Cucurbitacin B Inhibits the Hippo-YAP Signaling Pathway and Exerts Anticancer Activity in Colorectal Cancer Cells

Med Sci Monit. 2018 Dec 19:24:9251-9258. doi: 10.12659/MSM.911594.

Abstract

BACKGROUND Colorectal carcinoma (CRC) is one of the most frequently diagnosed malignancies. Cucurbitacin B (CuB) is a natural compound isolated from herbs and shows anticancer activity in several cancers. MATERIAL AND METHODS Here, we analyzed the effects of different CuB concentrations on the proliferative and invasive behaviors of CRC cells using MTT, clonogenic assay, Transwell invasion, and wound healing assays. Flow cytometry was performed to measure the apoptotic effects of CuB on CRC cells. Western blot and real-time PCR were used to investigate the expression of apoptosis and Hippo-YAP signaling pathway proteins. RESULTS CuB inhibited the proliferation and invasion of CRC cells while promoting apoptosis. In addition, the Western blot and real-time PCR results indicated that CuB suppressed YAP expression and its downstream target genes Cyr 61 and c-Myc in CRC cells. To assess the underlying mechanism, we investigated the upstream regulating factor LATS1, and the results revealed that CuB upregulated LATS1 expression in CRC cells. CONCLUSIONS In conclusion, our findings uncovered a novel therapeutic mechanism of CuB and suggest that there is therapeutic potential and feasibility in developing novel YAP inhibitors for cancer treatment.

MeSH terms

  • Adaptor Proteins, Signal Transducing / drug effects*
  • Apoptosis / drug effects
  • Apoptosis Regulatory Proteins / metabolism
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Colonic Neoplasms / genetics
  • Colorectal Neoplasms / drug therapy
  • Colorectal Neoplasms / metabolism
  • Gene Expression Regulation, Neoplastic / genetics
  • Hippo Signaling Pathway
  • Humans
  • Neoplasm Invasiveness / genetics
  • Phosphoproteins / drug effects*
  • Phosphorylation / drug effects
  • Protein Serine-Threonine Kinases / drug effects*
  • Signal Transduction / drug effects
  • Transcription Factors
  • Triterpenes / pharmacology*
  • Up-Regulation
  • YAP-Signaling Proteins

Substances

  • Adaptor Proteins, Signal Transducing
  • Apoptosis Regulatory Proteins
  • Phosphoproteins
  • Transcription Factors
  • Triterpenes
  • YAP-Signaling Proteins
  • YAP1 protein, human
  • cucurbitacin B
  • LATS1 protein, human
  • Protein Serine-Threonine Kinases