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PubMed1990

Antipsoriatic therapies inhibit epidermal plasminogen activator activity.

Urokinase (UK, Mr 55,000) and tissue-type plasminogen activator (tPA, Mr 74,000) are serine proteinases involved in many biological processes, ie, cell migration, neoplastic transformation, and extracellular proteolysis. Cutaneous fibrinolytic activity (dependent on the activity of UK and tPA) was studied with the autohistographic fibrin film method in 40 patients affected by psoriasis vulgaris before and after topical (anthralin, betamethasone valerate, hydrocolloid occlusive dressing) or systemic psoralen-ultraviolet-light (PUVA) treatments. Autohistographic studies also were performed after apposition of monoclonal antibodies directed against the catalytic site of UK and tPA. Finally, UK and tPA were localized immunohistochemically in the psoriatic plaques and in controls using the immunoperoxidase procedure based on the biotin/avidin system. UK and tPA immunoreactivity was present in the cytoplasm and around the outlines of keratinocytes in the psoriatic patches before treatment and in the patches not cleared after treatment, while it was not detectable in normal epidermis, in the unaffected psoriatic epidermis, and in the cleared psoriatic skin. Cutaneous fibrinolytic activity was present in the cases in which UK and tPA were detected histochemically and, in the psoriatic epidermis, it was abolished by preincubation with anti-tPA but not with anti-UK antibodies. This study suggests that established topical and systemic treatments for psoriasis possess UK and tPA antagonist activity.

Adult↗
PubMed1980

Oxidative metabolism of 4-aminobutyrate by rat brain mitochondria: inhibition by branched-chain fatty acid.

The oxidation of 4-aminobutyric acid (GABA) by nonsynaptosomal mitochondria isolated from rat forebrain and the inhibition of this metabolism by the branched-chain fatty acids 2-methyl-2-ethyl caproate (MEC) and 2.2-dimethyl valerate (DMV) were studied. The rate of GABA oxidation, as measured by O2 uptake, was determined in medium containing either 5 or 100 mM-[K+]. The apparent Km for GABA was 1.16 +/- 0.19 mM and the Vmax in state 3 was 23.8 +/- 5.5 ng-atoms O2 x min-1 x mg protein-1 in 5 m M-[K+]. In a medium with 100 mM-[K+] the apparent Km was 1.11 +/- 0.17 mM and Vmax was 47.4 +/- 5.7 ng-atoms O2 x min-1 x mg protein-1. The Ki for MEC was determined to be 0.58 +/- 0.24 or 0.32 +/- 0.08 mM, in 5 or 100 mM-[K+], respectively. For DMV, the Ki was 0.28 +/- 0.05 or 0.34 +/- 0.06 mM, in 5 or 100 mM-[K+] medium, respectively. The O2 uptake of the mitochondria in the presence of GABA was coupled to the formation of glutamate and aspartate; the ratio of oxygen uptake to the rate of amino acid formation was close to the theoretical value of 3. Neither the [K+] nor any of the above inhibitors had any effect on this ratio. The metabolism of exogenous succinic semialdehyde (SSA) by these same mitochondria was also examined. The Vmax for utilization of oxygen in the presence of SSA was much greater than that found with exogenously added GABA, indicating that the capacity for GABA oxidation by these mitochondria is not limited by SSA dehydrogenase. In addition, the branched-chain fatty acids did not inhibit the metabolism of exogenously added SSA. Thus, the inhibitors examined apparently act by competitively inhibiting the GABA transaminase system of the mitochondria.

Animals↗
PubMed1994

Inhibition of glucocorticoid-induced epidermal and dermal atrophy with KH 1060--a potent 20-epi analogue of 1,25-dihydroxyvitamin D3.

1. The possibility of preventing and treating glucocorticoid-induced skin atrophy with KH 1060 (the potent 20-epi-22-oxa-24a-homo-26,27-dimethyl analogue of 1,25-dihydroxyvitamin D3) was examined in a hairless mouse model. 2. KH 1060 (0.625-6.25 pmol cm-2 of skin) applied topically for 7 days together with 2.5 nmol cm-2 betamethasone-17-valerate prevented, in a concentration-dependent manner, the development of epidermal, dermal and total skin thinning caused by the glucocorticoid. The effect of KH 1060 on the epidermis occurred at a lower dose than on the dermis, and at doses above 1.25 pmol cm-2 KH 1060 caused epidermal hyperplasia. 3. KH 1060 (2.5 pmol cm-2) prevented the development of betamethasone-associated skin atrophy in mice during a long-term (4 weeks) treatment, and reversed established cutaneous glucocorticoid atrophy. 4. Radiolabelling experiments with [35S]-sulphate and [3H]-proline in vivo revealed that KH 1060 stimulated the synthesis of sulphated glycosaminoglycans and hydroxyproline in skin treated with betamethasone. 5. These findings strongly suggest that KH 1060 prevents and reverses glucocorticoid-induced skin atrophy by stimulating epidermal proliferation and enhancing synthesis of extracellular matrix in the dermis.

