New targeting system for antimycotic drugs: beta-glucosidase sensitive amphotericin B-star poly(ethylene glycol) conjugate.
A new targeting potentially intravenous conjugate Amphotericin B (AMB)-star poly(ethylene glycol) (sPEG) (M=25,160) has been synthesized and characterized. It contains a beta-d-glucopyranoside molecular switch which is sensitive to beta-glucosidases (E.C.3.2.1.21). The beta-glucosidase-catalyzed release of AMB from the polymeric carrier was proved in vitro by means of spectrophotometry and HPLC.
Sedlák
Milos
M
Department of Organic Chemistry, Faculty of Chemical Technology, University of Pardubice, Cs. legií 565, 532 10 Pardubice, Czech Republic. milos.sedlak@upce.cz
Drabina
Pavel
P
Bílková
Eliska
E
Simůnek
Petr
P
Buchta
Vladimír
V
D000666:Amphotericin B / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002384:Catalysis; D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D006801:Humans; D008956:Models, Chemical; D011092:Polyethylene Glycols / Q000138:chemical synthesis / Q000494:pharmacology*; D013056:Spectrophotometry, Ultraviolet; D001617:beta-Glucosidase / Q000378:metabolism*
D000935:Antifungal Agents; D011092:Polyethylene Glycols; D000666:Amphotericin B; D001617:beta-Glucosidase