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At least 1,063 records · Page 59Linked to original sources
PubMed1993

Activity of topically applied methylprednisolone aceponate in relation to other topical glucocorticosteroids in healthy volunteers.

Topical glucocorticosteroids are useful in the treatment of various skin diseases. Although there are already many corticosteroids available, there is still need for highly potent and well tolerated ones. The anti-inflammatory activity of methylprednisolone aceponate (MPA, CAS 86401-95-8) has been investigated in 165 healthy volunteers of either sex. UV-B irradiation or cellophane tape stripping has served to produce erythema. First, the dose response relationship of MPA ointment (0.01%, 0.05%, 0.1% and 0.5%) has been evaluated. MPA effects have been related to those of the vehicle and difluocortolone 21-valerate 0.1% (DFV) ointment. Then the activity of 0.1% MPA (cream, ointment and fatty ointment) has been related to those of the respective vehicles as well as commercially available preparations of five corticosteroids: betamethasone 17,21-dipropionate 0.64% (BDP), betamethasone 17-valerate 0.1% (BV), clobetasol 17-propionate 0.05% (CP), hydrocortisone 17-butyrate 0.1% (HCB), prednicarbate 0.25% (P). In each experiment, MPA activity significantly exceeded that of the respective vehicle (p < or = 0.05). MPA 0.01-0.5% ointment exhibited strong anti-inflammatory activity, at least corresponding to that of 0.1% DFV ointment. A dose-dependent activity could only be observed in the UV-B-erythema test using 3 fold MED (minimal erythema doses) for irradiation, a test model differentiating strong corticosteroids. The comparison of 0.1% MPA formulations with respective reference preparations showed the following results: On stripped skin no significant differences could be detected which is demonstrated in the example of cream formulations.(ABSTRACT TRUNCATED AT 250 WORDS)

Administration, Topical↗
PubMed1977

The use of cyclofenil in menopausal women.

On the basis of some reports, a double-blind experimental trial comparing the activity of cyclofenil, estradiol valerate and placebo in post-menopausal disturbances was carried out. 60 women among those attending the menopausal clinic and affected by climateric disorders have been treated. The objective criterium for the admission had been established on the basis of the value of plasma FSH (greater or equal to 800 ng/ml). Besides the gynecological examination (including objective and subjective examination, hormone dosage, endometrial biopsy) patients underwent psychological examination (individual interview and psychometric tests) before and after 28 days of therapy The statistical evaluation of the results obtained with the 3 drugs showed a statistically significant difference between the placebo and the active compounds: no significant difference between cyclofenil and estradiol valerate was observed.

Cresols↗
PubMedDate not supplied

Intrauterine or oral administration of levonorgestrel in combination with estradiol to perimenopausal women--effects on lipid metabolism during 12 months of treatment.

OBJECTIVE: Limited data concerning serum lipids and lipoproteins are available on the effect of HRT in perimenopausal women, who commonly have marked bleeding disturbances and may have severe climacteric symptoms. Almost all previously published data have utilized a simplified form of lipoprotein analysis, which includes an estimation and not a determination of LDL cholesterol. To delineate the role of locally administered progestogen, perimenopausal women were studied for a year. PATIENTS AND METHODS: 40 perimenopausal women with climacteric complaints. The continuous release of low-dose levonorgestrel from an intrauterine device was used as progestogen co-medication to estradiol in a new type of continuous combined hormone replacement therapy. Women were randomized to either cyclical treatment with 2 mg of oral estradiol valerate in combination with 250 micrograms of levonorgestrel for the last ten days (Cyclo Progynova) or continuously with 2 mg estradiol valerate orally in combination with a 20 micrograms per 24 hour levonorgestrel releasing intrauterine device. RESULTS: Reduced HDL cholesterol was initially recorded in both treatment arms and disappeared after 1 year of treatment. Triglycerides were reduced in the orally treated group, but not in the device group. No changes in LDL cholesterol were noted. CONCLUSIONS: The findings suggest that continuous combined HRT with intrauterine release of 20 micrograms levonorgestrel per 24 hours in perimenopausal women is neutral as far as lipid metabolism is concerned, since no alterations compared with pretreatment values could be noted after 12 months of treatment. Less marked lipid changes were obtained in perimenopausal women as compared with data on postmenopausal women. Differences in methodology may partly account for this.

