Monique Chéron

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Spectroscopic studies of four amphotericin B (AmB) lipid preparations--small negatively charged unilamellar vesicles "AmBisome", positively charged oligolamellar liposomes "Ampholiposomes", AmB Lipid Complex "L-AmpB33"--and AmB association with gamma cyclodextrin demonstrated that the composition of drug delivery system directly influences AmB organization.(More)
Superaggregation of amphotericin B (AmB) was previously shown to occur upon heating of solutions at 70 degrees C. In the present study, we demonstrate that heat pretreatment of Fungizone (deoxycholate salt of AmB [AmB-DOC]) solutions induces a drastic decrease in the in vitro toxicity of this antibiotic. Heated AmB-DOC colloidal solutions, which mainly(More)
The aggregation state of amphotericin B (AmB) was previously reported to modulate its therapeutic efficiency. As a preliminary study to test the biological effects of 'superaggregates' generated by heat treatment, we present spectroscopic data related to their formation in aqueous solutions. Drastic changes in the AmB aggregation state in water were shown(More)
The quantitative structure-activity relationships studies of amphotericin B and its 16 semisynthetic derivatives obtained by modification at carboxyl and amino groups have been done. The results of five biological tests were subjected to principal component analysis, a numerical method useful in the investigation of large sets of data. For some compounds,(More)
Rational chemical modification of amphotericin B (AMB) led to the synthesis of sterically hindered AMB derivatives. The selected optimal compound, N-methyl-N-D-fructosyl amphotericin B methyl ester (MF-AME) retains the broad spectrum of antifungal activity of the parent antibiotic, and exhibits a two orders of magnitude lower toxicity in vivo and in vitro(More)
AIM Heat treatment of deoxycholate-amphotericin B (AmB-DOC) leads to a therapeutically interesting supramolecular rearrangement (h-AmB-DOC); this reformulation improves the therapeutic index of AmB-DOC by reducing amphotericin B (AmB) toxicity in mammalian cell lines from 3- to 10-fold. Its activity in experimentally induced fungal infection in mice remains(More)
In an 82-year-old woman, presenting with fever and asthenia, cervical adenopathy was noted. Clinical and radiological investigations were fruitless. Laboratory examinations detected a refractory anemia. The lymph node was excised and showed numerous trichomonads on touch preparations. Histologically, the node showed caseous necrosis and macrophagic(More)
Amphotericin B-induced lysis of erythrocytes is diminished in the presence of Cu2+, but the prelytic amphotericin B-induced K+ leakage is unaffected. These results and the weak binding of Cu2+ to amphotericin B, demonstrated by circular dichroism and EPR studies, are consistent with the view that Cu2+ protects erythrocytes by increasing their resistance to(More)
INTRODUCTION Primary meningococcal arthritis is a rare form of meningococcal disease. It occurs as an isolated acute purulent arthritis without meningitis, and presence of Neisseria meningitidis in articular fluid. We report a new case of typical primary meningococcal arthritis. EXEGESIS A previously healthy 23-year-old female patient was admitted for(More)
OBJECTIVE To study the toxicity and activity of two new amphotericin B formulations: poly(epsilon-caprolactone) nanospheres coated with poloxamer 188 (AmB-NP) and mixed micelles with the same surfactant (AmB-MM). MATERIALS AND METHODS The toxicity of these formulations was evaluated in erythrocytes, J774.2 macrophages and LLCPK1 renal cells, as well as in(More)