Lycorine hydrochloride inhibits cell proliferation and induces apoptosis through promoting FBXW7-MCL1 axis in gastric cancer

J Exp Clin Cancer Res. 2020 Oct 30;39(1):230. doi: 10.1186/s13046-020-01743-3.

Abstract

Background: Lycorine hydrochloride (LH), an alkaloid extracted from the bulb of the Lycoris radiata, is considered to have anti-viral, anti-malarial, and anti-tumorous effects. At present, the underlying mechanisms of LH in gastric cancer remain unclear. MCL1, an anti-apoptotic protein of BCL2 family, is closely related to drug resistance of tumor. Therefore, MCL1 is considered as a potential target for cancer treatment.

Methods: The effect of LH on gastric cancer was assessed in vitro (by MTT, BrdU, western blotting…) and in vivo (by immunohistochemistry).

Results: In this study, we showed that LH has an anti-tumorous effect by down-regulating MCL1 in gastric cancer. Besides, we unveiled that LH reduced the protein stability of MCL1 by up-regulating ubiquitin E3 ligase FBXW7, arrested cell cycle at S phase and triggered apoptosis of gastric cancer cells. Meanwhile, we also demonstrated that LH could induce apoptosis of the BCL2-drug-resistant-cell-lines. Moreover, PDX (Patient-Derived tumor xenograft) model experiment proved that LH combined with HA14-1 (inhibitor of BCL2), had a more significant therapeutic effect on gastric cancer.

Conclusions: The efficacy showed in our data suggests that lycorine hydrochloride is a promising anti-tumor compound for gastric cancer.

Keywords: Apoptosis; Cell cycle; Drug-resistance; FBXW7; Gastric cancer; Lycorine hydrochloride; MCL1; PDX model.

MeSH terms

  • Amaryllidaceae Alkaloids / pharmacology*
  • Animals
  • Apoptosis / drug effects
  • Carcinogenesis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • F-Box-WD Repeat-Containing Protein 7 / metabolism*
  • Female
  • HEK293 Cells
  • Humans
  • Mice
  • Mice, Nude
  • Myeloid Cell Leukemia Sequence 1 Protein / metabolism*
  • Phenanthridines / pharmacology*
  • Signal Transduction / drug effects
  • Stomach Neoplasms / drug therapy*
  • Stomach Neoplasms / metabolism
  • Stomach Neoplasms / pathology
  • Xenograft Model Antitumor Assays

Substances

  • Amaryllidaceae Alkaloids
  • F-Box-WD Repeat-Containing Protein 7
  • FBXW7 protein, human
  • MCL1 protein, human
  • Myeloid Cell Leukemia Sequence 1 Protein
  • Phenanthridines
  • lycorine