Heat-induced reformulation of amphotericin B-deoxycholate favours drug uptake by the macrophage-like cell line J774 | Zendy

Monique Chéron | Zendy

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Heat-induced reformulation of amphotericin B-deoxycholate favours drug uptake by the macrophage-like cell line J774

Author(s) -

Monique Chéron

Publication year - 2003

Publication title -

journal of antimicrobial chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.124

H-Index - 194

eISSN - 1460-2091

pISSN - 0305-7453

DOI - 10.1093/jac/dkg455

Subject(s) - cell culture , toxicity , amphotericin b , pharmacology , cytotoxicity , biology , in vivo , in vitro , lactate dehydrogenase , chemistry , biochemistry , microbiology and biotechnology , enzyme , antifungal , genetics , organic chemistry

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 unchanged compared with AmB-DOC, whereas its activity is 2.5 times higher in Leishmania donovani-infected mice. This work investigates the in vitro mechanism that allows this improvement.

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