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Berlin Brandenburg

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  • 1
    In: Medicine & Science in Sports & Exercise, 2013, Vol.45(1), pp.29-35
    Description: PURPOSE: Anabolic androgenic steroids (AAS) are synthetic androgen-like compounds that are abused in sport communities despite their adverse effects. Nerve growth factor (NGF) influences neuronal differentiation and survival, and it also mediates higher brain functions such as learning and memory. Changes in NGF expression have been implicated in neurodegenerative disorders, including Alzheimer disease. Hence, we decided to study the effect of chronic AAS exposure on brain NGF profile, NGF-dependent cholinergic function, and related behavioral performance. METHODS: Male Wistar rats were injected for 4 wk with either nandrolone or stanozolol at daily doses (5.0 mg·kg, s.c.) that are considered equivalent to those abused by humans. NGF levels and NGF receptor (TrkA and p75NTR) expression were measured in the hippocampus and in the basal forebrain. Choline acetyltransferase expression was evaluated in basal forebrain. Spatial learning and memory were assessed using the Morris water maze. RESULTS: AAS treatment caused region-specific changes in the expression of NGF and its receptors. Both nandrolone and stanozolol increased NGF levels in the hippocampus and reduced NGF levels in the basal forebrain, reduced p75NTR expression in the hippocampus, and failed to affect TrkA expression in the basal forebrain. Finally, AAS treatment reduced the expression of choline acetyltransferase in the basal forebrain and impaired the behavioral performance in the Morris water maze. CONCLUSION: The evidence that supraphysiological doses of AAS cause neurotrophic unbalance and related behavioral disturbances raises the concern that AAS abuse in humans may affect mechanisms that lie at the core of neuronal plasticity.
    Keywords: Anabolic Agents -- Adverse Effects ; Androgens -- Adverse Effects ; Hippocampus -- Drug Effects ; Nandrolone -- Adverse Effects ; Nerve Growth Factor -- Metabolism ; Performance-Enhancing Substances -- Adverse Effects ; Stanozolol -- Adverse Effects;
    ISSN: 0195-9131
    E-ISSN: 15300315
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  • 2
    Language: English
    In: Journal of controlled release, 2012, Vol.164(1), pp.17-25
    Description: Today there is a very great deal of interest among members of the global natural products community in investigating new plant constituents. Recent studies demonstrate that liquorice extracts are useful in the treatment of dermatitis, eczema, and psoriasis, with an efficacy comparable to that of corticosteroids. In this work, niosomes made up of surfactants (Tween 85 and Span 20) and cholesterol at various concentrations were prepared to investigate the potential application of niosomes for the delivery of ammonium glycyrrhizinate (AG), useful for the treatment of various inflammatory based diseases. Vesicles were characterized evaluating dimensions, ζ potential, anisotropy, drug entrapment efficiency, stability, cytotoxicity evaluation and skin tolerability. Release profiles of ammonium glycyrrhizinate/niosomes were evaluated in vitro using cellulose membranes. The best formulation was used to evaluate the in vitro/in vivo efficacy of the ammonium glycyrrhizinate/niosomes in murine and human models of inflammation. The AG-loaded non-ionic surfactant vesicles showed no toxicity, good skin tolerability and were able to improve the drug anti-inflammatory activity in mice. Furthermore, an improvement of the anti-inflammatory activity of the niosome delivered drug was observed on chemically induced skin erythema in humans. ; p. 17-25.
    Keywords: Zeta Potential ; Inflammation ; Anti-Inflammatory Agents ; Psoriasis ; Adrenal Cortex Hormones ; Animal Models ; Cytotoxicity ; Eczema ; Humans ; Cholesterol ; Licorice ; Anti-Inflammatory Activity ; Erythema ; Mice ; Cellulose ; Surfactants ; Niosomes
    ISSN: 0168-3659
    E-ISSN: 18734995
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  • 3
    Language: English
    In: Journal of Controlled Release, 28 November 2012, Vol.164(1), pp.17-25
    Description: Today there is a very great deal of interest among members of the global natural products community in investigating new plant constituents. Recent studies demonstrate that liquorice extracts are useful in the treatment of dermatitis, eczema, and psoriasis, with an efficacy comparable to that of corticosteroids. In this work, niosomes made up of surfactants (Tween 85 and Span 20) and cholesterol at various concentrations were prepared to investigate the potential application of niosomes for the delivery of ammonium glycyrrhizinate (AG), useful for the treatment of various inflammatory based diseases. Vesicles were characterized evaluating dimensions, ζ potential, anisotropy, drug entrapment efficiency, stability, cytotoxicity evaluation and skin tolerability. Release profiles of ammonium glycyrrhizinate/niosomes were evaluated using cellulose membranes. The best formulation was used to evaluate the efficacy of the ammonium glycyrrhizinate/niosomes in murine and human models of inflammation. The AG-loaded non-ionic surfactant vesicles showed no toxicity, good skin tolerability and were able to improve the drug anti-inflammatory activity in mice. Furthermore, an improvement of the anti-inflammatory activity of the niosome delivered drug was observed on chemically induced skin erythema in humans.
