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1.
J Cardiothorac Vasc Anesth ; 26(3): 395-402, 2012 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-22206712

RESUMEN

OBJECTIVES: Neuropsychological disorders are some of the most common complications of coronary artery bypass graft (CABG) surgery. The early diagnosis of postoperative brain damage is difficult and mainly based on the observation of specific brain injury markers. The aim of this study was to analyze the effects of volatile anesthesia (VA) on plasma total and ionized arteriovenous magnesium concentrations in the brain circulation (a-vtMg and a-viMg), plasma matrix metalloproteinase-9 (MMP-9), and glial fibrillary acidic protein (GFAP) in adult patients undergoing CABG surgery. DESIGN: An observational study. SETTING: The Department of Cardiac Surgery in a Medical University Hospital. PATIENTS AND METHODS: Studied parameters were measured during surgery and in the early postoperative period. Patients were assigned to 3 groups: group O, patients who did not receive VA; group ISO, patients who received isoflurane; and group SEV, patients who received sevoflurane. RESULTS: Ninety-two patients were examined. CABG surgery increased MMP-9 and GFAP. The highest MMP-9, GFAP, and the most dramatic disorders in a-vtMg and a-viMg were noted in group O. CONCLUSIONS: Cardiac surgery increased plasma MMP-9 and GFAP concentrations. Changes in MMP-9, GFAP, and arteriovenous tMg and iMg were significantly higher in group O. Volatile anesthetics, such as ISO or SEV, reduced plasma MMP-9, GFAP concentrations, and disturbances in a-vtMg and a-viMg.


Asunto(s)
Anestésicos por Inhalación/uso terapéutico , Lesiones Encefálicas/prevención & control , Puente de Arteria Coronaria/efectos adversos , Magnesio/sangre , Fármacos Neuroprotectores/uso terapéutico , Anciano , Biomarcadores/sangre , Encéfalo/metabolismo , Lesiones Encefálicas/diagnóstico , Lesiones Encefálicas/etiología , Femenino , Proteína Ácida Fibrilar de la Glía/sangre , Humanos , Isoflurano/uso terapéutico , Masculino , Metaloproteinasa 9 de la Matriz/sangre , Éteres Metílicos/uso terapéutico , Persona de Mediana Edad , Sevoflurano
2.
Cell Biochem Funct ; 30(3): 211-6, 2012 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-22125185

RESUMEN

Total parenteral nutrition (TPN) is essential for patients with postoperative impairing gastrointestinal function who are unable to receive and absorb oral/enteral feeding for at least 7 days. Oxidative stress plays a major role in the ethiopathogenesis of cancers. In this study, total antioxidant status (TAS), glutathione peroxidase (GPx), superoxide dismutase, malondialdehyde and ascorbic acid were studied in patients operated because of small intestine, colorectal or pancreatic cancer and subsequently receiving TPN in comparison with patients receiving standard nutrition after the operation. TAS level and GPx activity were decreased in patients with small intestine cancer but did not differ in patients with colorectal and pancreatic cancer before and after surgery. In all patient groups receiving TPN, superoxide dismutase activity after the surgery was kept at the same level as before. On the fifth day after the surgery, malondialdehyde concentration in each group was restored to the value observed before surgery. On the fifth day of TPN treatment, ascorbic acid concentration was increased in every group of patients. TPN applied during the postoperative period alleviates oxidative stress resulting from surgery. In the case of small intestine cancer, the addition of vitamins and antioxidants to the nutrition mixture seems to result in depletion of antioxidant enzymes' activities.


Asunto(s)
Antioxidantes/metabolismo , Neoplasias Gastrointestinales/terapia , Nutrición Parenteral Total , Anciano , Ácido Ascórbico/metabolismo , Procedimientos Quirúrgicos del Sistema Digestivo , Femenino , Neoplasias Gastrointestinales/metabolismo , Neoplasias Gastrointestinales/cirugía , Glutatión Peroxidasa/metabolismo , Humanos , Masculino , Malondialdehído/metabolismo , Persona de Mediana Edad , Estrés Oxidativo , Cuidados Posoperatorios , Superóxido Dismutasa/metabolismo
3.
Bioorg Med Chem ; 19(17): 5103-16, 2011 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-21839643

