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21.
Effects of dietary hop (Humulus lupulus L.) β‐acids on quality attributes,composition and oxidative stability of pork meat 下载免费PDF全文
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Maicon F Silva Kátia Sivieri Elizeu A Rossi 《Journal of the International Society of Sports Nutrition》2009,6(1):1-6
It is well established that the ingestion of the omega-3 (N3) fatty acids docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA) positively benefit a variety of health indices. Despite these benefits the actual intake of fish derived N3 is relatively small in the United States. The primary aim of our study was to examine a technology capable of delivering omega-3 fatty acids in common foods via microencapsulation (MicroN3) in young, healthy, active participants who are at low risk for cardiovascular disease. Accordingly, we randomized 20 participants (25.4 ± 6.2 y; 73.4 ± 5.1 kg) to receive the double blind delivery of a placebo-matched breakfast meal (~2093 kJ) containing MicroN3 (450–550 mg EPA/DHA) during a 2-week pilot trial. Overall, we observed no differences in overall dietary macronutrient intake other than the N3 delivery during our treatment regimen. Post-test ANOVA analysis showed a significant elevation in mean (SE) plasma DHA (91.18 ± 9.3 vs. 125.58 ± 11.3 umol/L; P < 0.05) and a reduction in triacylglycerols (89.89 ± 12.8 vs. 80.78 ± 10.4 mg/dL; P < 0.05) accompanying the MicroN3 treatment that was significantly different from placebo (P < 0.05). In post study interviews, participants reported that the ingested food was well-tolerated, contained no fish taste, odor or gastrointestinal distress accompanying treatment. The use of MicroN3 foods provides a novel delivery system for the delivery of essential fatty acids. Our study demonstrates that MicroN3 foods promote the absorption of essential N3, demonstrate bioactivity within 2 weeks of ingestion and are well tolerated in young, active participants who are at low risk for cardiovascular disease. 相似文献
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Sabrina Castellano Dr. Ciro Milite Dr. Rino Ragno Dr. Silvia Simeoni Dr. Antonello Mai Prof. Vittorio Limongelli Dr. Ettore Novellino Prof. Ingo Bauer Dr. Gerald Brosch Prof. Astrid Spannhoff Dr. Donghang Cheng Dr. Mark T. Bedford Prof. Gianluca Sbardella Prof. 《ChemMedChem》2010,5(3):398-414
Here we report the synthesis of a number of compounds structurally related to arginine methyltransferase inhibitor 1 (AMI‐1). The structural alterations that we made included: 1) the substitution of the sulfonic groups with the bioisosteric carboxylic groups; 2) the replacement of the ureidic function with a bis‐amidic moiety; 3) the introduction of a N‐containing basic moiety; and 4) the positional isomerization of the aminohydroxynaphthoic moiety. We have assessed the biological activity of these compounds against a panel of arginine methyltransferases (fungal RmtA, hPRMT1, hCARM1, hPRMT3, hPRMT6) and a lysine methyltransferase (SET7/9) using histone and nonhistone proteins as substrates. Molecular modeling studies for a deep binding‐mode analysis of test compounds were also performed. The bis‐carboxylic acid derivatives 1 b and 7 b emerged as the most effective PRMT inhibitors, both in vitro and in vivo, being comparable or even better than the reference compound (AMI‐1) and practically inactive against the lysine methyltransferase SET7/9. 相似文献
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Fabrizio Dal Piaz Dr. Alessandra Tosco Dr. Daniela Eletto Dr. Anna L. Piccinelli Dr. Ornella Moltedo Dr. Silvia Franceschelli Dr. Gianluca Sbardella Prof. Paolo Remondelli Prof. Luca Rastrelli Prof. Loredana Vesci Dr. Claudio Pisano Dr. Nunziatina De Tommasi Prof. 《Chembiochem : a European journal of chemical biology》2010,11(6):818-827
