Abstract
Objectives: The objective of this study was to evaluate the β-monolinolein as a potential therapy for breast cancer treatment.
 Methods: The cytotoxic activity of β-monolinolein was evaluated by 3-(4,5-dimetylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and trypan blue exclusion assay. The cellular cytotoxicity and levels of cytosolic enzyme, lactate dehydrogenase (LDH), were measured by assessing μmoles of nicotinamide adenine dinucleotide/well/min. To confirm whether β-monolinolein induces apoptosis in 3,4-methylenedioxyamphetamine (MDA)- MB-231 cells, western blot and semiquantitative reverse transcription-polymerase chain reaction (RT-PCR) analysis were performed.
 Results: For the 1st time, it was demonstrated that β-monolinolein strongly inhibits the growth of MDA-MB-231 cells, with an half maximal inhibitory concentration value of 12.5 μg/ml. <90% of cell death was achieved at higher concentrations after 48 h of treatment. Trypan blue assay showed that the cell viability was significantly decreased in a dose-dependent manner in MDA-MB-231 cells after 48 h of treatment. On the other hand, LDH activities in the cultured media were significantly elevated in a dose-dependent manner as compared to the control. Further, the western blot analysis showed that β-monolinolein leads to change in expression levels of important cell cycle regulators such as p21, Bax, Bcl-Xl, and Bcl-2 in MDA-MB-231 cells. The semiquantitative RT-PCR results indicated a significant upregulation of proapoptotic genes such as p53, p21, and Bax and downregulation of antiapoptotic gene Bcl-2.
 Conclusion: These results indicate that β-monolinolein leads to change in expression of various cell cycle/apoptotic regulators and hence induces death in MDA-MB-231 cells.
Highlights
Cancer is defined as a complex series of life-threatening disease condition and a leading cause of death caused by persistent tissue injury and host-environment interactions [1]
MTT assay for cytotoxicity Treatment of MDA-MB-231 cells for 48 h with β-monolinolein showed a very significant and higher cytotoxic activity with an IC50 value of 12.5 μg/ml (Fig. 1)
These results indicated that β-monolinolein has a potent cytotoxic activity on MDA-MB-231 breast cancer cells
Summary
Cancer is defined as a complex series of life-threatening disease condition and a leading cause of death caused by persistent tissue injury and host-environment interactions [1]. Cancer is known to be the second leading cause of death and is responsible for an estimated 9.6 million deaths in 2018. About one in six deaths are due to cancer [2]. The repeated exposure of carcinogens such as tobacco, ultraviolet light, and infections leads to various genetic (mutations), epigenetic (loss of heterozygosity), and global transcriptome changes (through inflammation pathways) and is associated with increased cancer risk [3]. The latest WHO statistics suggests about 45% increase in the global cancer deaths by 2030, of which 70% would be contributed from developing countries like India [5]. Remain a high priority for scientific community across the world [6]
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