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PubMed1979

[Effect of 17-alpha-hydroxyprogesteronecapronate on sodium excretion and the renin-angiotensin-aldosterone-system in humans].

In seven healthy male subjects, a natriuretic effect of 17 alpha-hydroxyprogesterone caproate (17 alpha-OHPC) was demonstrated. Three of these subjects were kept on an uncontrolled diet and were examined over a period of 12 days. To the remaining four subjects, a single dose of 250 mg 17 alpha-OHPC was given intramuscularly after four days of intake of a chemically defined diet (Vivasorb). In this second test procedure, blood samples were taken in the recumbent position every two hours throughout a period of 12 h after the injection. For two more days and during the days before the administration of 17 alpha-OHPC, blood was taken at 8 a.m. before getting up from bed in same intervals, urine was collected for analysis of sodium and potassium excretion. During the first 12 h after the injection of 17 alpha-OHPC, the urinary sodium/potassium ratio significantly increased in all subjects. Plasma renin activity showed no characteristic changes at this time, whereas the plasma concentrations of aldosterone and cortisol decreased. The decrease of cortisol concentration started immediately after the injection and was more pronounced than that of plasma aldosterone. During the following 36 h, renin activity as well as aldosterone and cortisol concentrations in plasma showed an increase; in contrast, the sodium/potassium ratio decreased. On the basis of these results, the following effects of 17 alpha-OHPC are discussed: (1) an acute natriuresis which may be due to a competitive inhibition of aldosterone at the renal tubules, and (2) an inhibition of pituitary ACTH secretion or of adrenal steroid biosynthesis.

Adult↗
PubMed1979

High-risk prematurity--progestin treatment and steroid studies.

Studies have been undertaken regarding the efficacy and modus operandi of 17 alpha-hydroxyprogesterone caproate (17 alpha-OHP-C) in preventing premature labor in high-risk patients. In a total of 70 patients, the treated patient population had a prematurity rate (12.8%) and a perinatal mortality rate (5%) which were significantly lower than those of the total placebo or untreated patient group (40.9 and 25%, respectively). In addition, sequential plasma steroid values were determined in 21 patients, 10 of whom delivered prematurely. The results indicate that low plasma progesterone (P) and 17 alpha-hydroxyprogesterone (17 alpha-OHP) levels precede the onset of preterm labor by weeks. Successful treatment with 17 alpha-OHP-C was characterized by elevated P levels. Plasma estradiol (E2) and cortisol (C) values did not vary with time of delivery or treatment. These findings support the progesterone block theory as an important mechanism affecting preterm delivery in this high-risk population.

Estradiol↗
PubMed1978

Treatment of cystic ovarian disease in dairy cattle.

Fourty-four Holstein Friesian cows diagnosed as having ovarian follicular cysts from rectal palpation of the ovaries and observation of estrous behavior were used for the present experiments. Of the 16 cows injected intramuscularly (i.m.) with 110 mg of depot-progestins containing 100 mg of 17alpha-hydroxyprogesterone caproate and 10 mg of progesterone in oil, 8 cows responded with conception with 103 +/- 53 days in average after the treatment. The 8 cows not responding to depot-progestins were injected i.m. with 6,000 MU of HCG on the 10th day after the treatment. As a result, 2 cows of them conceived within 72 days in average after the initial treatment. Of the other 16 cows injected i.m. with 100 mg of progesteron in oil, 3 cows conceived. Interval between the treatment and conception was 36 +/- 9 days in average. In the 11 cows which failed to respond to progesterone treatment, an intramuscular injection of 6,000 MU of HCG on the 5th day after treatment resulted in conception of 7 cows within 42 +/- 10 days in average after the first treatment. Of the remaining 12 cows which received an i.m. injection with 10,000 MU of HCG, 4 cows responded with conception with 64 +/- 51 days in average after treatment. No remarkable rise in serum progesterone levels was observed either 10 days after depot-progestins injection or 5 days after progesterone treatment. Serum progesteron levels increased distinctly after HCG injections. The combined treatment with 100 mg of progesterone and 6,000 MU of HCG at 5 days interval gave the most successful results and this treatment was effective even when performed long after calving. Thus this method of treatment of cystic ovarian disease may be recommended for practical application.