RESUMEN

Eleven novel 3-(2-furanyl)-8-aryl-7,8-dihydroimidazo[2,1-c][1,2,4]triazin-4(6H)-ones (12-22) were designed and obtained from appropriate 1-aryl-2-hydrazonoimidazolidines (1-11) by condensation reaction with 2-oxo-2-furanacetic acid and subsequent cyclocondensation of intermediate chain derivatives. IR, (1)H NMR and (13)C NMR spectra and elemental analyses confirmed the chemical structure of all the synthesized compounds. The reversed-phase HPLC method was optimized and proved to be applicable and reliable for the analysis of these unknown small molecules (12-22). These compounds were chromatographed on octadecyl silica (ODS) stationary phase and their hydrophobic parameters expressed as the log k(w) values were determined by RP-HPLC, using mixtures of methanol and water as mobile phases with different methanol concentrations. Octane-1-sulfonic acid sodium salt (OSA-Na) and 20% acetate buffer (pH 3.5) was added to the mobile phase (eluent containing 0.01 M/L OSA-Na in organic modifier (MeOH)-buffered mobile phase). The high values of regression coefficients (r >0.9841) for all the compounds investigated proved the excellent fit between experimental data and the Snyder-Soczewinski equation. Results obtained from the reversed-phase HPLC were compared both with those theoretically calculated and with those obtained from an ALOGPS 2.1. software by the use of nine different computational methods for estimation of log P. The predicted values of log P by use of AB log P algorithm revealed the best correlation with the experimental log k(w) values for the investigated solutes, since a good correlation (r=0.7760) between these quantities was found. The majority of novel imidazotriazinones were found to be evidently effective in vitro against human cancerous cells (HeLa and T47D) in an effective concentration of 50 µg/mL. Five compounds (13, 15, 16, 18 and 22) revealed remarkable antiproliferative activities and selective cytotoxicities for cancer cells over normal HSF cells. Therefore these ones may be considered as a basis for the design of novel useful non-toxic (13, 15 and 16) and low toxic (18 and 22) anticancer agents.


Asunto(s)
Antineoplásicos/síntesis química , Fibroblastos/efectos de los fármacos , Imidazoles/química , Triazinas/química , Antineoplásicos/química , Antineoplásicos/toxicidad , Línea Celular Tumoral , Cromatografía de Fase Inversa , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Interacciones Hidrofóbicas e Hidrofílicas , Espectroscopía de Resonancia Magnética , Conformación Molecular , Triazinas/síntesis química , Triazinas/toxicidad
4.
Magnes Res ; 23(4): 169-79, 2010 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-21169130

RESUMEN

BACKGROUND: Changes in plasma matrix metalloproteinase 9 (MMP-9) concentrations and parallel changes in brain magnesium homeostasis have not been examined in cardiac surgery patients. The purpose of the present study was to analyse these relationships in patients undergoing coronary artery bypass surgery (CABG) with extracorporeal circulation (ECC). Additionally, the effect of volatile anaesthetics was considered. PATIENTS AND METHODS: Adult patients undergoing CABG with ECC under general anaesthesia were studied. Plasma MMP-9 and total (tMg) and ionized (iMg) magnesium concentrations were measured during surgery and during the early postoperative period. The plasma arteriovenous (a-v) tMg and iMg differences in the brain circulation were considered to be markers for brain magnesium homeostasis. The Mini-Mental State Examination test and computer tomography were used to diagnose postoperative neuropsychological disorders (PNPDs). RESULTS: In total, 92 patients were examined. PNPDs were noted in 17 cases. Cardiac surgery resulted in increased plasma levels of MMP-9. The highest MMP-9 concentrations were observed in patients with PNPDs. MMP-9 concentrations strongly correlated with a-v tMg and a-v iMg differences. Compared with arterial measurements, venous tMg and iMg concentrations were higher during and immediately after surgery and lower during the early postoperative period. The most severe differences in a-v tMg and iMg were noted in patients with PNPDs. CONCLUSION: 1. Cardiac surgery resulted in an increase in plasma MMP-9 concentrations. 2. This increase in MMP-9 was significantly greater in patients with PNPDs. 3. The plasma MMP-9 concentration was correlated with disorders of brain Mg homeostasis.


