Cytotoxicity and antitumoral activity of dichloromethane extract and its fractions from Pothomorphe umbellata

Abstract

The cytotoxicity of the dichloromethane crude extract (DCE), obtained from the aerial parts of Pothomorphe umbellata (L.) Miq (Piperaceae), was evaluated against nine human cancer cell lines (MCF-7, NCI-ADR/RES, OVCAR-3, PC-3, HT-29, NCI-H460, 786-O, UACC-62, K-562). The DCE presented antiproliferative activity with good potency against all cell lines at low concentrations (between 4.0 and 9.5 µg/mL) and with selectivity (1.55 µg/mL) for the leukemia cell line (K-652). DCE (100, 200, 300 and 400 mg/kg, ip) was also evaluated in the Ehrlich ascites tumor model. Both the survival number and the life span of the animals that died increased by at least 45 and 50%, respectively (8 animals per group), demonstrating P. umbellata extract potential anticancer activity. The results of the in vivo antitumor activity prompted the fractionation of the crude extract. The crude extract was submitted to dry column chromatography with dichloromethane-methanol (99:1). The column effluent fractions were extracted with methanol, dried under vacuum yielding fractions FR1 (less polar), FR2 (medium polarity), and FR3 (polar), which were analyzed for their growth inhibition or cytotoxic properties by a 48-h sulforhodamine B cell viability assay by measuring the total protein content. FR1 demonstrated high potency and cytotoxicity, a result compatible with the high toxicity of oxalic acid; FR2, containing 4-nerolidylcathecol, presented the lowest cytotoxic activity compared to the other two fractions but with selectivity for prostate cancer cell line; FR3, containing a mixture of steroids described in the literature as possessing various biological activities, also presented potent anticancer in vitro activity. These results suggest that P. umbellata DCE in vivo antitumor activity may be a consequence of the activity of different active principles.

Evaluation of mutagenicity and metabolism-mediated cytotoxicity of the naphthoquinone 5-methoxy-3,4-dehydroxanthomegnin from Paepalanthus latipes

“…Despite the development of organic synthesis, 25% of the drugs prescribed worldwide are derived from plant sources, showing that plant species are still an important source of new drugs" (Sacoman et al, 2008). Much research has been conducted on plants in popular use, with the objective of identifying natural products with therapeutic potential (Balunas and Kinghorn, 2005;Gurib-Fakim, 2006;Newman and Cragg, 2012).…”

Propagação vegetativa de Piper umbellatum L. (Piperaceae) em função de substratos e comprimentos de estacas

“…Caracteriza-se por possuir folhas com até 23 cm, cordatas, e pecíolos de 18 -24 cm (LORENZI; MATOS, 2002). Estudos farmacológicos relatam atividade anti-inflamatória e analgésica (PERAZZO et al, 2005), antimicrobiana (SPONCHIADO-JUNIOR et al, 2007), antitumoral (SACOMAN et al, 2008), sedativa (BIOKA; ABENA,1990), antioxidante e dermoprotetora contra raios UVA e UVB, sendo esta última uma das principais aplicações da planta, especialmente na indústria de cosméticos (ROPKE et al, 2005;MATTANA et al, 2009). Considerando a importância econômica da espécie são necessários estudos relativos à práticas agronômicas, uma vez que a obtenção da matéria prima é atualmente restrita ao extrativismo e às pequenas áreas de cultivo sob conhecimento agronômico científico incipiente (MAIA-ALMEIDA et al, 2011).…”

Constituents and antiproliferative activity of extracts from leaves of Croton macrobothrys

“…The crude dichloromethane extract of Virola sebifera Aubl., Myristicaceae, was shown to be highly active, with selectivity toward NCI460 (Denny et al, 2007). The cytotoxicity of the dichloromethane crude extract, obtained from the aerial parts of Pothomorphe umbellate (L.) Miq., Piperaceae, was evaluated against nine human cancer cell lines and presented antiproliferative activity against all cell lines, including leukemia (K-652) (Sacoman et al, 2008).…”