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[PMID]: 28799579 [Au] Autor: Montero Matamala A; Bertolotti M; Contini MP; Guerrero Bayón C; Nizzardo A; Paredes Lario I; Pizà Vallespir B; Scartoni S; Tonini G; Capriati A; Pellacani A [Ad] Endereço: Department of Anesthesiology, Reanimation and Pain Clinic, University Hospital Arnau de Vilanova, Lleida, Spain. [Ti] Título: Tramadol hydrochloride 75 mg/dexketoprofen 25 mg oral fixed-dose combination in moderate-to-severe acute pain: sustained analgesic effect over a 56-h period in the postoperative setting. [So] Source: Drugs Today (Barc);53(6):339-347, 2017 Jun. [Is] ISSN: 1699-3993 [Cp] País de publicação: Spain [La] Idioma: eng [Ab] Resumo: Multimodal analgesia constitutes a common strategy in pain management. A tramadol hydrochloride 75 mg/dexketoprofen 25 mg oral fixed combination (TRAM/DKP 75 mg/25 mg) has been recently registered and released in Europe for the treatment of moderate-to-severe acute pain. This paper provides additional analyses on the results of two phase III clinical trials (DEX-TRA-04 and DEX-TRA-05) on postoperative pain to document its sustained effect. The analysis was applied to a modified intention-to-treat population (mITT, n = 933) of patients undergoing active treatment from the first dose, to assess the sustained effect of TRAM/DKP 75 mg/25 mg on pain intensity (PI-VAS 0-100) over 56 h from first drug intake. The superior analgesic effect of TRAM/DKP 75 mg/25 mg over 56 h in terms of difference in PI-VAS (mean [SE]) was shown for DEX-TRA-04 (-11.0 [0.55] over dexketoprofen 25 mg and -9.1 [0.55] over tramadol 100 mg, P ≤ 0.0001) and for DEX-TRA-05 (-10.4 [0.51] over dexketoprofen 25 mg and -8.3 [0.51] over tramadol 100 mg, P ≤ 0.0001). The statistical analysis performed on data coming from both studies confirms the superior sustained analgesia of TRAM/DKP 75 mg/25 mg over tramadol 100 mg and dexketoprofen 25 mg. These results are consistent with the previously published data obtained on the ITT population and strongly support the role of this oral fixed-dose combination in the treatment of moderate-to-severe acute pain. [Mh] Termos MeSH primário: Analgésicos/uso terapêutico Cetoprofeno/análogos & derivados Dor Pós-Operatória/tratamento farmacológico Tramadol/administração & dosagem Trometamina/administração & dosagem [Mh] Termos MeSH secundário: Adulto Idoso Idoso de 80 Anos ou mais Artroplastia de Quadril/efeitos adversos Ensaios Clínicos Fase III como Assunto/estatística & dados numéricos Método Duplo-Cego Esquema de Medicação Combinação de Medicamentos Feminino Seres Humanos Histerectomia/efeitos adversos Cetoprofeno/administração & dosagem Masculino Meia-Idade Estudos Multicêntricos como Assunto/estatística & dados numéricos Medição da Dor Ensaios Clínicos Controlados Aleatórios como Assunto/estatística & dados numéricos Fatores de Tempo Resultado do Tratamento [Pt] Tipo de publicação: JOURNAL ARTICLE; REVIEW [Nm] Nome de substância: 0 (Analgesics); 0 (Drug Combinations); 023C2WHX2V (Tromethamine); 39J1LGJ30J (Tramadol); 90Y4QC304K (Ketoprofen); N674F7L21E (dexketoprofen trometamol) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171103 [Lr] Data última revisão: 171103 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170812 [St] Status: MEDLINE [do] DOI: 10.1358/dot.2017.53.6.2636487

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[PMID]: 28243920 [Au] Autor: Marina AS; Kutina AV; Shakhmatoba EI; Natochin YV [Ad] Endereço: I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia. annamarina@bk.ru. [Ti] Título: Involvement of Glucagon-Like Peptide-1 in the Regulation of Selective Excretion of Sodium or Chloride Ions by the Kidneys. [So] Source: Bull Exp Biol Med;162(4):436-440, 2017 Feb. [Is] ISSN: 1573-8221 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: An increase of total glucagon-like peptide-1 (GLP-1) concentration in the plasma in rats was revealed 5 min after oral, but not intraperitoneal administration of NaCl or Trizma HCl solutions. The increase in GLP-1 