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PubMed1992

Ionization of the heme propionate substituents in pseudomonad cytochromes c-551.

The heme propionate substituents in Pseudomonas cytochrome c-551 are partially buried by folds of polypeptide in the structure of the protein, and are involved in several hydrogen bonds. The ionization behavior of these groups has been of interest because the oxidation potential of the heme changes with pH in a manner that may parallel ionization of a propionate. The ionization pKa's of these groups have been determined by following the NMR chemical shifts of nearby protons acting as probes of the ionization state of the propionates. In Pseudomonas aeruginosa c-551 the 13-propionate (IUB-IUPAC porphyrin nomenclature) has been assigned a pKa of 3.1, and the 17-propionate a pKa of 7.2. In the homologous Pseudomonas stutzeri c-551, the respective propionates both have pKa values of 3.0.

Amino Acid Sequence↗
PubMed1985

Strain differences in the induction of mono-oxygenase activity in mouse skin by topical clobetasol propionate: evidence of a role for the hr locus.

The effect of the topical application of clobetasol propionate on cutaneous ethoxycoumarin O'dealkylation (EOD) has been studied in various strains of mice. Clobetasol propionate markedly increased cutaneous EOD activity in adult hairless mice only. Similar treatment of adult haired C57BL/6J mice, or adult haired DBA/2J mice had no significant effect on cutaneous EOD activity. In contrast 3 methylcholanthrene induced cutaneous EOD activity in both hairless and C57 strains to a far greater extent than in the DBA strain. EOD activity in hairless mice non-responsive to polycyclic hydrocarbons, derived by selective breeding of hairless and DBA strains was induced by clobetasol propionate to a similar extent to that observed in responsive hairless strains. Hepatic EOD activity was not induced by clobetasol propionate in any of the strains tested. Strain differences in the induction of EOD by clobetasol propionate were not related to differences in either the concentration of cytosolic glucocorticoid receptor in the skin, the dissociation constant of the cytosolic receptor, or differences in percutaneous absorption. Polycyclic hydrocarbons did not compete with triaminolone acetonide for binding to the cytosolic glucocorticoid receptor. Strain differences in the induction of EOD activity by clobetasol propionate appear therefore not to be related to strain differences in either the Ah receptor of the glucocorticoid receptor, but to be regulated by the hr locus.

7-Alkoxycoumarin O-Dealkylase↗
PubMed1991

Double-blind, comparative clinical trials with halobetasol propionate cream in patients with atopic dermatitis.

In two double-blind, parallel-group, multicenter trials, 0.05% halobetasol propionate cream was compared with 0.05% clobetasol 17-propionate cream and 0.05% betamethasone dipropionate cream in 264 patients with acute, severe exacerbations of atopic dermatitis. The efficacy of halobetasol propionate cream and betamethasone dipropionate cream was similar with regard to the success rate, as indicated by ratings of "healed" and "marked improvement" (88% versus 90%) and by an onset of therapeutic effect within 3 days of the start of treatment (40% versus 39%). The efficacy of halobetasol propionate cream and clobetasol 17-propionate cream was also similar with regard to success rates (89% versus 93%) and an onset of therapeutic effect within 3 days of the start of treatment (41% versus 38%). All three creams were well tolerated. Dryness of the skin and itching at the site of application were the reported adverse effects. Treatment was discontinued because of severe dryness of the skin in 1 of the 121 patients treated with halobetasol propionate cream and in 1 of the 59 patients treated with betamethasone dipropionate cream.

Administration, Cutaneous↗
PubMed1985

Determination of testosterone propionate in human plasma by gas chromatography-mass spectrometry.

A specific, sensitive and accurate quantitative analysis of testosterone propionate in human plasma was developed using gas chromatography-mass spectrometry-selected-ion monitoring. For the calculation of testosterone propionate in plasma, peak height ratios were measured by selected-ion monitoring performed on the molecular ions of the trifluoroacetyl derivative of testosterone propionate (m/z 440) and testosterone propionate-19,19,19-d3 (m/z 443). The sensitivity of the method was judged from the lower limit of the detection of the mass spectrometer which was at 20 pg. The inter-assay coefficients of variation and relative error at a concentration of 1.31 ng/ml of plasma were 5.47% and -2.3%, respectively. The method described was applied to the determination of plasma concentrations of testosterone propionate-19,19,19-d3 following an intramuscular dose of testosterone propionate-19,19,19-d3 in a healthy male volunteer.

