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At least 19 recordsLinked to original sources
PubMed1976

Onset of the vasoconstrictor effect of diflucortolone valerate, betamethasone valerate, and fluocinolone acetonide ointments applied for varying periods under occlusive dressings.

Evaluation of cutaneous vasoconstriction after applications of varying duration of topical corticoids on the flexor surfaces of the forearms of 20 patients with intact skin shows a significantly faster blanching effect with diflucortolone valerate ointment than with fluocinolone acetonide and betamethasone valerate ointments. Furthermore, the test shows that even for a highly active preparation, such as the diflucortolone valerate ointment, an application time of less than 3 h only exceptionally leads to vasoconstriction in the healthy skin.

Administration, Topical↗
PubMed1976

[Comparative studies in man on the percutaneous absorption of diflucortolone valerate, betamethasone-17-valerate, beclomethasone dipropionate and fluocinolone acetonide].

Percutaneous absorption of 6alpha,9-difluor-11beta-hydroxy-16alpha-methyl-21-valeryloxy-1,4-pregnadience-3,20-dione (diflucortolone valerate, DFV, Nerisona), betamethasone 17-valerate (BV), beclomethasone dipropionate (BDP) and fluocinolone acetonide (FA) by damaged skin was examined on the backs of 4 healthy males from whom the stratum corneum had been removed by "stripping". The determination of percutaneous absorption was performed on the one hand by a method employing radioactive labelled compounds (DFV, BV) and measuring the elimination with the urine and faeces and on the other hand by photometric determination (DFV, BV, BD, fa) of the corticoid remaining on the skin immediately following application and at the end of a 24-h period of exposure. Direct measurement of the radioactivity in the urine and faeces revealed that percutaneous absorption from a new W/O emulsion takes place up to 2.2+/-0.8% in the case of DFV (0.1%) and to at least 12.2+/-3.3% in the case of BV (0.12%) within 24 h. The determination of percutaneous absorption via recovery from the skin produced the following results for the 4 corticoid preparations examined: DFV (14.8+/-4.2%) and BDP (14.0+/-4.3%) approximately equal, BV (23.5+/-4.1%) a marked increase and FA (39.2+/-2.4%) the highest level of absorption. This order for percutaneous absorption appears to correlate to the frequency of systemic side effects.

Administration, Topical↗
PubMed1992

Resistance to N-benzyladriamycin-14-valerate in mouse J774.2 cells: P-glycoprotein expression without reduced N-benzyladriamycin-14-valerate accumulation.

N-Benzyladriamycin-14-valerate (AD 198) is a highly lipophilic analogue of Adriamycin with novel cytotoxic mechanisms, greater in vivo antitumor activity, and the ability to circumvent multidrug resistance due to P-glycoprotein-mediated drug efflux or decreased topoisomerase II activity. To identify the mechanism(s) which may confer AD 198 resistance, J774.2 mouse macrophage-like cells were selected for growth in cytotoxic levels of AD 198 (AD 198R). AD 198R cells exhibited over-expression of the mdr1b (P-glycoprotein) gene, cross-resistance to Adriamycin and vinblastine, and potentiation of drug cytotoxicity by verapamil. However, net intracellular accumulation of AD 198 in AD 198R cells was unchanged compared to parental cells, while Adriamycin and vinblastine accumulations were reduced 40% and 95%, respectively. AD 198 was localized in the perinuclear region of the cytoplasm in both parental and AD 198R cells, with additional vesicular compartmentalization in AD 198R cells. Verapamil-induced reversal of AD 198 resistance coincided with some drug redistribution from cytoplasmic vesicles, but without redistribution of AD 198 into the nucleus. These results suggest that AD 198 resistance was not conferred through a P-glycoprotein-mediated reduction in intracellular drug accumulation but through other cytoplasmic mechanisms, including, but not limited to, drug compartmentalization.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
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↗
PubMed2003

Kinetics of thermophilic, anaerobic oxidation of straight and branched chain butyrate and valerate.