level was similar to that after oral glucose administration. After intraperitoneal administration of 2.5% NaCl, GLP-1 mimetic exenatide accelerated natriuresis and urinary chloride excretion. Under conditions of normonatriemia and hyperchloremia induced by injection of 6.7% Trizma HCl, exenatide stimulated chloride excretion and reabsorption of sodium ions in the kidneys. These findings suggest that GLP-1 participates in selective regulation of the balance of sodium and chloride ions. [Mh] Termos MeSH primário: Cloretos/urina Peptídeo 1 Semelhante ao Glucagon/metabolismo Hipoglicemiantes/farmacologia Rim/efeitos dos fármacos Peptídeos/farmacologia Sódio/urina Peçonhas/farmacologia [Mh] Termos MeSH secundário: Administração Oral Animais Feminino Taxa de Filtração Glomerular/efeitos dos fármacos Glucose/metabolismo Glucose/farmacologia Injeções Intraperitoneais Íons Rim/fisiologia Ratos Ratos Wistar Cloreto de Sódio/farmacologia Trometamina/farmacologia Equilíbrio Hidroeletrolítico/efeitos dos fármacos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Chlorides); 0 (Hypoglycemic Agents); 0 (Ions); 0 (Peptides); 0 (Venoms); 023C2WHX2V (Tromethamine); 451W47IQ8X (Sodium Chloride); 89750-14-1 (Glucagon-Like Peptide 1); 9NEZ333N27 (Sodium); 9P1872D4OL (exenatide); IY9XDZ35W2 (Glucose) [Em] Mês de entrada: 1703 [Cu] Atualização por classe: 170315 [Lr] Data última revisão: 170315 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170301 [St] Status: MEDLINE [do] DOI: 10.1007/s10517-017-3634-0

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[PMID]: 28223021 [Au] Autor: Zhu Z; Fan X; Pan Y; Lu Y; Zeng W [Ad] Endereço: College of Animal Science and Technology, Northwest A&F University, Shaanxi, 712100, China. [Ti] Título: Trehalose improves rabbit sperm quality during cryopreservation. [So] Source: Cryobiology;75:45-51, 2017 Apr. [Is] ISSN: 1090-2392 [Cp] País de publicação: Netherlands [La] Idioma: eng [Ab] Resumo: High levels of reactive oxygen species are associated with spermatozoa cryopreservation, which bring damage to functional spermatozoa. The aim of the present study was to investigate whether and how the freezing extenders supplemented with trehalose was beneficial for the survival of rabbit spermatozoa. semen was diluted with Tris-citrate-glucose extender addition of different concentrations of trehalose. Addition of 100 mM trehaose significantly improved post-thaw rabbit sperm parameters, such as motility, acrosome integriy, membrane integrity and mitochondrial membrane potential. Moreover, when freezing extenders supplemented with trehalose, activities of catalase (CAT), superoxide dismutase (SOD) and total antioxidant capacity (T-AOC) of post-thaw spermatozoa were enhanced, meanwhile, reactive oxygen species (ROS) level and Malondialdehyde (MDA) content were decreased. The results suggest that freezing extenders supplemented with 100 mM trehalose resulted in less ROS level and MDA content, higher motility and mitochondrial membrane potential as well as the integrity of acrosome and plasma membrane. Supplementation of trehalose with freezing extenders is beneficial to the rabbit breeding industry. [Mh] Termos MeSH primário: Criopreservação/métodos Crioprotetores/farmacologia Preservação do Sêmen/métodos Trealose/farmacologia [Mh] Termos MeSH secundário: Acrossomo/efeitos dos fármacos Animais Catalase/metabolismo Ácido Cítrico/farmacologia Criopreservação/veterinária Congelamento Glucose/farmacologia Masculino Malondialdeído/metabolismo Potencial da Membrana Mitocondrial/efeitos dos fármacos Coelhos Espécies Reativas de Oxigênio/metabolismo Preservação do Sêmen/veterinária Motilidade Espermática/efeitos dos fármacos Superóxido Dismutase/metabolismo Trometamina/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Cryoprotective Agents); 0 (Reactive Oxygen Species); 023C2WHX2V (Tromethamine); 2968PHW8QP (Citric Acid); 4Y8F71G49Q (Malondialdehyde); B8WCK70T7I (Trehalose); EC 1.11.1.6 (Catalase); EC 1.15.1.1 (Superoxide Dismutase); IY9XDZ35W2 (Glucose) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170907 [Lr] Data última revisão: 170907 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170223 [St] Status: MEDLINE