Asunto(s)
Encéfalo/metabolismo , Puente de Arteria Coronaria , Magnesio/metabolismo , Metaloproteinasa 9 de la Matriz/sangre , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad
5.
Pharmacol Rep ; 61(5): 885-91, 2009.
Artículo en Inglés | MEDLINE | ID: mdl-19904012

RESUMEN

The aim of this work was to evaluate the possibility of using of the new selenoorganic ring compound, 3-(o-chlorobenzoylamino)-2-(o-tolylimino)-4-methyl-4-selenazoline, as a selenium supplement by investigating the influence of its short-term administration on Se accumulation and antioxidant status in kidney. For 10 days, adolescent male Wistar rats were treated with saline (control group), Na(2)SeO(3) (Se-IN group) or the studied compound (Se-ORG group) (5 x 10(-4) mg Se/g of once a day) via a stomach tube. The selenium concentration, total antioxidant status (TAS), activities of the antioxidant enzymes superoxide dismutase (SOD) and glutathione peroxidase (GPx), concentrations of ascorbic acid (AA) and reduced glutathione (GSH) and concentration of malonyldialdehyde (MDA) were determined in the kidney homogenates. TAS was significantly reduced in the Se-ORG group compared to the control. Reduced glutathione was markedly decreased in Se-treated animals compared to the control and in the Se-ORG group compared to the Se-IN group. Malonyldialdehyde was significantly increased in the Se-supplemented groups compared to the control group but considerably less so in the Se-ORG group. All other studied parameters displayed no significant differences. No increase in the accumulation of selenium and the partial impairment of the antioxidant status and enhancement of lipid peroxidation in the kidneys resulting from Se treatment could suggest that in the first period of administration, excess selenium was excreted with urine, leading to a disturbance of kidney functions. Comparison of the effect of our compound with that exerted by inorganic Na(2)SeO(3) suggests that the studied compound could be considered as a possible supplement after further investigations, including determination of selenium excretion with urine, as well as repetition of this study using a wide range of doses and periods of supplementation.


Asunto(s)
Antioxidantes/metabolismo , Riñón/efectos de los fármacos , Compuestos de Organoselenio/farmacología , Selenito de Sodio/farmacología , Animales , Ácido Ascórbico/metabolismo , Suplementos Dietéticos , Glutatión/efectos de los fármacos , Glutatión/metabolismo , Riñón/metabolismo , Peroxidación de Lípido/efectos de los fármacos , Masculino , Malondialdehído/metabolismo , Ratas , Ratas Wistar , Selenio/metabolismo
6.
Bioorg Med Chem Lett ; 19(17): 5095-100, 2009 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-19631534

RESUMEN

Molecular structure of 3,8-disubstituted 7,8-dihydroimidazo[2,1-c][1,2,4]triazin-4(6H)-ones (8-14) was confirmed by X-ray crystallography of 14. All the compounds were evaluated for their antitumour and antimetastatic activities in vitro. Furthermore, their cytotoxicities towards human normal cell line-HSF cells were established, allowing us to point out some structure-activity relationships. Among them, imidazotriazinone 12, revealing remarkable dose-dependent viability decreases in human myeloma RPMI 8226 cells, was found to be completely non-toxic towards normal HSF cells. In addition, heterobicycles 8-12 were proved to exhibit significant antimetastatic potentials in the motility assay.


Asunto(s)
Antineoplásicos/química , Triazinas/química , Antineoplásicos/síntesis química , Antineoplásicos/toxicidad , Línea Celular , Movimiento Celular/efectos de los fármacos , Cristalografía por Rayos X , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Conformación Molecular , Metástasis de la Neoplasia , Relación Estructura-Actividad , Triazinas/síntesis química , Triazinas/toxicidad
7.
Eur J Med Chem ; 43(2): 404-19, 2008 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-17531354

