Kaurenoic Acid Isolated from the Root Bark ofAnnona senegalensis Induces Cytotoxic andAntiproliferative Effects against PANC-1 andHeLa cells

摘要

Aims: Cancer is one of the leading causes of death worldwide with an estimated 6.7 million deaths and 24.6 million people living with cancer in 2002. Presently, there is a global increase in prevalence, mortality and health burden of various malignancies. World Health Organization (WHO) report projected that cancer prevalence rates could further increase by 50% to 15 million new cases in the year 2020. The bioactivity guided isolation of the bioactive constituent and its characterization, responsible for the anticonvulsant effects of the root bark extract of A. senegalensis yielded kaur-16-en-19-oic acid (KA). Therefore, the aim of this study was to evaluate the anti-proliferative activity of kaurenoic acid from A. senegalensis on selected cancer cell lines.Study Design: The study was designed to ascertain the antiproliferative and cytotoxic effects of kaurenoic acid, a diterpenoid isolated from the root bark of Nigerian Annona senegalensis (Annonaceae).Place and Duration of Study: Department of Pharmacology and Toxicology, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria, between October 2010 and June, 2012.Methodology: Human embryonic kidney cells expressing SV40 Large T-antigen (293 T), Pancreatic tumour (PANC-1) and Henrietta Lacks’ cervical (HeLa) cell lines were used in the study using standard MTT, 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl-tetrazoliumbromide, assay method. Results: Kaurenoic acid (KA) exhibited cytotoxic effects against the cells with estimated IC50 values of 0.93, 0.74 and 0.52 M concentrations for 293 T, HeLa and PANC-1 cells respectively. This is an indication of the possible potentials of KA in the treatment of cervical and pancreatic cancers. Conclusions: Kaurenoic acid (KA), a diterpenoid, possesses antiproliferative effect against HeLa and PANC-1 cell lines, and could be the anticancer constituent in the root bark extract of A. senegalensis with potentials as a lead in the chemical synthesis of standard anti cancer agents.