瓜蒌皮抗缺氧作用的研究

实验结果显示，瓜蒌皮提取液（ＥＰＴ）腹腔注射４０ ｇ·ｋｇ－１能明显延长常压缺氧、组织缺氧、特异性心肌缺氧小鼠的存活时间，延长率分别为 １４５％， ２．７９％， １１０．７％，使减压缺氧小鼠的存活率达８５％．表明瓜蒌皮确能增强整体动物的抗缺氧能力．     

Glucose and Cation Transport in Rat Jejunum,Ileum and Colon in vivo: Effects of Anionic and Nonionic Surfactants,and of Desoxycholate

Abstract Osmotically balanced solutions of glucose (0.5–300 mM) and sodium chloride, containing surfactants, were instilled into the small or large intestine of anaesthetized rats. Net absorption or secretion of glucose, sodium and potassium was studied. The surfactants tested were dodecylsulphate (3.4–17 mM), dioctyl-sulphosuccinate (1.8–11 m/M), Lubrol WX (0.1–0.5%), Triton × 100 (0.25%) and desoxycholate (2.5 mM). Qualitatively, the results were similar to those obtained previously with cationic compounds, suggesting a common mode of action for all surfactants studied. 17 mM dodecylsulphate seemed to abolish completely physiological glucose transport in the jejunum and ileum. At a lower concentration, and with the other surfactants, normal glucose transport was affected to an intermediate extent.     

Acute and chronic effects of dextropropoxyphene on behaviour and central inhibitory neurotransmission in the rat

There was no overt evidence of the development of physical dependence, as shown by a decrease in the body weight of rats following the abrupt withdrawal of dextropropoxyphene after two weeks administration. The ambulation and rearing scores in the 'open field' apparatus were increased after chronic, but not acute drug administration and returned to control values two days following drug withdrawal. GABA turnover, determined from the rise in GABA concentrations following GABA-transaminase inhibition, was reduced in the frontal and amygdaloid cortex after acute and chronic drug administration; a compensatory rise in GABA turnover in the amygdaloid cortex occurred two days after drug withdrawal. Na+, K+, ATP'ase activity, determined in a synaptosomal fraction from the mid-brain and hippocampus, was decreased in the latter region only during drug administration; a compensatory increase in the activity of this enzyme was found two days after drug withdrawal. These results support the view that chronically administered dextropropoxyphene may cause changes in inhibitory transmission and central neurotransmitter transport.     

Selective acquisition of plasma proteins by Trichomonas vaginalis and human lipoproteins as a growth requirement for this species

Trichomonas vaginalis avidly bound numerous host macromolecules which were not removed by repeated washing in phosphate buffered saline. The use of radioiodinated Cohn plasma fractions in binding studies allowed the identification of plasminogen, fibrinogen, immunoglobulin G, lipoproteins A and B, transferrin, α₁-antitrypsin, and albumin on intact organisms. The binding of immunoglobulin G, albumin, transferrin, and lipoproteins to intact, motile trichomonads was further demonstrated using ¹²⁵I-labeled plasma that was chromatographically depleted of these proteins. Kinetic studies indicated that ¹²⁵I-labeled lipoproteins bind to T. vaginalis in a receptor-ligand-like manner. The surface localization and uptake of bound lipoproteins was shown by treatment of intact organisms with pronase at various times after incubation with lipoproteins. Purified lipoproteins could be substituted for plasma or serum as a growth supplement in a complex medium of trypticase/yeast extract/maltose and supported growth and multiplication rates equal to those in the same medium with plasma.     

Physical properties of bovine white matter proteolipid apoprotein–sodium dodecyl sulfate complexes

The interaction of bovine white matter proteolipid apoproteins with sodium dodecyl sulfate (SDS) was studied. Equilibrium dialysis binding measurements show that the apoprotein binds approximately 1.5 gm SDS per gram protein at high ionic strength (T/2 =0.17). At low ionic strength (T/2 = 0.01) the protein binds only 0.90 gm per gram protein. The Stokes radius of the proteolipid protein is 40 Å. Based on the circular dichroism spectrum, the apoprotein contains less than 20% α-helix structure in either aqueous or 0.1% sodium dodecyl sulfate solution. Analytical SDS-PAGE (polyacrylamide gel electrophoresis) revealed two polypeptides. The major proteolipid protein migrated with an apparent molecular weight of 26,000 daltons. The minor proteolipid protein exhibited a molecular weight of 22,200 daltons. The apoprotein showed a marked tendency to aggregate on 8 M urea-SDS-polyacrylamide gels or when heated at 100° in excess detergent. These results suggest that the proteolipid proteins have hydrophobic regions that are not embedded within the detergent micelle but are exposed to the solvent. These regions may serve as sites for intermolecular aggregation.     