RESUMEN

3-Unsubstituted and 3-substituted-7-aryl-5H-6,7-dihydroimidazo[2,1-c][1,2,4]triazoles (1-14) were designed and obtained from biologically active 1-aryl-2-hydrazonoimidazolidines by cyclocondensation reaction with triethyl orthoformates (1-4), phenoxyacetic acid derivatives (5-13) and carbon disulfide (14), respectively. Their chemical structures were confirmed by IR, (1)H NMR, (13)C NMR, MS spectra and elemental analysis. In the high performance liquid chromatographic series of experiments, fourteen synthesized compounds (1-14) were chromatographed on octadecyl silica adsorbent and their lipophilicity parameter (logk(W)) was determined using various aqueous systems: mixture of water and organic modifiers (methanol - MeOH, acetonitrile - MeCN or dioxane - DX). Compounds 7 and 12 were evaluated for their cytotoxic activity against three cancer cell lines: human Caucasian colon adenocarcinoma cell line - LS180 (ECACC 87021202), human uterus carcinoma cell line - SiHa (ECACC 85060701) and human breast carcinoma cell line - T47D (ECACC 85102201). Compound 12 was found to be the most effective in vitro against human colon adenocarcinoma cell line (LS180). Moreover, the distinctly marked lower cytotoxicity of compounds 7 and 12 against the normal cell line - human skin fibroblasts (HSF) and almost several-fold higher against the examined cancer cell lines was ascertained. The cytotoxic effect of imidazotriazole 7 was noticed on DNA structure of breast cancer cell line (T47D) by using the comet assay. Compound 7 in concentration of 29.3 microM was found to possess efficiency for DNA strand breakage. In particular, this led to cutting of the DNA strands and formation of small fragments of DNA - two higher and one lighter in comparison with control DNA. Moreover, significant viability decreases in the human leukaemic RPMI 8226 cells treated with different concentrations of imidazotriazoles 8-12 were observed, suggesting their antiproliferative properties. Besides, three tested compounds (9, 13, 14) revealed significant antimicrobial activities with MIC values in the range of 30.9-44.0 microM. Compound 13 showed superior antibacterial activity to ampicillin and chloramphenicol in vitro, whereas 14 displayed superior antifungal activity to miconazole.


Asunto(s)
Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Lípidos/química , Triazoles/síntesis química , Triazoles/farmacología , Antiinfecciosos/química , Antineoplásicos/química , Línea Celular Tumoral , Daño del ADN , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Espectrofotometría Infrarroja , Triazoles/química
8.
Eur J Med Chem ; 43(5): 1085-94, 2008 May.
Artículo en Inglés | MEDLINE | ID: mdl-17868955

RESUMEN

Synthesis, structure elucidation and anticancer activities of novel fused 1,2,4-triazine aryl derivatives containing the ethoxycarbonyl (6-10) and carbohydrazide formations (11-15) are presented. Molecular structures of the synthesized compounds were confirmed by IR, (1)H NMR, (13)C NMR, EI-MS spectra and elemental analyses. Antitumour activities in vitro for heterobicyclic hydrazides of the type 11-14 were evaluated by BrdU method for human LS180, SiHa and T47D carcinoma cells. Amongst them, hydrazide 14 has exhibited remarkable inhibitory effect against SiHa and LS180 tumour cells, and simultaneously was found to be non-toxic towards the human normal cell line-HSF cells. Furthermore, the pulse field gel electrophoresis experiment was performed for characterizing DNA-cleaving activity of heterobicycle 14. The DNA fragments of 2500, 2000 and 500 kilobase pairs (kbp) were commonly detected in the cancer cell lines (SiHa, LS180 and T47D) treated with compound 14. DNA fragmentation pattern, since three types of fragments induced by the tested hydrazide of the type 14 were detected, suggesting a way of interaction with DNA. It is worth pointing out, that DNA strand breaks were also produced in human breast cancer (T47D) cells, a cell line where the induction of DNA fragmentation is very difficult. Moreover, the statistically significant apoptotic activity in T47D human breast cancer cells for the tested heterobicycle 14 was proved using the annexin V-binding assay. The antiproliferative properties in vitro for compounds 6-14 were evaluated by MTT method for human leukaemic Jurkat cells. Significant viability decreases in Jurkat cells treated with different concentrations of compounds 10 and 11 were observed, suggesting that these derivatives have antiproliferative activities. Their acute toxicities were established. For these compounds the influence on the central nervous system of mice in behavioural tests was examined. Molecular structure for free base of the intermediate 4 was confirmed by (1)H-(1)H COSY, HMBC and HMQC correlations.


Asunto(s)
Antineoplásicos/síntesis química , Compuestos Heterocíclicos con 2 Anillos/síntesis química , Hidrazinas/síntesis química , Imidazoles/síntesis química , Triazinas/síntesis química , Animales , Antineoplásicos/química , Antineoplásicos/farmacología , Apoptosis , Conducta Animal/efectos de los fármacos , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Roturas del ADN , Ensayos de Selección de Medicamentos Antitumorales , Compuestos Heterocíclicos con 2 Anillos/química , Compuestos Heterocíclicos con 2 Anillos/farmacología , Humanos , Hidrazinas/química , Hidrazinas/farmacología , Imidazoles/química , Imidazoles/farmacología , Masculino , Ratones , Relación Estructura-Actividad , Pruebas de Toxicidad Aguda , Triazinas/química , Triazinas/farmacología
9.
Magnes Res ; 21(4): 205-17, 2008 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-19271418