Administration, Oral↗
PubMed1978

Hemoglobin A1C separation by isoelectric focusing.

A modified type of isolectric focusing has been applied successfully to the separation of hemoglobin A1C (HbA1C) from HbA in normal and diabetic cell lysates. It consists of transforming a linear pH gradient into a nonlinear one, by the addition of an amphoteric substance ("separator" or "pH gradient modifier") with an isoelectric point (pI) close to the pI's of the two hemoglobins. Among the "modifiers" tested, histidine, proline, threonine, beta-alanine, 6-amino caproic acid, and 5-amino valeric acid are not useful in the hemoglobin pI range (pH 6.9--7.0). The dipeptide histidyl-glycine (pI = 6.8; pI-pK1 = 1) is very efficient in flattening the pH gradient, in the hemoglobin region. even when added in low concentrations (10--100 mM), thus affording full resolution of the two hemoglobin species.

Alanine↗
PubMed2005

Bioconversion of naltrexone and its 3-O-alkyl-ester prodrugs in a human skin equivalent.

The purpose of this study was to compare the percutaneous absorption and bioconversion of naltrexone (NTX), naltrexone-3-O-valerate (VAL), and naltrexone-3-O-(2'-ethylbutyrate) (ETBUT) in a human skin equivalent model (EpiDerm) and in fresh human skin in vitro. NTX diffusion and metabolism to 6-beta-naltrexol (NTXol) were quantitated and compared in the EpiDerm and in excised fresh human skin. VAL and ETBUT diffusion and bioconversion studies were also completed in EpiDerm. Naltrexone bioconverted to levels of 3+/-2% NTXol in the EpiDerm and 1+/-0.5% in fresh human skin. VAL hydrolyzed rapidly in the EpiDerm and mainly (93+/-4%) NTX was found in the receiver compartment, similar to human skin. More intact ETBUT permeated the EpiDerm tissue compared to VAL, and only 15+/-11% NTX was found in the receiver. Significantly higher fluxes of NTX and the prodrugs were observed with the EpiDerm compared to human skin. A similar flux enhancement level was observed for VAL, compared to NTX base, in the EpiDerm and the human skin. Metabolically active human epidermal models like EpiDerm are useful as an alternative experimental system to human skin for prediction of topical/transdermal drug/prodrug bioconversion.

Algorithms↗
PubMedDate not supplied

Anchor-linked intermediates in peptide amide synthesis are caused by dimeric anchors on the solid supports.

Cleavage and kinetic studies have been carried out using commercially obtained H-Tyr(tBu)-5-(4'-aminomethyl-3',5'-dimethoxyphenoxy)valeric acid-TentaGelS (H-Tyr(tBu)-4-ADPV-TentaGelS) and H-Tyr (tBu)-4-ADPV-Ala-aminomethyl-resin (H-Tyr(tBu)-4-ADPV-AM-resin) prepared from commercially available resin and loaded with commercially available Fmoc-4-ADPV-OH amide anchor. Cleavage with pure trifluoroacetic acid (TFA) gave the intermediate H-Tyr-4-ADPV-NH2, which was then degraded to H-Tyr-NH2, and cleavage with TFA/dichloromethane (1:9) yielded H-Tyr-4-ADPV-NH2 which could be isolated in preparative amounts. Cleavage reactions with 15N-labelled H-Ala-4-ADPV-(15N)-Gly-AM-resin yielded the intermediate H-Ala-4-ADPV-NH2, which contained no 15N as demonstrated by 1H-NMR. The analysis of the commercial Fmoc-4-ADPV-OH amide anchor showed the presence of Fmoc-4-ADPV-4-ADPV-OH as an impurity in high amounts. This dimeric anchor molecule is the cause of formation of the anchor-linked peptide intermediate obtained during the cleavage from the resin. The particularly high acid-lability of the amide bond between the two ADPV moieties was utilized to synthesize sidechain and C-terminally 4-ADPV protected pentagastrin on a double-anchor resin, and to cleave it using 5% trifluoroacetic acid in dichloromethane. This method may offer a new way for the synthesis of protected peptide amides with improved solubility to be used in fragment condensation.