Animals↗
PubMed1997

A case of contact dermatitis due to impurities of cetyl alcohol.

A 29-year-old man being treated for itchy lesions on the amputation stump of the thigh became allergic to betamethasone valerate and gentamicin sulfate cream (Rinderon VG). Closed patch tests with all the ingredients of the cream revealed positive reactions to cetyl alcohol 30% to 5% pet. Gas chromatographic analysis of the cetyl alcohol in the cream base detected stearyl alcohol (C18), myristyl alcohol (C14) and lauryl alcohol (C12) in addition to the main component of cetyl alcohol (C16). Patch testing with 99% pure analytical reagent grade saturated alcohols (C10, C11, C12, C13, C14, C15, C16, C17, C18, C19, C20) showed negative reactions. Thus, it is concluded that some minor impurities in cetyl alcohol not detected by gas chromatography might be the cause of this dermatitis.

Adult↗
PubMed1968

Sex attractant of sugar beet wireworm: identification and biological activity.

The sex attractant produced by adult females of the sugar beet wire-worm, Limonius californicus (Mannerheim) has been isolated and identified as valeric acid. In the laboratory, male wireworm beetles are repelled by the pure attractant but are drawn with intense sexual excitement to its dilute solutions; in the field, male beetles are lured from a distance of 12 meters. The pheromone occurs in unusually large amounts in the female's body.

Animals↗
PubMed1977

Leakage of cellular material from Thiobacillus ferrooxidans in the presence of organic acids.

Thiobacillus ferroodixans cells released varying amounts of iron, phosphate, sugar, ribonucleic acid, deoxyribonucleic acid, and substances that absorbed light at both 260 and 280 nm, when exposed to 10(-2) to 10(-1) M concentrations of these organic acids: propionic, butyric, valeric, hexanoic, and oxalacetic. These acids also retarded iron oxidation by the cells. Electron microscope observation of cells after exposure to the organic acids showed varying degrees of cell envelope disruption, suggesting that the mode of inhibition of autotrophic iron oxidation in the cell involves interference with the function of the cell envelope, possibly the cell membrane.

Acids↗
PubMed1969

Biochemical decomposition of the herbicide N-(3,4-dichlorophenyl)-2-methylpentanamide and related compounds.

Organisms capable of decomposing N-(3,4-dichlorophenyl)-2-methylpentanamide (Karsil) were isolated, identified, and tested for their ability to hydrolyze this herbicide. Primary products of Karsil decomposition by cells and cell-free extracts of a Penicillium sp. were identified as 2-methyl-valeric acid and 3,4-dichloroaniline. The Karsil acylamidase (EC 3.5.1.a aryl acylamine amidohydrolase) was an induced enzyme. It was partially purified and tested for its ability to hydrolyze 25 related compounds. Some relations between the structures of these compounds and their susceptibility to enzymatic hydrolysis were discerned.

Amidohydrolases↗
PubMed1970

Effects of omega-amino acids and related compounds on staphylococcal infections in mice: a combined prophylactic-therapeutic procedure.

By a short-term combined prophylactic-therapeutic procedure, the following compounds were found to be active against staphylococcal infections in Swiss mice: gamma-aminobutyric acid, gamma-amino-beta-hydroxybutyric acid (GABOB), delta-amino-valeric acid (DAVA), epsilon-aminocaproic acid (EACA), trans-4-aminomethylcyclohexanecarboxylic acid (trans-AMCHA), taurine, and cysteic acid. Many of these compounds had displayed limited or no activity by a previously used prophylactic procedure. Although DAVA and GABOB were the most potent of the straight-chain omega-amino acids, trans-AMCHA displayed the greatest antistaphylococcic activity of the omega-amino acids thus far investigated. Homocarnosine (gamma-aminobutyrl histidine, which also was active by the prophylactic procedure) equalled trans-AMCHA in activity. Taurine was similar in potency to DAVA, and the activity of cysteic acid approximated that of EACA.