The degradation kinetics of normal and branched chain butyrate and valerate are important in protein-fed anaerobic systems, as a number of amino acids degrade to these organic acids. Including activated and primary wastewater sludge digesters, the majority of full-scale systems digest feeds with a significant or major fraction of COD as protein. This study assesses the validity of using a common kinetic parameter set and biological catalyst to represent butyrate, n-valerate, and i-valerate degradation in dynamic models. The i-valerate degradation stoichiometry in a continuous, mixed population system is also addressed, extending previous pure-culture and batch studies. A previously published mathematical model was modified to allow competitive uptake of i-valerate, and used to model a thermophilic manure digester operated over 180 days. The digester was periodically pulsed with straight and branched chain butyrate and valerate. Parameters were separately optimized to describe butyrate, i-valerate, and n-valerate degradation, as well as a lumped set optimized for all three substrates, and nonlinear, correlated parameter spaces estimated using an F distribution in the objective function (J). Each parameter set occupied mutually exclusive parameter spaces, indicating that all were statistically different from each other. However, qualitatively, the influence on model outputs was similar, and the lumped set would be reasonable for mixed acid digestion. The main characteristic not represented by Monod kinetics was a delay in i-valerate uptake, and was compensated for by a decreased maximum uptake rate (k(m)). Therefore, the kinetics need modification if fed predominantly i-valerate. Butyrate (i- and n-) and n-valerate could be modeled using stoichiometry consistent with beta-oxidation degradation pathways. However, i-valerate produced acetate only, supporting the stoichiometry of a reaction determined by other researchers in pure culture. Therefore, lumping i-valerate stoichiometry with that of n-valerate will not allow good system representation, especially when the feed consists of proteins high in leucine (which produces i-valerate), and the modified model structure and stoichiometry as proposed here should be used. This requires no additional kinetic parameters and one additional dynamic concentration state variable (i-valerate) in addition to the variables in the base model.

Acetates↗
PubMed2001

Effect of estradiol valerate alone or in association with cyproterone acetate upon vascular function of postmenopausal women at increased risk for cardiovascular disease.

OBJECTIVES: a large body of evidence has been accumulated suggesting that impairment of vascular endothelial function is an initial step in the development of atherosclerosis. Recent studies have shown that estrogen replacement therapy in postmenopausal women (PMW) improves endothelium-dependent, flow-mediated dilatation (FMD) while the cyclical adjunct of a progestin may reverse this effect. METHODS: the purpose of this study was to evaluate endothelium-dependent, FMD in the brachial artery and the plasma levels of Endothelin-1 in menopausal females treated with estradiol valerate with and without cyclical cyproterone acetate in 20 PMW (mean age 64+/-6 years) with more than one risk factor for coronary artery disease. After a baseline evaluation, PMW entered a double-blinded, placebo controlled single cross-over study and were randomized to receive either estradiol valerate (2 mg) for 21 days or estradiol valerate (2 mg) for 11 days and estradiol valerate (2 mg) and cyproterone acetate (1 mg) for 10 days. Patients were crossed-over the complementary treatment 7 days after completing the first treatment phase. The study of forearm blood flow was repeated at the end of each treatment period. RESULTS: estradiol valerate significantly increased FMD as compared with baseline (12+/-3 vs. 7+/-4%, P<0.01) the adjunct of cyproterone acetate did not affect the effect of estradiol valerate upon FMD (12+/-3 vs. 11+/-4%, P=NS). Similarly reactive hyperemic flow increased after estradiol valerate alone (24%) or in association with cyproterone acetate (24%) compared with baseline. Plasma levels of Endothelin-1 were significantly reduced by estradiol valerate alone or in association with cyproterone acetate. CONCLUSIONS: in conclusion hormone replacement therapy with estradiol valerate and cyproterone acetate improves endothelial function and reduces plasma levels of Endothelin-1 in PMW at risk of coronary artery disease. These effects may be relevant for cardioprotection.

Brachial Artery↗
PubMed1995

Simultaneous diffusion and metabolism of betamethasone 17-valerate in the living skin equivalent.

Simultaneous diffusion and metabolism of betamethasone 17-valerate was studied using betamethasone 17-valerate, betamethasone 21-valerate, and betamethasone as permeants. These corticosteroids were suspended in silicone adhesive and applied to an artificial living skin equivalent (LSE) for 72 h. When betamethasone was applied, no metabolites were detected in the receptor medium. Conversely, with betamethasone 21-valerate application, only betamethasone but no betamethasone 21-valerate was detected in the receptor medium indicating the metabolism of the latter by skin esterases. When tested with the theory for simultaneous diffusion and metabolism, the result is consistent with the enzyme rate constant in the LSE homogenate measured in a previous study. When betamethasone 17-valerate was applied to the LSE, more than half of the total amount of corticosteroids detected in the receptor medium was unchanged, consistent with the previously reported chemical (as opposed to enzymatic) degradation half-life of about 8 h. This result also indicated that very little metabolism of betamethasone 17-valerate occurred in the skin.

Betamethasone↗
PubMed1989

A fluorescence study examining how 14-valerate side chain substitution modulates anthracycline binding to small unilamellar phospholipid vesicles.