Amides↗
PubMed2001

Bioelectrochemical analysis of neuropathy target esterase activity in blood.

Bioelectrochemical analysis of neuropathy target esterase (NTE) and its inhibitors is based on the combination of the NTE-catalyzed hydrolysis of phenyl valerate and phenol detection by a tyrosinase carbon-paste electrode. The use of the tyrosinase electrode improves 10-fold the sensitivity of NTE detection in comparison with a spectrophotometric method. The tyrosinase electrode was found to be suitable for measurements in whole human blood where spectrophotometric detection is considerably restricted. The specificity of NTE in blood for mipafox and di-2-propyl phosphorofluoridate was close to that for neuronal NTE. The NTE-like activity in blood was determined to be 0.19 +/- 0.02 nmol/min/mg of protein.

Animals↗
PubMed1993

Corticosteroids induce proliferation but do not influence TNF- or IL-1 beta-induced ICAM-1 expression of human dermal microvascular endothelial cells in vitro.

The effects of hydrocortisone, dexamethasone, betamethasone 17-valerate and clobetasol propionate at concentrations of 10(-5)-10(-12) M on the proliferation of human dermal microvascular endothelial cells (HDMEC) were studied in vitro. In addition, confluent HDMEC were treated with TNF (1000 U/ml) or IL-1 beta (1000 U/ml) alone or in combination with the corticosteroids (10(-5) M, 10(-6) M) for 24 h, and cytokine-induced expression of intercellular adhesion molecule-1 (ICAM-1) was assessed by immunocytochemistry. Controls were treated either with growth medium or with the corticosteroids alone. All tested corticosteroids stimulated HDMEC growth after 4 and 6 days of treatment in a dose-dependent manner, as assessed by 3H-thymidine incorporation and the 4-methyl-umbelliferyl heptanoate (MUH) assay. The minimal effective concentration was 10(-9) M for hydrocortisone, 10(-10) M for dexamethasone and betamethasone, and 10(-12) M for clobetasol. In untreated and in corticosteroid-treated cultures, less than 5% of the cells expressed ICAM-1. TNF and IL-1 beta were strong inducers of ICAM-1 expression on 74% and 82% of the cells, respectively. None of the tested corticosteroids significantly influenced cytokine-induced ICAM-1 expression, suggesting that the anti-inflammatory effects of corticosteroids are not related to ICAM-1 modulation on HDMEC.

Adrenal Cortex Hormones↗
PubMed1985

Antibodies to orthokeratotic keratinocytes in monitoring the drug-induced inhibition of parakeratotic differentiation in adult and infant mice.

Parakeratosis (PK) is a common feature of the abnormal epidermis in several disorders of keratinization. Tar phenols, retinoids and steroids which cause the inhibition of PK and the restoration of orthokeratosis (OK) are used for treating psoriasiform conditions. In this work, we studied two experimental models of the drug-induced inhibition of PK: (1) the suppression of the normal development of PK in the infant mouse tail and (2) the OK conversion of established PK in the adult tail. Two markers of OK were studied: the histological evaluation of the granular layer and the expression of cytoplasmic antigens linked to OK differentiation. It was demonstrated that high-boiling tar phenols cause a more potent inhibition of PK than betamethasone valerate. Most importantly, immunofluorescence showed that the switch to OK differentiation was located in the cells situated in a suprabasal position. The use of these immunological markers to investigate and anti-parakeratotic mechanisms has revealed that these drugs act at stages of keratinocyte differentiation which are distinct from those previously suggested.

Acids↗
PubMed1985

Glucocorticoid-induced vasoconstriction in canine skin.

Vasoconstriction, manifest as a reduction in blood flow necessary to maintain a constant pressure, was observed over 4 h in the arteries supplying isolated abdominal skin flaps of greyhound dogs treated with intravenously administered betamethasone-17-valerate. Norepinephrine concentration-response curves performed initially and after 4 h showed no significant difference between the treated or control animals.

Animals↗
PubMed1977

Effects of glucocorticosteroids on primary human skin fibroblasts. I. Inhibition of the proliferation of cultured primary human skin and mouse L929 fibroblasts.