RESUMEN

UNLABELLED: The purpose of the study was to analyse the effects of different forms of magnesium supplementation on its serum concentrations and the frequency of atrial fibrillation in patients undergoing coronary artery bypass graft surgery with extracorporeal circulation (ECC). One hundred and twenty adult patients were examined. All of them received intravenous infusions of MgSO4 during surgery and the early postoperative period (18 hours). Moreover, some of them received preoperative Mg supplementation. Therefore, patients were divided into six groups: A) patients, receiving an intravenous infusion 3.33 mg of MgSO4 per min; B) those receiving preoperative, oral Mg supplementation (OPS-Mg) and intravenous 3.33 mg of MgSO4 per min; C) patients receiving intravenous 6.66 mg of MgSO4 per min; D) patients receiving OPS-Mg and 6.66 mg of MgSO4 per min; E) patients receiving intravenous 10 mg of MgSO4 per min; F) those receiving OPS-Mg and 10 mg of MgSO4 per min. Additionally, all patients were divided into three groups: O (patients, who did not receive dopamine or dobutamine infusions), DOP (those receiving dopamine infusions in doses dependent on their clinical state) and DOB (those receiving dobutamine infusions in doses dependent on their clinical state). Total serum Mg concentrations (Mg(t)) were measured at five points: 1) 10 min before anaesthesia; 2) 10 min after ECC; 3) 10 min after surgery, 4) in the morning of postoperative day 1, 5) in the morning of postoperative day 2. The data were analyzed statistically; values at the first measurement points were considered as baseline. In group A, Mg(t) decreased at time points 2, 3, 4. Similar changes were observed in group B, however, in both groups Mg(t) returned to the baseline value at time point 5. In groups C and D, Mg(t) decreased at point 2 and 3, whereas in groups E and F it was increased during all the study period. The changes in Mg(t) were slightly less in patients receiving OPS-Mg, these patients had a significantly higher Mg(t) at time point 1. Mg(t) decreased in the O, DOP and DOB groups at measurement points 2 and 3. Moreover, the lowest Mg(t) was observed in the DOP group. Atrial fibrillation (AF) was noted in 33 patients (27.5%). The highest percentage of patients with AF during the early postoperative days was observed in groups A and B (45%). In groups C, D, E and F, AF was detected in 25%, 20%, 20% and 10% of patients, respectively. The incidence of AF was significantly higher in groups A and B compared to the other groups. Moreover, episodes of AF were rarer in patients receiving preoperative, oral Mg supplementation. CONCLUSIONS: 1) ECC resulted in a decrease in Mg(t); 2) Mg infusion at the dose of 3.33 mg/min had little effect for the prevention of postoperative AF; 3) the infusion of 10 mg/min of MgSO4 maintained the level of Mg(t) during CABG and most effectively reduced AF; 4) OPS-Mg played a beneficial role in Mg(t) disturbances during CABG; 5) dopamine caused the most severe disturbances in serum Mg(t) concentration.


Asunto(s)
Fibrilación Atrial/prevención & control , Puente Cardiopulmonar , Magnesio , Adulto , Anciano , Anciano de 80 o más Años , Femenino , Humanos , Infusiones Intravenosas , Magnesio/administración & dosificación , Magnesio/sangre , Magnesio/uso terapéutico , Masculino , Persona de Mediana Edad
10.
Bioorg Med Chem ; 15(16): 5480-6, 2007 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-17572093

RESUMEN

The in vitro biological activities of novel derivatives of methyl and ethyl 2-(4-oxo-8-aryl-2H-3,4,6,7-tetrahydroimidazo[2,1-c][1,2,4]triazin-3-yl)acetates (3a, 3d-j) have been evaluated and are reported. The final heterobicycles (3a-j) were obtained from monocyclic 1-aryl-2-hydrazonoimidazolidines (2a-f) by addition and cyclization reaction with fumaric acid esters. In particular, compounds 3d and 3e were found to exhibit comparable antibacterial potencies in vitro as that of ampicillin. Heterobicycles of the 3e, 3g and 3j type were screened for their antiviral activities against the selected viruses' DNA (human adenovirus type 5-Ad-5) and RNA (human enterovirus-Echo-9). Simultaneously, their cytotoxicities towards HEK-293 and GMK cells were established. In particular, heterobicycle 3j, completely non-toxic for GMK cells, was found to exhibit virucidal properties against Echo-9 virus justifying its further investigation as the potential antiviral agent.


