title: Evaluation of antimicrobial and antimalarial activities of crude extract, fractions and 4-nerolidylcathecol from the aerial parts of Piper umbellata L. (Piperaceae).
abstract: Presently, natural products, such as Piper umbellata L. (Piperaceae), have been evaluated as sources of antimicrobial agents with efficacies against microorganisms. The in vitro antimicrobial activity was performed by broth micro-dilution susceptibility assay, according to the protocols of the National Committee for Clinical Laboratory Standards, and described the antibacterial and antifungal activities of crude ethanolic extract and fractions obtained by partitions sequentially among water-methanol, methylene chloride and ethyl acetate, as well as the major constituent, 4-nerolidylcatechol from the aerial parts of P. umbellata L. Amphotericin B and ciprofloxacin were used as controls. Among the microorganism cultures, hydromethanol fraction demonstrated the pre-eminent antifungal activity. 4-Nerolidylcathecol was the only tested plant component that exhibited activity against all the selected microorganisms, suggesting its great potential as a source for the development of new drugs. In order to estimate the antimalarial activity of P. umbellata L., a micro-dilution method protocol, parasite lactate dehydrogenase assay, with a Plasmodium falciparum Sierra Leone (D6) clone was utilised. The antimalarial agent artemisinin was used as control. 4-Nerolidylcathecol exhibited the best antimalarial activity; however, it was not significant when compared with control. These in vitro results do not justify the use of P. umbellata L. in malaria patients. However, there is a possibility of 4-nerolidylcathecol, after biotransformation, exhibiting a significant antimalarial activity in in vivo assays. However, 4-nerolidylcathecol demonstrated to possess a broad antimicrobial activity which is, in fact, a promising source for the development of new therapeutic agents.
authors.affiliation: a Department of Exact and Earth Sciences , Institute of Environmental, Chemical and Pharmaceutical Sciences, Federal University of São Paulo , São Nicolau Street 210, 09913-030 Diadema, São Paulo , Brazil.
authors.forename: Bianca Souza
authors.initials: BS
authors.lastname: Bagatela
authors.forename: Andrey Pereira
authors.initials: AP
authors.lastname: Lopes
authors.forename: Fernando Luiz Affonso
authors.initials: FL
authors.lastname: Fonseca
authors.forename: Márcio Adriano
authors.initials: MA
authors.lastname: Andreo
authors.forename: Dhammika N P
authors.initials: DN
authors.lastname: Nanayakkara
authors.forename: Jairo Kenupp
authors.initials: JK
authors.lastname: Bastos
authors.forename: Fábio Ferreira
authors.initials: FF
authors.lastname: Perazzo
mesh_terms: D000890:Anti-Infective Agents / Q000302:isolation & purification / Q000494:pharmacology*; D000962:Antimalarials / Q000302:isolation & purification / Q000494:pharmacology*; D002396:Catechols / Q000302:isolation & purification / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D031701:Piper / Q000737:chemistry*; D035261:Plant Components, Aerial / Q000737:chemistry*; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: C110583:4-nerolidylcatechol; D000890:Anti-Infective Agents; D000962:Antimalarials; D002396:Catechols; D010936:Plant Extracts; D007770:L-Lactate Dehydrogenase