Dehydrozingerone, a Curcumin Analog, as a Potential Anti-Prostate Cancer Inhibitor In Vitro and In Vivo

Molecules. 2020 Jun 12;25(12):2737. doi: 10.3390/molecules25122737.

Abstract

Curcumin (Cur) exhibits biological activities that support its candidacy for cancer treatment. However, there are limitations to its pharmacological effects, such as poor solubility and bioavailability. Notably, the use of Cur analogs has potential for addressing these limitations. Dehydrozingerone (DZG) is a representative of the half-chemical structure of Cur, and many reports have indicated that it is anticancer in vitro. We, therefore, have hypothesized that DZG could inhibit prostate cancer progression both in vitro and in vivo. Results revealed that DZG decreased cell proliferation of rat castration-resistant prostate cancer, PLS10 cells, via induction of the cell cycle arrest in the G1 phase in vitro. In the PLS10 xenograft model, DZG significantly decreased the growth of subcutaneous tumors when compared to the control via the inhibition of cell proliferation and angiogenesis. To prove that DZG could improve the limitations of Cur, an in vivo pharmacokinetic was determined. DZG was detected in the serum at higher concentrations and remained up to 3 h after intraperitoneal injections, which was longer than Cur. DZG also showed superior in vivo tissue distribution than Cur. The results suggest that DZG could be a candidate of the Cur analog that can potentially exert anticancer capabilities in vivo and thereby improve its bioavailability.

Keywords: anticancer; curcumin analogs; dehydrozingerone; pharmacokinetic; prostate cancer.

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / pharmacology
  • Apoptosis / drug effects
  • Biological Availability
  • Cell Culture Techniques / methods
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Curcumin / analogs & derivatives
  • Curcumin / pharmacology
  • Drug Carriers / chemistry
  • Humans
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Nanoparticles / chemistry
  • Particle Size
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / metabolism
  • Rats
  • Styrenes / metabolism
  • Styrenes / pharmacology*

Substances

  • Antineoplastic Agents, Phytogenic
  • Drug Carriers
  • Styrenes
  • methyl-3-methoxy-4-hydroxystyryl ketone
  • Curcumin