Asunto(s)
Antibacterianos/síntesis química , Antibacterianos/toxicidad , Antivirales/síntesis química , Antivirales/toxicidad , Ésteres/síntesis química , Ésteres/toxicidad , Triazinas/química , Antibacterianos/química , Antivirales/química , Línea Celular , Supervivencia Celular/efectos de los fármacos , Ésteres/química , Compuestos Heterocíclicos/síntesis química , Compuestos Heterocíclicos/química , Compuestos Heterocíclicos/toxicidad , Humanos , Estructura Molecular , Relación Estructura-Actividad
11.
Bioorg Med Chem ; 15(8): 2837-49, 2007 Apr 15.
Artículo en Inglés | MEDLINE | ID: mdl-17331732

RESUMEN

The series of 8-aryl-2,6,7,8-tetrahydroimidazo[2,1-c][1,2,4]triazine-3,4-diones (11-20) and 8-aryl-4-imino-2,3,7,8-tetrahydroimidazo[2,1-c][1,2,4]triazin-3(6H)-ones (21-25) were designed and their in vitro cytotoxic activities against human LS180, HeLa, T47D, A549 and RPMI 8226 carcinoma cells are presented. In the crystalline state molecule 12 exists as the predominant tautomeric 3-oxo form, whereas the second possible 3-hydroxy tautomer is not observed. Compound 19 revealed a strong affection to LS180 cancer cells at lower tested concentration (37.9 microM) and simultaneously was found to be non-toxic towards the normal cell line investigated--GMK cells. Furthermore, this compound was proved to possess the efficiency for DNA strand breakage of the examined cancer cell lines. However, imidazotriazin-3,4-dione 20 was able to cause significant viability decreases in human RPMI 8226 peripheral blood myeloma cells. Compound 22 has exhibited remarkable inhibitory effects against LS180 and A549 carcinoma cells, whereas 24 revealed the highest growth inhibition against A549 cell line. Simultaneously, at lower tested concentration these compounds were proved to be completely non-toxic for GMK cells. Moreover, cytotoxic and antibacterial properties of starting, tautomeric 1-aryl-2-hydrazonoimidazolidines (1-6 and 8-9) are presented. Six of them (1-2, 4-6 and 9) proved active as antimicrobials. All these compounds revealed MIC values in the range of 15.0-78.6 microM. Their activities were compared to those of ampicillin and chloramphenicol.


Asunto(s)
Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Imidazoles/síntesis química , Imidazoles/farmacología , Triazinas/síntesis química , Triazinas/farmacología , Ampicilina/farmacología , Animales , Antibacterianos/síntesis química , Antibacterianos/farmacología , Bacterias/efectos de los fármacos , Línea Celular Tumoral , Fenómenos Químicos , Química Física , Cloranfenicol/farmacología , Chlorocebus aethiops , Cristalografía por Rayos X , Daño del ADN , ADN de Neoplasias/química , ADN de Neoplasias/efectos de los fármacos , Células HeLa , Humanos , Indicadores y Reactivos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Pruebas de Sensibilidad Microbiana , Modelos Moleculares , Conformación Molecular , Estereoisomerismo , Relación Estructura-Actividad
12.
Bone ; 39(1): 100-5, 2006 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-16469550

RESUMEN

Skeletal disorders in rapidly growing poultry are commonplace. This study was performed to investigate the effect of ornithine alpha-ketoglutarate (OKG) administration during the last 7 weeks of life on structural properties, mineralization, and mechanical endurance of skeleton in turkeys at slaughter. Healthy HB Medium Bronze female turkeys were randomly assigned to two weight-matched groups at the age of 12 weeks. OKG was administered orally to the experimental group (N=17) at the dose of 0.4 g/kg body weight per day, while the control group (N=16) received an equal dose of the vehicle. The turkeys were slaughtered at the age of 19 weeks and the tibiae were isolated for analysis. The effect of OKG on skeletal system development in turkeys was evaluated in relation to both geometrical and mechanical properties as well as quantitative computed tomography (QCT). Free amino acids concentrations were assessed with the use of ion-exchange chromatography. Significantly increased bone mineral density of the trabecular and the cortical bone of tibia in the turkeys given OKG for the last 7 weeks of production cycle were observed (P<0.05). OKG administration improved mechanical endurance of the tibia estimated by the three-point bending test (P<0.01). Plasma amino acid analyses showed increased level of aspartate, proline, alanine, valine, isoleucine, leucine, and ornithine (all P<0.05) after OKG treatment, whereas cystathionine concentration was decreased (P=0.03). Obtained results indicate that oral OKG administration has beneficial effects on skeletal development in fast growing turkeys and this effect is connected with increased amino acid synthesis. These observations may serve to improve skeletal properties in birds, especially when considering that skeletal disorders often affect the tibia and the proper function of the skeletal system plays an essential role in animal welfare and poultry production.