The intrinsic fluorescence properties of the anthracycline antitumor antibiotics were studied in an effort to understand how 14-valerate side chain substitution modulates drug associations with small unilamellar phospholipid vesicles (SUVs) under near physiological conditions. Drug location and dynamics in fluid-phase dimyristoylphosphatidylcholine (DMPC) bilayers were evaluated for several analogs; accessibilities of bound fluorophores to membrane-impermeable iodide were evaluated in quenching experiments, while the diffusive motions of these agents were studied using lifetime-resolved anisotropy plots. The bulky and hydrophobic valerate substituent was found to further hinder the rotations experienced by a bound drug molecule, with apparent limiting anisotropy (a infinity) values showing increases of 13-82% upon valerate group substitution. In addition, the bimolecular quenching rate constants (unit, 10(9) M-1.s-1) for membrane-bound adriamycin (1.4), N-trifluoroacetyladriamycin (0.4), and their corresponding valerate-substituted analogs (kq values of 1.1 and 0.5, respectively) reveal that the side chain is a weak modulator of fluorophore penetration into the bilayer, with stronger modulation being achieved through amino group substitution. Similar results were obtained for drugs bound to negatively-charged dimyristoylphosphatidylglycerol (DMPG) bilayers. Finally, comparison of the equilibrium binding affinities of the various congeners for electroneutral DMPC versus negatively-charged DMPG bilayers demonstrate that positively-charged parent anthracyclines display high levels of selective binding to negatively-charged phospholipids, unlike valerate-substituted analogs which display no such selectivity. The modulation of anthracycline-membrane interactions achieved through valerate substitution offers potential explanations, at least in part, for some of the novel biological properties of valerate-containing anthracyclines.

Antibiotics, Antineoplastic↗
PubMed1982

Pharmacokinetic and pharmacological features of oestradiol valerate.

Natural oestrogenic hormones are the appropriate substances for the therapy of climacteric complaints. After oral or parenteral administration, oestradiol valerate, the synthesis compound contained in various commercially available preparations, is completely converted into the natural substances 17 beta-oestradiol and valeric acid. The 17 beta-oestradiol produced on cleavage of the ester behaves in the organism like the endogenous steroid hormone. Oestradiol valerate and 17 beta-oestradiol are virtually dose-equivalent. No differences in the spectrum of action of the oestrogen and its ester have been found either in animal experiments or man. The pharmacokinetic behaviour and the biotransformation of the 17 beta-oestradiol originating from oestradiol valerate are no different from those of natural 17 beta-oestradiol. Differences of practical significance exist in respect of the quantitative effect of oestradiol valerate following oral and intramuscular administration, whereas 4 mg oestradiol valerate administered intramuscularly is therapeutically sufficient for a period of 2-4 wk (depot effect). As much as 2 mg daily over 3 wk must be administered via the oral route to achieve the same effect. This difference is due to the greatly diverging pharmacokinetic behaviour of oestradiol valerate depending on which of the two modes of administration is employed.

Administration, Oral↗
PubMed2003

Effects of hydrochloric, valeric, and other volatile fatty acids on pathogenesis of ulcers in the nonglandular portion of the stomach of horses.

OBJECTIVE: To identify in vitro effects of hydrochloric acid, valeric acid, and other volatile fatty acids (VFAs) on the pathogenesis of ulcers in the nonglandular portion of the equine stomach. SAMPLE POPULATION: Gastric tissues from 13 adult horses. PROCEDURE: Nonglandular gastric mucosa was studied by use of Ussing chambers. Short-circuit current (Isc) and potential difference were measured and electrical resistance and conductance calculated after tissues were bathed in normal Ringer's solution (NRS) or NRS and hydrochloric, valeric, acetic, propionic, and butyric acids. Treated tissues were examined histologically. RESULTS: Incubation in 60mM valeric acid at pH < or = 7.0 abruptly and irreversibly abolished Isc, which was followed by a slower decrease in resistance and an increase in conductance. Incubation in 60mM acetic, propionic, and butyric acids and, to a lesser extent, hydrochloric acid at pH < or = 7.0 significantly decreased Isc, which was followed by an increase in resistance and a decrease in conductance. CONCLUSIONS AND CLINICAL RELEVANCE: Incubation in valeric acid at pH < or = 7.0 caused a dramatic decrease in mucosal barrier function in the nonglandular portion of the stomach. Changes in barrier function attributable to exposure to valeric acid were associated with histopathologic evidence of cellular swelling in all layers of the nonglandular mucosa. Because of its high lipid solubility, valeric acid penetrates the nonglandular gastric mucosa, resulting in inhibition of sodium transport and cellular swelling. Valeric acid and other VFAs in gastric contents may contribute to the pathogenesis of ulcers in the nonglandular portion of the stomach of horses.