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[PMID]: 28167741 [Au] Autor: De Min A; Matera C; Bock A; Holze J; Kloeckner J; Muth M; Traenkle C; De Amici M; Kenakin T; Holzgrabe U; Dallanoce C; Kostenis E; Mohr K; Schrage R [Ad] Endereço: Pharmacology and Toxicology Section, Institute of Pharmacy (A.D.M., J.H., C.T., K.M., R.S.), Research Training Group 1873 (A.D.M., E.K., K.M.), and Molecular-, Cellular-, and Pharmacobiology Section, Institute of Pharmaceutical Biology (E.K.), University of Bonn, Bonn, Germany; Dipartimento di Scien [Ti] Título: A New Molecular Mechanism To Engineer Protean Agonism at a G Protein-Coupled Receptor. [So] Source: Mol Pharmacol;91(4):348-356, 2017 Apr. [Is] ISSN: 1521-0111 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Protean agonists are of great pharmacological interest as their behavior may change in magnitude and direction depending on the constitutive activity of a receptor. Yet, this intriguing phenomenon has been poorly described and understood, due to the lack of stable experimental systems and design strategies. In this study, we overcome both limitations: First, we demonstrate that modulation of the ionic strength in a defined experimental set-up allows for analysis of G protein-coupled receptor activation in the absence and presence of a specific amount of spontaneous receptor activity using the muscarinic M acetylcholine receptor as a model. Second, we employ this assay system to show that a dualsteric design principle, that is, molecular probes, carrying two pharmacophores to simultaneously adopt orthosteric and allosteric topography within a G protein-coupled receptor, may represent a novel approach to achieve protean agonism. We pinpoint three molecular requirements within dualsteric compounds that elicit protean agonism at the muscarinic M acetylcholine receptor. Using radioligand-binding and functional assays, we posit that dynamic ligand binding may be the mechanism underlying protean agonism of dualsteric ligands. Our findings provide both new mechanistic insights into the still enigmatic phenomenon of protean agonism and a rationale for the design of such compounds for a G protein-coupled receptor. [Mh] Termos MeSH primário: Engenharia de Proteínas Receptores Acoplados a Proteínas-G/agonistas [Mh] Termos MeSH secundário: Regulação Alostérica Animais Células CHO Cricetinae Cricetulus Seres Humanos Ligantes Ligação Proteica Receptor Muscarínico M2/metabolismo Receptores Acoplados a Proteínas-G/metabolismo Trometamina [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Ligands); 0 (Receptor, Muscarinic M2); 0 (Receptors, G-Protein-Coupled); 023C2WHX2V (Tromethamine) [Em] Mês de entrada: 1705 [Cu] Atualização por classe: 170509 [Lr] Data última revisão: 170509 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170208 [St] Status: MEDLINE [do] DOI: 10.1124/mol.116.107276

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[PMID]: 28161633 [Au] Autor: Okai M; Yamamura A; Hayakawa K; Tsutsui S; Miyazono KI; Lee WC; Nagata K; Inoue Y; Tanokura M [Ad] Endereço: Department of Applied Biological Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-8657, Japan; Tokyo University of Marine Science and Technology, 4-5-7 Konan, Minato-ku, Tokyo 108-8477, Japan. [Ti] Título: Insight into the transition between the open and closed conformations of Thermus thermophilus carboxypeptidase. [So] Source: Biochem Biophys Res Commun;484(4):787-793, 2017 Mar 18. [Is] ISSN: 1090-2104 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Carboxypeptidase cleaves the C-terminal amino acid residue from proteins and peptides. Here, we report the functional and structural characterizations of carboxypeptidase belonging to the M32 family from the thermophilic bacterium Thermus thermophilus HB8 (TthCP). TthCP exhibits a relatively broad specificity for both hydrophilic (neutral and basic) and hydrophobic (aliphatic and aromatic) residues at the C-terminus and shows optimal activity in the temperature range of 75-80 °C and in the pH range of 6.8-7.2. Enzyme activity was significantly enhanced by cobalt or cadmium and was moderately inhibited by Tris at 25 °C. We also determined the crystal structure of TthCP at 2.6 Å resolution. Two dimer types of TthCP are present in the crystal. One type consists of two subunits in different states, open and closed, with a C RMSD value of 2.2 Å; the other type consists of two subunits in the same open state. This structure enables us to compare the open and closed states of an M32 carboxypeptidase. The TthCP subunit can be divided into two domains, L and S, which are separated by a substrate-binding groove. The L and S domains in the open state are almost identical to those in the closed state, with C RMSD values of 0.84 and 0.53 Å, respectively, suggesting that the transition between the open and closed states proceeds with a large hinge-bending motion. The superimposition between the closed states of TthCP and BsuCP, another M32 family member, revealed that most putative substrate-binding residues in the grooves are oriented in the same direction. [Mh] Termos MeSH primário: Carboxipeptidases/química Modelos Químicos Simulação de Dinâmica Molecular Thermus thermophilus/enzimologia [Mh] Termos MeSH secundário: Sítios de Ligação Ativação Enzimática Ligação Proteica Conformação Proteica Relação Estrutura-Atividade Especificidade por Substrato Trometamina [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 023C2WHX2V (Tromethamine); EC 3.4.- (Carboxypeptidases) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 171120 [Lr] Data última revisão: 171120 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170206 [St] Status: MEDLINE

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[PMID]: 28126741 [Au] Autor: Paranagama N; Bonnett SA; Alvarez J; Luthra A; Stec B; Gustafson A; Iwata-Reuyl D; Swairjo MA [Ad] Endereço: Department of Chemistry and Biochemistry, San Diego State University, 5500 Campanile Drive, San Diego, CA 92182, U.S.A. [Ti] Título: Mechanism and catalytic strategy of the prokaryotic-specific GTP cyclohydrolase-IB. [So] Source: Biochem J;474(6):1017-1039, 2017 Mar 07. [Is] ISSN: 1470-8728 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Guanosine 5'-triphosphate (GTP) cyclohydrolase-I (GCYH-I) catalyzes the first step in folic acid biosynthesis in bacteria and plants, biopterin biosynthesis in mammals, and the biosynthesis of 7-deazaguanosine-modified tRNA nucleosides in bacteria and archaea. The type IB GCYH (GCYH-IB) is a prokaryotic-specific enzyme found in many pathogens. GCYH-IB is structurally distinct from the canonical type IA GCYH involved in biopterin biosynthesis in humans and animals, and thus is of interest as a potential antibacterial drug target. We report kinetic and inhibition data of GCYH-IB and two high-resolution crystal structures of the enzyme; one in complex with the reaction intermediate analog and competitive inhibitor 8-oxoguanosine 5'-triphosphate (8-oxo-GTP), and one with a tris(hydroxymethyl)aminomethane molecule bound in the active site and mimicking another reaction intermediate. Comparison with the type IA enzyme bound to 8-oxo-GTP (guanosine 5'-triphosphate) reveals an inverted mode of binding of the inhibitor ribosyl moiety and, together with site-directed mutagenesis data, shows that the two enzymes utilize different strategies for catalysis. Notably, the inhibitor interacts with a conserved active-site Cys149, and this residue is S-nitrosylated in the structures. This is the first structural characterization of a biologically S-nitrosylated bacterial protein. Mutagenesis and biochemical analyses demonstrate that Cys149 is essential for the cyclohydrolase reaction, and S-nitrosylation maintains enzyme activity, suggesting a potential role of the -nitrosothiol in catalysis. [Mh] Termos MeSH primário: Proteínas de Bactérias/química GTP Cicloidrolase/química