Alanine↗
PubMed1970

Inhibition of carotenoid hydroxylation in Staphylococcus aureus by mixed-function oxidase inhibitors.

Compounds known to be inhibitors of mixed-function oxidase systems inhibited the aerobic synthesis of hydroxylated carotenoids in Staphylococcus aureus U-71. Growth of the cells in the presence of 2-diethylaminoethyl-2,2-diphenyl valerate, 2,4-dichloro-6-phenylphenoxyethylamine, 2,4-dichloro-6-phenylphenoxyethyldiethylamine, and piperonyl butoxide reduced the levels of the rubixanthins found in stationary-phase cells by 75 to 97%. In cells grown with mevalonate-2-(14)C, the turnover rate of phytoene was reduced and the turnover rate of phytofluenol was increased in the presence of these inhibitors. The zeta- and delta-carotenes, which turn over in the absence of the inhibitors, accumulated (14)C in the presence of the inhibitors. This suggested that a mixed-function oxidase was responsible for the aerobic hydroxylation of delta-carotene in S. aureus U-71.

Carbon Isotopes↗
PubMed1971

Growth of Escherichia coli on short-chain fatty acids: growth characteristics of mutants.

The parent Escherichia coli K-12 is constitutive for the enzymes of the glyoxylate bypass and adapts to growth on long-chain fatty acids (C(12) to C(18)). It does not utilize medium-chain (C(6) to C(11)) or short-chain (C(4), C(5)) n-monocarboxylic acids. Several mutants of this strain which grow using short- or medium-chain acids, or both, as the sole carbon source were selected and characterized. One mutant (D(1)) synthesizes the beta-oxidation enzymes constitutively and grows on medium-chain but not on short-chain acids. A second (N(3)) is partially derepressed for synthesis of these enzymes and grows both on medium-chain and on short-chain acids. Secondary mutants (N(3)V(-), N(3)B(-), N(3)OL(-)) were derived from N(3). N(3)V(-) grows on even-chain but not on odd-chain acids and exhibits a lesion in propionate oxidation. N(3)B(-) grows on odd-chain but not on even-chain acids and exhibits no crotonase activity as assayed by hydration of crotonyl-CoA. N(3)OL(-) grows on acetate and propionate but does not utilize fatty acids C(4) to C(18); it exhibits multiple deficiencies in the beta-oxidation pathway. Growth on acetate of N(3), but not of the parent strain, is inhibited by 4-pentenoate. Revertants of N(3) which are resistant to growth inhibition by 4-pentenoate (N(3)PR) exhibit loss of ability to grow on short-chain acids but retain the ability to grow on medium-chain and long-chain acids. The growth characteristics of these mutants suggest that in order to grow at the expense of butyrate and valerate, E. coli must be (i) derepressed for synthesis of the beta-oxidation enzymes and (ii) derepressed for synthesis of a short-chain fatty acid uptake system.

Acetates↗
PubMed1989

Soluble interleukin 2 receptor in atopic eczema.

OBJECTIVE: To determine whether serum soluble interleukin 2 receptor concentrations are related to disease activity in atopic eczema. DESIGN: Single cohort longitudinal study with controls. SETTING: Outpatient and general medicine departments in secondary referral centre. PATIENTS: Of 15 patients aged 17-57 with severe atopic eczema, all with acute exacerbations of disease, 13 were admitted to hospital and two treated as outpatients until the skin lesions had resolved or greatly improved. Nineteen controls gave single blood samples. INTERVENTIONS: Daily skin dressing with betamethasone valerate (0.025%) and ichthammol paste and tubular dressings. END POINT: Resolution of or considerable improvement in skin lesions. MEASUREMENTS AND MAIN RESULTS: Enzyme linked immunosorbent assays (ELISA) were used to measure serum soluble interleukin 2 receptor concentrations in blood samples taken on admission, at intervals subsequently, and on discharge. Clinical scores of disease activity were also made. Median concentrations on admission were significantly higher (770 U/ml) in the patients than the controls (300 U/ml). Concentrations fell significantly during treatment. In 25 assessments made at different times in 13 patients serum soluble interleukin 2 receptor concentration correlated significantly (R = 0.73) with clinical disease activity. CONCLUSIONS: Cellular immunopathogenic mechanisms contribute to atopic eczema. Immune activation can be measured in atopic eczema by measurements of soluble interleukin 2 receptor, and this should facilitate assessment of response to treatment.