Animals↗
PubMed2005

Effects of adding valerate, caproate, and heptanoate to ruminal buffers on splanchnic metabolism in steers under washed-rumen conditions.

Four steers fitted with a ruminal cannula and chronic indwelling catheters in the mesenteric artery, mesenteric vein, hepatic portal vein, hepatic vein, and the right ruminal vein were used to study VFA absorption from bicarbonate buffers incubated in the washed reticulorumen, and metabolism by splanchnic tissues. Portal and hepatic vein blood flows were determined by infusion of p-aminohippurate into the mesenteric vein. The steers were subjected to four experimental treatments in a Latin square design. The treatments were Control (ruminal bicarbonate buffer with [mmol/kg]: acetate = 72; propionate = 30; isobutyrate = 2.1; butyrate = 12; valerate = 1.2; caproate = 0; and heptanoate = 0); Val (same as control except for valerate = 8 mmol/kg); Cap (same as control except for caproate = 3.5 mmol/kg); and Hep (same as control except for heptanoate = 3 mmol/kg). All buffers were incubated for 90 min in the rumen, and ruminal VFA absorption rates were maintained by continuous intraruminal infusion of VFA. The arterial concentrations of valerate and heptanoate showed a small increase (< or = 1 micromol/L; P < 0.05) with inclusion of the respective acid in the ruminal buffer, but no change (P = 0.57) in arterial concentration of caproate was detected. Valerate increased (P < 0.05) the net portal flux of butyrate and valerate, as well as the net splanchnic flux of propionate, butyrate, and valerate. With Cap and Hep, the net portal flux of caproate and heptanoate accounted for 54 and 45% of ruminal disappearance rates, respectively, indicating that these acids were extensively metabolized by the ruminal epithelium. Caproate was ketogenic both in the ruminal epithelium and in the liver, and Cap increased (P < 0.05) the arterial concentration, ruminal vein minus arterial concentration difference, net hepatic flux, and net splanchnic flux of 3-hydroxybutyrate. The net hepatic flux of glucose decreased (P = 0.02) with Cap and Hep compared with Control and Val; however, no effect (P = 0.14) on the net splanchnic flux of glucose could be detected. We conclude that the strong biological activity of valerate, caproate, and heptanoate warrant increased emphasis on monitoring their ruminal presence and their potential systemic effects on ruminant metabolism.

Absorption↗
PubMed1994

Metabolism and degradation of betamethasone 17-valerate in homogenized living skin equivalent.

The metabolism of betamethasone 17-valerate was estimated using an artificial living skin equivalent (LSE). Betamethasone 17-valerate, betamethasone 21-valerate and betamethasone were measured by a normal-phase high-performance liquid chromatographic (HPLC) method. Betamethasone 17-valerate was added to the culture medium with or without LSE homogenate. Degradation profiles (%) of betamethasone 17-valerate remaining in the culture medium with skin homogenate did not differ from those without homogenate. However, the conversion of betamethasone 21-valerate to betamethasone was accelerated by skin homogenate, indicating that LSE has a sufficient level of esterase.

Betamethasone↗
PubMed1993

In vitro percutaneous permeation of betamethasone and betamethasone 17-valerate.

The percutaneous permeation and sorption isotherm (equilibrium) profiles of betamethasone and betamethasone 17-valerate were estimated in an in vitro study with excised human skin. Corticosteroids were measured by HPLC. The stratum corneum (dry weight)/water partition coefficient of betamethasone 17-valerate was 20 times greater than that of betamethasone. Nevertheless, when aqueous saturation was maintained in the donor solution, the mean steady-state flux of betamethasone 17-valerate through split-thickness skin was 57.6 ng/cm2/h, whereas that of betamethasone was 15.2 ng/cm2/h. This was presumably because the aqueous saturation concentration of betamethasone (60 micrograms/mL) was 11 times greater than that of betamethasone 17-valerate (5.4 micrograms/mL), so that the calculated saturation concentrations of the two corticosteroids in stratum corneum were within a factor of 2. However, the drug amounts or concentrations of the more lipophilic corticosteroid (betamethasone 17-valerate) attained in viable layers (viable epidermis and dermis) at steady state were predicted to be greater than those of the less lipophilic corticosteroid (betamethasone) when the results in the permeation and equilibrium studies were interpreted by a mathematical model. The drug distribution pattern predicted (i.e., that a more lipophilic corticosteroid preferentially partitions into viable layers) was reasonable when compared with that observed in the permeation study. The mean drug amount of betamethasone 17-valerate in dermis was four times greater than that of betamethasone, whereas the drug amounts of both corticosteroids in epidermis were similar to each other.