Guanosina Trifosfato/análogos & derivados Neisseria gonorrhoeae/química Trometamina/química [Mh] Termos MeSH secundário: Proteínas de Bactérias/antagonistas & inibidores Proteínas de Bactérias/genética Proteínas de Bactérias/metabolismo Domínio Catalítico Clonagem Molecular Cristalografia por Raios X Inibidores Enzimáticos/química Escherichia coli/genética Escherichia coli/metabolismo GTP Cicloidrolase/antagonistas & inibidores GTP Cicloidrolase/genética GTP Cicloidrolase/metabolismo Expressão Gênica Guanosina Trifosfato/química Cinética Modelos Moleculares Mutação Neisseria gonorrhoeae/enzimologia Ligação Proteica Conformação Proteica em alfa-Hélice Conformação Proteica em Folha beta Domínios e Motivos de Interação entre Proteínas Proteínas Recombinantes/química Proteínas Recombinantes/genética Proteínas Recombinantes/metabolismo S-Nitrosotióis/química Especificidade por Substrato [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Bacterial Proteins); 0 (Enzyme Inhibitors); 0 (Recombinant Proteins); 0 (S-Nitrosothiols); 023C2WHX2V (Tromethamine); 21238-36-8 (8-hydroxyguanosine triphosphate); 86-01-1 (Guanosine Triphosphate); EC 3.5.4.16 (GTP Cyclohydrolase) [Em] Mês de entrada: 1706 [Cu] Atualização por classe: 170818 [Lr] Data última revisão: 170818 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170128 [St] Status: MEDLINE [do] DOI: 10.1042/BCJ20161025

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[PMID]: 28029371 [Au] Autor: Siyve S; Ulusoy O; Karakus OZ; Murat N; Uslu ME; Ates O; Hakgüder G; Olguner M; Akgür FM [Ad] Endereço: Department of Pediatric Surgery, Dokuz Eylül University, Medical School, Izmir, Turkey. [Ti] Título: The role of water-soluble meconium subfraction and lipid-soluble meconium subfraction on the superior mesenteric artery vasoconstriction in chick embryos. [So] Source: J Pediatr Surg;52(3):481-483, 2017 Mar. [Is] ISSN: 1531-5037 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: OBJECTIVE: Intraamniotic meconium has been responsible for intestinal damage in gastroschisis and meconium-dependent intestinal ischemia has been proposed to induce additional intestinal damage in gastroschisis. This study is aimed to determine the effects of lipid and water-soluble meconium subfractions on the contractility of the superior mesenteric artery (SMA). MATERIALS AND METHODS: The study was conducted on 18-day fertilized chick embryos (Gallus Domesticus). Meconium is fractioned into water and lipid-soluble components. Only one SMA tissue was prepared from each embryo and suspended in the organ bath. Isometric contraction responses (ICR) were created in SMA tissues by one hour of incubation in Krebs-Henseleit solution for each group. Groups consisted of control, meconium, water-soluble meconium subfraction and lipid-soluble meconium subfraction. ICR of the SMA specimens were evaluated with a transducer-amplifier system on a computer. The data were expressed (mean±1SD) as milliNewton (mN). RESULTS: The ICR of the meconium, water-soluble meconium subfraction and lipid-soluble meconium subfraction groups were significantly high when compared to the control group (p<0.01). The meconium and water-soluble meconium subfraction created more contraction response than the lipid-soluble meconium subfraction (p<0.01). The ICR of the meconium group was not different from the ICR of the water-soluble meconium subfraction group (p>0.05). CONCLUSION: Water-soluble meconium subfraction has a profound vasoconstrictor effect on the SMA compared to the lipid-soluble meconium subfraction. [Mh] Termos MeSH primário: Gastrosquise/fisiopatologia Enteropatias/fisiopatologia Mecônio/química Artéria Mesentérica Superior/fisiopatologia Vasoconstrição [Mh] Termos MeSH secundário: Animais Embrião de Galinha Gastrosquise/complicações Glucose/química Enteropatias/etiologia Intestinos/fisiopatologia Lipídeos/química Trometamina/química Água/química [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Krebs-Henseleit solution); 0 (Lipids); 023C2WHX2V (Tromethamine); 059QF0KO0R (Water); IY9XDZ35W2 (Glucose) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 170426 [Lr] Data última revisão: 170426 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161229 [St] Status: MEDLINE