Adult↗
PubMed1990

A dose-ranging study of fluticasone propionate aqueous nasal spray for seasonal allergic rhinitis assessed by symptoms, rhinomanometry, and nasal cytology.

Fluticasone propionate is a new glucocorticosteroid with potent topical activity. In a double-blind, randomized, parallel-group study, 423 adult patients with moderate to severe seasonal allergic rhinitis received placebo or fluticasone propionate aqueous nasal spray at doses of 25, 100, or 400 micrograms twice daily (b.i.d.) for 2 weeks. Efficacy was evaluated by nasal symptom scores, nasal airflow, nasal cytology, and global evaluation. All doses of fluticasone propionate were significantly better than placebo in reducing symptoms of seasonal allergic rhinitis. Patients receiving the largest dose of fluticasone propionate (400 micrograms b.i.d.) had a slightly greater reduction (not significant) in symptom scores than patients receiving the smallest dose (25 micrograms b.i.d.). Symptom improvement was evident within 3 days of treatment. Nasal airflow improved in the groups treated with fluticasone propionate, 100 and 400 micrograms b.i.d. Examination of nasal cytograms revealed a striking decrease in both eosinophils and basophils in all three groups receiving active treatment compared with placebo. There were few adverse events and no treatment-related abnormalities in laboratory assays or evaluations of hypothalamo-pituitary-adrenocortical axis function. Comparison of treatment groups indicated that fluticasone propionate aqueous nasal spray was as safe as placebo at the doses studied.

Administration, Intranasal↗
PubMed1996

Once daily intranasal fluticasone propionate (200 micrograms) reduces nasal symptoms and inflammation but also attenuates the increase in bronchial responsiveness during the pollen season in allergic rhinitis.

BACKGROUND: Fluticasone propionate aqueous nasal spray, a new topical corticosteroid, has been proved to be an effective treatment for seasonal allergic rhinitis. OBJECTIVES: We studied the effect of fluticasone propionate on nasal symptoms, circulating eosinophils, and nasal inflammation in patients with seasonal allergic rhinitis after high-load pollen exposure. Moreover, we examined its efficacy in preventing the increase in bronchial responsiveness to methacholine (PD20) during the pollen season. METHODS: We conducted a double-blind, placebo-controlled, parallel-group study in patients who had a history of allergic rhinitis in response to pollens of grass and Parietaria species and were living in northern Italy. After a run-in period of 2 weeks, 24 patients were treated with fluticasone propionate (200 micrograms, once daily), and 26 patients received matched placebo for 6 weeks, starting from the beginning of the pollen season. Assessment of efficacy was based on scores of daily nasal symptoms. Nasal lavage was performed at the end of the season, and differential cell count was expressed as percent of total cells. PD20 methacholine was measured at the beginning and end of the season and after the season had ended. RESULTS: Fluticasone propionate significantly reduced nasal obstruction, itching, and rhinorrhea. Eosinophils in blood (p < 0.01) and nasal lavage (p < 0.001) were also reduced. Moreover, fluticasone significantly attenuated the decrease in mean PD20 methacholine (from 1.95 to 0.89 mg) compared with placebo (from 1.38 to 0.37 mg: p < 0.01). After the season, no difference in PD20 methacholine was found between treatment groups. CONCLUSIONS: The results of this study indicate that fluticasone propionate is effective in decreasing nasal symptoms and eosinophil inflammation in patients with seasonal allergic rhinitis after high-load pollen exposure. Our results also demonstrate that treatment with fluticasone propionate partially prevents the increase in bronchial responsiveness provoked by the inhalation of seasonal pollens in allergic rhinitis.

Administration, Intranasal↗
PubMed1996

Fluticasone propionate aqueous nasal spray compared with terfenadine tablets in the treatment of seasonal allergic rhinitis.

