Antitumor Effects of a Sesquiterpene Derivative from Marine Sponge in Human Breast Cancer Cells

Mar Drugs. 2021 Apr 26;19(5):244. doi: 10.3390/md19050244.

Abstract

In this study, the anti-proliferative effect of ilimaquinone, a sesquiterpene derivative from the marine sponge, in breast cancer cells was investigated. Ilimaquinone inhibited the proliferation of MCF-7 and MDA-MB-231 breast cancer cells with IC50 values of 10.6 μM and 13.5 μM, respectively. Non-tumorigenic human breast epithelial cells were less sensitive to ilimaquinone than breast cancer cells. Flow cytometric and Western blot analysis showed that ilimaquinone induced S-phase arrest by modulating the expression of p-CDC-2 and p21. Ilimaquinone induces apoptosis, which is accompanied by multiple biological biomarkers, including the downregulation of Akt, ERK, and Bax, upregulation of p38, loss of mitochondrial membrane potential, increased reactive oxygen species generation, and induced autophagy. Collectively, these findings suggest that ilimaquinone causes cell cycle arrest as well as induces apoptosis and autophagy in breast cancer cells.

Keywords: apoptosis; autophagy; breast cancer; cell cycle arrest; ilimaquinone; sponge.

MeSH terms

  • Animals
  • Antineoplastic Agents / isolation & purification
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Autophagy / drug effects
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / enzymology
  • Breast Neoplasms / pathology
  • Female
  • Humans
  • MCF-7 Cells
  • Membrane Potential, Mitochondrial / drug effects
  • Oxidative Stress / drug effects
  • Porifera / metabolism*
  • Quinones / isolation & purification
  • Quinones / pharmacology*
  • Reactive Oxygen Species / metabolism
  • S Phase Cell Cycle Checkpoints / drug effects
  • Sesquiterpenes / isolation & purification
  • Sesquiterpenes / pharmacology*
  • Signal Transduction

Substances

  • Antineoplastic Agents
  • Quinones
  • Reactive Oxygen Species
  • Sesquiterpenes
  • ilimaquinone