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See detailGlucocorticoid receptors bound to the antagonist RU486 are not downregulated despite their capacity to interact in vitro with defined gene regions
Rajpert, E. J.; Lemaigre, F. P.; Eliard, P. H. et al

in Journal of Steroid Biochemistry (1987), 26(5), 513-20

Modulation of gene expression by glucocorticoids involves interaction of these hormones with an intracellular receptor followed by 'transformation' of the hormone-receptor complex into a nuclear binding ... [more ▼]

Modulation of gene expression by glucocorticoids involves interaction of these hormones with an intracellular receptor followed by 'transformation' of the hormone-receptor complex into a nuclear binding form. The molecular basis for the antiglucocorticoid action of high-affinity steroid analogues such as RU486 remains controversial. The effects of dexamethasone and RU486 on in vitro and in vivo properties of the receptor were compared using human lymphoblastoid IM-9 cells. In these cells, RU486 fully antagonized the glucocorticoid-specific induction of 5'-nucleotidase activity by dexamethasone. In vitro, however, RU486-bound receptor could be transformed and shown to interact specifically with cloned DNA fragments containing glucocorticoid response elements. These fragments included one from the mouse mammary tumour virus and two from the human growth hormone gene. In vivo, RU486-bound receptor did not behave like dexamethasone-bound receptor. While receptor downregulation, a property of the transformed receptor, was achieved by dexamethasone, this did not occur with RU486. Likewise, RU486 did not affect receptor half-life under conditions when this was shortened by dexamethasone. These seemingly contradictory results can be reconciled by proposing that receptor transformation by agonists involves dissociation of the receptor oligomer to reveal a DNA-binding site that pre-exists on this protein. Although cell-free receptor dissociation and therefore DNA binding can occur even when the receptor is bound to RU486, this steroid maintains receptors in the untransformed state in the intact cell and therefore behaves a glucocorticoid antagonist in vivo. [less ▲]

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See detailLes glucocorticoïdes, de puissants immunomodulateurs naturels
Geenen, Vincent ULg

Conference given outside the academic context (2008)

Detailed reference viewed: 41 (3 ULg)
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See detailGLUCOCORTICOIDS AS DOPING AGENTS IN HOMING PIGEONS
Duchatel, Jean-Pierre ULg; Beduin, Jean-Marie ULg; Jauniaux, Thierry ULg et al

in Annales de Médecine Vétérinaire (1993), 137(8), 557-564

Different commercially available glucocorticoids that could be used to dope racing pigeons have been evaluated using zootechnical and biological parameters. The influence of these corticosteroids on blood ... [more ▼]

Different commercially available glucocorticoids that could be used to dope racing pigeons have been evaluated using zootechnical and biological parameters. The influence of these corticosteroids on blood values have been investigated. Toxicity of triamcinolone diacetate varied proportionally to injected doses and the main effects observed were lymphoid tissue alterations, muscular atrophy with breast muscles fibers vacuolation, fatty degeneration of liver and kidneys, hypoplasia or atrophy of gonads, and, in the blood, a significant increase of calcium and triglycerides levels. Prednisolone acetate in ocular drops was less toxic than dexemathasone and fluocinolone acetonide. The type of corticoids also had an influence on hemoglobin, glucose, and creatinine levels. The inhibition of the molt was also observed and varied with the sort of product used. [less ▲]

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See detailGlucocorticoids Modulate Tumor Radiation Response through a Decrease in Tumor Oxygen Consumption
Crokart, Nathalie; JORDAN, Bénédicte; BAUDELET, Christine et al

in Clinical Cancer Research : An Official Journal of the American Association for Cancer Research (2007), 15(13), 6305

Purpose: We hypothesized that glucocorticoids may enhance tumor radiosensitivity by increasing tumor oxygenation (pO2) through inhibition of mitochondrial respiration. <br /> <br />Experimental Design ... [more ▼]

Purpose: We hypothesized that glucocorticoids may enhance tumor radiosensitivity by increasing tumor oxygenation (pO2) through inhibition of mitochondrial respiration. <br /> <br />Experimental Design: The effect of three glucocorticoids (hydrocortisone, dexamethasone, and prednisolone) on pO2 was studied in murine TLT liver tumors and FSaII fibrosarcomas. At the time of maximum pO2 (tmax, 30 min after administration), perfusion, oxygen consumption, and radiation sensitivity were studied. Local pO2 measurements were done using electron paramagnetic resonance. The oxygen consumption rate of tumor cells after in vivo glucocorticoid administration was measured using high-frequency electron paramagnetic resonance. Tumor perfusion and permeability measurements were assessed by dynamic contrast-enhanced magnetic resonance imaging. <br /> <br />Results: All glucocorticoids tested caused a rapid increase in pO2. At tmax, tumor perfusion decreased, indicating that the increase in pO2 was not caused by an increase in oxygen supply. Also at tmax, global oxygen consumption decreased. When irradiation (25 Gy) was applied at tmax, the tumor radiosensitivity was enhanced (regrowth delay increased by a factor of 1.7). <br /> <br />Conclusion: These results show the potential usefulness of the administration of glucocorticoids before irradiation. [less ▲]

