A rapid procedure based on a direct extraction and HPLC determination of dihydroergocristine in a pharmaceutical preparation with fluorescence detection has been developed and validated. The optimized chromatographic conditions included a Purospher RP18e column, 5 microm particle size, 250 x 4.0 mm, and 25 mM potassium dihydrogen phosphate buffer (pH 2.8)-acetonitrile (60 + 40, v/v) mobile phase at a flow rate of 1 ml/min. The separation was carried out at 50 degrees C, and the injection volume was 5 microL. Fluorescence detection was performed at an excitation and emission wavelength of 224 and 344 nm, respectively. The mobile phase parameters such as organic solvent composition, temperature, and pH were studied. The proposed method has the advantages of a very simple sample pretreatment and fast HPLC determination.
- MeSH
- anthrachinony MeSH
- dihydroergokristin analýza normy MeSH
- farmaceutická chemie MeSH
- fluorescenční spektrometrie MeSH
- koncentrace vodíkových iontů MeSH
- referenční standardy MeSH
- teplota MeSH
- vysokoúčinná kapalinová chromatografie metody normy statistika a číselné údaje MeSH
- Publikační typ
- časopisecké články MeSH
- validační studie MeSH
- Názvy látek
- anthrachinony MeSH
- cyanine green G base MeSH Prohlížeč
- dihydroergokristin MeSH
A novel natural peptide ergot alkaloid gamma-ergokryptinine containing norleucine has been isolated from ergot sclerotia of the field-growing parasitic fungus Claviceps purpurea CCM 8059. Its structure was deduced from the NMR and mass spectral data. The final structural proof was provided by the crystal structure determination, which is the first X-ray structure of a natural Nle-containing secondary metabolite. The conformations of three ergopeptinines: gamma-ergokryptinine, ergoladinine, and alpha-ergokryptinine were compared.
- MeSH
- Claviceps chemie MeSH
- ergotaminy chemie MeSH
- krystalizace MeSH
- námelové alkaloidy chemie MeSH
- norleucin izolace a purifikace MeSH
- nukleární magnetická rezonance biomolekulární MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- ergotaminy MeSH
- gamma-ergokryptinine MeSH Prohlížeč
- námelové alkaloidy MeSH
- norleucin MeSH
OBJECTIVES: To assess in venous cord blood the distribution of major lymphocyte subsets according to pH and medications used during labor. DESIGN AND METHODS: Venous cord blood was sampled immediately after labor from 70 newborns (35 males and 35 females) delivered vaginally. Lymphocytes were immunophenotyped by flow cytometry and pH was measured using the AVL 900 automated blood gas analysis system. Data on birth weight, gestational age at delivery, length of labor, presence of stained amniotic fluid, medications used during labor, maternal risk factors, age and parity were collected. RESULTS: The percentage of T lymphocytes decreased while the percentage of NK lymphocytes increased with decreasing pH over the whole range of pH values. The proportions of T and NK lymphocytes were associated with the administration of neuroplegics, spasmolytics or dihydroergotoxin in the first stage of labor. CONCLUSIONS: Cord blood pH and labor-associated variables should be taken into account to adequately interpret the profile of major lymphocyte subsets as a marker of the effect of different prenatal factors on the immune system of neonates.
