Abstract
Piceatannol (PIC), a naturally occurring polyphenolic stilbene, has pleiotropic pharmacological activities. It has reported cytotoxic activities against different cancer cells. In the present study, PIC emulsomes (PIC-E) were formulated and assessed for cytotoxic activity. A Box–Behnken design was employed to investigate the influence of formulation factors on particle size and drug entrapment. After optimization, the formulation had a spherical shape with a particle size of 125.45 ± 1.62 nm and entrapment efficiency of 93.14% ± 2.15%. Assessment of cytotoxic activities indicated that the optimized PIC-E formula exhibited significantly lower IC50 against HCT 116 cells. Analysis of the cell cycle revealed the accumulation of cells in the G2-M phase as well as increased cell fraction in the sub-G1 phase, an indication of apoptotic-enhancing activity. Staining of cells with Annexin V indicated increased early and late apoptosis. Further, the cellular contents of caspase - 3 and Bax/Bcl-2 mRNA expression were significantly elevated by PIC-E. In addition, the mitochondrial membrane potential (MMP) was disturbed and reactive oxygen species (ROS) production was increased. In conclusion, PIC-E exhibited superior cell death-inducing activities against HCT 116 cells as compared to pure PIC. This is mediated, at least partly, by enhanced pro-apoptotic activity, disruption of MMP, and stimulation of ROS generation.
Highlights
Colorectal cancer (CRC) creates a high disease burden globally, and it has been projected to further increase by 60% by the year 2030 [1]
Piceatannol, cholesterol, and tristearin were purchased from Sigma–Aldrich Inc
The HCT 116, HCT 29, and EA.hy926 cells were obtained from NCCS, Pune, India
Summary
Colorectal cancer (CRC) creates a high disease burden globally, and it has been projected to further increase by 60% by the year 2030 [1]. Natural products are gaining much attention as colon cancer chemotherapeutics [2]. A wide variety of chemical classes of plant active constituents have been reported for their potential role in colon cancer treatment. These include alkaloids and polyphenols [3]. Piceatannol (PIC) is a phenolic compound belonging to the stilbenoids class. Piceatannol has a plethora of pharmacological activities, including antitumor activity which has been found to be superior to resveratrol [4]. Piceatannol cytotoxicity has been reported against melanoma, leukemia, lymphoma, prostate, and colon cancer cells [5]
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