action mechanism of EF is lacking. AIM OF THE STUDY: In this study, the authors established an in vitro screening tool to identify promising new drug candidates in herbal medicines for the prevention and treatment of premature ovarian failure...
October 18, 2016: Journal of Ethnopharmacology
Hung-Yi Liu, Tanja Greene, Tsai-Yu Lin, Camron S Dawes, Murray Korc, Chien-Chi Lin
: The complex network of biochemical and biophysical cues in the pancreatic desmoplasia not only presents challenges to the fundamental understanding of tumor progression, but also hinders the development of therapeutic strategies against pancreatic cancer. Residing in the desmoplasia, pancreatic stellate cells (PSCs) are the major stromal cells affecting the growth and metastasis of pancreatic cancer cells by means of paracrine effects and extracellular matrix protein deposition. PSCs remain in a quiescent/dormant state until they are 'activated' by various environmental cues...
October 18, 2016: Acta Biomaterialia
Sarsvat Patel, Xiang Kou, Hao Helen Hou, Ye Bill Huang, John C Strong, Geoff G Z Zhang, Changquan Calvin Sun
Amorphous solid dispersions (ASDs) consisting of acetaminophen (APAP) and copovidone were systematically studied to identify effects of drug loading and moisture content on mechanical properties, thermal properties, and tableting behavior. ASDs containing APAP at different levels were prepared by film casting and characterized by differential scanning calorimetry and nanoindentation. The glass transition temperature (Tg) continuously decreased with increasing amount of APAP, but the hardness of ASDs was increased at a low APAP content and reduced at high APAP content...
October 18, 2016: Journal of Pharmaceutical Sciences
Meng Li Liu, Bin Bin Chen, Ze Xi Liu, Cheng Zhi Huang
Though many methods of detecting 2,4,6-trinitrophenol (TNP) mainly have been developed recent years, quantification of TNP in environmental matrixes still faces up to great challenges because all the nitroaromatic explosives reveal highly similar chemical structure. In the present work, we have developed a selective and sensitive method for detection of TNP by amorphous photoluminescent carbon nanodots (CNDs), which are prepared through a simple hydrothermal route using spermine and m-phenylenediamine (MPD) as precursors...
December 1, 2016: Talanta
Shuyun Zhu, Lei He, Fang Zhang, Mengyuan Li, Shulin Jiao, Yan Li, Mengyuan Chen, Xian-En Zhao, Hua Wang
A highly sensitive fluorimetric assay has been developed for the evaluation of glutathione reductase (GR) activity and the screening of its inhibitors by using carbon quantum dots (CQDs) as the signal reporter. The detection mechanism is based on the following facts: (1) the fluorescence of CQDs can be quenched by Hg(II) through the strong CQDs-Hg(II) coordination; (2) GR can catalyze the reduction of oxidized glutathione (GSSG) into reduced glutathione (GSH), so that the fluorescence recovery of CQDs would take place resulting from the strong GSH-Hg(II) interaction; (3) GR can lose its catalytic reduction of GSSG in the presence of its inhibitors, which will inhibit the recovery of the quenched fluorescence of CQDs...
December 1, 2016: Talanta
Xiyue Xiong, Haiqin He, Yan Shu, Yuxin Li, Zihui Yang, Yingzhuang Chen, Ming Ma, Bo Chen
A facile, flexible process was developed for the preparation of surface-glycosylated porous monolithic columns via aqueous two-phase graft copolymerization of polyethylene glycol diacrylate (PEGDA) and water-soluble dextran (dextran sulfate). The formation of poly(PEGDA) porous skeletons and surface glycosylation were achieved via a one-step process without pre-modification of the dextran. The synthesis conditions were thoroughly optimized. The optimal monolithic column exhibited a large dry state surface area (greater than 400m(2)/g), and it was evaluated as a hydrophilic liquid chromatography (HILIC) stationary phase...
