Planta Med 2011; 77(13): 1482-1488
DOI: 10.1055/s-0030-1270889
Biological and Pharmacological Activity
Original Papers
© Georg Thieme Verlag KG Stuttgart · New York

In vitro and In vivo Anticancer Activity of Extracts, Fractions, and Eupomatenoid-5 Obtained from Piper regnellii Leaves

Giovanna Barbarini Longato1 , 2 , Larissa Yokota Rizzo1 , 2 , Ilza Maria de Oliveira Sousa3 , Sirlene Valério Tinti2 , Ana Possenti2 , Glyn Mara Figueira4 , Ana Lúcia Tasca Gois Ruiz2 , Mary Ann Foglio3 , João Ernesto de Carvalho2
  • 1Programa de Pós-graduação em Biologia Celular e Estrutural, Instituto de Biologia, Universidade Estadual de Campinas – UNICAMP, Campinas, SP, Brasil
  • 2Divisão de Farmacologia e Toxicologia, Centro Pluridisciplinar de Pesquisas Químicas, Biológicas e Agrícolas (CPQBA), UNICAMP, Campinas, SP, Brasil
  • 3Divisão de Fitoquímica, CPQBA, UNICAMP, Campinas, SP, Brasil
  • 4Divisão de Agrotecnologia, CPQBA, UNICAMP, Campinas, SP, Brasil
Further Information

Publication History

received January 17, 2011 revised February 9, 2011

accepted February 10, 2011

Publication Date:
09 March 2011 (online)

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Abstract

Despite numerous studies with the Piper genus, there are no previous results reporting in vitro or in vivo Piper regnellii (Miq.) C. DC. var. regnellii anticancer activity. The aim of this study was to investigate P. regnellii in vitro and in vivo anticancer activity and further identify its active compounds. In vitro antiproliferative activity was evaluated in 8 human cancer cell lines: melanoma (UACC-62), breast (MCF7), kidney (786–0), lung (NCI-H460), prostate (PC-3), ovary (OVCAR-3), colon (HT29), and leukemia (K-562). Total growth inhibition (TGI) values were chosen to measure antiproliferative activity. Among the cell lines evaluated, eupomatenoid-5 demonstrated better in vitro antiproliferative activity towards prostate, ovary, kidney, and breast cancer cell lines. In vivo studies were carried out with Ehrlich solid tumor on Balb/C mice treated with 100, 300, and 1000 mg/kg of P. regnellii leaves dichloromethane crude extract (DCE), with 30 and 100 mg/kg of the active fraction (FRB), and with 30 mg/kg of eupomatenoid-5. The i. p. administration of DCE, FRB, and eupomatenoid-5 significantly inhibited tumor progression in comparison to control mice (saline). Therefore, this study showed that neolignans of Piper regnellii have promising anticancer activity. Further studies will be undertaken to determine the mechanism of action and toxicity of these compounds.