BACKGROUND: Comparative studies with topical corticosteroids and antihistamines for treatment of allergic rhinitis have not always demonstrated clear distinctions between the two on the basis of therapeutic efficacy. OBJECTIVE: This study was designed to compare the efficacy and tolerability of fluticasone propionate aqueous nasal spray with those of terfenadine in the treatment of seasonal allergic rhinitis. METHODS: Three hundred forty-eight patients with allergic rhinitis were given fluticasone propionate aqueous nasal spray (200 micrograms once daily), terfenadine tablets (60 mg twice daily), or placebo for 4 weeks in a multicenter, randomized, double-blind, double-dummy, parallel-group study. RESULTS: Clinician-rated total nasal symptom scores after 1, 2, 3, and 4 weeks of therapy and patient-rated total nasal symptom scores throughout treatment were significantly (p <0.05) lower in the fluticasone propionate group compared with the terfenadine group or the placebo group. Terfenadine was not statistically different from placebo on the basis of clinician-related nasal symptom scores, except for sneezing. Total nasal airflow, measured by rhinomanometry, significantly (p <0.05) improved in the fluticasone propionate group compared with the terfenadine group or the placebo group. More fluticasone propionate-treated patients compared with placebo-treated patients had reduced nasal mucosal eosinophil counts after 4 weeks of therapy (p <0.05). No serious or unusual drug-related adverse events were reported. Morning plasma cortisol concentrations after 4 weeks of therapy did not differ among groups. CONCLUSION: Fluticasone propionate aqueous nasal spray is more effective than terfenadine tablets for treatment of seasonal allergic rhinitis.

Administration, Intranasal↗
PubMed1998

The role of heme propionate in controlling the redox potential of heme: square wave voltammetry of protoporphyrinato IX iron (III) in aqueous surfactant micelles.

The proton equilibrium in aqueous surfactant solutions of hemin, (PPIX)Fe(H2O)+2, involving the propionic acid groups is reported (PPIX = protoporphyrinato IX). The surfactant used are sodium dodecyl sulphate (SDS), triton X-100 (TX-100) and hexadecyl trimethylammonium bromide (CTAB). The pKa values, determined spectroscopically from the pH variations of the Soret absorption, are found at ca. 3.5 in SDS and TX-100 micelles. In the cationic surfactant (CTAB) the absorbance of hemin is independent of the hydrogen ion concentration in solution and this surfactant form a salt-link with the heme propionate group. The dependence of mid-point potential on pH indicates that the heme propionate undergoes a redox-linked changed in pKa from 3.2-3.5 in the ferric form to 4.4-4.5 in the ferrous form (27 degrees C, mu = 0.2 M). The change in the mid-point potential per unit change in pH. delta E/delta pH, is ca. -59 mV. Replacement of the water molecules in hemin by tetrahydrofuran, (PPIX)Fe(thf)+2, induces a considerable shift of pKa of the heme propionate: 6.2-6.8 in the ferric form and 7.5-7.8 in the ferrous form. The lower value of pKa in diaquo hemin is attributed to stabilisation of the propionate by a hydrogen bond with coordinated water molecules. All these results may be interpreted in terms of the involvement of a heme propionate group in redox linked uptake of protons and the influence of hydrogen bonding and salt-link formation on the pKa of the proton equilibrium.

Cetrimonium↗
PubMed2003

Modulation of the constitutive or cytokine-induced bronchial epithelial cell functions in vitro by fluticasone propionate.

When exposed to proinflammatory mediators, human bronchial epithelial cells (HBECs) upregulate the 'constitutive' adhesion molecule expression and cytokine/chemokine release. We tested whether and to what extent the inhibitory effect of fluticasone propionate on HBECs could involve the 'constitutive' and 'cytokine-induced' proinflammatory functions. Stimulation of the HBECs with interleukin (IL)-4 plus tumour necrosis factor (TNF)-alpha was more effective in upregulating intercellular adhesion molecule (ICAM)-1 ( approximately 2.2-fold increase) than vascular adhesion molecule (VCAM)-1 ( approximately 1.6-fold increase) expression (P<0.05) and in increasing the release of 'regulated on activation normal T cell expressed' (RANTES, 5.7-fold increase) than of IL-8 (3.5-fold increase) and granulocyte macrophage-colony stimulating factor (GM-CSF, 2.8-fold increase), (P<0.01). Fluticasone propionate, at the two concentrations tested (10 and 100 nM), was more effective in inhibiting the 'IL-4 plus TNF-alpha-induced' ICAM-1 expression than VCAM-1 expression (P<0.05) and in downregulating RANTES than IL-8 or GM-CSF secretion (P<0.05). The degree of inhibition demonstrated by fluticasone propionate appeared to be related to the degree of cell activation. In addition, for both adhesion molecules, the effect of fluticasone propionate at both concentrations tested appeared to be related to a complete inhibition of 'IL-4 plus TNF-alpha-induced' expression with no involvement of the 'constitutive' expression. Slightly different results were observed for cytokine/chemokine release. Indeed, evaluating RANTES, a complete inhibition of the 'IL-4 plus TNF-alpha-induced' release with a partial inhibition also of the 'constitutive' release at both concentrations of the drug tested was found, whereas for GM-CSF and IL-8, only a partial inhibition of the 'IL-4 plus TNF-alpha-induced' release in the presence of fluticasone propionate 10 and 100 nM. Thus, HBECs can constitutively or upon activation express adhesion molecules and secrete proinflammatory proteins at various levels and the different ability of fluticasone propionate to modulate the HBEC functions appears to be mostly related to the different inhibition of the various 'IL-4 plus TNF-alpha-induced' responses.