Animals↗
PubMed1982

Medroxyprogesterone acetate (MAP) relative bioavailability after single high-dose administration in cancer patients.

A pharmacokinetic evaluation of medroxyprogesterone acetate (MAP, 6 alpha-methyl-17 alpha-hydroxyprogesterone acetate) was undertaken in 70 patients with advanced cancer treated either orally or im with single high doses. MAP plasma levels were determined by gas chromatography (63Ni electron capture detector) after derivatization with heptafluorobutyric anhydride, using 17 alpha-hydroxyprogesterone caproate as internal standard. Plasma levels after oral administration can be approximated by a triexponential function in agreement with a pharmacokinetic two-compartment open model with first-order absorption; peak levels are dose-related, but high interindividual variance is present. Following the administration, both decay phases are masked by prolonged absorption; peak levels are lower than after oral administration, but long-term bioavailability is higher, as demonstrated by comparison of the values for areas under curves in the 0-146-hour interval. The high interindividual ranges in the observed MAP plasma levels indicate that if any significant clinical evaluation is to be made, routine analysis of plasma MAP is mandatory.

Administration, Oral↗
PubMed1977

Further studies on a new bioassay of progestational activity (traumatic deciduoma formation in immature rats).

Six synthetic steroids were tested subcutaneously in a new bio-assay for short- and long-lasting progestational activity, using traumatic deciduoma production in immature female rats. As reference standard, a daily subcutaneous dose of 0.25 mg progesterone regularly induced a distinct deciduomagenic effect. A single dose of 12.5 mg of progesterone showed a prolonged activity. Medroxyprogesterone acetate showed a distinct deciduomagenic effect at the 0.05 mg daily s.c. dose level; a distinct prolonged effect was induced with a single s.c. injection of 0.5 mg. 16alpha-Aethylprogesterone induced regularly decidual reaction at the 0.1 mg s.c. dose level, it showed prolonged activity at the 0.25 mg dose level. The daily threshold dose for chlormadinone acetate was 0.25 mg; prolonged activity was shown with 2.5 mg. The daily threshold dose for duphaston is between 0.5 mg and 1.0 mg. A single s.c. dose of as much as 20.0 mg of 17alpha- hydroxyprogesterone caproate did not have a deciduomagenic effect.

Animals↗
PubMed1995

Mechanisms of absorption enhancement by medium chain fatty acids in intestinal epithelial Caco-2 cell monolayers.

Sodium salts of medium chain fatty acids (MCFAs) enhance the absorption of hydrophilic drugs across the intestinal mucosa, but the mechanism behind the effect is largely unknown. In this study, the dose-dependent effects of the sodium salts of four MCFAs, C6 (caproate), C8 (caprylate), C10 (caprate) and C12 (laurate), on the permeability of the hydrophilic marker molecule [14C]mannitol were studied in monolayers of the human intestinal epithelial cell line, Caco-2, grown on permeable supports. C8, C10 and C12, but not C6, enhanced the permeability of [14C]mannitol in a dose-dependent manner. Comparison of the cellular effects of the MCFAs at concentrations that gave comparable (8.1- to 8.5-fold) absorption enhancement showed that: 1) C8 was active as absorption enhancer only when the tonicity of the medium was increased; 2) absorption enhancement mediated by C10 was related to a redistribution of the cytoskeleton and structural dilatations in the tight junctions; and 3) C12 was without effect on the cytoskeleton and cellular morphology. Studies on C10 under anisotonic conditions showed that deviations from isotonicity enhanced its effect. These results suggest that structurally similar MCFAs display dramatic differences in their mechanism of action. In addition, the effects of osmolality provide an explanation for the previously reported variability in the efficacy of MCFAs as absorption enhancers.

Caco-2 Cells↗
PubMed1994

Expression of a 46 kDa protein in human pancreatic tumors and its possible relationship with the bile salt-dependent lipase.

