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Bioorg Chem ; 105: 104402, 2020 12.
Article in English | MEDLINE | ID: mdl-33130347

ABSTRACT

ATP-Binding Cassette (ABC) transporters are the main class of transmembrane transporters involved in pathogenic fungal resistance against chemotherapeutic agents. Herein we report results which show that batzelladine D (1) and norbatzelladine L (2) reverse the fluconazole resistance phenotype mediated by Pdr5p transporter on Saccharomyces cerevisiae. Both alkaloids were able to chemosensitize the Pdr5p-overexpressing strain by synergistic interaction with fluconazole. Both compounds also showed an inhibitory effect on the catalytic activity and on the intracellular accumulation of rhodamine 6G, and did not show significant in vitro mammalian cells toxicity.


Subject(s)
Alkaloids/pharmacology , Fluconazole/pharmacology , Porifera/chemistry , Pyrimidines/pharmacology , Rhodamines/antagonists & inhibitors , ATP-Binding Cassette Transporters/metabolism , Alkaloids/chemistry , Alkaloids/isolation & purification , Animals , Cells, Cultured , Dose-Response Relationship, Drug , Mice , Molecular Structure , Pyrimidines/chemistry , Pyrimidines/isolation & purification , Rhodamines/metabolism , Saccharomyces cerevisiae Proteins/metabolism , Structure-Activity Relationship
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