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1.
Braz. j. med. biol. res ; 50(11): e6353, 2017. tab, graf
Article in English | LILACS | ID: biblio-888951

ABSTRACT

This study aimed to investigate the absorption mechanism of three curcumin constituents in rat small intestines. Self-emulsification was used to solubilize the three curcumin constituents, and the rat in situ intestinal perfusion method was used to study factors on drug absorption, including drug mass concentration, absorption site, and the different types and concentrations of absorption inhibitors. Within the scope of experimental concentrations, three curcumin constituents were absorbed in rat small intestines through the active transport mechanism.


Subject(s)
Animals , Male , Female , Adjuvants, Pharmaceutic/pharmacology , Curcumin/analogs & derivatives , Curcumin/pharmacokinetics , Enzyme Inhibitors/pharmacokinetics , Intestinal Absorption , Intestine, Small/metabolism , Reference Values , Time Factors , Uncoupling Agents/pharmacology , Verapamil/pharmacology , Probenecid/pharmacology , Reproducibility of Results , Chromatography, High Pressure Liquid/methods , Rats, Sprague-Dawley , ATP-Binding Cassette Transporters/antagonists & inhibitors , 2,4-Dinitrophenol/pharmacokinetics , Curcumin/chemistry , Multidrug Resistance-Associated Proteins/analysis , Multidrug Resistance-Associated Proteins/antagonists & inhibitors , Emulsions , Perfusion Imaging/methods , Intestinal Absorption/drug effects , Intestine, Small/drug effects
2.
Rev. bras. parasitol. vet ; 23(4): 428-434, Oct-Dec/2014. tab, graf
Article in English | LILACS | ID: lil-731249

ABSTRACT

Three hemoplasma species are recognized in domestic cats: Mycoplasma haemofelis, ‘Candidatus Mycoplasma haemominutum’ and ‘Candidatus Mycoplasma turicensis’. We report the prevalence and hematological abnormalities of hemoplasma infection in 369 domestic cats from three different populations (blood donors, hospitalized cats and shelter cats) from Southern Brazil. Complete blood counts were performed at the time of blood collection, and DNA was extracted and tested by conventional PCR for each hemoplasma species. A total of 79 samples (21.40%) were positive for at least one species. The most prevalent hemoplasma was ‘Candidatus Mycoplasma haemominutum’, with 50/369 (13.55%) positive cats, followed by ‘Candidatus Mycoplasma turicensis’, 10/369 (2.71%), and Mycoplasma haemofelis, 8/369 (2.16%). Mycoplasma haemofelis and ‘Candidatus Mycoplasma haemominutum’ coinfection was observed in 4/369 (1.08%), whereas ‘Candidatus Mycoplasma haemominutum’ and ‘Candidatus Mycoplasma turicensis’ in 5/369 (1.35%). Three cats (0.81%) were infected with all three hemoplasmas. There was no association between infection and the different populations. Anemia was associated with Mycoplasma haemofelis and ‘Candidatus Mycoplasma haemominutum’, but not with ‘Candidatus Mycoplasma turicensis’. Male cats and cats with outdoor access were more likely to be infected. Although ‘Candidatus Mycoplasma haemominutum’ is believed to cause minimal or no hematological alterations, the infected cats studied herein were more likely to be anemic.


Três espécies de hemoplasmas são reconhecidas em gatos domésticos: Mycoplasma haemofelis, ‘Candidatus Mycoplasma haemominutum’ e ‘Candidatus Mycoplasma turicensis’. A prevalência e alterações hematológicas associadas à infecção por hemoplasmas foi estudada, em 369 gatos domésticos de três populações distintas (doadores de sangue, hospitais e gatos de abrigo) do Sul do Brasil. Foram realizados hemogramas completos no momento da coleta de sangue e as amostras tiveram seu DNA extraído e testado por PCR convencional para cada espécie de hemoplasmas. Setenta e nove amostras (21,40%) foram positivas para pelo menos uma espécie. O mais prevalente foi ‘Candidatus Mycoplasma haemominutum’ com 50/369 (13,55%) gatos positivos, seguidos por ‘Candidatus Mycoplasma turicensis’ com 10/369 (2,71%) e Mycoplasma haemofelis com 8/369 (2,16%). Coinfecção por Mycoplasma haemofelis e ‘Candidatus Mycoplasma haemominutum’ foi observada em 4/369 (1,08%), enquanto ‘Candidatus Mycoplasma haemominutum’ e ‘Candidatus Mycoplasma turicensis’ coinfectaram 5/369 (1,35%) gatos. Três (0,81%) gatos apresentaram infecção pelos três hemoplasmas. Não houve associação entre a infecção e as diferentes populações. Anemia foi associada com a infecção por Mycoplasma haemofelis e ‘Candidatus Mycoplasma haemominutum’, mas não com ‘Candidatus Mycoplasma turicensis’. Gatos machos e com acesso à rua apresentaram maior probabilidade de serem infectados. Embora se acredite que ‘Candidatus Mycoplasma haemominutum’ possa causar alterações hematológicas mínimas ou ausentes, gatos infectados encontrados neste estudo foram mais propensos à anemia.


