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Antiproliferative Effects of Nerium oleander Leaves and Their Cardiac Glycosides Odoroside A and Oleandrin on MCF-7 Cancer Cells

[ Vol. 3 , Issue. 2 ]

Author(s):

Kehkashan Arshad Qamar*, Ahsana Dar Farooq, Bina S. Siddiqui, Nurul Kabir, Naseema Khatoon, Shakil Ahmed, Shaista Erum and Sabira Begum   Pages 136 - 145 ( 10 )

Abstract:


Background: Nerium oleander leaves extract preparations have been used for centuries against sores, abscesses and solid tumors.

Objective: The aim of this study was to identify active compound(s) responsible for the antiproliferative activity of N. oleander leaves against MCF-7 breast cancer cell line and to explore their mechanisms of action.

Methods: The methanolic extract and fractions were screened against four human cancer cell lines: HT-144, MCF-7, NCI-H460 and SF-268 using sulforhodamine B assay. The most active ethyl acetate soluble fraction led to the isolation of eleven pure compounds viz adynerigenin, adynerin, odoroside A, odoroside B, 5-O-kaempferobinoside, β-neriursate, oleanderocioic acid, oleandiginoside, oleandrin, 5-O-quercetibinoside and ursolic acid. The methanolic extract and the ethyl acetate soluble fraction exhibited significant growth inhibition (TGI: 0.14 to 3.3 μg/ml) against HT-144, MCF-7, NCI-H460 and SF-268 cell lines. The effects of the methanolic extract, ethyl acetate soluble fraction, odoroside A and oleandrin on the cytoskeleton and nuclei of MCF-7 cells were evaluated using immunofluorescence microscopy. Significant reduction in the mitotic index of MCF-7 cells were exhibited by the methanolic extract, ethyl acetate soluble fraction, odoroside A and oleandrin accompanied by morphological changes such as band-like arrangement of cells, reduction in F-actin processes, disruption of interphase microtubule network and condensation of nuclei.

Results: These results support that the N. oleander leaves possess antiproliferative activity against the aforementioned cell lines particularly estrogen receptor positive MCF-7 cells, thereby justifying its traditional use against tumors. Moreover, the antiproliferative effects induced by the methanolic extract, ethyl acetate soluble fraction, odoroside A and oleandrin were possibly related to skeletal and nuclear morphological changes.

Keywords:

Antiproliferative, cytoskeleton, human cancer cell lines, Nerium oleander, odoroside A, oleandrin.

Affiliation:

H.E.J. Research Institute of Chemistry, University of Karachi, Karachi, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi, Dr. Panjwani Center for Molecular Medicine and Drug Research, University of Karachi, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi, Industrial Analytical Center, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Industrial Analytical Center, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi

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