Adjuvants, Immunologic↗
PubMed2001

Effect of dietary propionate on intake patterns and fatty acid composition of adipose tissues in lambs.

The aim of the present trial was to study the effect of dietary propionate supplementation on growth performance, intake patterns and on the proportion of odd-numbered and methyl-branched chain fatty acids in internal or in subcutaneous adipose tissues. These fatty acids are responsible, in part, for abnormally soft subcutaneous adipose tissue. Eleven male lambs were fed ad libitum carbohydrate-rich diets based mainly on barley, supplemented (P diet) or not supplemented (C diet) with 5.6% DM of sodium propionate. During the trial, the intake patterns were recorded on three non-consecutive days over a 9h-period. The fatty acid compositions of four adipose tissue sites, two subcutaneous (dorsal, caudal) and two internal (omental, perirenal) were analysed. The ME intake (3.32+/-0.44Mcal per day) and average daily gain (316+/-64g per day) were not different (P>0.10) between the C and P treatments. The intake patterns of these lambs given ad libitum access to feed did not show any large meal even after the morning distribution of feed. No differences in intake patterns were observed between the two diets. The dietary propionate supplementation increased (P<0.05) the proportion of odd-numbered fatty acids (Odd FA) in both internal (increase of 0.7wt.% of total fatty acids) and subcutaneous adipose tissues (increase of 1.7% of total fatty acids). The effect of dietary propionate supplementation on branched-chain fatty acids was less conclusive although it tended to increase (P=0.09) the proportion of branched-chain fatty acids other than the iso and anteiso fatty acids (BCFAO) in dorsal adipose tissue. This experiment confirms the role of propionate as an important precursor of odd-numbered and methyl-branched chain fatty acids. Moreover, the dorsal adipose tissue seems to be the most sensitive adipose tissue to dietary increment in ruminal propionate content. A positive relationship between the mean ME intake rate measured over 8.5h and the proportions of Odd FA and BCFA in dorsal adipose tissue was shown. However, it does not appear to play a predominant role in the explanation of the individual variability in dorsal fatty acid composition.

Journal Article↗
PubMed2005

Determining economic feasibility of fluticasone propionate-salmeterol vs montelukast in the treatment of persistent asthma using a net benefit approach and cost-effectiveness acceptability curves.

BACKGROUND: The choice of treatment can have a major impact on the total costs associated with asthma care. OBJECTIVE: To determine the relative cost-effectiveness of twice-daily treatment with inhaled fluticasone propionate-salmeterol via Diskus, 100/50 microg, with that of once-daily treatment with oral montelukast as initial maintenance therapy in patients with persistent asthma uncontrolled with a short-acting beta2-agonist alone. METHODS: Data from a randomized, double-blind, double-dummy, 12-week clinical trial were analyzed. Efficacy end points included (1) symptom-free days (SFDs) during the 12-week period and (2) a 12% or greater increase in forced expiratory volume in 1 second (FEV1) from baseline. The economic analysis was performed from a payer's perspective, and hence only direct costs were included in the analysis. The incremental cost-effectiveness ratio (ICER), which is the mean difference in average costs divided by the mean difference in average effectiveness, was calculated for both effectiveness outcomes (SFDs and FEV1). RESULTS: For the SFDs end point, the ICER for fluticasone propionate-salmeterol vs montelukast was $2.87 (95% confidence interval, -$1.08 to $6.65), indicating that it costs, on average, an extra $2.87 per day for an additional SFD with fluticasone propionate-salmeterol than with montelukast. With regard to FEV1, the ICER was $1.79 (95% confidence interval, -$0.72 to $3.86), indicating that it costs, on average, an extra $1.79 per day to achieve a lung function improvement of 12% or greater from baseline with fluticasone propionate-salmeterol than with montelukast. At a widely acceptable ceiling ratio of $9.95 per day, the probability of fluticasone propionate-salmeterol being more cost-effective than montelukast was 99.8% for SFDs and was almost 100% for an FEV1 improvement of 12% of greater. CONCLUSIONS: Treating 2 main components of asthma, inflammation and smooth muscle dysfunction, using fluticasone propionate-salmeterol is more cost-effective than using a single mediator antagonist alone, such as montelukast, as initial maintenance therapy for persistent asthma in patients treated with a short-acting beta2-agonist only.

