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

Author(s)

Freitas, Jolindo A. ^{[1, 2]} ; Sorrechia, Rodrigo ^[1] ; Politi, Flavio A. S. ^[1] ; Santos, Andre G. ^[3] ; Rodrigues, Edvanio R. ^[1] ; Santos, Lourdes C. ^[4] ; Fusco-Almeida, Ana M. ^[5] ; Oliveira, Andrew A. ^[6] ; Guido, Rafael V. C. ^[6] ; Pietro, Rosemeire C. L. R. ^[1]

Affiliation

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

^[2] Univ Sao Paulo, Sch Pharmaceut Sci Ribeirao Preto, Ribeirao Preto, SP - Brazil

^[3] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, Dept Nat Principles & Toxicol, Araraquara, SP - Brazil

^[4] Sao Paulo State Univ UNESP, Inst Chem, Dept Organ Chem, Araraquara, SP - Brazil

^[5] Sao Paulo State Univ UNESP, Sch Pharmaceut Sci, Dept Clin Anal, Araraquara, SP - Brazil

^[6] Univ Sao Paulo, Sao Carlos Inst Phys, Sao Carlos, SP - Brazil

• Document type: Journal article
• Source: NATURAL PRODUCT RESEARCH; v. 34, n. 23, p. 3423-3427, DEC 1 2020.
• Web of Science Citations: 1

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 mu g/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 7.6 mu M to M. canisand 15.6 mu M 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. {[}GRAPHICS] . (AU)

• FAPESP's process: 13/10578-0 - Investigation of antifungal activity, mechanism of action and analysis of protein profile of T. rubrum and M. canis to Piper umbellatum derivatives
• Grantee: Jolindo Alencar Freitas
• Support Opportunities: Scholarships in Brazil - Master
• FAPESP's process: 13/25243-3 - Investigation of antifungal activity, mechanisms of action and analysis of protein profile against Pothomorphe umbellata extracts
• Grantee: Rosemeire Cristina Linhari Rodrigues Pietro
• Support Opportunities: Regular Research Grants
• FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
• Grantee: Glaucius Oliva
• Support Opportunities: Research Grants - Research, Innovation and Dissemination Centers - RIDC