December 1, 2016: Talanta
Mingyang Liu, Lijun Yang, Lei Zhang
In this study, a functionalized magnetic hollow porous oval-shape NiFe2O4 (MHPO-NiFe2O4) was designed by a facile synthesis procedure, and employed as magnetic solid phase extraction (MSPE) material to extract several heavy metal ions. As-prepared MHPO-NiFe2O4 exhibited superior adsorption capacities of 20.17, 16.64, 16.82, 9.69 and 16.58mgg(-1), for Cu(II), Cd(II), Cr(III), Co(II) and Zn(II), and was then used to detect these heavy metals elements in real samples by combining with inductively coupled plasma optical emission spectroscopy (ICP-OES)...
December 1, 2016: Talanta
Yu Cheng, Srinivasa Rao Avula, Wei-Wei Gao, Dinesh Addla, Vijai Kumar Reddy Tangadanchu, Ling Zhang, Jian-Mei Lin, Cheng-He Zhou
A series of new potentially multi-targeting antimicrobial 2-aminothiazolyl quinolones were designed, synthesized and characterized by (1)H NMR, (13)C NMR, IR, MS and HRMS spectra. Bioactive assay manifested that some of the prepared compounds showed moderate to good antibacterial and antifungal activities. Noticeably, compound 10f could effectively inhibit the growth of B. typhi and MRSA with MIC values of 1 and 8 μg/mL, respectively. Experimental results revealed that compound 10f was membrane-active and had the ability to rapidly kill the tested strains and effectively prevent the development of bacterial resistance...
October 7, 2016: European Journal of Medicinal Chemistry
Chencheng Sun, Bowen Xiong, Yang Pan, Hao Cui
Polyaniline (PANI) prepared by chemical oxidation was studied for adsorption removal of tannic acid (TA) from aqueous solution. Batch adsorption studies were carried out under different adsorbent dosages, pH, ionic strength, initial TA concentration and coexisting anions. Solution pH had an important impact on TA adsorption onto PANI with optimal removal in the pH range of 8-11. TA adsorption on PANI at three ionic strength levels (0.02, 0.2 and 2molL(-1) NaCl) could be well described by Langmuir model (monolayer adsorption process) and the maximum adsorption capacity was 230, 223 and 1023mgg(-1), respectively...
October 15, 2016: Journal of Colloid and Interface Science
Yu-Dong Ma, Varadharajan Thiyagarajan, May-Jywan Tsai, Sheng-I Lue, Yi-Chen Chia, Song-Kun Shyue, Ching-Feng Weng
Migration of vascular smooth muscle cells (VSMCs) contributes to intimal hyperplasia and other vascular diseases. Caveolin-1 (Cav-1) has been recognized as a proliferative inhibitor of VSMCs and is likely to be an important regulator of VSMC migration. The underlying mechanism of pyrogallol on the VSMC migration is not fully understood. This study attempted to dissect the role of Cav-1 and matrix metalloproteinase (MMP) in VSMC migration and to investigate the effect of pyrogallol on VSMC mobility during carotid artery ligation mice...
October 15, 2016: Environmental Toxicology and Pharmacology
Shufang Yang, Ran Wang, Guang Wan, Zhimin Wu, Shujuan Guo, Xingxing Dai, Xinyuan Shi, Yanjiang Qiao
Menthol is a widely used penetration enhancer in clinical medicine due to its high efficiency and relative safety. However, details of the penetration enhancement mechanism of menthol on molecular level is rarely involved in the discussion. In this work, the penetration enhancement (PE) mechanism of menthol is explored by a multiscale method containing molecular dynamics simulations, in vitro penetration experiments and transmission electron microscopy. Osthole is chosen to be the tested drug due to its common-using in external preparations and its representative-accompanying with menthol as a PE in the preparations...
October 21, 2016: Journal of Chemical Information and Modeling
Bhavisha Bakrania, Joey P Granger, Romain Harmancey
The mammalian heart is a major consumer of ATP and requires a constant supply of energy substrates for contraction. Not surprisingly, alterations of myocardial metabolism have been linked to the development of contractile dysfunction and heart failure. Therefore, unraveling the link between metabolism and contraction should shed light on some of the mechanisms governing cardiac adaptation or maladaptation in disease states. The isolated working rat heart preparation can be used to follow, simultaneously and in real time, cardiac contractile function and flux of energy providing substrates into oxidative metabolic pathways...
