Lopes, Andrey P.Bagatela, Bianca S.Rosa, Paulo C. P.Nanayakkara, Dhammika N. P.Carlos Tavares Carvalho, JoséMaistro, Edson Luis [UNESP]Bastos, Jairo K.Perazzo, Fábio F.2014-05-272014-05-272013-03-11BioMed Research International, v. 2013.2314-61332314-6141http://hdl.handle.net/11449/74820The crude ethanolic extract from aerial parts of Pothomorphe umbellata L. (Piperaceae) and fractions obtained by partitions sequentially among water-methanol, methylene chloride, and ethyl acetate, as well as the major constituent, 4-nerolidylcatechol, were, respectively, evaluated and evidenced for antioxidant and cytotoxic effects through fluorometric microplate and microculture tetrazolium assays in HL-60 cells. The crude ethanolic extract demonstrated the preeminent antioxidant activity (IC50 = 1.2 μg/mL) against exogenous cytoplasmic reactive oxygen species, followed by the water-methanolic (IC50 = 4.5 μg/mL), methylene chloride (IC 50 = 5.9 g/mL), ethyl acetate (IC50 = 8.0 g/mL), 4-nerolidylcatechol (IC50 = 8.6 g/mL), and the sterol fractions (IC50 > 12.5 μg/mL). Vitamin C, the positive control used in this assay, presented IC50 value equivalent to 1.7 μg/mL. 4-Nerolidylcatechol (IC50 = 0.4 μg/mL) and methylene chloride fraction (IC50 = 2.3 μg/mL) presented considerable cytotoxicity probably because of the presence of an o-quinone, an auto-oxidation by product of the catechol. Polar compounds, present in the ethanol extract, appear to increase the solubility and stability of the major active constituent, acting synergistically with 4-nerolidylcatechol, improving its pharmacokinetic parameters and increasing significantly its antioxidant activity which, in turn, suggests that the aqueous-ethanolic extract, used in folklore medicine, is safe and effective. © 2013 Andrey P. Lopes et al.eng4 nerolidylcatecholacetic acid ethyl esteralcoholcatechol derivativedichloromethaneplant extractPothomorphe umbellata plant extractsterolunclassified drugantioxidant activitycontrolled studycytotoxicitydrug solubilitydrug stabilityhumanhuman cellmedicinal plantoxidationPiperaceaeplant leafPothomorphe umbellataArtigo10.1155/2013/206581WOS:000313686800001Acesso aberto2-s2.0-848745868812-s2.0-84874586881.pdf47875216130383150000-0003-0757-7876