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[PMID]: 27787885 [Au] Autor: Zhou C; Yool AJ; Byard RW [Ad] Endereço: The University of Adelaide School of Medicine, Frome Road, Adelaide, SA, 5005, Australia. [Ti] Título: An Isolated Perfused Rat Kidney Model for the Evaluation of the Effect of Glucose on Renal Tubular Epithelial Morphology. [So] Source: J Forensic Sci;62(1):126-130, 2017 01. [Is] ISSN: 1556-4029 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: An isolated perfused kidney model was used to evaluate the effect of hyperglycemia on renal tubular epithelial cell morphology. Ten Sprague-Dawley rat kidneys were perfused with Krebs-Henseleit buffer containing 70 mmol/L of glucose (five for 1 h and five for 2 h). Two control groups consisted of 10 kidneys perfused with Krebs-Henseleit buffer without hyperglycemia (five for 1 h and five for 2 h), and 10 nonperfused contralateral kidneys placed in the same environment for the same duration. The hyperglycemia group had significantly increased renal tubular vacuolization (p < 0.001) compared to both control groups at 1 and 2 h. The isolated perfused kidney model recapitulates the renal tubular vacuolization phenotype found in hyperglycemia and may be a potential tool for the investigation into causal factors in renal histology. The full pattern of the Armanni-Ebstein phenomenon was not, however, reproduced, suggesting that this change requires more time or involves more complex factors. [Mh] Termos MeSH primário: Células Epiteliais/patologia Túbulos Renais/patologia Vacúolos [Mh] Termos MeSH secundário: Animais Glucose/farmacologia Hiperglicemia/patologia Modelos Animais Ratos Sprague-Dawley Trometamina/farmacologia [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Krebs-Henseleit solution); 023C2WHX2V (Tromethamine); IY9XDZ35W2 (Glucose) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171011 [Lr] Data última revisão: 171011 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 161028 [St] Status: MEDLINE [do] DOI: 10.1111/1556-4029.13229

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[PMID]: 27491272 [Au] Autor: Ilbasmis-Tamer S; Tugcu-Demiroz F; Degim IT [Ad] Endereço: a Faculty of Pharmacy, Department of Pharmaceutical Technology , Gazi University , Etiler , Ankara , Turkey. [Ti] Título: Carbon nanotube membranes to predict skin permeability of compounds. [So] Source: Pharm Dev Technol;22(4):606-616, 2017 Jun. [Is] ISSN: 1097-9867 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: In the present study, carbon nanotube (CNT) membranes were prepared to predict skin penetration properties of compounds. A series of penetration experiments using Franz diffusion cells were performed with 16 different membrane compositions for model chemicals. Similar experiments were also carried out with same model molecules using five different commercially available synthetic membranes and human skins for the comparison. Model chemicals were selected as diclofenac, dexketoprofen and salicylic acid. Their permeability coefficients and flux values were calculated. Correlations between permeability values of model compounds for human skins and developed model membranes were investigated. Good correlations were obtained for CNT membrane, isopropyl myristate-treated CNT membrane (IM-CNT membrane) and bovine serum albumin-cholesterol, dipalmitoyl phosphatidyl choline-treated membrane (BSA-Cholesterol-DPPC-IM-CNT membrane). An artificial neural network (ANN) model was developed using some molecular properties and penetration coefficients from pristine CNT membranes to predict skin permeability values and quite good predictions were made. [Mh] Termos MeSH primário: Anti-Infecciosos/farmacocinética Anti-Inflamatórios não Esteroides/farmacocinética Diclofenaco/farmacocinética Cetoprofeno/análogos & derivados