Various glucocorticosteroids were added to logarithmically growing cultures of primary human skin fibroblasts and of mouse L929 fibroblasts. These steroids inhibited proliferation of the human fibroblasts at concentrations which fall in a range expected to occur during the topical treatment of skin disorders. In terms of the concentrations required for the inhibition hydrocortisone was least and clobetasol-17-propionate most effective. All other steroids studied (hydrocortisone-17-butyrate, triamcinolone acetonide, betamethasone-17-valerate and hydrocortisone-21-acetate) showed medium effectiveness. Fluorination as such may not enhance the inhibitory effect. The inhibition was independent of the source (baby foreskin or adult arm skin) and passage number (7th to 13th or 15th and 16th passage, respectively) of the cells. The possible relationship between the inhibition of cell proliferation by such steroids and their therapeutic effect in psoriasis and their atrophic side effects is discussed. Mouse L929 fibroblasts were affected at 10(3)--10(4)-fold lower steroid concentrations and the range of the effective concentrations was 10(4)--10(5) times as wide as that for the primary human skin fibroblasts. It was concluded that these mouse fibroblasts are a poor model system for the study of in vivo effects of glucocorticosteroids in man.

Administration, Topical↗
PubMed1977

Effects of glucocorticosteroids on primary human skin fibroblasts. II. Effects on total protein and collagen biosynthesis by confluent cell cultures.

Confluent cultures of normal primary human skin fibroblasts were incubated with various glucocorticosteroids which are in current use clinically for the treatment of various skin disorders. For all steroids concentrations were found at which collagen hydroxyproline formation was inhibited, while total protein synthesis was little affected. The concentration effective for inhibition was highest for hydrocortisone and lowest for clobetasol-17-propionate. All other steroids (hydrocortisone-17-butyrate, triamcinolone acetonide and betamethasone-17-valerate) showed medium effectiveness. Fluorination as such was not a factor in the degree of inhibition. The inhibition observed was shown to be independent of concomitant specific effects on cell proliferation or cell turnover. The possible implications of these findings on the therapeutic effects in psoriasis and the frequently occurring atrophic side-effects of these steroids are discussed.

Administration, Topical↗
PubMed1991

Production of poly-D(-)-3-hydroxybutyrate and poly-D(-)-3-hydroxyvalerate by strains of Alcaligenes latus.

Alcaligenes latus strains can accumulate poly-D(-)-3-hydroxybutyrate (PHB) up to about 85% of cell dry weight. The abilities to store poly-D(-)-3-hydroxyvalerate (PHV) of three strains of A. latus were investigated. With Na-propionate as PHV precursor, strain A. latusDSM 1122 had better PHV accumulation ability than strains A. latus DSM 1123 and 1124. Strain A. latus DSM 1123 could store PHV when Na-valerate but not Na-propionate served as the PHV precursor. PHB and PHV accumulation by A. latus DSM 1124 rapidly increased when propionic acid and acetic acid were together added to the fermentor. This increase was not obtained in the culture shaker flask and fermentor growing the same strain when Na-propionate alone served as a PHV precursor.

Acetates↗
PubMed1975

Inhibition of glucose-6-phosphate dehydrogenase activity by betamethasone and three of its esters with dermatological importance.

Betamethasone, betamethasone-17-valerate, betamethasone-17-benzoate, and betamethasone-17,21-diproprionate were investigated for their inhbitory action on glucose-beta-phosphate dehydrogenase (G-6-PDH) activity (pure enzyme from yeast, enzyme from human skin homogenate). Between these four compounds, marked differences were encountered which could not be attributed to the presence of an esterified or unesterified steroid. According to these data it does not seem to be justified to consider betamethasone esters simply as the transport forms of the topically inactive betamethasone but one must consider the betamethasone esters having biochemical actions of their own.

Betamethasone↗
PubMed1978

Comparative study of the vasoconstrictor activity of halopredone acetate in a modified McKenzie test.

The vasoconstrictor activity of four steroids, administered in solution and in the commercially available form, were compared in healthy volunteer subjects. Evaluation was based on conventional visual observations and photometric measurement of reflectance. Statistical analysis showed that halopredone acetate had less vasoconstrictor action on healthy skin than fluocinolone acetonide, beta-methasone valerate and hydrocortisone acetate. The halopredone acetate results were identical to those of th excipient, although it was found that halopredone acetate cream (Topicon) had a marked anti-inflammatory effect in animals and on human dermatoses. The validity of the McKenzie test, as an unequivocal screening procedure for the potency of topical steroids is discussed, and the accuracy and precision of photometric evaluation is emphasized.

