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Kaurenoic acid isolated from the root bark of 3 Annona senegalensis induces cytotoxic and 4 antiproliferative effects against PANC-1 and 5 HeLa cells

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Abstract

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 terpenoid 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
agentsCancer 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 terpenoid 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.