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Mycobiology. 2015 Jun;43(2):150-6. doi: 10.5941/MYCO.2015.43.2.150. Epub 2015 Jun 30.

In Vitro Antifungal Activity and Mode of Action of 2',4'-Dihydroxychalcone against Aspergillus fumigatus.

Author information

1
College of Pharmacy, Keimyung University, Daegu 704-701, Korea.
2
Department of Biomedical Laboratory Science, Daejeon University, Daejeon 300-716, Korea.
3
Division of Life Sciences, Daejeon University, Daejeon 300-716, Korea.

Abstract

2',4'-Dihydroxychalcone (2',4'-DHC) was identified from a heat shock protein 90 (Hsp90)-targeting library as a compound with Hsp90 inhibitory and antifungal effects. In the presence of 2',4'-DHC (8 µg/mL), radial growth of Aspergillus fumigatus was inhibited 20% compared to the control, and green pigmentation was completely blocked. The expression of the conidiation-associated genes abaA, brlA, and wetA was significantly decreased (approximately 3- to 5-fold) by treatment with 2',4'-DHC. The expression of calcineurin signaling components, cnaA and crzA, was also significantly reduced. The inhibitory effects of 2',4'-DHC on metabolic activity and mycelial growth were significantly enhanced by combination treatment with itraconazole and caspofungin. Docking studies indicated that 2',4'-DHC bind to the ATPase domain of Hsp90. These results suggest that 2',4'-DHC act as an Hsp90-calcinurin pathway inhibitor.

KEYWORDS:

2',4'-Dihydroxychalcone; Antifungal activity; Aspergillus fumigatus; Hsp90 inhibitor

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