RESUMEN
Leucoselect (grape seed selected proanthocyanidins) was analyzed. HPLC thermospray mass spectrometry (TSP-MS) allowed the detection of monomeric flavan-3-ols and dimeric proanthocyanidins. Fractionation over Sephadex LH-20 resin and analysis of the isolated fractions by gel permeation chromatography (GPC) and electrospray mass spectrometry (ESI-MS) led to the complete characterization of the proanthocyanidin constituents of Leucoselect. The analysis revealed the presence of approximately 15% of (+)-catechin (1) and (-)-epicatechin (2), 80% of (-)-epicatechin 3-O-gallate (3), dimers, trimers, tetramers and their gallates and 5% of pentamers, hexamers, heptamers and their gallates.
Asunto(s)
Antocianinas/química , Proantocianidinas , Rosales , Semillas , Cromatografía en Gel , Cromatografía Líquida de Alta Presión , Humanos , Espectrometría de MasasRESUMEN
A high-performance liquid chromatographic method was developed for electrospray mass spectrometric analysis of ginsenosides in Panax ginseng roots. The analyses were performed on a reversed-phase C18 column using a binary eluent (aqueous 8 mM NH4OAc, buffered to pH 7 with NH4OH-acetonitrile) under gradient conditions. Twenty-five ginsenosides could be separated and detected. The mass spectra obtained provided information on their molecular masses. A MS-MS experiment was undertaken in order to determine the sugar unit sequences and the aglycone moieties.
Asunto(s)
Cromatografía Líquida de Alta Presión/métodos , Espectrometría de Masas/métodos , Panax/química , Raíces de Plantas/química , Plantas Medicinales , Saponinas/análisis , Ginsenósidos , Sensibilidad y EspecificidadRESUMEN
The roots of T. x media Rehd. cv. Hicksii gave three novel analogues of paclitaxel modified at the N-acyl residue (N-debenzoyl-N-alpha-methylbutyryl paclitaxel and N-debenzoyl-N-cinnamoyl paclitaxel, 1b and 1c, respectively) or at the ester group at C-2 (2-debenzoyl-2-tigloyl paclitaxel, 1d). Compounds 1b and 1d showed reduced cytotoxicity and tubulin binding compared to paclitaxel, while 1c retained substantial activity in these assays.
Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Paclitaxel/análogos & derivados , Árboles/química , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Cromatografía Liquida , Ensayos de Selección de Medicamentos Antitumorales , Raíces de Plantas/química , Análisis Espectral , Relación Estructura-ActividadRESUMEN
The efficacies and safety of nicorandil, 20 mg b.d., and diltiazem, 60 mg t.d., in the treatment of stable angina pectoris were compared in a double-blind randomized parallel group study involving 123 patients. The duration of the study was 3 months. Exercise tolerance tests were performed by the patients when on placebo (day 0) and at the end of the study period (day 90). Both groups were comparable at day 0 in terms of demography and cardiovascular status. Nicorandil and diltiazem were both found to decrease the frequency of anginal attacks and the consumption of nitroglycerin tablets (P < 0.01). Maximum exercise capacity, the amount of work that could be performed before reaching ischaemic threshold, and the amount of work required to reach onset of angina were significantly increased for both groups of patients on day 90 compared with day 0 (increase in maximum exercise capacity: nicorandil--6.9 +/- 18.9 kj, diltiazem--9.6 +/- 16.2 kj, P = 0.44 ns; increase in work to ischaemic threshold: nicorandil--9.4 +/- 18.1 kJ, diltiazem--14.7 +/- 15.4 kJ, P = 0.10 ns; increase in work to onset of angina: nicorandil--10.0 +/- 20.1 kJ, diltiazem--11.4 +/- 14.9 kJ, P = 0.68 ns). Differences between the two groups were not significant. The double product of systolic blood pressure x heart rate and peak exercise for both drugs was either unchanged or slightly decreased at ischaemic threshold.(ABSTRACT TRUNCATED AT 250 WORDS)
Asunto(s)
Angina de Pecho/tratamiento farmacológico , Enfermedad Coronaria/tratamiento farmacológico , Diltiazem/administración & dosificación , Infarto del Miocardio/tratamiento farmacológico , Niacinamida/análogos & derivados , Canales de Potasio/efectos de los fármacos , Vasodilatadores/administración & dosificación , Anciano , Angina de Pecho/fisiopatología , Circulación Coronaria/efectos de los fármacos , Circulación Coronaria/fisiología , Enfermedad Coronaria/fisiopatología , Diltiazem/efectos adversos , Relación Dosis-Respuesta a Droga , Método Doble Ciego , Esquema de Medicación , Electrocardiografía/efectos de los fármacos , Prueba de Esfuerzo/efectos de los fármacos , Femenino , Humanos , Masculino , Persona de Mediana Edad , Infarto del Miocardio/fisiopatología , Niacinamida/administración & dosificación , Niacinamida/efectos adversos , Nicorandil , Canales de Potasio/fisiología , Vasodilatadores/efectos adversosRESUMEN
Fast atom bombardment mass spectrometry was used to characterize phospholipids from tubuli and glomeruli of normal rats and rats with acute renal failure. It was possible to assess the molecular species of the principal phospholipidic classes. In all of them, the most abundant species contained a residue of arachidonic acid. The phospholipids of urine were also analyzed, showing the presence of the major molecular species of several phospholipid classes. Excretion of phospholipids was greater in urine from rats with acute renal failure.
