Antioxidants (May 2020)

Piceatannol-Loaded Emulsomes Exhibit Enhanced Cytostatic and Apoptotic Activities in Colon Cancer Cells

  • Nabil A. Alhakamy,
  • Shaimaa M. Badr-Eldin,
  • Osama A. A. Ahmed,
  • Hani Z. Asfour,
  • Hibah M. Aldawsari,
  • Mardi M. Algandaby,
  • Basma G. Eid,
  • Ashraf B. Abdel-Naim,
  • Zuhier A. Awan,
  • Adel F. Alghaith,
  • Ahmed L. Alaofi,
  • Amir I. Mohamed,
  • Solomon Z. Okbazghi,
  • Mohammed W. Al-Rabia,
  • Usama A. Fahmy

DOI
https://doi.org/10.3390/antiox9050419
Journal volume & issue
Vol. 9, no. 5
p. 419

Abstract

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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.

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