Acute Disease↗
PubMed2002

Randomised controlled trial of short bursts of a potent topical corticosteroid versus prolonged use of a mild preparation for children with mild or moderate atopic eczema.

OBJECTIVE: To determine whether a three day burst of a potent corticosteroid is more effective than a mild preparation used for seven days in children with mild or moderate atopic eczema. DESIGN: Randomised, double blind, parallel group study of 18 weeks' duration. SETTING: 13 general practices and a teaching hospital in the Nottingham area. PARTICIPANTS: 174 children with mild or moderate atopic eczema recruited from general practices and 33 from a hospital outpatient clinic. INTERVENTIONS: 0.1% betamethasone valerate applied for three days followed by the base ointment for four days versus 1% hydrocortisone applied for seven days. MAIN OUTCOME MEASURES: Primary outcomes were total number of scratch-free days and number of relapses. Secondary outcomes were median duration of relapses, number of undisturbed nights, disease severity (six area, six sign atopic dermatitis severity scale), scores on two quality of life measures (children's life quality index and dermatitis family impact questionnaire), and number of patients in whom treatment failed in each arm. RESULTS: No differences were found between the two groups. This was consistent for all outcomes. The median number of scratch-free days was 118.0 for the mild group and 117.5 for the potent group (difference 0.5, 95% confidence interval -2.0 to 4.0, P=0.53). The median number of relapses for both groups was 1.0. Both groups showed clinically important improvements in disease severity and quality of life compared with baseline. CONCLUSION: A short burst of a potent topical corticosteroid is just as effective as prolonged use of a milder preparation for controlling mild or moderate atopic eczema in children.

Administration, Topical↗
PubMed1978

A comparison of oral and inhaled steroids in patients with chronic airways obstruction: features determining response.

Two trials comparing aerosol and oral steroid treatment were carried out in patients with chronic airways obstruction. All patients had a history of chronic productive cough and an FEV1 less than 70% predicted but did not have episodic or seasonal breathlessness with wheezing. One trial involved 18 outpatients, the other 18 inpatients. Both studies involved three consecutive treatment periods, the first with placebo aerosol, the second with active aerosol (betamethasone valerate, 800 microgram/day), and the third with oral prednisone or prednisolone (30 mg/day). Six patients showed a significant improvement in ventilatory capacity on steroids. Initial assessment included a comprehensive history using a questionnaire, skin tests, blood and sputum eosinophil counts, and chest radiography. In addition, for the inpatients, response to isoprenaline, daily sputum volume, and PaCO2 were measured. Only blood eosinophilia and variability in ventilatory capacity during the placebo period seemed indicative of a likely response to steroids. However, there was a large overlap between various features on assessment in the responders and non-responders, and the management of every patient with chronic airways obstruction should include a controlled trial of steroids. The steroid aerosol produced a good improvement in ventilatory capacity in the responsive patients who were hospitalised and this was thought to be helped by supervision of aerosol technique. Such an aerosol could therefore be used for a steroid trial although oral steroids were found to give a more definitive response.

Administration, Oral↗
PubMed1983

Dysphonia caused by inhaled steroids: recognition of a characteristic laryngeal abnormality.

Nine of 14 asthmatic patients who presented with persistent dysphonia while taking inhaled corticosteroids had a bilateral adductor vocal cord deformity with bowing of the cords on phonation. This causes the dysphonia and usually occurs without candidiasis. It was seen with beclomethasone dipropionate (in both pressurised aerosol and dry powder preparations), betamethasone valerate, and budesonide. It was related to the dose and potency of inhaled steroid and may represent a local steroid myopathy. It was reversed when the inhaled steroid was stopped, although resolution sometimes took weeks. Laryngeal candidiasis may have contributed to the vocal cord abnormality in two of these nine patients. Of the five patients without vocal cord deformity, laryngeal candidiasis was the sole cause of dysphonia in three. In the remaining two dysphonia was thought to be psychogenic. The vocal cord deformity may exist subclinically. Of nine patients who started to take aerosol steroid and who were examined monthly for one year, three developed vocal cord deformity but only one had persistent dysphonia. Vocal abuse did not appear to contribute to dysphonia.

Adult↗
PubMed1975

The lipids of four unusual non-pathogenic host-associated spirochetes.