September 28, 2016: Journal of Visualized Experiments: JoVE
Erlin Zhang, Jing Ren, Shengyi Li, Lei Yang, Gaowu Qin
Ti-Cu sintered alloys have shown good antibacterial abilities. However, the sintered method (powder metallurgy) is not convenient to produce devices with a complex structure. In this paper, Ti-Cu alloys with 2.0, 3.0 and 4.0 wt.% Cu were prepared in an arc melting furnace and subjected to different heat treatments: solid solution and ageing, to explore the possibility of preparing an antibacterial Ti-Cu alloy by a casting method and to examine the effect of Cu content. Phase identification was conducted on an XRD diffraction meter, and the microstructure was observed by a metallographic microscope, a scanning electron microscope (SEM) with energy disperse spectroscopy (EDS) and transmission electron microscopy (TEM)...
October 21, 2016: Biomedical Materials
Zhen Wang, Eric P Chang, Vern L Schramm
Transition path sampling simulations have proposed that human heart lactate dehydrogenase (LDH) employs protein promoting vibrations (PPVs) on the femtosecond (fs) to picosecond (ps) timescale to promote crossing of the chemical barrier. This chemical barrier involves both hydride and proton transfers to pyruvate to form L-lactate, using reduced nicotinamide adenine dinucleotide (NADH) as the cofactor. Here we report experimental evidence from three types of isotope effect experiments that support coupling of the promoting vibrations to barrier crossing and the coincidence of hydride and proton transfer...
October 21, 2016: Journal of the American Chemical Society
Ummara Butt, Amr ElShaer, Lori A S Snyder, Athina Chaidemenou, Raid G Alany
Fatty acids (FAs) are used by many organisms as defence mechanism against virulent bacteria. The high safety profile and broad spectrum of activity make them potential alternatives to currently used topical antibiotics for the treatment of eye infections in neonates. The current study utilised a Design of Experiment approach to optimise the quantification of five fatty acids namely; lauric acid, tridecanoic acid, myristoleic acid, palmitoleic acid and α-linolenic acid. The significance of the influence of the experimental parameters such as volume of catalyst, volume of n-hexane, incubation temperature, incubation time and the number of extraction steps on derivatisation was established by statistical screening with a factorial approach...
October 20, 2016: Drug Delivery and Translational Research
Apisada Ket-On, Natkritta Pongmongkol, Anongnat Somwangthanaroj, Theeranun Janjarasskul, Kanitha Tananuwong
The impact of spice powders on physical, mechanical, thermal and barrier properties, and on storage stability, of whey protein isolate (WPI)-based films was determined. Films with added spices were prepared from casting solution containing 10 % (w/w) heat-denatured WPI, glycerol (WPI:glycerol of 3:2 w/w), sodium chloride (0.4 g/100 g solution), garlic and pepper powders (≤3 g each/100 g solution). Water activity (aw) of all films was 0.53-0.57. Addition of spice powders increased thickness, darkness and yellowness of the WPI films...
July 2016: Journal of Food Science and Technology
Ming Yang, Haiyong Wang, Mo Zhou, Weilin Liu, Pengqun Kuang, Hao Liang, Qipeng Yuan
Lung cancer is one of the leading causes of cancer death worldwide. Isothiocyanates from cruciferous vegetables been shown to possess anticarcinogenic activities in lung malignances. We previously found sulforaphene (4-methylsufinyl-3-butenyl isothiocyanate, SFE), one new kind of isothiocyanates, existing in a relative high abundance in radish seeds. An efficient methodology based on macroporous resin and preparative high-performance liquid chromatography was developed to isolate SFE in reasonably large quantities, high purity and low cost...
September 28, 2016: Oncotarget
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