Acetates↗
PubMed2001

Suppression of hypothalamic-pituitary-adrenal axis activity with inhaled flunisolide and fluticasone propionate in adult asthma patients.

BACKGROUND: Suppression of the hypothalamic-pituitary-adrenal (HPA) axis, a potential systemic effect of inhaled corticosteroid therapy, can be quantified by monitoring serum, urinary, and salivary cortisol levels. OBJECTIVES: 1) Compare the effects on HPA axis of the inhaled corticosteroids flunisolide and fluticasone propionate versus placebo and oral prednisone. 2) Estimate dose-potency ratio for HPA-axis suppression. METHODS: Multicenter, randomized, placebo-controlled, open-label, 21-day trial. Active regimens were flunisolide 500 and 1,000 microg, twice daily; fluticasone propionate 110, 220, 330, and 440 microg, twice daily; and prednisone, 7.5 mg daily. Enrolled patients were nonsmokers, 18 to 50 years of age, with persistent mild-to-moderate asthma and had not used oral, nasal, or inhaled corticosteroids for 6 months before study. Main outcome measures were area under serum cortisol concentration curve for 22 hours (AUC(0-22h)); 24-hour urinary cortisol level; and 8 AM salivary cortisol level. RESULTS: One hundred fifty-three patients were randomly assigned to active treatment or placebo; 125 patients completed the study and were at least 80% compliant with their regimens. Both fluticasone propionate and flunisolide caused dose-dependent suppression of HPA axis, which was statistically greater for fluticasone propionate (P = 0.0003). Dose-potency ratio showed 4.4 times more serum-cortisol suppression/microgram increase in dose with fluticasone propionate than with flunisolide. Diurnal pattern of serum cortisol suppression was persistent with fluticasone propionate and "remitting" with flunisolide. Salivary and urinary cortisol data were qualitatively similar to serum cortisol results. CONCLUSIONS: Fluticasone caused significantly more suppression of HPA axis than flunisolide. Flunisolide may provide a safe option for patients with asthma requiring long-term inhaled corticosteroid therapy.

Administration, Inhalation↗
PubMed1997

Comparison of once daily mometasone furoate (Nasonex) and fluticasone propionate aqueous nasal sprays for the treatment of perennial rhinitis. 194-079 Study Group.

BACKGROUND: Mometasone furoate (Nasonex), in a new once-daily aqueous nasal spray formulation, has been shown to be as effective and well-tolerated as twice-daily beclomethasone dipropionate aqueous nasal spray in treating symptoms of seasonal allergic rhinitis and perennial rhinitis. OBJECTIVE: To compare the effectiveness and tolerability of mometasone furoate to placebo and of fluticasone propionate aqueous nasal spray, all treatments administered once-daily, in patients with perennial rhinitis. METHODS: This was a 3-month, randomized, double-blind, double dummy, parallel group study in 550 patients, aged 12 to 77 years, at 25 centers in Canada, Latin America, and Europe. Patients allergic to at least one perennial allergen, with confirmed allergy history, skin test positivity, and moderate to severe symptomatology, were eligible to receive one of the following treatments, once daily in the morning: mometasone furoate 200 micrograms, fluticasone propionate 200 micrograms, or placebo. The primary efficacy variable was the change from baseline in total AM plus PM diary nasal symptom score over the first 15 days of treatment. RESULTS: Four hundred fifty-nine patients were valid for efficacy. For the primary efficacy variable, mometasone furoate was significantly (P < .01) more effective than placebo and was not statistically different from fluticasone propionate (percent reductions from baseline were 37, 39, and 22 for mometasone furoate, fluticasone propionate, and placebo, respectively). Generally, similar trends were seen for physician-evaluated total nasal symptoms, and patient-rated and physician-rated overall condition and response to therapy. Overall, mometasone furoate was at least as effective as fluticasone propionate at equivalent doses. There was no evidence of tachyphylaxis. All treatments were well tolerated. CONCLUSION: Mometasone furoate and fluticasone propionate adequately controlled symptoms of perennial rhinitis and were well tolerated.