Subject(s)
Animals , Male , Rats , Hepatocytes/drug effects , Mitochondria, Liver/drug effects , NAD(P)H Dehydrogenase (Quinone)/metabolism , Oxidative Stress/drug effects , Ubiquinone/pharmacology , Cells, Cultured , Cytoprotection , Cell Membrane/drug effects , Cell Survival/drug effects , Glutathione/metabolism , Hepatocytes/enzymology , Membrane Potentials/drug effects , Mitochondria, Liver/enzymology , NAD , Oxidation-Reduction , Rats, Sprague-Dawley , Reactive Oxygen Species/metabolism , Rotenone/toxicity , Uncoupling Agents/toxicity , /pharmacology
3.
Journal of Korean Medical Science ; : 113-120, 2005.
Article in English | WPRIM | ID: wpr-110310

ABSTRACT

Apoptosis is a programmed, physiologic mode of cell death that plays an important role in tissue homeostasis. As for the central nervous system, ischemic insults can induce pathophysiologic cascade of apoptosis in neurophils. Impairment of astroctye functions during brain ischemia can critically influence neuron survival by neuronglia interactions. We aimed to elucidate the protective effect of ketamine on apoptosis by energy deprivation in astrocytes. Ischemic insults was induced with iodoacetate/ carbonylcyanide mchlorophenylhydrazone (IAA/CCCP) 1.5 mM/ 20 micrometer or 150 micrometer/2 micrometer for 1 hr in the HTB-15 and CRL-1690 astrocytoma cells. Then these cells were reperfused with normal media or ketamine (0.1 mM) containing media for 1 hr or 24 hr. FITC-annexin-V staining and propidium iodide binding were determined by using flow cytometry. Cell size and granularity were measured by forward and side light scattering properties of flow cytometry system, respectively. An addition of keta-mine during reperfusion increased the proportion of viable cells. Ketamine alleviated cell shrinkage and increased granularity during the early period, and ameliorated cell swelling during the late reperfusion period. Ketamine may have a valuable effect on amelioration of early and late apoptosis in the astrocytoma cells, even though the exact mechanism remains to be verified.


Subject(s)
Humans , Anesthetics, Dissociative/pharmacology , Annexin A5/pharmacology , Apoptosis , Astrocytes/metabolism , Astrocytoma/drug therapy , Brain/pathology , Carbonyl Cyanide m-Chlorophenyl Hydrazone/pharmacology , Cell Line, Tumor , Cell Size , Cell Survival , Central Nervous System/drug effects , Enzyme Inhibitors/pharmacology , Flow Cytometry/methods , Indicators and Reagents/pharmacology , Iodoacetates/pharmacology , Ischemia/pathology , Ketamine/metabolism , Light , Neurons/metabolism , Neutrophils/metabolism , Perfusion , Propidium/pharmacology , Scattering, Radiation , Time Factors , Uncoupling Agents/pharmacology
4.
Rev. chil. obes ; 6(1): 5-15, 2001. tab
Article in Spanish | LILACS | ID: lil-314845

ABSTRACT

In the last decade, specially after the discovery of leptin, several neuropeptides that regulate energy intake and expenditure have been described in animal models. This has partially unvelied the underlying mechanisms that regulate body composition and weight and therefore a promise of a more effective treatment of obesity and its comorbidities is ad portas


Subject(s)
Humans , Diabetes Mellitus, Type 2 , Insulin Resistance , Obesity , Appetite Regulation/genetics , Fatty Acids/genetics , Acylation , Diabetes Mellitus, Type 2 , Dopamine , Atrial Natriuretic Factor/pharmacology , Hypertension/etiology , Leptin , Lipolysis , Molecular Biology , Mutation/genetics , Neuropeptides/pharmacology , Obesity , Natriuretic Peptide, Brain/pharmacology , Natriuretic Peptide, C-Type/pharmacology , Peroxisome Proliferators , Protein Tyrosine Phosphatases/pharmacology , Receptors, Adrenergic, beta/genetics , Uncoupling Agents
5.
Braz. j. med. biol. res ; 33(12): 1413-20, Dec. 2000. graf
Article in English | LILACS | ID: lil-274906