- MeSH
- analgetika farmakologie MeSH
- buňky NK cytologie MeSH
- dihydroergotoxin farmakologie MeSH
- dospělí MeSH
- fetální krev cytologie MeSH
- imunofenotypizace MeSH
- koncentrace vodíkových iontů MeSH
- lidé MeSH
- lineární modely MeSH
- lymfocyty cytologie MeSH
- mladiství MeSH
- multivariační analýza MeSH
- neuroprotektivní látky farmakologie MeSH
- novorozenec MeSH
- parasympatolytika farmakologie MeSH
- průtoková cytometrie MeSH
- T-lymfocyty cytologie MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- mladiství MeSH
- mužské pohlaví MeSH
- novorozenec MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- analgetika MeSH
- dihydroergotoxin MeSH
- neuroprotektivní látky MeSH
- parasympatolytika MeSH
Ergot alkaloids possess some properties potentially beneficial in ischemia of organs. Therefore the effect of pretreatment by nicergoline and bromocriptine was established in ischemia-reperfusion injury of rat liver. PGE2 and verapamil were used as comparative agents. Hepatic ischemia (60 min) of anesthetized rats was induced by clamping of vessels supplying the median and left lateral lobe. Tested drugs were given i.v. 2 or 5 min prior to inducing ischemia. ALT and AST activities in serum two hours after the end of ischemia were used as markers of hepatocellular injury. Only PGE2 (0.1 mg.kg-1) pretreatment minimized the postischemic rise of both ALT and AST activities. Pretreatment with various doses of nicergoline (1 or 4 mg.kg-1), bromocriptine (1 or 4 mg.kg-1) and verapamil (0.9 or 4.5 mg.kg-1) did not influence significantly serum transaminases activities after ischemia. Bromocriptine (4 mg.kg-1) given together with PGE2 did not improve a protective effect against ischemia achieved by the administration of PGE2 (0.1 microgram.kg-1).
- MeSH
- bromokriptin farmakologie MeSH
- dinoproston farmakologie MeSH
- játra krevní zásobení MeSH
- krysa rodu Rattus MeSH
- nicergolin farmakologie MeSH
- potkani Wistar MeSH
- reperfuzní poškození prevence a kontrola MeSH
- verapamil farmakologie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- bromokriptin MeSH
- dinoproston MeSH
- nicergolin MeSH
- verapamil MeSH
Glucose tolerance, total plasma cholesterol and plasma triglycerides were studied in the genetically hypertensive obese Koletsky rats (SHR/N-cp) and in their lean siblings. The initial part of the glucose tolerance curve was substantially elevated in both obese and lean Koletsky animals compared to normotensive Wistar rats. The abnormal glucose tolerance in hypertensive rats was accompanied by increased total plasma cholesterol and plasma triglycerides. Long-term treatment with dopaminergic agonists terguride or bromocriptine (0.2 and 2.0 mg/kg/day, respectively) exerted similar effects on lipid metabolism but both drugs differed in their influence on glucose tolerance. Terguride lowered plasma lipids and normalized glucose tolerance in both obese and lean Koletsky rats. Bromocriptine reduced hyperlipidaemia but did not attenuate the abnormalities of glucose tolerance in either lean or obese Koletsky animals.
- MeSH
- bromokriptin farmakologie MeSH
- hyperlipidemie krev MeSH
- hypertenze krev MeSH
- inzulin krev MeSH
- krevní tlak účinky léků MeSH
- krysa rodu Rattus MeSH
- lipidy krev MeSH
- lisurid analogy a deriváty farmakologie MeSH
- modely nemocí na zvířatech MeSH
- obezita krev MeSH
- porucha glukózové tolerance krev MeSH
- potkani inbrední SHR MeSH
- potkani Sprague-Dawley MeSH
- potkani Wistar MeSH
- sexuální faktory MeSH
- tělesná hmotnost účinky léků MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- bromokriptin MeSH
- dironyl MeSH Prohlížeč
- inzulin MeSH
- lipidy MeSH
- lisurid MeSH
Parenteral, depot, repeatable bromocriptine Parlodel LARR (PLO LAR) was used in the treatment of 10 women with hyperprolactinaemia. Two of them had previously an operation of a prolactinoma, eight did not have adenomas. Twenty eight days following administration of 50 mg PLO LAR, the PRL levels ere significantly lower than before treatment; in patients without adenomas they were quite normal. The action of the mentioned 50 mg PLO LAR corresponded roughly to a daily dose of 7.5 mg ParlodelR (PLO) by the oral route, i.e. in 28 days a total of 185 mg bromocriptine. After administration of five PLO LAR injections (50 and later 100 mg), the mean PRL levels in patients without adenomas were normal after 6 months. There were no significant nor pathological changes 28 days following i.m. PLO LAR 50 mg as regards T3, T4 levels, the blood sugar, cholesterol, FSH, LH, STH, TSH, testosterone cortisol, progesterone, 17 beta-estradiol, androstendione, 11 beta-OH androstendione, DHEA-S, 17 alpha-OH progesterone, aldosterone, 17-ketosteroids and 17-ketogenic steroids (in urine). LHRH + TRH + insulin tolerance tests were made repeatedly. Significant changes were found only in PRL levels (decline). In three amenorrhoic patients the originally low progesterone level rose significantly to levels of postovulation progesterone. One of these three women became pregnant after 18 years of unsuccessful treatment of sterility, incl. various oral dopaminergic preparations. The patients tolerated the preparation well and various biochemical and haematological tests were normal. The effect on galactorrhoea was favourable, seven amenorrhoic women had normal menstruation.
