Mycobiology.  2015 Jun;43(2):150-156. 10.5941/MYCO.2015.43.2.150.

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

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

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 microg/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.

Keyword

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

MeSH Terms

Adenosine Triphosphatases
Aspergillus fumigatus*
Calcineurin
Heat-Shock Proteins
Itraconazole
Pigmentation
Adenosine Triphosphatases
Calcineurin
Heat-Shock Proteins
Itraconazole
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