Asunto(s)
Densidad Ósea/efectos de los fármacos , Ornitina/análogos & derivados , Tibia/efectos de los fármacos , Pavos/metabolismo , Aminoácidos/sangre , Animales , Fenómenos Biomecánicos , Femenino , Ornitina/administración & dosificación , Ornitina/metabolismo , Ornitina/farmacología , Distribución Aleatoria , Pavos/sangre
13.
Magnes Res ; 17(2): 79-84, 2004 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-15319138

RESUMEN

The neoplasmic process causes the disturbance of magnesium metabolism in the organism. The studies were conducted in order to determine magnesium concentration in the tissues and serum of dogs with malignant and non-malignant mammary tumours in comparison to its concentration in the tissue and serum of healthy dogs. From the studies presented in the paper it turns out that magnesium concentration in the mammary neoplasmic tissue increases with the increase of tumour malignancy and in comparison to its concentration in the control tissue. Magnesium concentration in the blood serum decreases with the increase of tumour malignancy and in comparison to the control tissue. Therefore it was shown that there is a connection between the degree of tumour malignancy and magnesium concentration in the tissue and serum.


Asunto(s)
Magnesio/metabolismo , Neoplasias Mamarias Animales/metabolismo , Animales , Perros , Femenino , Humanos , Magnesio/sangre , Neoplasias Mamarias Animales/etiología
14.
Pol Merkur Lekarski ; 17(101): 523-7, 2004 Nov.
Artículo en Polaco | MEDLINE | ID: mdl-15754649

RESUMEN

Melatonin is a hormone produced in human by the pineal body, the endocrine gland localized in the central part of cerebrum. It regulates many vital processes. Its main and best known effect is restoring the natural cycle of organism functions. It is safe and non-addictive sleep-inducing drug, which can eliminate disruptions in our circadian rhythm, in such situations as shift working, changing of time zones (during intercontinental air travelling) or insomnia. It improves mood and quality of sleep. Melatonin function consisting in stabilization of biological rhythms, free radical scavenging or immune system stimulating can delay aging processes. Its appropriate supplementation can prolong life even by decades, keeping our body in good both physical and psychological condition. Additionally, profitable for health properties of melatonin include ability to control some illnesses (prophylaxis of cardiovascular system diseases, neoplastic diseases and other functional disorders of organisms). It makes the immune system stronger, decreases susceptibility of the organism to stress, and improves mood and general feeling.


Asunto(s)
Ritmo Circadiano/efectos de los fármacos , Melatonina/farmacología , Afecto/efectos de los fármacos , Envejecimiento/efectos de los fármacos , Humanos , Sistema Inmunológico/efectos de los fármacos , Trastornos del Sueño del Ritmo Circadiano/tratamiento farmacológico
15.
Artículo en Inglés | MEDLINE | ID: mdl-16146056

RESUMEN

Acute and chronic ischaemic diseases are among the main death reasons and civilized world menace. Branched chain amino acids (BCAAs): valine (Val), leucine (Leu), and isoleucine (Ile) are the main source of nitrogen to glutamine (Gln) and alanine (Ala) synthesis in muscles. In numerous cachexy-producing illnesses such as cancer, sepsis, diverse injuries and heart diseases increased consumption of BCAAs occurs. In myocardial ischemia BCAAs derived from the mobilization of muscle protein may be an important alternative energy substrate for the heart. BCAAs are oxidative energy substrates for the heart and may exert anabolic effects on myocardial protein (8). The aim of our study was to determine branched chain amino acids (BCAAs) concentrations in blood plasma of patients with chronic and acute ischeamic heart disease and to find out changes that those amino acids undergo during the first five days of patients' hospitalization.