- MeSH
- aplikace orální MeSH
- bromokriptin aplikace a dávkování MeSH
- dospělí MeSH
- hyperprolaktinemie krev farmakoterapie MeSH
- implantované léky MeSH
- injekce MeSH
- léky s prodlouženým účinkem MeSH
- lidé MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- ženské pohlaví MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- srovnávací studie MeSH
- Názvy látek
- bromokriptin MeSH
- implantované léky MeSH
- léky s prodlouženým účinkem MeSH
In ergot alkaloids a disproportion between the size of the peroral dose and the achieved area under the curve concentrations was described. This process can be explained by nonlinearity in the absorption, distribution or elimination of alkaloids. The aim of the present paper is to find whether elimination of tritiated DH-ergotoxine (3HDHE) in the liver is a linear, dose-independent process. Therefore on the model of the isolated rat liver disappearance of radioactivity in perfusate after the administration of two doses of 3HDHE, viz. 60 ng g-1 of the liver and 3030 ng g-1 of the liver, was investigated. The disappearance curves of radioactivity expressed as the percentage of the administered dose did not significantly differ between both groups. No significant changes between the groups were found either in the size of pharmacokinetic parameters, or in the portion of the administered radioactivity excreted in bile. Therefore the present authors think that disappearance of radioactivity in perfusate of the isolated liver after administration of 3HDHE is a linear process following first-order kinetics.
- MeSH
- dihydroergotoxin farmakokinetika MeSH
- inbrední kmeny potkanů MeSH
- játra metabolismus MeSH
- krysa rodu Rattus MeSH
- perfuze MeSH
- tritium MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- dihydroergotoxin MeSH
- tritium MeSH
Experiments were performed in the adult normotensive rats of Wistar strain and in the genetically hypertensive rats developed by Koletsky, i.e., in the strain where it is decreased turnover-rate of diencephalomesencephalic norepinephrine, increased CNS cholinergic activity, cholinergic supersensitivity and reduced stress resistance. The behavior in control and in drugged animals was traced in holeboard and in elevated plus-maze. In the control animals, when compared to the normotensive rats of Wistar strain, the genetically hypertensive rats of both sexes show in the first session elevated locomotor-exploratory activity, lower rate of intrassession habituation of the latter activity; in the genetically hypertensive males in the first session there is reduced percentage of time spent head dipping. The latter type of animals show lower number of entries into centre and in open arms by forepaws and by all four feet in the first session; in the first session time spent in centre and in open arms by forepaws and by all four feet is increased in normotensive males relative to hypertensive ones. Chronic Bromocriptine treatment shows in all traced parameters strain dependence. The drug only in the genetically hypertensive rats reduced total time of locomotor-exploratory activity in both sessions, elevated rate of intrasession habituation of locomotor-exploratory activity in both sessions, elevated directed exploration in hole-board in both sessions, alleviated aversion towards open space and height in the elevated plus-maze in both sessions.