Many severe human pathologies are related to alterations of the fine balance between histone acetylation and deacetylation; because not all such diseases involve hypoacetylation, but also hyperacetylation, compounds able to enhance or repress the activities of histone acetyltransferases (HATs) could be promising therapeutic agents. We evaluated in vitro and in cell the ability of eleven natural polyisoprenylated benzophenone derivatives to modulate the HAT activity of p300/CBP, an enzyme that plays a pivotal role in a variety of cellular processes. Some of the tested compounds bound efficiently to the p300/CBP protein: in particular, guttiferone A, guttiferone E and clusianone inhibit its HAT activity, whereas nemorosone showed a surprising ability to activate the enzyme. The ability of nemorosone to penetrate cell membranes and modulate histone acetylation into the cell together with its high affinity for the p300/CBP enzyme made this compound a suitable lead for the design of optimized anticancer drugs. Besides, the studies performed at a cellular and molecular level on both the inhibitors and the activator provided new insights into the modulation mechanism of p300/CBP by small molecules. 相似文献
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Dr. Anna Maria Santoro Dr. Valeria Lanza Dr. Francesco Bellia Dr. Diego Sbardella Dr. Grazia R. Tundo Alessandra Cannizzo Prof. Giuseppe Grasso Dr. Mariaconcetta Arizzi Prof. Vincenzo G. Nicoletti Prof. Stefano Alcaro Dr. Giosuè Costa Dr. Adriana Pietropaolo Prof. Gaetano Malgieri Dr. Gianluca D'Abrosca Prof. Roberto Fattorusso Sara García-Viñuales Ikhlas M. M. Ahmed Prof. Massimiliano Coletta Dr. Danilo Milardi 《ChemMedChem》2020,15(3):302-316
Proteasome malfunction parallels abnormal amyloid accumulation in Alzheimer's Disease (AD). Here we scrutinize a small library of pyrazolones by assaying their ability to enhance proteasome activity and protect neuronal cells from amyloid toxicity. Tube tests evidenced that aminopyrine and nifenazone behave as 20S proteasome activators. Enzyme assays carried out on an “open gate” mutant (α3ΔN) proteasome demonstrated that aminopyrine activates proteasome through binding the α-ring surfaces and influencing gating dynamics. Docking studies coupled with STD-NMR experiments showed that H-bonds and π-π stacking interactions between pyrazolones and the enzyme play a key role in bridging α1 to α2 and, alternatively, α5 to α6 subunits of the outer α-ring. Aminopyrine and nifenazone exhibit neurotrophic properties and protect differentiated human neuroblastoma SH-SY5Y cells from β-amyloid (Aβ) toxicity. ESI-MS studies confirmed that aminopyrine enhances Aβ degradation by proteasome in a dose-dependent manner. Our results suggest that some pyrazolones and, in particular, aminopyrine are promising compounds for the development of proteasome activators for AD treatment. 相似文献
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Effects of dietary supplementation of red pepper (Schinus terebinthifolius Raddi) essential oil on performance,small intestinal morphology and microbial counts of weanling pigs 总被引:1,自引:0,他引:1 下载免费PDF全文
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Inside Cover: Identification of Structural Features of 2‐Alkylidene‐1,3‐Dicarbonyl Derivatives that Induce Inhibition and/or Activation of Histone Acetyltransferases KAT3B/p300 and KAT2B/PCAF (ChemMedChem 1/2015) 下载免费PDF全文
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Maicon Waltrich Christian J.L. Hermes Joaquim M. Goncalves Cláudio Melo 《Applied Thermal Engineering》2010,30(14-15):2011-2018
This paper outlines a novel first-principles mathematical model to simulate the thermo-hydraulic behavior of compact fan-supplied tube-fin heat exchangers for light commercial refrigeration applications, i.e., with heat duties ranging from 0.5 to 2.0 kW. The model is based on the mass, momentum and energy conservation equations applied to both the refrigerant and air streams. The model predictions were compared with experimental data taken at several operating and geometric conditions. It was found that the model predictions for the air-side heat transfer and pressure drop were very close to the experimental data with maximum deviations of ±10% and ±15%, respectively. The model was employed to assess the thermal-hydraulic performance of a gas cooler running with supercritical CO2 as working fluid. 相似文献