In Vitro Antifungal Activity and Mode of Action of 2',4'-Dihydroxychalcone against Aspergillus fumigatus.
10.5941/MYCO.2015.43.2.150
- Author:
Young Ho SEO
1
;
Sung Su KIM
;
Kwang Soo SHIN
Author Information
1. College of Pharmacy, Keimyung University, Daegu 704-701, Korea.
- Publication Type:In Vitro ; Original Article
- Keywords:
2',4'-Dihydroxychalcone;
Antifungal activity;
Aspergillus fumigatus;
Hsp90 inhibitor
- MeSH:
Adenosine Triphosphatases;
Aspergillus fumigatus*;
Calcineurin;
Heat-Shock Proteins;
Itraconazole;
Pigmentation
- From:Mycobiology
2015;43(2):150-156
- CountryRepublic of Korea
- Language:English
-
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.