- MeSH
- bromokriptin farmakologie terapeutické užití MeSH
- chování zvířat účinky léků MeSH
- hypertenze patofyziologie psychologie MeSH
- inbrední kmeny potkanů MeSH
- krysa rodu Rattus MeSH
- potkani inbrední SHR MeSH
- úzkost farmakoterapie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- bromokriptin MeSH
The observations were carried out in the adult normotensive rats of Wistar strain and in the genetically hypertensive rats developed by Koletsky, i.e., in the strain where is decreased turnover-rate of diencephalo-mesecephalic norepinephrine, increased CNS cholinergic activity accompanied by cholinergic supersensitivity and reduced stress-resistance. The effect of dihydroergotoxine was traced in holeboard and in the elevated plus-maze. Chronic dihydroergotoxine treatment shows "anxiolytic" effect in the elevated plus-maze (i.e., this drug alleviates aversion towards open space and height), increases directed exploration, elevates the rate of habituation of the locomotor-exploratory activity at all, and elevates the rate of habituation of directed exploration especially. The drug in the above mentioned parameters shows very expressive dependent effect, i.e., the effect being more or solely expressed in the genetically hypertensive rats of Koletsky type. The results of our recent series of experiments again suggest that is is well founded to use for the screening of the drugs with potential anxiolytic effect the genetically hypertensive rats of Koletsky type, i.e., the strain which by its CNS neurotransmitter abnormalities resembles deviations observed in the patients suffering from anxio-depressive disorders.
- MeSH
- chování zvířat účinky léků MeSH
- dihydroergotoxin farmakologie terapeutické užití MeSH
- hypertenze patofyziologie psychologie MeSH
- inbrední kmeny potkanů MeSH
- krysa rodu Rattus MeSH
- potkani inbrední SHR MeSH
- úzkost farmakoterapie MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- dihydroergotoxin MeSH
Using the methods of rat intestine perfusion in situ and kinetics examination in vivo, absorption of 3H-dihydroergotoxine (3HDHE) from the gastrointestinal tract into systemic blood was investigated. The aim of the study was to increase absorption of the ergot alkaloid with palmitoyl-DL-carnitine (5 mg/rat). Low absorption of 3HDHE was demonstrated in contrast to fast and almost complete absorption of the model drug theophylline (5 mg kg-1). In the experiment this was evidenced by in situ continuous measurement of the administered activity (125 micrograms kg-1) into a reservoir. At the end of the experiment (120 min) the plasma activity reached 0.034 +/- 0.014%, retention in the intestine achieved more than 60%, uptake in the brain 0.044 +/- 0.015%, cumulative excretion in bile 1.50 +/- 0.31% of administered activity. Palmitoyl-DL-carnitine did not influenced the percentage of activity in the plasma and did not affect bile excretion, retention in the intestine and uptake in the brain. In the vivo experiment oral administration of 3HDHE into the stomach (222 micrograms kg-1) increased activity in plasma (0.069 +/- 0.020% within 24 h), cumulative excretion in urine was 6.1 +/- 3.6%, retention of the drug in the stomach and intestine 46 +/- 12%, activity of the brain 0.11 +/- 0.02%, in the kidney 0.39 +/- 0.17%, and in the liver 0.80 +/- 0.30%. After palmitoyl-DL-carnitine administration the activity of plasma reached 0.084 +/- 0.022% (NS), retention in gastrointestinal tract 39 +/- 9% (NS), activity in the liver 0.71 +/- 0.17% (NS), and activity in the kidney 0.42 +/- 0.13% (NS).(ABSTRACT TRUNCATED AT 250 WORDS)
- MeSH
- dihydroergotoxin farmakokinetika MeSH
- inbrední kmeny potkanů MeSH
- intestinální absorpce účinky léků MeSH
- karnitin analogy a deriváty MeSH
- krysa rodu Rattus MeSH
- palmitoyl karnitin farmakologie MeSH
- theofylin krev MeSH
- vysokoúčinná kapalinová chromatografie MeSH
- žaludeční sliznice metabolismus MeSH
- žaludek účinky léků MeSH
- žluč metabolismus MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- dihydroergotoxin MeSH
- karnitin MeSH
- palmitoyl karnitin MeSH
- theofylin MeSH
