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In vitro bioassay guided anti-dermatophyte and cytotoxic activities from Piper umbellatum L. Miq. led to 4-nerolidylcatechol.
FREITAS, Jolindo A.; SORRECHIA, Rodrigo; POLITI, Flávio A. S.; SANTOS, André G.; RODRIGUES, Edvânio R.; SANTOS, Lourdes C.; FUSCO-ALMEIDA, Ana M.; OLIVEIRA, Andrew Albert de; GUIDO, Rafael Victorio Carvalho; PIETRO, Rosemeire C. L. R.
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 lg/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 7.6lM to M. canis and 15.6lM to Trichophyton rubrum. 4-NC presented activity against M. canis 14 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.
Natural Product Research
v. 34, n. 23, p. 3423-3427 - Ano: 2020
Fator de Impacto: 2,158
    @article={003012316,author = {FREITAS, Jolindo A.; SORRECHIA, Rodrigo; POLITI, Flávio A. S.; SANTOS, André G.; RODRIGUES, Edvânio R.; SANTOS, Lourdes C.; FUSCO-ALMEIDA, Ana M.; OLIVEIRA, Andrew Albert de; GUIDO, Rafael Victorio Carvalho; PIETRO, Rosemeire C. L. R.},title={In vitro bioassay guided anti-dermatophyte and cytotoxic activities from Piper umbellatum L. Miq. led to 4-nerolidylcatechol},journal={Natural Product Research},note={v. 34, n. 23, p. 3423-3427},year={2020}}