ABSTRACT

Chemical modifications were used to identify some of the functionally important amino acid residues of the potato plant uncoupling protein (StUCP). The proton-dependent swelling of potato mitochondria in K+-acetate in the presence of linoleic acid and valinomycin was inhibited by mersalyl (Ki = 5 æM) and other hydrophilic SH reagents such as Thiolyte MB, iodoacetate and 5,5'-dithio-bis-(2-nitrobenzoate), but not by hydrophobic N-ethylmaleimide. This pattern of inhibition by SH reagents was similar to that of brown adipose tissue uncoupling protein (UCP1). As with UCP1, the arginine reagent 2,3-butadione, but not N-ethylmaleimide or other hydrophobic SH reagents, prevented the inhibition of StUCP-mediated transport by ATP in isolated potato mitochondria or with reconstituted StUCP. The results indicate that the most reactive amino acid residues in UCP1 and StUCP are similar, with the exception of N-ethylmaleimide-reactive cysteines in the purine nucleotide-binding site


Subject(s)
Animals , Cattle , Amino Acids/metabolism , Carrier Proteins/metabolism , Mitochondria/metabolism , Solanum tuberosum/metabolism , Uncoupling Agents/metabolism , Bridged Bicyclo Compounds/metabolism , Carrier Proteins/isolation & purification , Fluorescent Dyes/metabolism , Mitochondrial Swelling , Solanum tuberosum/chemistry
7.
Indian J Biochem Biophys ; 1998 Jun; 35(3): 161-5
Article in English | IMSEAR | ID: sea-26513

ABSTRACT

The effect of psychosine on the rate of respiration at different segments of the electron transport chain, respiratory control ratio and the efficiency of phosphorylation was studied. The transfer of electrons through site I, site II and site III was studied independently. The transfer through site I and site III was inhibited by psychosine, whereas the transfer through site II was not inhibited. Cardiolipin, which is essential for the electron transfer through site I and III, was implicated to be responsible for the inhibition of electron transfer by psychosine. Electron carriers of site II are not sensitive to cardiolipin, so psychosine could not inhibit the electron transfer through this site. The ADP/O ratio and respiratory control ratio were inhibited by psychosine showing that it has an uncoupler like effect. Mitochondria isolated from rat liver, kidney and brain behaved essentially the same way in their response to psychosine. Cytochrome c oxidase was significantly inhibited by psychosine and the degree of inhibition was almost same in mitochondria and sub mitochondrial particles. The preence of outer membrane in mitochondria did not make any difference with respect to the action of psychosine on electron transport chain. Psychosine interacts at site I and site III and a change in the lipid environment of the membrane is responsible for the mitochondrial dysfunctions induced by psychosine. This represents a possible mechanism for the destruction of cells in Gaucher's and Krabbe's disease.


Subject(s)
Animals , Brain/physiology , Cardiolipins/metabolism , Cell Respiration/drug effects , Electron Transport/drug effects , Electron Transport Complex IV , Enzyme Inhibitors/pharmacology , Gaucher Disease/physiopathology , Kidney/physiology , Leukodystrophy, Globoid Cell/physiopathology , Liver/physiology , Male , Mitochondria/drug effects , Oxidative Phosphorylation/drug effects , Phosphorylation , Psychosine/pharmacology , Rats , Rats, Wistar , Succinate Cytochrome c Oxidoreductase/metabolism , Uncoupling Agents/pharmacology
8.
Acta bioquím. clín. latinoam ; 30(4): 357-69, dic. 1996. ilus
Article in Spanish | LILACS | ID: lil-195413