The lipid compositions of two spirochetes isolated from the human oral cavity and two isolated from pig feces were examined. These isolates were unusual in that they did not require long-chain fatty acids for growth, as do the other host-associated spirochetes, but rather required isobutyric and valeric acids. Therefore, they could be cultured in a medium free of serum or fatty acid - albumin supplements. The major fatty acids synthesized were normal and iso fatty acids with 14 and 16 carbons. No unsaturated fatty acids were detected, nor were chain lengths longer than 16 carbons. The major complex lipids found were monogalactosyl diglyceride, phosphatidyl glycerol, and bis-phosphatidyl glycerol. Nitrogenous phospholipids, present in Treponema and Leptospira, were not synthesized by these novel strains. The data indicate an intermediate position of these isolates between Treponema and free-living Spriochaeta.

Animals↗
PubMed1982

Kinetics of erythrocyte penetration by aliphatic acids.

The rate of entry of aliphatic acids into human red blood cells was studied using a new stopped-flow technique. Solutions of aliphatic acids and erythrocyte suspensions were rapidly mixed in a stopped-flow reaction apparatus. The change in extracellular pH resulting from entry of acid into the cell was monitored using chlorophenol red as an extracellular indicator. Extracellular pH of the mixture was linearly related to differential light transmission at 480 and 560 nm. Values of membrane permeability were fitted to data using a model of passive exchange with flux proportional to the transmembrane concentration gradient. At all temperatures the permeabilities were in the order: valeric acid greater than butyric acid greater than propionic acid. Permeabilities were highly temperature dependent and the activation energy (10.5 kcal/mol) remained constant between 7 and 37 degrees C. Despite rapid rates of exchange, permeability measurements did not exhibit evidence of artifact secondary to an unstirred solvent layer on the cell surface. The data are compatible with the hypothesis that aliphatic acid transport across the erythrocyte membrane is passive in nature and proportional to the transmembrane concentration gradient.

Butyrates↗
PubMed2002

Comparison of the effects of daily applications between topical corticosteroid and tacrolimus ointments on normal skin: evaluation with noninvasive methods.

OBJECTIVE: To evaluate the skin changes of the neck of normal individuals after repeated applications of moderate-strength corticosteroid or tracrolimus ointment for 3 weeks by use of noninvasive biophysical measurements. METHODS: A 0.12% betamethasone-17-valerate ointment or a 0.1% tacrolimus ointment was applied to the right side of the neck of 8 adult volunteers twice daily for 3 weeks together with control petrolatum applied to the left side of the neck for comparison. Biophysical skin measurements were performed on the neck skin before, 1 and 3 weeks after the start of the treatment and 1 week after the cessation of the treatment. RESULTS: A decrease in hygroscopicity and water-holding capacity of the stratum corneum (SC) when evaluated with the in vivo water sorption-desorption test was found on the corticosteroid-ointment-treated side after 3 weeks of the treatment as compared with the petrolatum-treated side. The erythematous reaction to a topically applied 0.1% aqueous solution of methyl nicotinate, a vasodilator, appeared more slowly on the corticosteroid-ointment-treated skin than on the control skin. No such changes were observed on the skin treated with 0.1% tacrolimus ointment. CONCLUSION: Tacrolimus appears to cause few if any functional changes in the SC of healthy human skin because of its poor permeability into skin with an intact barrier function.

Administration, Topical↗
PubMedDate not supplied

Transcriptional activity of potent glucocorticoids: relevance of glucocorticoid receptor isoforms and drug metabolites.

As compared to standard glucocorticoids (GC), prednicarbate (PC) is favorable in the treatment of eczema due to its high benefit/risk ratio. The remarkable anti-inflammatory effects of PC are in strong contrast to its reported low glucocorticoid receptor (GR) binding affinity. In transfected COS-7 cells we related the transcriptional potencies of PC, its metabolites and conventional GC to their receptor binding properties. Moreover, the expression pattern of the human GR isoform hGRalpha and its mutual dominant negative inhibitor hGRbeta in skin cells have been investigated as well as the influence of hGRbeta on receptor binding and transactivation. hGRalpha mRNA and protein was largely overexpressed in skin cells. hGRbeta showed no influence on hGRalpha binding and transactivation. Concentration response curves indicated the greater transactivation potency of betamethasone 17-valerate followed by dexamethasone and prednisolone 17-ethylcarbonate. Native PC appeared almost as potent as dexamethasone. With both a strong correlation was observed between transactivation and GR binding.

Animals↗