Autor(es):
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]
Data: 2021
Identificador Persistente: http://hdl.handle.net/11449/206494
Origem: Oasisbr
Assunto(s): 4-Nerolidylcatechol; antifungal; cytotoxicity; dermatophytes;Piper umbellatum
Descrição
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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.).
School of Pharmaceutical Sciences Department of Drugs and Medicines São Paulo State University(UNESP)
School of Pharmaceutical Sciences Department of Natural Principles and Toxicology São Paulo State University (UNESP)
Institute of Chemistry Department of Organic Chemistry São Paulo State University (UNESP)
School of Pharmaceutical Sciences Department of Clinical Analysis São Paulo State University(UNESP)
São Carlos Institute of Physics University of São Paulo (USP)
Jolindo A. Freitas School of Pharmaceutical Sciences of Ribeirão Preto University of São Paulo
School of Pharmaceutical Sciences Department of Drugs and Medicines São Paulo State University(UNESP)
School of Pharmaceutical Sciences Department of Natural Principles and Toxicology São Paulo State University (UNESP)
Institute of Chemistry Department of Organic Chemistry São Paulo State University (UNESP)
School of Pharmaceutical Sciences Department of Clinical Analysis São Paulo State University(UNESP)