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García Graciela Gutiérrez Verónica Ríos Néstor Papa Nicolás Serra Sebastián Loureiro Marcelo 《Hydrobiologia》2020,847(19):4141-4142
Hydrobiologia - Due to an unfortunate turn of events, the incorrect caption of Fig. 2 appeared in the original publication. Figure 2 and its correct caption is published here and should be treated... 相似文献
34.
This study contributes to the investigation related to guest–host interactions between the chemotherapeutic agent cisplatin and a functionalised silica matrix in order to improve and find new materials such as drug carriers. The adsorption of cisplatin and its complexes, cis-[PtCl(NH3)2]+ and cis-[Pt(NH3)2]2+, on a SH-functionalised SiO2(111) surface has been studied by the atom superposition and electron delocalisation method. The adiabatic energy curves for the adsorption of the drug and its products on the delivery system were considered. The electronic structure and bonding analysis were also performed. The molecule and their complex are adsorbed on the functionalised surface resulting in a major absorption of the cis-[Pt(NH3)2]2+ complex. The molecule–surface interactions are formed via –SH group. The molecule/complexes SH electron-donating effect plays an important role in the catalytic reaction. The more important drug–carrier interactions occur through the Cl–H bond for the adsorption of cis-[PtCl2(NH3)2] and cis-[PtCl(NH3)2]+, and through the Pt–S and Pt–H interactions for cis-[Pt(NH3)2]2+ adsorption. When the new interactions are formed, the functionalised carrier maintains their matrix properties while the molecule is the most affected after adsorption. The Pt atomic orbitals present the most important changes during adsorption. 相似文献
35.
Micaela Pescuma María Beatriz Espeche Turbay Fernanda Mozzi Graciela Font de Valdez Graciela Savoy de Giori Elvira María Hebert 《Applied microbiology and biotechnology》2013,97(17):7831-7844
Ability of industrially relevant species of thermophilic lactobacilli strains to hydrolyze proteins from animal (caseins and β-lactoglobulin) and vegetable (soybean and wheat) sources, as well as influence of peptide content of growth medium on cell envelope-associated proteinase (CEP) activity, was evaluated. Lactobacillus delbrueckii subsp. lactis (CRL 581 and 654), L. delbrueckii subsp. bulgaricus (CRL 454 and 656), Lactobacillus acidophilus (CRL 636 and 1063), and Lactobacillus helveticus (CRL 1062 and 1177) were grown in a chemically defined medium supplemented or not with 1 % Casitone. All strains hydrolyzed mainly β-casein, while degradation of αs-caseins was strain dependent. Contrariwise, κ-Casein was poorly degraded by the studied lactobacilli. β-Lactoglobulin was mainly hydrolyzed by CRL 656, CRL 636, and CRL 1062 strains. The L. delbrueckii subsp. lactis strains, L. delbrueckii subsp. bulgaricus CRL 656, and L. helveticus CRL 1177 degraded gliadins in high extent, while the L. acidophilus and L. helveticus strains highly hydrolyzed soy proteins. Proteinase production was inhibited by Casitone, the most affected being the L. delbrueckii subsp. lactis species. This study highlights the importance of proteolytic diversity of lactobacilli for rational strain selection when formulating hydrolyzed dairy or vegetable food products. 相似文献
36.
Graciela B. Arhancet Daniel P. Walker Sue Metz Yvette M. Fobian Steven E. Heasley Jeffrey S. Carter John R. Springer Darin E. Jones Michael J. Hayes Alexander F. Shaffer Gina M. Jerome Michael T. Baratta Ben Zweifel William M. Moore Jaime L. Masferrer Michael L. Vazquez 《Bioorganic & medicinal chemistry letters》2013,23(4):1114-1119
Inhibition of mPGES-1, the terminal enzyme in the arachidonic acid/COX pathway to regulate the production of pro-inflammatory prostaglandin PGE2, is considered an attractive new therapeutic target for safe and effective anti-inflammatory drugs. The discovery of a novel series of orally active, selective benzoxazole piperidinecarboxamides as mPGES-1 inhibitors is described. Structure–activity optimization of lead 5 with cyclohexyl carbinols resulted in compound 12, which showed excellent in vitro potency and selectivity against COX-2, and reasonable pharmacokinetic properties. Further SAR studies of the benzoxazole ring substituents lead to a novel series of highly potent compounds with improved PK profile, including 23, 26, and 29, which were effective in a carrageenan-stimulated guinea pig air pouch model of inflammation. Based on its excellent in vitro and in vivo pharmacological, pharmacokinetic and safety profile and ease of synthesis, compound 26 (PF-4693627) was advanced to clinical studies. 相似文献
37.
