Sinomenine hydrochloride sensitizes cervical cancer cells to ionizing radiation by impairing DNA damage response

Oncol Rep. 2018 Nov;40(5):2886-2895. doi: 10.3892/or.2018.6693. Epub 2018 Sep 10.

Abstract

The use of plant‑based compounds derived from traditional medicine to improve human diseases has been gaining momentum, due to their high bioavailability and moderate adverse effects. Sinomenine is one such biomonomer alkali compound derived from Sinomenium acutum and is known for its anti‑inflammatory and antitumor effects. However, the molecular mechanism(s) of its antitumor properties are not fully characterized. In the present study, we evaluated the radiosensitizing effects of the water‑soluble sinomenine, sinomenine hydrochloride (SH) in human cervical cancer cell line (HeLa). SH sensitized HeLa cells to ionizing radiation (IR) by promoting accumulation of IR‑induced DNA double‑strand breaks (DSBs) and also by interfering with DNA damage checkpoint activation. We then investigated the molecular mechanisms underlying the SH‑mediated cellular sensitization to IR and found that SH inhibited the expression of DNA damage response (DDR) factors Ku80 and Rad51 at the transcription level. Finally, the radiosensitizing activity of SH was confirmed in a cervical cancer mouse xenograft model. The combinatorial treatment of SH and IR significantly slowed the tumor growth rate compared with IR alone. Collectively, our study not only provides molecular insights into the novel role of SH in cellular response to IR, but also suggests a therapeutic potential of SH as a radiosensitizer in cervical cancer therapy.

MeSH terms

  • Animals
  • Cell Cycle Checkpoints / drug effects
  • Cell Cycle Checkpoints / radiation effects
  • DNA Breaks, Double-Stranded / drug effects
  • DNA Breaks, Double-Stranded / radiation effects
  • DNA Damage / drug effects
  • DNA Damage / radiation effects
  • Female
  • HeLa Cells
  • Humans
  • Mice
  • Morphinans / chemistry
  • Morphinans / pharmacology*
  • Radiation Tolerance / genetics
  • Radiation, Ionizing
  • Radiation-Sensitizing Agents / chemistry
  • Radiation-Sensitizing Agents / pharmacology*
  • Sinomenium / chemistry
  • Uterine Cervical Neoplasms / drug therapy*
  • Uterine Cervical Neoplasms / pathology
  • Uterine Cervical Neoplasms / radiotherapy*
  • Xenograft Model Antitumor Assays

Substances

  • Morphinans
  • Radiation-Sensitizing Agents
  • sinomenine