Antineoplastic activity of rinvanil and phenylacetylrinvanil in leukaemia cell lines.
In the search for novel chemotherapeutic agents for cancer treatment, capsaicin has been shown to inhibit proliferation and induce apoptosis in various types of cancer cell line, including leukaemia cell lines. The capsaicin analogues, rinvanil and phenylacetylrinvanil (PhAR), share a binding affinity for vanilloid receptors and may have biological activities similar to capsaicin; however, their anticancer potential has not yet been reported. This study analyses the antineoplastic activities of rinvanil and PhAR in leukaemia versus normal cells. P388, J774 and WEHI-3 leukaemia cell lines, as well as mouse bone marrow mononuclear cells, were cultured with varying concentrations of rinvanil and PhAR. Following this, proliferation and apoptosis were determined by the sulforhodamine B (SRB) assay and DNA ladder. Cultured leukaemia cell lines and mouse bone marrow mononuclear cells demonstrated a dose-dependent inhibition of proliferation, while non-diseased cells were less sensitive to the cytotoxic effect of capsaicin, rinvanil and PhAR. Rinvanil and PhAR also induced apoptosis in leukaemia cell lines but not in bone marrow. Given the lower IC50values for apoptosis induction in leukaemia cells compared with that of normal cells, PhAR is a promising selective anticancer agent.
Laboratory of Drug Synthesis, L9-PA, Research Unit on Cell Differentiation and Cancer, L8-PB, Campus II, UMIEZ FES-Zaragoza, UNAM, Iztapalapa, Mexico City 09230, Mexico.
Axel
A
Luviano
Hematopoiesis and Leukaemia Laboratory, Research Unit on Cell Differentiation and Cancer, L8-PB, Campus II, UMIEZ FES-Zaragoza, UNAM, Iztapalapa, Mexico City 09230, Mexico.
Itzen
I
Aguiñiga-Sánchez
Laboratory of Drug Synthesis, L9-PA, Research Unit on Cell Differentiation and Cancer, L8-PB, Campus II, UMIEZ FES-Zaragoza, UNAM, Iztapalapa, Mexico City 09230, Mexico.
Patricia
P
Demare
Hematopoiesis and Leukaemia Laboratory, Research Unit on Cell Differentiation and Cancer, L8-PB, Campus II, UMIEZ FES-Zaragoza, UNAM, Iztapalapa, Mexico City 09230, Mexico.
Reynaldo
R
Tiburcio
Hematopoiesis and Leukaemia Laboratory, Research Unit on Cell Differentiation and Cancer, L8-PB, Campus II, UMIEZ FES-Zaragoza, UNAM, Iztapalapa, Mexico City 09230, Mexico.
Edgar
E
Ledesma-Martínez
Hematopoiesis and Leukaemia Laboratory, Research Unit on Cell Differentiation and Cancer, L8-PB, Campus II, UMIEZ FES-Zaragoza, UNAM, Iztapalapa, Mexico City 09230, Mexico.
Edelmiro
E
Santiago-Osorio
Hematopoiesis and Leukaemia Laboratory, Research Unit on Cell Differentiation and Cancer, L8-PB, Campus II, UMIEZ FES-Zaragoza, UNAM, Iztapalapa, Mexico City 09230, Mexico.
Ignacio
I
Regla
apoptosis; cancer; capsaicin; proliferative activity; vanilloid receptor