Adolescent↗
PubMed1999

Adsorptive and electrochemical behaviors of estradiol valerate at a mercury electrode.

It was found that estradiol valerate could be adsorbed at a mercury electrode under open circuit. The adsorptive and electrochemical behaviors of estradiol valerate on a static mercury electrode were investigated by cyclic voltammetry, linear scan voltammetry and chronocoulometry. Based on this, a sensitive and selective adsorptive stripping square-wave voltammetric method was developed for the determination of estradiol valerate based on the optimization of solution conditions and electrochemical parameters. It was found that in a Britton-Robinson buffer solution containing 18% alcohol (pH 9.5), estradiol valerate gave a sensitive reductive peak at potential -1.29 V (vs. SCE) and the peak current was linear with the concentration of estradiol valerate in the range 2.0 x 10(-8)-2.5 x 10(-6) mol L-1. The detection limit was 1.1 x 10(-8) mol L-1. The interference of some common steroid estrogens was examined and it was found that they did not interfere in the determination of estradiol valerate in the present system.

Adsorption↗
PubMed2025

Versatile sugar and valerate metabolic pathways in Paraburkholderia xenovorans LB400 enable tailored poly(3-hydroxybutyrate-co-3-hydroxyvalerate) production.

Poly(3-hydroxybutyrate) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) polymers are accumulated by diverse prokaryotes. Their distinct monomer compositions enable their use as tailored bioplastics. The aims were to characterize the poly(3-hydroxybutyrate) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) synthesis by Paraburkholderia xenovorans LB400 using different sugars and valerate, and to gain genome-oriented insights into polyhydroxyalkanoate production. d-Glucose, d-mannitol, d-gluconate, and d-xylose were evaluated as sole carbon sources or supplemented with valerate. Polyhydroxyalkanoates synthesized by strain LB400 were characterized through GC-MS, GC-FID, FTIR, and 1H and 13C-NMR. P. xenovorans LB400 reached 1.00-1.39&#xa0;g L-1 of dry cell weight (DCW) with a P(3HB) content of 21-43% w w-1 when grown on different sugars. The addition of valerate to the sugar-grown LB400 cultures yielded a DCW of 1.79 to 2.29&#xa0;g L-1 and a P(3HB-co-3HV) content of 50.0&#x2012;51.2% w w-1, with varying 3HV compositions (28&#x2012;43&#xa0;mol%). The highest 3HV incorporation was observed with d-xylose and valerate. Genomic analyses of strain LB400 revealed key elements of sugar metabolism influencing growth, polymer accumulation, and monomer composition. LB400 genome encodes the PhaJ-like R-specific hydratase and FadJ epimerase, which are potentially useful for modulating copolymer composition. PHA production under bioreactor conditions was evaluated. In a bioreactor fed with d-glucose, LB400 achieved a P(3HB) concentration of 2.2&#xa0;g L-1. These findings highlight the metabolic versatility of P. xenovorans LB400 in utilizing diverse sugars to produce either P(3HB) or tailor-made P(3HB-co-3HV), supporting the development of bioplastics for specific applications. KEY POINTS: &#x2022; Strain LB400 produced P(3HB-co-3HV) from various sugars and valerate. &#x2022; Sugar type drives LB400 PHA copolymer synthesis and composition. &#x2022; Strain LB400 PHA production was scaled up to a bioreactor.

Polyesters↗
PubMed1978

Topical betamethasone 17-valerate is an anticorticosteroid in the rat. 2. Anti-inflammatory and anti-lymphocyte activities.

In the oxazolone-induced delayed hypersensitivity inflammation in the rat ear, betamethasone 17-valerate, in contrast to other topical corticosteroids, is incapable of suppressing oedema. When given in combination with triamcinolone acetonide, betamethasone 17-valerate competitively antagonizes the anti-inflammatory action of the active steroid. When tested in the mouse, betamethasone 17-valerate behaved as an anti-inflammatory agent 15 and 80 times as potent as betamethasone and hydrocortisone respectively. In an in vivo lymphocyte culture system in which preincubation with corticosteroids prevents subsequent phytohaemagglutinin induced DNA synthesis, betamethasone 17-valerate was less active than even hydrocortisone when rat lymph node cells were used, but with human cell preparations it was more potent than either hydrocortisone or betamethasone. Betamethasone 17-valerate behaves uniquely in the rat as an anticorticosteroid; in mouse and in man the compound behaves as a normal corticosteroid.

Administration, Topical↗