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

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2020-01-01

Autores

Freitas, Jolindo A. [UNESP]
Sorrechia, Rodrigo [UNESP]
Politi, Flávio A. S. [UNESP]
Santos, André G. [UNESP]
Rodrigues, Edvânio R. [UNESP]
Santos, Lourdes C. [UNESP]
Fusco-Almeida, Ana M. [UNESP]
Oliveira, Andrew A.
Guido, Rafael V. C.
Pietro, Rosemeire C. L. R. [UNESP]

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Resumo

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. (Figure presented.).

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

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Natural Product Research, v. 34, n. 23, p. 3423-3427, 2020.