Biosynthesis of amphotericin B

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Plasma protein binding of amphotericin B and pharmacokinetics of bound versus unbound amphotericin B after administration of intravenous liposomal amphotericin B (AmBisome) and amphotericin B deoxycholate.

Unilamellar liposomal amphotericin B (AmBisome) (liposomal AMB) reduces the toxicity of this antifungal drug. The unique composition of liposomal AMB stabilizes the liposomes, producing higher sustained drug levels in plasma and reducing renal and hepatic excretion. When liposomes release their drug payload, unbound, protein-bound, and liposomal drug pools may exist simultaneously in the body. ...

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Inhibitors of sterol biosynthesis and amphotericin B reduce the viability of pneumocystis carinii f. sp. carinii.

Pneumocystis carinii synthesizes sterols with a double bond at C-7 of the sterol nucleus and an alkyl group with one or two carbons at C-24 of the side chain. Also, some human-derived Pneumocystis carinii f. sp. hominis strains contain lanosterol derivatives with an alkyl group at C-24. These unique sterols have not been found in other pathogens of mammalian lungs. Thus, P. carinii may have imp...

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Inhibition of Nucleotide Biosynthesis Potentiates the Antifungal Activity of Amphotericin B

The polyene antifungal agent Amphotericin B exhibits potent and broad spectrum fungicidal activity. However, high nephrotoxicity can hinder its administration in resource poor settings. Quantification of early fungicidal activity in studies of HIV patients with cryptococcosis demonstrate that 5-Fluorocytosine therapy in combination with Amphotericin B results in faster clearance than with Ampho...

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Potentiation of antifungal effect of amphotericin B by squalene, an intermediate for sterol biosynthesis.

The antifungal effect of a polyene antibiotic amphotericin B (AMB) was almost completely abrogated by exogenous addition of 0.1 microgram/ml ergosterol in the medium. The cytocidal effect of AMB on Saccharomyces cerevisiae was synergistically enhanced when cultured for more than 4 hours with squalene, an obligatory intermediate molecule for sterol formation. However, we could not find significa...

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Neutrophil toxicity of amphotericin B.

The toxicity of amphotericin B (AmB) for neutrophils and the protective effect of serum cholesterol were investigated. Neutrophils were exposed in vitro to varying concentrations of AmB. As judged by trypan blue exclusion, neutrophil viability decreased by 40% (P < 0.001) within 30 min of incubation in sterol-free buffer containing 5 mug of AmB per ml. In the presence of 4 mg of cholesterol per...

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ژورنال

عنوان ژورنال: Journal of the Chemical Society, Perkin Transactions 1

سال: 1998

ISSN: 0300-922X,1364-5463

DOI: 10.1039/a704545j