Activity of 3 `-hydroxychalcone against Cryptococcus gattii and toxicity, and efficacy in alternative animal models

Author(s):Show less -

Palanco, Ana Cerrejn ^[1] ; Singulani, Junya de lacorte ^[1] ; Costa-Orlandi, Caroline Barcelos ^[1] ; Gullo, Fernanda Patricia ^[1] ; Strohmayer Lourencetti, Natalia Manuela ^[1] ; Gomes, Paulo Cesar ^[1] ; Ayusso, Gabriela Miranda ^[2] ; Dutra, Luiz Antonio ^[3] ; Bolzani, Vanderlan da Silva ^[3] ; Regasini, Luis Octavio ^[2] ; Soares Mendes-Giannini, Maria Jose ^[1] ; Fusco-Almeida, Ana Marisa ^[1]

Affiliation

^[1] Sao Paulo State Univ, UNESP, Sch Pharmaceut Sci, Araraquara, SP - Brazil

^[2] UNESP, Inst Biosci Letters & Exact Sci, Sao Jose Do Rio Preto, SP - Brazil

^[3] UNESP, Inst Chem, Araraquara, SP - Brazil

• Document type: Journal article
• Source: FUTURE MICROBIOLOGY; v. 12, n. 13, p. 1123-1134, OCT 2017.
• Web of Science Citations: 9

Abstract

Aim: This work aimed to evaluate the activity of 3'-hydroxychalcone against Cryptococcus gattii in planktonic and biofilm forms and their toxicity using alternative animal models. Materials \& methods: Minimum inhibitory concentration and minimum fungicide concentration were determined. Biofilm formation and the susceptibility tests were performed by the 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-5-{[}carbonyl(phenylamino)]2H- tetrazolium hydroxide assay. Toxicity and efficacy were checked in Danio rerio and Galleria mellonella models. Results: The compound 3'-hydroxychalcone showed fungicidal activity against C. gattii in both planktonic and biofilm forms. The toxicity in zebrafish embryos revealed a low lethal concentration. In G. mellonella, the compound did not show antifungal activity and larvae toxicity. Conclusion: Because of the activity of 3'-hydroxychalcone against C. gattii in vitro, molecular modifications should be made to improve efficacy and to reduce toxicity in vivo. (AU)

• FAPESP's process: 14/18330-0 - Synthesis and biological evaluation of curcumin-cinnamaldehyde hybrids as bacterial cell division inhibitors
• Grantee: Luis Octávio Regasini
• Support type: Regular Research Grants
• FAPESP's process: 14/10446-9 - Evaluation of new therapies and biomarkers in paracoccidioidomycosis: antifungal activity of alkyl gallates in alternative models and mice and identification of circulating microRNAs
• Grantee: Junya de Lacorte Singulani
• Support type: Scholarships in Brazil - Doctorate