Asunto(s)
Lesión Renal Aguda/metabolismo , Glomérulos Renales/química , Túbulos Renales Proximales/química , Fosfolípidos/análisis , Espectrometría de Masa Bombardeada por Átomos Veloces , Animales , Masculino , Fosfolípidos/orina , Ratas , Ratas Sprague-DawleyRESUMEN
The origin of platelet-activating factor (PAF) in the urine remains ill defined. The present study documents that [3H]PAF (3.5 mu Ci) injected into the renal artery of isolated control rat kidney preparations perfused at constant pressure with a cell-free medium containing 1% bovine serum albumin (BSA) was excreted in negligible amounts (0.034%) in the urine, whereas 6% was retained by the kidney. When kidneys were perfused with a BSA-free medium, 0.029 and 71% of the total radioactivity added to the perfusate was recovered in the urine and in the renal tissue, respectively. [3H]PAF urine excretion in proteinuric kidneys from adriamycin-treated rats was still negligible (0.015%). Analysis of the renal tissue-retained radioactivity in control and proteinuric kidneys perfused with 1% BSA indicated metabolism into long chain acyl-sn-glycero-3-phosphorylcholine species, lyso-PAF, glycerols, and intact PAF. Thin layer chromatography analysis of [3H]glycerol fraction in these renal extracts showed two major components comigrating with 1-O-alkylglycerol and 1-O-alkyl-2-fatty acylglycerol. Isolated proximal tubules, but not glomeruli from nephrotic rats exposed to increasing concentrations of BSA (0-4%), had a higher PAF uptake than control tubules for BSA concentrations ranging from 0 to 0.1%. Our findings in the isolated perfused kidneys indicate that, in normal conditions, circulating PAF is excreted in the urine in negligible amounts and that the altered glomerular permeability to proteins does not affect this excretion rate. Moreover, analysis of renal tissue radioactivity documented that the renal metabolism of PAF is comparable in control and nephrotic kidneys.
Asunto(s)
Riñón/metabolismo , Factor de Activación Plaquetaria/orina , Animales , Cromatografía Líquida de Alta Presión , Doxorrubicina , Glicerol/metabolismo , Glomérulos Renales/metabolismo , Túbulos Renales Proximales/metabolismo , Cinética , Lisofosfatidilcolinas/metabolismo , Nefrosis/inducido químicamente , Nefrosis/metabolismo , Fosfolípidos/metabolismo , Factor de Activación Plaquetaria/análogos & derivados , Factor de Activación Plaquetaria/metabolismo , Proteinuria/orina , Ratas , Ratas Endogámicas , Albúmina Sérica Bovina/farmacología , TritioRESUMEN
Recombinant human erythropoietin (rHu-EPO) was given during 12 to 20 months in 15 long term haemodialysis anaemic (mean Hb: 6.6 +/- 1 g/dl) patients who required no blood transfusion. Patients over 65, or with severe arterial disease or with uncontrolled hypertension were not included in this trial. Correction of anaemia (mean Hb 12.1 +/- 0.6 g/dl) was achieved in all patients and maintained all along the study. An improved sense of wellbeing and increased exercise tolerance were reported by all patients. Appropriate maintenance dosage of rHu-EPO was 74 +/- 6 U/kg i.v. twice weekly. High dose oral and/or intravenous iron therapy was necessary in the absence of previous marked iron overload. One retinal venous thrombosis was the sole severe side-effect encountered. A slight but significant increase of blood pressure was observed with the need of intensifying previous anti-hypertensive therapy in one patient and of starting one in one another. Fine adjustment of the dry weight was necessary to maintain blood pressure in the normal range. Heparin requirements increased in the majority of patients because of hollow fibre clotting but there was no evidence of decreased efficacy of dialysis. In two patients clotting of arteriovenous fistula was not obviously related to the rHu-EPO treatment.
Asunto(s)
Anemia/tratamiento farmacológico , Eritropoyetina/uso terapéutico , Diálisis Renal/efectos adversos , Adulto , Anemia/etiología , Peso Corporal , Evaluación de Medicamentos , Eritropoyetina/efectos adversos , Femenino , Humanos , Hipertensión Renal/etiología , Hierro/uso terapéutico , Fallo Renal Crónico/complicaciones , Fallo Renal Crónico/terapia , Masculino , Persona de Mediana Edad , Proteínas Recombinantes/uso terapéutico , Oclusión de la Vena Retiniana/etiologíaRESUMEN
Administration of recombinant erythropoietin constitutes a revolution in treatment of the anemia of chronic dialysis patients. Such treatment has been anxiously awaited. Its realization has been possible thanks to the spectacular progress allowed by the newly developed techniques of recombinant genetics. Correction of this type of anemia can be obtained rapidly and permanently if treatment is continued without interruption. It is followed by a remarkable transformation of the patient's physical and psychic status. The occurrence of certain side effects (e.g., elevation of blood pressure and an increased tendency toward vascular thrombosis), however, requires increased awareness in the follow-up of patients at risk and adaptation of erythropoietin administration to individual needs.