Administration, Intranasal↗
PubMed1997

Fluticasone propionate aqueous nasal spray treatment for perennial allergic rhinitis in children.

BACKGROUND: Topical corticosteroid is now accepted as safe and most effective in controlling all symptoms of both allergic and nonallergic rhinitis. Fluticasone propionate aqueous nasal spray is a new once daily topical corticosteroid preparation. OBJECTIVE: To evaluate the efficacy and safety of fluticasone propionate in children 5 to 11 years of age with perennial allergic rhinitis. METHOD: A double-blind, placebo-controlled, parallel group of 127 recruited patients of whom 106 were evaluated. Treatment with once daily fluticasone propionate 100 micrograms or placebo for 4 weeks followed by a 2-week followup period. Fifty-three patients of each group were treated with fluticasone propionate or placebo by randomized assignment. RESULTS: There was no statistical significance of the sex, mean age, weight, and height of the two groups. Patients treated with fluticasone propionate showed a significant decrease in total symptom scores rated by physicians at 2 weeks and 4 weeks, respectively (P < .01, P < .05). The rhinitis symptom scores in treatment group rated by patients (nasal blockage, sneezing, rhinorrhea) were significantly decreased at 2 weeks (P < .05, P < .01). Nasal symptoms as assessed by doctors (turbinate swelling, color of nasal mucosa, secretion, and postnasal drip) also decreased at 2 and 4 weeks, but were not statistically significant, except for the secretion at 2 weeks and postnasal drip at 4 weeks (P < .05). There was no evidence of effects on adrenal function by morning plasma cortisol concentration between the two groups. CONCLUSION: Fluticasone propionate was safe and effective in children aged 5 to 11 years with perennial allergic rhinitis.

Administration, Inhalation↗
PubMed1999

Adrenal suppression secondary to inhaled fluticasone propionate.

BACKGROUND: Inhaled glucocorticoids are the medical treatment of choice in many of patients with asthma. Fluticasone propionate is an inhaled glucocorticoid with little systemic bioavailability via the oral route and infrequent association with systemic adverse effects at the recommended dosage. OBJECTIVE: To report a case of adrenal suppression and exogenous glucocorticoid excess from inhaled fluticasone propionate. METHODS: A 9-year-old girl with a previous history of episodic asthma was placed on 550 microg of fluticasone propionate daily for severe labile asthma diagnosed by history and methacholine challenge. The patient returned 6 months later with complaints of increased appetite, nausea, and feeling "hot and flushed." On physical exam she had stigmata of Cushing's syndrome. The patient subsequently developed orthostatic hypotension and moderate dehydration following a viral illness. After a long taper of fluticasone propionate the patient' s adrenal function returned to normal and she had no acute or chronic exacerbations of her asthma. RESULTS: Her 8 AM cortisol was undetectable with an ACTH of 21 pg/mL. The serum prolactin, TSH, free thyroxine, insulin-like growth factor I, and renin activity were all normal. An MRI study of her head was also normal. Repeat methacholine challenges while receiving a much smaller dose fluticasone propionate showed a significant decrease in airway reactivity. CONCLUSION: Adrenal suppression can occur from inhaled fluticasone propionate at a dosage less than has been previously reported.

Administration, Inhalation↗
PubMed2000

Regulating the molar fraction of 4-hydroxybutyrate in poly(3-hydroxybutyrate-4-hydroxybutyrate) biosynthesis by Ralstonia eutropha using propionate as a stimulator.