Asunto(s)
Aminoácidos de Cadena Ramificada/sangre , Infarto del Miocardio/sangre , Isquemia Miocárdica/sangre , 3-Metil-2-Oxobutanoato Deshidrogenasa (Lipoamida)/metabolismo , Adulto , Anciano , Femenino , Humanos , Masculino , Persona de Mediana Edad
16.
Artículo en Inglés | MEDLINE | ID: mdl-16146061

RESUMEN

Magnesium plays very important metabolic and regulatory roles in the animal organism. On this element tissues' concentration may have an influence other factors, such as sex hormones and vitamin E. The aim of our paper was to determine the influence of various testosterone doses given to male rats and various estradiol doses given to female rats on tissue magnesium concentration. Moreover, we analysed the influence of vitamin E applied with sex hormones on magnesium concentration in the tested groups of male and female rats. Testosterone was given to male rats at the doses of 0.01 mg kg(-1) of b.w. and 0.1 mg kg(-1) of b.w. Estradiol was given to female rats at the doses of 0.01 mg kg(-1) of b.w. and 0.1 mg kg(-1) of b.w. Some groups of animals additionally received vitamin E at the dose of 100 mg kg(-1) of b.w. The experiment was conducted for two weeks and next the brain, liver, kidneys and heart were taken for analysis. Tissue magnesium concentration was studied. We showed that sex hormones (estradiol in females, testosterone in males) influenced magnesium concentration reduction in the tested tissues. This decrease depended on the dose of applied hormone and only insignificantly on its kind. It was showed that simultaneously applied vitamin E diminished the effect of sex hormones action on magnesium concentration in the tested tissues.


Asunto(s)
Estradiol/farmacología , Magnesio/análisis , Testosterona/farmacología , Vitamina E/farmacología , Animales , Relación Dosis-Respuesta a Droga , Femenino , Magnesio/metabolismo , Masculino , Ratas , Ratas Wistar
17.
Artículo en Inglés | MEDLINE | ID: mdl-16146065

RESUMEN

Ascorbic acid concentration in a living body undergoes alterations continually. The changes in homeostasis of this important antioxidant may be induced by the effect of sex hormones for example. Based on this, the aim of our work was to estimate the influence of sex hormones administration and vitamin E supplementation on tissue ascorbic acid concentration in female and male rats. It has been showed that estrogen administration to females resulted in vitamin C loss, while testosterone administration to males elevated this level in all the tested tissues. However, the supplementation of vitamin E during sex hormones administration had beneficial effects on the tissue ascorbic acid concentration.


Asunto(s)
Ácido Ascórbico/análisis , Estradiol/farmacología , Testosterona/farmacología , Vitamina E/farmacología , Animales , Ácido Ascórbico/metabolismo , Relación Dosis-Respuesta a Droga , Femenino , Masculino , Ratas , Ratas Wistar
18.
Artículo en Inglés | MEDLINE | ID: mdl-16146140

RESUMEN

Heavy metals are too well-known environmental pollutants of particularly dangerous effect to human health. Because of their wide usage in many industrial branches they are present everywhere in the air, water and soils. Food contamination by heavy elements is hard to avoid and it is a result of environmental contamination by dusts, industrial gases, sewage, waste and coal burning processes. One of the most harmful heavy metals, widely spread in nature is cadmium. Toxic cadmium action involves free oxygen generation and inactivation of protein containing cysteine residues with -SH groups. It influences many metabolic processes causing great damage in many organs. Cadmium can also interact with some essential elements leading to their homeostasis disorders.


Asunto(s)
Cadmio/toxicidad , Cadmio/metabolismo , Calcio/metabolismo , Exposición a Riesgos Ambientales , Humanos , Sistema Inmunológico/efectos de los fármacos , Oxígeno/metabolismo
19.
Artículo en Inglés | MEDLINE | ID: mdl-12898914

RESUMEN

Ascorbic acid and selenium are important antioxidants for the reactive forms of oxygen. The purpose of these experiments was to determine the influence of various concentrations of cadmium on ascorbic acid and selenium concentrations in certain tissues of rats. The results showed that cadmium, added to rats' feed, influenced the concentration of ascorbic acid in blood serum and tested rats' tissues. Cadmium influenced the concentration of selenium in certain tissues as well. Furthermore, it has been demonstrated that ascorbic acid and selenium concentrations are dependent on the type of tissue tested as well as on the size of cadmium concentrations and length of the experiments.


Asunto(s)
Ácido Ascórbico/sangre , Intoxicación por Cadmio/sangre , Selenio/sangre , Animales , Cadmio/farmacocinética , Cadmio/toxicidad , Relación Dosis-Respuesta a Droga , Masculino , Ratas , Ratas Wistar , Factores de Tiempo , Distribución Tisular
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