In vitro bioassay guided anti-dermatophyte and cytotoxic activities from Piper umbellatum L. Miq. led to 4-nerolidylcatechol

Abstract

Dermatophytosis is a dermic disease caused by fungi. The aim of this study was to search anti-dermatophyte bioactive compounds in Piper umbellatum leaves. Cytotoxicity evaluation was performed against MRC-5 and HepG2 as a selectivity parameter. Crude ethanol extract presented MIC value of 39.1 μg/mL against M. canis and no cytotoxicity to Hep G2 (human liver cancer) and MRC-5 (normal lung fibroblast). 4-nerolydilcatechol was isolated from P. umbellatum ethanolic extract. MIC values for 4-NC were 7.6μM to M. canisand 15.6μM to Trichophyton rubrum. 4-NC presented activity against M. canis14 times lower than to MRC-5 (non-tumoral human cell line), which suggest selective activity for this fungus. Molecular modeling suggests 4-NC could bind to CYP51, present in lanosterol synthesis, blocking fungi development. In conclusion, P. umbellatum crude ethanol extract and 4-NC demonstrated high and selective in vitro antifungal activity.

Keywords:

• 4-Nerolidylcatechol
• antifungal
• cytotoxicity
• dermatophytes;Piper umbellatum

Acknowledgments

This work had financial support by São Paulo Foundation Research (FAPESP, Brazil)grant#2013/10578-0, grant#2013/25243-3, grant#2013/07600-3, National Council for Scientific and Technological Development (CNPq)grant#477786/2013-8 and in part by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior – Brasil (CAPES) – Finance Code 001. We acknowledge Cláudia Tavares dos Santos, Caio Humberto Perego, Flávio Alexandre Carvalho, Jussara Bergamo and Cláudia Scalize for technicalsupport.

Disclosure statement

No potential conflict of interest was reported by the authors.