Effect of a Moderately Energy- and Salt-reduced Diet on Body Compartments and Blood Pressure Control in Obese Men with Mild Hypertension

Abstract Ten middle-aged moderately obese men with untreated mild hypertension were studied during a 6-week weight maintenance period and a 9-week period on a diet containing 5 MJ when body mass decreased by 8.4 kg (SE 1.4). According to urinary sodium excretion there was a mean reduction of 89 mmol/day (SE 16) in sodium intake. Mean arterial pressure fell by 2.5 to 14.1 mmHg (95% confidence interval) which was correlated to the reduction of body mass. The sympathetic nervous activity diminished with decreasing noradrenaline excretion and heart rate. There were no changes in the renin-aldosterone system. Estimation of the body composition with a four-compartment model utilizing determinations of body mass, total body potassium and total body water (TBW) showed reductions of body fat (8.4 kg (SE 1.4)) and body cell mass (BCM) (2.4 kg (SE 0.6)), but not of TBW. Extracellular water (ECW) increased significantly as judged from ECW/BCM calculations. Plasma volume was determined by Evan's blue and did not change significantly. We suggest that the observed changes in body composition represent one aspect of the adjustment to a weight reducing diet, while blood pressure is lowered by another mechanism in the adaptive response to dieting, i.e. reduction in sympathetic nervous activity.     

Acute acetylsalicylic acid poisoning: Treatment with forced alkaline diuresis and diuretics

Summary The effect of acetylsalicylic acid (ASA) in patients with renal insufficiency has been examined. In one investigation (A), in patients with a mean GFR of 23.0 ml/min the acute effects of ASA 750 mg i.v. (lysine-ASA 7.5 ml) and 0.9% NaCl 7.5 ml on renal water and solute output and on the clearance of inulin, creatinine and PAH were compared. In another (B) the effects of simultaneous administration of ASA 750 mg or 0.9% NaCl 7.5 ml i.v. with an infusion of furosemide 250 mg were investigated in six patients (mean GFR 12.9 ml/min) in a cross-over study. In study A there was a significant fall in urinary sodium excretion within the first 15 min after ASA administration, with a maximal decrease to 21% of the control period. Urine flow fell to 35%, osmolal clearance to 41%, inulin clearance to 54% and PAH clearance to 66%, whilst tubular reabsorption of sodium increased. The effect of ASA lasted for 2–6 h. The mean salicylic acid concentration during the first two hours after ASA administration was 60.0 µg/ml, and the mean protein bound salicylic acid (SA) was 70.4%. There was no effect of placebo (0.9% NaCl7.5 ml) on renal function. Pretreatment with ASA 750 mg i.v. attenuated the diuretic effect of furosemide 250 mg, and reduced creatinine clearance significantly within 0–2 h after drug administration.     

Pharmacokinetics and relative bioavailability of heptabarbital and heptabarbital sodium after oral administration to man

Summary A method has been developed for the quantitative determination of heptabarbital [5-(1-cyclohepten-1-yl)-5-ethylbarbituric acid] in human plasma after administration of single therapeutic doses of the drug. It involves a single extraction step followed by gas chromatography with alkali flame ionization detection, and the results were linear in the concentration range 0.125 – 5.0 µg/ml plasma. The pharmacokinetics and relative bioavailability of heptabarbital and heptabarbital sodium were studied in a crossover design in 7 healthy volunteers after oral administration of 20 tablets containing 200 mg heptabarbital and hard gelatine capsules containing an equivalent amount of its sodium salt. Heptabarbital concentrations in plasma were determined at regular intervals. The absorption of heptabarbital from the tablets was quite slow and peak level times varied from 1.5 to 4 h. The sodium salt was absorbed more rapidly and peak concentrations occurred between 1/3 and 2 h. In all cases the elimination of heptabarbital could be described by a single first-order process with an average half-life of 7.6 h (range 6.1 – 11.2 h). The half-life of the drug in each individual was about the same in the two trials. The relative bioavailability in each volunteer was estimated by comparing the areas under the plasma concentration curves. The sodium salt had an average bioavailability of 83% relative to the free acid. In some volunteers urinary excretion of unchanged heptabarbital was measured; cumulative excretion amounted to 0.16 – 0.30% of the administered dose. Four volunteers received one tablet each night for eight or ten days, but no accumulation was found. In three volunteers the half-life of the drug prior to and after these experiments did not change, whereas in the other volunteer the half-life decreased from 7.1 to 4.6 h. The possibility of enzyme induction should be considered when heptabarbital is taken regularly. It was concluded that heptabarbital was a suitable drug for the treatment of insomnia, since its half-life was rather short. Heptabarbital sodium may be used for induction of sleep, whereas Medomin^® tablets, i.e. heptabarbital free acid, may be prescribed when the maintenance of sleep is the primary reason for treatment with a hypnotic drug.     

The action of different coronary active drugs on intraand extravascular components of local myocardial perfusion

Summary In isolated guinea pig hearts epicardial perfusion was estimated by analysis of the transit profile of different fluorescence indicators. Several coronary dilating agents were tested with regard to their influence on local perfusion kinetics revealing distinct patterns of microcirculatory drug action.Supported by the Deutsche Forschungsgemeinschaft (SFB 68 A 18)     

Hyperglycemia and net transintestinal glucose and sodium transport in the rat

Hyperglycemia produced by intravenous infusion of glucose causes, in the everted jejunum of rat, an increase of net transintestinal transport of glucose, Na and water without modifying their cell concentration. The concentration of glucose in the fluid pouring out at the serosal side is higher than the calculated intracellular concentration, especially in the experiments in which the serosal compartment is initially empty. This fact could be explained by the possible existence of an active extrusion mechanism in the basolateral membrane of the enterocyte.