Administration, Topical↗
PubMed1986

The effects of short-chain fatty acids on the neuronal membrane functions of Helix pomatia. I. Electrical properties.

The effects of short-chain fatty acids on the membrane excitability, current-voltage (I-V) characteristics, and cell volume of Helix pomatia neurons were studied. 2-Decenoic acid (DA), having 10 carbon atoms in the hydrocarbon chain, suppressed the excitability of bursting neurons RPa1 (Sakharov and Salanki, 1969) for 30-60 min, while valeric acid (VA), having 5 carbon atoms, had no significant effect on excitability. DA had three different effects on the excitability of beating neurons: in some neurons DA suppressed excitability as in bursting neurons; in a second type of neuron DA had a negligible effect on excitability; and in the neuron located near RPa1 DA had a pentylentetrazol (PTZ)-like effect, i.e., it converted the discharge of the neuron from beating to bursting. DA decreased the peak value of the current, inducing a negative-resistance region in the I-V curve of the bursting neuron without any change in the level of the voltage at which the current reaches its maximal value. DA inhibited the hyperpolarization induced by activation of the Na+ pump, tested after preliminary enrichment of neurons with Na+ ions by incubation in a potassium-free solution for 20 min. DA caused a swelling of the neuron by about 10% which was independent of the Na+ pump. In all the above-mentioned cases VA had no significant effect.

Animals↗
PubMed1986

The effects of short-chain fatty acids on the neuronal membrane functions of Helix pomatia. II. Cholinoreceptive properties.

We have examined the effects of short-chain fatty acids on acetylcholine (ACh)-induced transmembrane currents using internally dialyzed neurons of Helix. Decenoic acid, which increased the fluidity of excitable membranes, caused dramatic changes in the voltage sensitivity of ACh currents consisting of an ACh-induced increase in membrane permeability for K+ and Na+ ions and a shift of the Erev of these ACh responses to more positive potentials. Valeric acid, which did not change the membrane fluidity, had no effect on this type of ACh response. Changes of the ENa and ECl had no effect on the size of the decenoic acid-induced shift of the Erev. But the influence of decenoic acid on the voltage sensitivity of ACh-induced currents almost disappeared after the change of the EK by the reduction of the internal K concentration. Decenoic acid had no effect on ACh responses in which K+ ions were not involved in the generation of ACh-induced currents. The results suggest that decenoic acid-induced changes in membrane fluidity modulate cholinoreceptive properties of the neuronal membrane by the inhibition of the K+ carrier involved in the generation of ACh responses.

Animals↗
PubMed1994

Induction of lipocortin 1 by topical steroid in rat skin.

Western blotting and densitometric analysis of extracts obtained from EDTA extraction of skin segments showed greater extracellular Lipocortin 1 (LC1) in skin sites from steroid-treated animals compared to that seen in matched vehicle treated animals. Extracellular LC1 was maximal 3 hr after steroid, less was found in skin after 6 hr and levels had returned to basal at 18 hr. Pre-treatment of rats with the glucocorticoid receptor antagonist RU38486 (20 mg/kg) prevented the steroid induction of extracellular LC1 at both the 3 and 6 hr time-points. Systemic treatment of rats with betamethasone sodium phosphate (0.1-1 mg/kg) showed that the induction of LC1 on the cell surface was both time- and dose-dependent. Oedema in rat skin caused by 5-hydroxytryptamine (5-HT), platelet activating factor (PAF) and zymosan activated serum (ZAS) was assessed using 125I-labelled human serum albumin. Following a 3 hr topical treatment with betamethasone-17-valerate the inflammatory activities of all of the tested stimuli were significantly attenuated demonstrating that at this time-point the topical steroid was biologically active. Topical steroid treatment of the skin resulted in a translocation of LC1 to the cell surface, which was maximal after a 3 hr period and was also temporally associated with the anti-inflammatory effect of these agents.

Administration, Topical↗