Bile salt-dependent lipase (BSDL), an enzyme normally found in human pancreatic secretions is a 100 kDa glycoprotein. A BSDL-specific 477 bp cDNA probe was prepared by performing polymerase chain reaction experiments. This cDNA was used to probe mRNAs extracted from human pancreatic tissue and tumoral cell lines. Two mRNAs were detected in normal human pancreas at 2.2 and 1.3 to 1.5 kb. In human pancreatic tumoral cells, mRNAs encoding for the BSDL were detected using in situ hybridization, and proteins with an M(r) of 46,000 to 48,000 were translated into an in vitro system using mRNAs extracted from these cells. Using an immunoprecipitation procedure, we observed here that the specific BSDL polyclonal antibodies recognized three proteins of 100 +/- 5 (p100), 46 +/- 2 (p46) and 22.7 +/- 1.2 (p23) kDa, respectively in the soluble extracts of normal adult human pancreas. The p100 protein was probably the glycosylated product resulting from the translation of the 2.2 kb transcript. The p46 protein, which electrophoresed as a doublet was the main component immunoprecipitated from extract of a differentiated human pancreatic adenocarcinoma as well as from the extracts of two pancreatic cell lines, BxPC-3 and SOJ-6. In addition, the p46 immunoform of the BSDL was detected in cell-free medium from SOJ-6 cell line and its expression was found to be correlated with the secretion of an esterolytic activity on 4-nitrophenyl caproate, whereas the BxPC-3 cell line neither secreted the p46 nor showed any esterolytic activity on this substrate. The p46 may be either a short variant of BSDL resulting from the translation of the 1.3 to 1.5 kb transcript or a protein structurally related to the enzyme. The p46 doublet immunoform was detected in the human pancreatic secretion.

Base Sequence↗
PubMed1994

Augmentation of gamma-globin gene promoter activity by carboxylic acids and components of the human beta-globin locus control region.

Butyric acid increases fetal hemoglobin synthesis in adult animals and in erythroid cells in culture and induces the gamma-globin gene promoter in transient expression experiments in K562 cells (McDonagh KT, Nienhuis AW, Blood 78:255a, 1992 [abstr, suppl 1]). We compared the effect of butyrate and other short-chain carboxylic acids in transient expression studies with K562 cells using an expression plasmid bearing a luciferase reporter gene driven by the normal human A gamma-globin gene promoter. Butyrate (4 carbons) increased the activity of the human A gamma-globin gene promoter up to 123 times. Marked augmentation of the normal gamma-promoter activity was also noted with 5-carbon valeric acid (up to 394 times) and 3-carbon propionic acid (up to 129 times). The branched isobutyric acid as well as phenylacetate showed less ability to increase promoter activity. Addition of the tandemly repeated AP-1/NF-E2 (AP) enhancer sequences from hypersensitive site 2 (HS2) of the locus control region (LCR) increased gamma-promoter activity up to 24 times. Addition of a nearby 16-bp conserved motif (CM) in HS2 (Safaya S, Rieder RF, Blood 78:146a, 1992 [abstr, suppl 1]) to the AP-containing plasmid construct further increased gamma-promoter activity. In the presence of butyrate, the plasmid bearing both the AP and CM sequences showed gene expression up to 477 times greater than that of the basal gamma-promoter-driven luciferase plasmid in the absence of inducer. A plasmid bearing the herpes simplex thymidine kinase promoter was also tested and gene expression was markedly increased by the same organic acids. MEL cells responded to butyrate, valerate, and propionate with induction of hemoglobin synthesis. Responses to isobutyrate and 6-carbon caproate required higher concentrations of the compounds. Thus, other short-chain organic acids as well as butyrate increase gamma-promoter activity in the transient expression system, and this activity can be further augmented by incorporating LCR elements into the expression vector. Nonglobin promoters also respond to the same carboxylic acids.

Animals↗
PubMed1976

[Multicentre-clinical trial of the novel corticosteroid diflucortolone valerate in the forms of cream, ointment and fatty ointment. Part I: Comparative study of diflucortolone valerate with fluocortolone, -capronate, -pivalate in a double-blind contralateral design with topical application (author's transl)].