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See detailGlucoindole alkaloids from stem bark of Strychnos mellodora
Brandt, V; Tits, Monique ULg; Angenot, Luc ULg

Poster (1996, February)

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See detailGlucoindole Alkaloids from Stem Bark of Strychnos Mellodora
Tits, Monique ULg; Brandt, V.; Wauters, Jean-Noël ULg et al

in Planta Medica (1996), 62(1), 73-4

Three glucoindole alkaloids, dolichantoside (1), strictosidine (2), and palicoside (3), have been identified in the stem bark of Strychnos mellodora (Loganiaceae), collected in Zimbabwe. The chiroptical ... [more ▼]

Three glucoindole alkaloids, dolichantoside (1), strictosidine (2), and palicoside (3), have been identified in the stem bark of Strychnos mellodora (Loganiaceae), collected in Zimbabwe. The chiroptical (CD) data are compared. [less ▲]

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See detailGlucoindole alkaloids from stem bark of Strychnos mellodora
Brandt, Viviane; Tits, Monique ULg; Angenot, Luc ULg

Conference (1996, May)

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See detailGlucosamine and chondroitin sulfate as therapeutic agents for knee and hip Osteoarthritis
Bruyère, Olivier ULg; Reginster, Jean-Yves ULg

in Drugs & Aging (2007), 24(7), 573-580

Osteoarthritis (OA), the most common form of arthritis, is a public health problem throughout the world. Several entities have been carefully investigated for the symptomatic and structural management of ... [more ▼]

Osteoarthritis (OA), the most common form of arthritis, is a public health problem throughout the world. Several entities have been carefully investigated for the symptomatic and structural management of OA. This review evaluates published studies of the effect of glucosamine salts and chondroitin sulfate preparations on the progression of knee or hip OA. Despite multiple double-blind, controlled clinical trials of the use of glucosamine and chondroitin sulfate in OA, controversy regarding the efficacy of these agents with respect to symptomatic improvement remains. Several potential confounders, including placebo response, use of prescription medicines versus over-the-counter pills or food supplements, or use of glucosamine sulfate versus glucosamine hydrochloride, may have relevance when attempting to interpret the seemingly contradictory results of different clinical trials. The National Institutes of Health-sponsored GAIT (Glucosamine/chondroitin Arthritis Intervention Trial) compared placebo, glucosamine hydrochloride, chondroitin sulfate, a combination of glucosamine and chondroitin sulfate and celecoxib in a parallel, blinded 6-month multicentre study of patients with knee OA. This trial showed that glucosamine hydrochloride and chondroitin sulfate alone or in combination did not reduce pain effectively in the overall group of patients with OA of the knee. However, exploratory analyses suggest that the combination of glucosamine hydrochloride and chondroitin sulfate may be effective in the subgroup of patients with moderate-to-severe knee pain. For decades, the traditional pharmacological management of OA has been mainly symptomatic. However, in recent years, several randomised controlled studies have assessed the structure-modifying effect of glucosamine sulfate and chondroitin sulfate using plain radiography to measure joint space narrowing over years. There is some evidence to suggest a structure-modifying effect of glucosamine sulfate and chondroitin sulfate. On the basis of the results of recent randomised controlled trials and meta-analyses, we can conclude that glucosamine sulfate (but not glucosamine hydrochloride) and chondroitin sulfate have small-to-moderate symptomatic efficacy in OA, although this is still debated. With respect to the structure-modifying effect, there is compelling evidence that glucosamine sulfate and chondroitin sulfate may interfere with progression of OA. [less ▲]

Detailed reference viewed: 134 (10 ULg)
See detailGlucosamine and chondroitine sulfate
Reginster, Jean-Yves ULg; Kvasz, Angela ULg; Bruyère, Olivier ULg et al

in Anti Aging Medizin 2001 : Konferenz der German Society of Anti-Aging Medicine (2002)

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See detailGlucosamine sulfate for structure modification in osteoarthritis : fact of fantasy ?
Reginster, Jean-Yves ULg

in Ortopedia, Traumatologia, Rehabilitacja (2011), 13(S1), 44

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See detailGlucosamine sulfate in the treatment of knee osteoarthritis: impact on health utility.
Scholtissen, S.; Bruyère, Olivier ULg; Hiligsmann, Mickaël ULg et al

in Osteoporosis International (2009, March), 20(Suppl.1), 149

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See detailGlucosamine sulfate reduces osteoarthritis progression in postmenopausal women with knee osteoarthritis: evidence from two 3-year studies
Bruyère, Olivier ULg; Pavelka, K.; Rovati, Lucio C et al

in Menopause (2004), 11(2), 138-143

OBJECTIVE: To investigate the effect of glucosamine sulfate on long-term symptoms and structure progression in postmenopausal women with knee osteoarthritis (OA). DESIGN: This study consisted of a ... [more ▼]