The regulation of the molar fraction of 4-hydroxybutyrate (4-HB) in the poly(3-hydroxybutyrate-4-hydroxybutyrate) [P(3HB-4HB)] biosynthesis by Ralstonia eutropha (formerly Alcaligenes eutrophus) was attempted by the supplemental addition of propionate. The molar fraction of 4-HB in P(3HB-4HB) was increased significantly from 12.3 to 51.8 mol% by the addition of a small amount of propionate along with gamma-butyrolactone commonly used as a precursor for the biosynthesis of P(3HB-4HB). The mechanism of regulation by propionate was investigated by measuring the variation of enzyme activities related to the biosynthesis of P(3HB-4HB) and the level of intermediate metabolite acetyl-CoA. PHB synthase activity was induced significantly by propionate, and the acetyl-CoA concentration also increased significantly due to the additional supply of propionate. The overflowing acetyl-CoA seems to cause an inhibitory effect on the ketolysis reaction catalysing the lysis of 4-hydroxybutyryl-CoA to two molecules of acetyl-CoA; consequently, the 4-HB fraction available for polymerization increased. Accordingly, the molar fraction of 4-HB in P(3HB-4HB) biosynthesis seems to be regulated by both an increased 4-HB fraction and an activated PHB synthase due to the supplemental addition of propionate as a stimulator.

Journal Article↗
PubMed2005

Regioselectively nucleus and/or side-chain fluorinated 2-(Phenanthryl)propionic acids by an effective combination of radical and organometallic chemistry.

Regioselectively nucleus and/or side-chain fluorinated 2-(phenanthr-1-yl)- and 2-(phenanthr-2-yl)propionic acids 1-5 were prepared using phenanthren-1(2H)-ones 6a-c as key intermediates. Thus, ethyl 2-(fluorophenanthryl)propionates 11 were obtained in good yields by Reformatsky reaction of 6a-c with ethyl 2-bromopropionate followed by dehydratation and DDQ-promoted aromatization of the resulting beta-hydroxyesters. Side-chain alkyl 2-hydroxy-2-(phenanthr-1-yl)propionates 14 were obtained by bromine/lithium permutation of dihydrophenanthryl bromides 12a-c with butyllithium followed by quenching of the lithiated intermediates with methyl pyruvate or ethyl 3,3,3-trifluoropyruvate and subsequent DDQ-promoted aromatization. The alkyl 2-hydroxy-2-(phenanthr-1-yl)propionates 25 were prepared by reacting 8-bromo-1,3-difluorophenanthrene 24 with butyllithium for 10 seconds at -110 degrees C and subsequent addition of the suitable pyruvate to the lithiated intermediates. Alkyl 2-hydroxy-2-(phenanthr-2-yl)propionates 26 and 29 were suitably obtained by site-selective metalation of 1,3-difluorophenanthrene 28 and the bromophenanthrene 24, respectively, with LDA followed by quenching of the metalated intermediates with the suitable alkyl pyruvate. Fluorination of the above alpha-hydroxypropionates with DAST, followed by the alkaline hydrolysis, allowed the expected 2-(phenanthryl)propionic acids 1-5 to be obtained in satisfactory overall yields.

Journal Article↗
PubMed2001

The treatment of oral aphthous ulceration or erosive lichen planus with topical clobetasol propionate in three preparations: a clinical and pilot study on 54 patients.

BACKGROUND: This study evaluated the clinical use of a corticosteroid in three preparations (topical clobetasol propionate ointment, clobetasol propionate in an oral analgesic base, and clobetasol propionate in an adhesive denture paste). METHODS: Fifty-four patients (34 males and 20 females) with a history of vesiculo-ulcero-erosive oral lesions were selected: 24 with oral erosive lichen planus and 30 with aphthae. The subjects enrolled were randomly divided into three groups, each of 18 patients (10 with aphthae and 8 with lichen planus): the first was treated with topical clobetasol propionate ointment (0.05%) directly on the lesion(s) three times a day; the second with clobetasol propionate in an adhesive denture paste in equal amounts (1:1) two times a day; the third with clobetasol propionate in an oral analgesic base (Orabase-B) in equal amounts (1:1) two times a day. Each subject scored his or her symptoms daily from most severe (7) to none (0) by verbal assessments using a categorical scale. RESULTS: In all cases, the administration of the corticosteroid was effective in producing remission of symptoms in each group of patients. Significant differences (P<0.05) between groups were determined by the Kruskal-Wallis test. The Dunn test was used in order to detect which group differs from the others; clobetasol and adhesive denture paste correlated with an early remission of pain in lichen and apthous lesions. CONCLUSION: The results suggest that topical application of clobetasol in an adhesive denture paste is an effective drug for symptomatic oral vesiculo-erosive and/or ulcerative lesions.

Adhesives↗