6alpha,9-Difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadiene-3,20-dione (diflucortolone valerate, Nerisona) 0.1% as a cream, ointment and fatty ointment was investigated in a double-blind contralateral design in 925 patients in comparison to fluocortolone (Ultralan), fluocortolone caproate and fluocortolone pivalate in three concurrently performed studies. The results of the contralateral study show Nerisona cream and ointment to be more effective (P less than 0.01) than Ultralan. The fatty ointment was also superior, but the difference was statistically significant (P less than 0.05) only in the indication psoriasis. No differences could be established in the less sensitive absolute assessment. The therapeutic success rate of 76-92% according to strict criteria-only complete healing and distinct improvement were counted as a success-clearly demonstrates the efficacy of the preparations. The local side effects recorded-mainly irritation and burning- were of a mild nature.

Administration, Topical↗
PubMed1993

Evidence for lysine 80 as general base catalyst of leucine dehydrogenase.

To elucidate the functional role of the lysyl residue highly conserved in NAD(P)(+)-dependent amino acid dehydrogenases, Lys-80 of leucine dehydrogenase from Bacillus stearothermophilus has been mutated into Ala, Arg, or Gln. All of the mutant enzymes had markedly reduced activities in the oxidative deamination, whereas the Michaelis constants for substrate and coenzyme did not change significantly upon the mutation, except for a 10-30-fold increase in Km values for alpha-keto-iso-caproate in the Ala and Gln mutants. The pH profiles of kinetic parameters of the mutants considerably differed from those of the wild type, in which two ionizable groups with pKa values of 8.9 and 10.7 must be unprotonated for catalysis and protonated for substrate binding, respectively. Combined with the analyses of solvent isotope effect and inhibition by substrate analogs, these results unequivocally show that the epsilon-amino group of Lys-80 participates in catalysis as a general base, assisting the nucleophilic attack of a water molecule to the substrate alpha-carbon atom. Furthermore, the Ala mutant was markedly stimulated by primary amines depending on the pKa and molecular volume, suggesting that in the Ala mutant the added amines can partially replace the general base function of Lys-80 in the wild type enzyme.

Amines↗
PubMed1993

[Optimization of mobile phase composition for RP-HPLC separation and determination of long acting steroidal contraceptives].

The optimization of the reversed phase high performance liquid chromatographic separation of six steroids of long acting contraceptives is described. A procedure is used to determine the design space, calculate the coefficients of a seven-term special cubic equation, and modify the model using the optimum experiment. Assisted with the computer, an optimum area could be predicted by overlapping the minimum resolution map with the analysis time map. It is likely that the method described in this paper will provide the basis or the simultaneous optimization of both separation and analysis time and prove to be a useful tool for the optimization of RP-HPLC of known compounds. We firstly utilized the time programming function to improve the detection sensitivities of estrogenic compounds. This method is successfully applied to the analysis of compound megestrol acetate injection and compound hydroxyprogesterone caproate injection. The method is sufficiently simple and rapid yet sensitive and accurate enough for the quality assurance of these types of pharmaceuticals.

Chromatography, High Pressure Liquid↗
PubMed1995

Thermodesulforhabdus norvegicus gen. nov., sp. nov., a novel thermophilic sulfate-reducing bacterium from oil field water.

A novel gram-negative, thermophilic, acetate-oxidizing, sulfate-reducing bacterium, strain A8444, isolated from hot North Sea oil field water, is described. The rod-shaped cells averaged 1 micron in width and 2.5 microns in length. They were motile by means of a single polar flagellum. Growth was observed between 44 and 74 degrees C, with an optimum at 60 degrees C. Spores were not produced. Sulfate and sulfite were used as electron acceptors. Sulfur, thiosulfate, nitrate, fumarate, and pyruvate were not reduced. In the presence of sulfate, growth was observed with acetate, lactate, pyruvate, butyrate, succinate, malate, fumarate, valerate, caproate, heptanoate, octanoate, nonadecanoate, decanoate, tridecanoate, pentadecanoate, palmitate, heptadecanoate, stearate, and ethanol. Pyruvate, lactate, and fumarate did not support fermentative growth. Cytochromes of the c-type were present. Desulfoviridin, desulforubidin, P582, and desulfofuscidin were not present. The G+C content of the DNA was 51 mol%. Sequence analysis of 16S rDNA showed that phylogenetically strain A8444 belongs to the delta subdivision of the Proteobacteria. The closest relatives are Desulfacinum infernum and Syntrophobacter wolinii: Strain A8444 is described as the type strain of the new taxon Thermodesulforhabdus norvegicus gen. nov., sp. nov.