Membranas Artificiais Ácido Salicílico/farmacocinética Absorção Cutânea Trometamina/farmacocinética [Mh] Termos MeSH secundário: Animais Bovinos Colesterol/química Simulação por Computador Seres Humanos Cetoprofeno/farmacocinética Modelos Biológicos Miristatos/química Nanotubos de Carbono/química Nanotubos de Carbono/ultraestrutura Redes Neurais (Computação) Permeabilidade Soroalbumina Bovina/química Pele/metabolismo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Anti-Infective Agents); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Membranes, Artificial); 0 (Myristates); 0 (Nanotubes, Carbon); 023C2WHX2V (Tromethamine); 0RE8K4LNJS (isopropyl myristate); 144O8QL0L1 (Diclofenac); 27432CM55Q (Serum Albumin, Bovine); 90Y4QC304K (Ketoprofen); 97C5T2UQ7J (Cholesterol); N674F7L21E (dexketoprofen trometamol); O414PZ4LPZ (Salicylic Acid) [Em] Mês de entrada: 1704 [Cu] Atualização por classe: 171116 [Lr] Data última revisão: 171116 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160806 [St] Status: MEDLINE [do] DOI: 10.1080/10837450.2016.1221430

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[PMID]: 27375281 [Au] Autor: Pradiee J; Esteso MC; Castaño C; Toledano-Díaz A; Lopez-Sebastián A; Guerra R; Santiago-Moreno J [Ad] Endereço: Departamento de Reproducción Animal, INIA, Madrid, Spain. [Ti] Título: Conventional slow freezing cryopreserves mouflon spermatozoa better than vitrification. [So] Source: Andrologia;49(3), 2017 Apr. [Is] ISSN: 1439-0272 [Cp] País de publicação: Germany [La] Idioma: eng [Ab] Resumo: This work examines the effectiveness of a TCG (Tris, citric acid, glucose, 6% egg yolk and 5% glycerol) and a TEST (TES, Tris, glucose, 6% egg yolk and 5% glycerol) sperm extender in the freezing of mouflon spermatozoa at slow cooling rates, using different pre-freezing equilibration times (2-3 hr). It also examines the tolerance of mouflon spermatozoa to different concentrations of cryoprotectants (5, 10, 20% glycerol; 5%, 10%, 20% dimethyl sulfoxide; 6% polyvinylpyrrolidone) and/or sucrose (100, 300, 500 mm). The highest quality (p < .01) thawed spermatozoa were obtained when using the TEST extender and an equilibration time of 3 hr. Sperm motility and membrane integrity were strongly reduced when using rapid freezing rates (60-85°C min ), independent of the concentration of cryoprotectants. The lowest sucrose concentration (100 mm) provided the highest (p < .05) percentage of motile spermatozoa and live spermatozoa with an intact acrosome. Vitrified-warmed sperm variables were at their best when the spermatozoa was diluted in TCG-6% egg yolk + 100 mm sucrose and warmed at 60°C. Slow warming at 37°C strongly reduced (p < .05) sperm motility and viability. However, sperm vitrification returned lower fertility, sperm motility and sperm viability values than conventional sperm freezing. [Mh] Termos MeSH primário: Criopreservação/veterinária Crioprotetores/farmacologia Preservação do Sêmen/veterinária Carneiro Doméstico Motilidade Espermática/efeitos dos fármacos Espermatozoides/efeitos dos fármacos Vitrificação [Mh] Termos MeSH secundário: Animais Sobrevivência Celular/efeitos dos fármacos Ácido Cítrico/farmacologia Criopreservação/métodos Congelamento Glucose/farmacologia Glicerol/farmacologia Masculino Propano/análogos & derivados Propano/farmacologia Sacarose/farmacologia Ácidos Sulfônicos/farmacologia Fatores de Tempo Trometamina/farmacologia [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE [Nm] Nome de substância: 0 (2-((1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)amino)ethanesulfonic acid); 0 (Cryoprotective Agents); 0 (Sulfonic Acids); 023C2WHX2V (Tromethamine); 2968PHW8QP (Citric Acid); 57-50-1 (Sucrose); IY9XDZ35W2 (Glucose); PDC6A3C0OX (Glycerol); T75W9911L6 (Propane) [Em] Mês de entrada: 1705 [Cu] Atualização por classe: 170505 [Lr] Data última revisão: 170505 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 160705 [St] Status: MEDLINE [do] DOI: 10.1111/and.12629

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