OBJECTIVE: To investigate the effect of glucosamine sulfate on long-term symptoms and structure progression in postmenopausal women with knee osteoarthritis (OA). DESIGN: This study consisted of a preplanned combination of two three-year, randomized, placebo-controlled, prospective, independent studies evaluating the effect of glucosamine sulfate on symptoms and structure modification in OA and post-hoc analysis of the results obtained in postmenopausal women with knee OA. Minimal joint space width was assessed at baseline and after 3 years from standing anteroposterior knee radiographs. Symptoms were scored by the algo-functional WOMAC index at baseline and after 3 years. All primary statistical analyses were performed in intention-to-treat, comparing joint space width and WOMAC changes between groups by ANOVA. RESULTS: Of 414 participants randomized in the two studies, 319 were postmenopausal women. At baseline, glucosamine sulfate and placebo groups were comparable for demographic and disease characteristics, both in the general population and in the postmenopausal women subset. After 3 years, postmenopausal participants in the glucosamine sulfate group showed no joint space narrowing [joint space change of +0.003 mm (95% CI, -0.09 to 0.11)], whereas participants in the placebo group experienced a narrowing of -0.33 mm (95% CI, -0.44 to -0.22; P < 0.0001 between the two groups). Percent changes after 3 years in the WOMAC index showed an improvement in the glucosamine sulfate group [-14.1% (95%, -22.2 to -5.9)] and a trend for worsening in the placebo group (5.4% (95% CI, -4.9 to 15.7) (P = 0.003 between the two groups). CONCLUSION: This analysis, focusing on a large cohort of postmenopausal women, demonstrated for the first time that a pharmacological intervention for OA has a disease-modifying effect in this particular population, the most frequently affected by knee OA. [less ▲]

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See detailGlucosamine Sulphate in Osteoarthritis
Reginster, Jean-Yves ULg; Tancredi, Annalisa ULg; Rabenda, Véronique ULg

in Business Briefing : Long Term Healthcare Strategies (2003)

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See detailGlucosamine sulphate in osteoarthritis: from symptoms to structure modification
Reginster, Jean-Yves ULg; LECART, Marie-Paule ULg; Bruyère, Olivier ULg et al

in Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry (2005), 4

Several chemical entities have been carefully investigated for the symptomatic and structural management of osteoarthritis. The most compelling evidence of a potential for inhibiting the structural ... [more ▼]

Several chemical entities have been carefully investigated for the symptomatic and structural management of osteoarthritis. The most compelling evidence of a potential for inhibiting the structural progression of osteoarthritis has been obtained with glucosamine sulfate. At any rate, this compoind has clearly demonstrated a symptomatic action, mainly in osteoarthritis of the lower limbs, on pain relief an improvement of functional disability. An important issue is that all the conclusive studies with such chyemical entities resulted from the use of prescription medicines and not over-the-counter pills of food supplements. [less ▲]

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See detailGlucosamine sulphate in the treatment of knee osteoarthritis: cost-effectiveness comparison with paracetamol.
Scholtissen, S.; Bruyère, Olivier ULg; Neuprez, A. et al

in International Journal of Clinical Practice (2010), 64(6), 756-62

INTRODUCTION: The aim of this study was to explore the cost-effectiveness of glucosamine sulphate (GS) compared with paracetamol and placebo (PBO) in the treatment of knee osteoarthritis. For this purpose ... [more ▼]

INTRODUCTION: The aim of this study was to explore the cost-effectiveness of glucosamine sulphate (GS) compared with paracetamol and placebo (PBO) in the treatment of knee osteoarthritis. For this purpose, a 6-month time horizon and a health care perspective was used. MATERIAL AND METHODS: The cost and effectiveness data were derived from Western Ontario and McMaster Universities Osteoarthritis Index data of the Glucosamine Unum In Die (once-a-day) Efficacy trial study by Herrero-Beaumont et al. Clinical effectiveness was converted into utility scores to allow for the computation of cost per quality-adjusted life year (QALY) For the three treatment arms Incremental Cost-Effectiveness Ratio were calculated and statistical uncertainty was explored using a bootstrap simulation. RESULTS: In terms of mean utility score at baseline, 3 and 6 months, no statistically significant difference was observed between the three groups. When considering the mean utility score changes from baseline to 3 and 6 months, no difference was observed in the first case but there was a statistically significant difference from baseline to 6 months with a p-value of 0.047. When comparing GS with paracetamol, the mean baseline incremental cost-effectiveness ratio (ICER) was dominant and the mean ICER after bootstrapping was -1376 euro/QALY indicating dominance (with 79% probability). When comparing GS with PBO, the mean baseline and after bootstrapping ICER were 3617.47 and 4285 euro/QALY, respectively. CONCLUSION: The results of the present cost-effectiveness analysis suggested that GS is a highly cost-effective therapy alternative compared with paracetamol and PBO to treat patients diagnosed with primary knee OA. [less ▲]

Detailed reference viewed: 59 (11 ULg)