Base Composition↗
PubMed1977

[Clinico-experimental testing for anti-inflammatory activity of external corticosteroids].

Clinical trials of the anti-inflammatory activity of corticosteroids for external use The influence on skin temperature of 4 corticoid-containing formulations and 3 steroid-free bases was tested in 9 subjects in whom no pathological skin changes were present but who were known to be sensitive to metal ions (chromium and nickel). The effect of the preparations on the healthy skin (vasoconstrictive effect) after a duration of action of 2 and 6 h was compared with the effect on skin sites treated subsequently with the contact allergens for a period of 24 h. In the procedure used the trial preparations were allowed to act for 2 and 6 h under occlusive dressing, or for 4 and 8 h, the dressing being removed for 2 h in each case. The allergization produced an increase in temperature at the skin surface which was influenced in various ways by the trial preparations. Whereas no statistically significant differences in the effect of the individual steroid topicals were found the healthy skin, in the evaluatin of the overall anti-inflammatory effect on the pathological skin processes, some distinct differences in effect were found. On comparing the results the following lowing order was obtained for the overall anti-inflammatory effect: 1. Fluprednylidene acetate 0.1% score 4.5, 2. Difluocortolone-valerate 0.1% score 8.5, 3. Fluocortolone trimethylacetate 0.25% + fluocortolone caproate 0.25% score 12, 4. Desoxymethasone 0.1% score 15, The steroid-free bases tested simultaneously did not exhibit clear effects on the temperature in the normal or inflamed skin. The results of the test procedure described are reproducible and can be evaluated by statistical method; the method thus seems appropriate for comparative studies of steroid-containing topicals. The special value in the procedure is the possibility of testing the effect of the preparations directly in a standardised inflammation model which is directly related to use in patients with inflammatory skin diseases, and of establishing in this way in which preparations the anti-inflammatory effect obtained exceeds the general effect common to all steroids.

Administration, Topical↗
PubMed1976

[Additive treatment of metastasizing breast cancer with special reference to postmenopausal age (results of a randomized study)].

Two therapy groups were formed at random out of 82 patients with progressive carcinoma of the breast. One was treated with estrogens, namely 17-ethinyl 1,3,5-estratriene 3,17 diol (SH 8.1083). The second group was treated with depot preparations consisting of a combination of estrogens and gestagens; these patients received 90 mg estradiol valerianate and 300 mg 17-hydroxy-19-norprogesterone caproate (SH 8.0834) weekly. The estrogen therapy resulted in a remission rate of 48% (complete remission 21.1%, partial remission 26.9%). The remission rate of the combination treatment was 46.6% (complete remission 23.3%, partial remission 23.3%). There was no considerable difference between the remission rates produced by the two therapeutik methods. It is remarkable that much more osseous remissions were found under the combination therapy of estrogens and gestagens. There were no substantial differences between the remission rates of the soft-tissue metastases and the pleuropulmonary metastases. In the estrogen group the remissions took 7.7 months, whereas an average remission period of 8.3 months was observed in the estrogen-gestagen group.

Age Factors↗
PubMed1976

[A Czechoslovak injection-contraceptive agent administered once a month].

During a 20-month period, 26 women aged 38 years on the average (27 to 45 years) received single intramuscular injections of a combination, containing 60 mg of Superlutin caproate plus 10 mg of oestradiol valerate in 1 ml of oily solution, at 4-week intervals as a contraceptive. Altogether 255 cycles were checked. In 6 cycles, minor accessory bleeding occurred, mostly in younger women. No undesired pregnancy took place. Under the name Lutofollin, the injections were prepared at the Research Institute for Pharmacy and Biochemistry in Prague. The preparation is especially suitable for women aged 30 to 45 years, as well as for those intolerant to oral hormonal contraceptives.

Adult↗