ABSTRACT

La importancia de los pesticidas sintéticos orgánicos continuará creciendo acompañando al aumento de la población mundial y en tanto la proporción de tierra cultivable se mantenga relativamente constante. Los pesticidas permiten salvar el 10 por ciento de los cultivos pero todavía un 37 por ciento se pierden anualmente debido a la acción de las plagas. Se pueden tomar a los insecticidas como modelo para ilustrar la necesidad y posibilidades futuras de agroquímicos más eficaces y seguros para el hombre y su medio. Los insecticidas más importantes en ventas constituyen el 88 por ciento del total y actúan a nivel de sólo cuatro blancos moleculares (targets) nerviosos: Acetilcolinesterasa (AChE) el 62 por ciento; Canales de Sodio-dependientes de voltaje el 18 por ciento; Canales de Cloruro-dependientes de GABA (ácido gama aminobutírico) el 6 por ciento y Receptor Nicotínico para la acetilcolina el 2 por ciento. La utilidad de los tres "targets" primeros, será gradualmente comprometida debido a problemas de resistencia de insectos, en tanto que el receptor nicotínico para acetilcolina se espera que crezca significativamente. Los compuestos que actúan sobre targets No-Nerviosos se convertirán progresivamente en mucho más importantes. Dentro de éstos se incluyen a los desacoplantes de la fosforilación oxidativa, a los inhibidores de la NADH/Ubiquinona óxido-reductasa y a los inhibidores de la ATP-asa, a los reguladores del crecimiento (juvenoides, ecdisona) y a los pesticidas microbianos que actúan en varios nuevos targets. Con un panorama de 300 insecticidas comerciales disponibles en la actualidad y la prospectiva de introducción de no más de 2 ó 3 nuevos compuestos por año en promedio, sería esencial que se hiciera un uso lo más efectivo posible de los insecticidas corrientes. Los compuestos químicos más nuevos son en general más complejos y más costosos comparados con los anteriores, pero se los usa en general a dosis mucho menores resultando una relación costo/efectividad que resulta favorable a la economía minimizando además el impacto ambiental. Los nuevos compuestos son en general activos en contra de las cepas resistentes, integrales además a los programas de M.I.P. (manejo integrado de plagas) y suelen poseer una mínima toxicidad en los mamíferos


Subject(s)
Humans , Animals , Acetylcholinesterase/drug effects , Insect Control/statistics & numerical data , Insecticides/pharmacology , Pesticides/pharmacology , Chloride Channels , Cholinesterase Inhibitors/metabolism , Cholinesterase Inhibitors/pharmacokinetics , Pest Control, Biological/methods , Insect Control , Insect Control/economics , Insect Hormones , Insecticide Resistance/physiology , Insecticides/classification , Insecticides/toxicity , Pesticides/classification , Pesticides/toxicity , Receptors, Nicotinic , Sodium Channels/drug effects , Uncoupling Agents
9.
Braz. j. med. biol. res ; 26(4): 343-6, Apr. 1993. tab
Article in English | LILACS | ID: lil-148746

ABSTRACT

A mitochondrial pyrophosphatase (PPase) from yeast cells (Saccharomyces cerevisiae) was studied and characterized. The hydrolytic activity towards inorganic pyrophosphate (PPi) was inhibited by different SH-reagents and increased in the presence of uncouplers, indicating a possible involvement of this enzyme in energy-linked processes. This view was also supported by the observation that these mitochondria were able to hydrolyze PPi, generating an electrical membrane potential (delta psi) of the same magnitude as that obtained with ATP. Both ATP and PPi inhibited the pyruvate dehydrogenase complex and it was demonstrated that PPi can be used as substrate by mitochondrial kinases leading to the same pattern of protein phosphorylation as when ATP is used


Subject(s)
Diphosphates/metabolism , Mitochondria/enzymology , Saccharomyces cerevisiae/enzymology , Hydrolysis , Mitochondria/drug effects , Pyrophosphatases/drug effects , Pyrophosphatases/metabolism , Saccharomyces cerevisiae/drug effects , Sulfhydryl Reagents/pharmacology , Uncoupling Agents/pharmacology
10.
Bulletin of the Faculty of Science-University of Alexandria. 1987; 27 (4): 261-276
in English | IMEMR | ID: emr-8560

ABSTRACT

Light increased the capacity for nitrite absorption by Scenedesmus obliquus posaibly through the increased energy supply and/or the increased nitrite reductase activity. Assimilation was observed when normal algal cells were illuminated in the absence of CO[2]under aerobic condition. The rate of assimilation by-carbohydrate-deficient cultures depends on light and the presence of CO[2]. The failure of illuminated carbohydrate-deficient cells to reduce nitrite in absence of CO[2] seems to be due to the exhaustion of the respiratory substrates in the cells. The effect of uncoupling agents was studied in an attempt to clarify the relation between the photochemical reductant and the reduction of nitrite. Addition of DNP or KCN inhibited the utilization of nitrite by about 80% compared to about 28 percent with DCMU. Under heterotrophic conditions inhibition was almost the same. These results indicate that high energy phosphate is involved in the assimilation of nitrite by this alga


Subject(s)
Nitrites , Uncoupling Agents
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