Mikhail S. Novikov Vladimir T. Valuev-Elliston Denis A. Babkov Maria P. Paramonova Alexander V. Ivanov Sergey A Gavryushov Anastasia L. Khandazhinskaya Sergey N. Kochetkov Christophe Pannecouque Graciela Andrei Robert Snoeck Jan Balzarini Katherine L. Seley-Radtke 《Bioorganic & medicinal chemistry》2013,21(5):1150-1158
A series of phenyloxyethyl and cinnamyl derivatives of substituted uracils were synthesized and found to exhibit potent activity against HIV-RT and HIV replication in cell culture. In general, the cinnamyl derivatives proved superior to the phenyloxyethyl derivatives, however 1-[2-(4-methylphenoxy)ethyl]-3-(3,5-dimethylbenzyl)uracil (19) exhibited the highest activity (EC50 = 0.27 μM) thus confirming that the 3-benzyluracil fragment in the NNRTI structure can be regarded as a functional analogue of the benzophenone pharmacophore typically found in NNRTIs. 相似文献
38.
Mikhail S. Novikov Denis A. Babkov Maria P. Paramonova Anastasia L. Khandazhinskaya Alexander A. Ozerov Alexander O. Chizhov Graciela Andrei Robert Snoeck Jan Balzarini Katherine L. Seley-Radtke 《Bioorganic & medicinal chemistry》2013,21(14):4151-4157
HCMV infection represents a life-threatening condition for immunocompromised patients and newborn infants and novel anti-HCMV agents are clearly needed. In this regard, a series of 1-[ω-(phenoxy)alkyl]uracil derivatives were synthesized and examined for antiviral properties. Compounds 17, 20, 24 and 28 were found to exhibit highly specific and promising inhibitory activity against HCMV replication in HEL cell cultures with EC50 values within 5.5–12 μM range. Further studies should be undertaken to elucidate the mechanism of action of these compounds and the structure–activity relationship for the linker region. 相似文献
39.
Maria Bromley Milton Bj?rn B?rsbo Graciela Rovner ?sa Lundgren-Nilsson Katharina Stibrant-Sunnerhagen Bj?rn Gerdle 《PloS one》2013,8(6)
Background
Incorporating the patient''s view on care and treatment has become increasingly important for health care. Patients describe the variety of consequences of their chronic pain conditions as significant pain intensity, depression, and anxiety. We hypothesised that intensities of common symptoms in chronic pain conditions carry important information that can be used to identify clinically relevant subgroups. This study has three aims: 1) to determine the importance of different symptoms with respect to participation and ill-health; 2) to identify subgroups based on data concerning important symptoms; and 3) to determine the secondary consequences for the identified subgroups with respect to participation and health factors.Methods and Subjects
This study is based on a cohort of patients referred to a multidisciplinary pain centre at a university hospital (n = 4645, participation rate 88%) in Sweden. The patients answered a number of questionnaires concerning symptoms, participation, and health aspects as a part of the Swedish Quality Registry for Pain Rehabilitation (SQRP).Results
Common symptoms (such as pain intensity, depression, and anxiety) in patients with chronic pain showed great variability across subjects and 60% of the cohort had normal values with respect to depressive and anxiety symptoms. Pain intensity more than psychological symptoms showed stronger relationships with participation and health. It was possible to identify subgroups based on pain intensity, depression, and anxiety. With respect to participation and health, high depressive symptomatology had greater negative consequences than high anxiety.Conclusions
Common symptoms (such as pain intensity and depressive and anxiety symptoms) in chronic pain conditions carry important information that can be used to identify clinically relevant subgroups. 相似文献40.
Delfino B. M. Campos R. G. Pereira T. M. Mantovani S. A. S. Oliart-Guzmán H. Martins A. C. Braña A. M. Branco F. L. C. C. Filgueira-Júnior J. A. Santos A. P. Araújo T. S. Oliveira C. S. M. Ramalho A. A. Muniz P. T. Codeço C. T. da Silva-Nunes M. 《EcoHealth》2016,13(4):743-760
EcoHealth - This study analyzed the evolution of socioeconomic, sanitary, and personal factors as well as spatiotemporal changes in the prevalence of helminthiasis and giardiasis in urban Amazonian... 相似文献