    Keywords: Niosomes ; Ammonium Glycyrrhizinate ; Toxicity ; Skin Tolerability ; Inflammation ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0168-3659
    E-ISSN: 1873-4995
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  • 4
    Language: English
    In: International journal of nanomedicine, 2014, Vol.9, pp.635-51
    Description: Liquorice extracts demonstrate therapeutic efficacy in treating dermatitis, eczema, and psoriasis when compared with corticosteroids. In this work, nonionic surfactant vesicles (niosomes, NSVs) containing polysorbate 20 (Tween 20), cholesterol, and cholesteryl hemisuccinate at different molar concentrations were used to prepare monoammonium glycyrrhizinate (AG)-loaded NSVs. The anti-inflammatory properties of AG-loaded NSVs were investigated in murine models. The physicochemical properties of the NSVs were characterized using dynamic light scattering. The fluidity of the lipid bilayer was evaluated by measuring the fluorescence intensity of diphenylhexatriene. The drug entrapment efficiency of AG was assessed using high-performance liquid chromatography. The physicochemical stability of the NSVs was evaluated as a function of time using dynamic light scattering combined with Turbiscan Lab Expert analysis. Serum stability was determined by incubating the NSVs with 10% v/v fetal bovine serum. The cytotoxic effects of the NSVs were investigated in human dermal fibroblasts using the Trypan blue dye exclusion assay (for cell mortality) and an MTT assay (for cell viability). Release profiles for the AG-loaded NSVs were studied in vitro using cellulose membranes. NSVs showing the most desirable physicochemical properties were selected to test for in vivo anti-inflammatory activity in murine models. The anti-inflammatory activity of the NSVs was investigated by measuring edema and nociception in mice stimulated with chemical agents. NSVs showed favorable physicochemical properties for in vitro and in vivo administration. In addition, they demonstrated long-term stability based on Turbiscan Lab Expert analysis. The membrane fluidity of the NSVs was not affected by self-assembling of the surfactants into colloidal structures. Fluorescence anisotropy was found to be independent of the molar ratios of cholesteryl hemisuccinate and/or cholesterol during preparation of the NSVs. The anti-inflammatory AG drug showed no effect on the stability of the NSVs. In vivo experiments demonstrated that AG-loaded NSVs decreased edema and nociceptive responses when compared with AG alone and empty NSVs. In vitro and in vivo results demonstrated that pH sensitive and neutral NSVs show no statistical significant difference. NSVs were nontoxic and showed features favorable for potential administration in vivo. In addition, neutral NSVs showed signs of increased anti-inflammatory and antinociceptive responses when compared with AG.
    Keywords: Ammonium Glycyrrhizinate ; Cytotoxicity ; Inflammation ; Niosomes ; Ph Sensitivity ; Edema -- Drug Therapy ; Glycyrrhizic Acid -- Administration & Dosage ; Liposomes -- Chemical Synthesis ; Nanocapsules -- Administration & Dosage ; Pain -- Drug Therapy
    E-ISSN: 1178-2013
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  • 5
    Language: English
    In: Peptides, 2011, Vol.32(2), pp.266-271
    Description: ▶ The formyl peptide receptor agonist N-formyl-Met-Leu-Phe-OH (fMLF) induces a dose-dependent contraction of guinea pig ileum (GPI). ▶ fMLF contracts GPI through the release of the excitatory neurotransmitters acetylcholine and substance P from myenteric motorneurons. ▶ fMLF also induces the release of prostanoids such as PGE probably from inflammatory cells that are in close proximity to the myenteric plexus and intestinal smooth muscle cells. In guinea-pig ileum (GPI), the chemotactic peptide N-formyl-Met-Leu-Phe-OH (fMLF) possesses spasmogenic properties through the activation of formyl peptide receptors (FPRs). Despite this, the mediators involved remain to be elucidated. fMLF (1 nM–1 μM) induced a dose-dependent contraction of GPI (EC = 24 nM), that is blocked by pre-treatment with the FPRs antagonist Boc . The pre-treatment with tetrodotoxin (TTX) atropine or with SR140333 reduced the fMLF-induced contraction, whereas with hexamethonium, MEN10627, SB222200, mepyramine, cimetidine, thioperamide or methysergide did not produce any effect. With DuP697 pre-treatment, but not with piroxicam, reduced the fMLF-induced contraction. After stimulation with 24 nM fMLF, a strong increase in the PGE levels was observed. Finally, the concomitant blocking of the NK receptor, the muscarinic receptors and COX-2 abolished the GPI contractions induced by fMLF. fMLF induced a concentration-dependent contraction of guinea-pig jejunum (EC = 11 nM), proximal colon (EC = 3.5 nM) and distal colon (EC = 2.2 nM), with a time-course similar to that observed in GPI. In these preparations as well, the co-administration of atropine, SR140333 and DuP697 abolished the contractions induced by fMLF. Intraperitoneal injection of fMLF (0.1 or 1 μmol/kg) enhanced the gastrointestinal motility in mice, abolished by the co-administration of atropine, SR140333 and DuP697. In conclusion, we showed that fMLF exerts spasmogenic actions on guinea-pig intestine both and through the release of acetylcholine and substance P from myenteric motorneurons and through prostanoids, probably from the inflammatory cells of the enteric immune system.
    Keywords: Fpr ; Formyl Peptide Receptors ; Gpi ; Guinea-Pig Intestine ; Fmlf ; Gastrointestinal Transit ; Chemistry ; Anatomy & Physiology
    ISSN: 0196-9781
    E-ISSN: 1873-5169
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