Planta Med 2008; 74 - PB105
DOI: 10.1055/s-0028-1084450

A new cytotoxic 2-amino-n-alkyl-carboxylic acid mixture obtained from the zoanthid Protopalythoa variabilis collected at Paracuru beach, Ceará State, Brazil

DV Wilke 1, PC Jimenez 1, RM Araújo 2, ODL Pessoa 2, ER Silveira 2, C Pessoa 1, MO Moraes 1, NP Lopes 3, LV Costa-Lotufo 1
  • 1Departamento de Fisiologia e Farmacologia, Universidade Federal do Ceará – Rua Cel. Nunes de Melo, 1127, 60.430–270, Fortaleza, Ceará, Brazil
  • 2Departamento de Química Orgânica e Inorgânica, Univeridade Federal do Ceará, Brazil
  • 3Departamento de Física e Química, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Brazil

This work performed a cytotoxicity-guided fractionation of a hydromethanolic extract obtained from the zoanthid Protopalythoa variabilis (PV-HM) collected at Paracuru beach (Ceará State, Brazil). The cytotoxicity of samples was evaluated by the MTT assay against 4 human tumor cell lines: HL-60 (leukemia), MDA MB-435 (melanoma), SF-295 (CNS glioblastoma) and HCT-8 (colon). The PV-HM and its 4 derived fractions (PV-MeOH; -Hex; -EtOAc; -DCM) were cytotoxic against all cell lines tested (IC50 ranging from 0.36 to 4.24µg/mL for PV-HM and from 0.09 to 2.9 for fractions). PV-Hex, the most potent, was purified by successive partitions with acetonitrile:water and pyridine, yielding PV-Hex-SIIS. For structure elucidation, NMR, MS and IR analysis were performed. PV-Hex-SIIS correspond to a new 2-amino-n-alkyl-carboxylic acid mixture of two compounds differing from each other by one methylene among their aliphatic chains (figure1). Preliminary analysis by flow cytometry and morphological observations of HL-60 cells treated with PV-Hex-SIIS indicates that cells are suffering apoptosis by the intrinsic pathway and showed intense cell membrane disruption. Further studies are necessary to elucidate the specific mechanism of action of these compounds.

Acknowledgement: Supported by CNPq, FINEP, Claude Bernard Institute.