TargetRx Atlas

MRNA basic information

  • mRNA ID:ENST00000241393
  • Gene Name:CXCR4
  • mRNA database:Ensembl
  • mRNA expression :down-regulated
  • mRNA Method:qRT-PCR
  • mRNA Pathway:NA
  • Evidence:validated
  • (mRNA-drug)

Drug basic information

  • Drug ID:DB15584
  • Drug Name:Luteolin
  • Drug Method:down-regulated the gene expression

Disease basic infommation

  • Disease:breast cancer
  • Tissue:cell line DA?MB?231

Other information

  • Title:Luteolin, an aryl hydrocarbon receptor ligand, suppresses tumor metastasis in vitro and in vivo
  • Journal:Oncology Reports
  • Published:2020
  • PubMed ID:33000272
  • Abstract:Estrogen receptor (ER)-negative breast tumors are associated with low survival rates, which is related to their ability to grow and metastasize into distal organs. The aryl hydrocarbon receptor (AhR), a ligand-activated transcription factor that is involved in several biological processes, is a promising anti-metastatic target. Luteolin, a non-toxic naturally occurring plant flavonoid with diverse biological activities, has been demonstrated to be effective against certain types of cancer, and has also been described as a ligand of AhR. In the present study, various cancer cell lines were first investigated following treatment with luteolin, and luteolin exhibited the lowest IC50 in MDA-MB-231 cells. Then, the efficiency of luteolin in suppressing the metastasis of ER-negative breast cancer in vitro was assessed. MDA-MB-231 cells were treated with luteolin in vitro. Subsequently, MTT assay and flow cytometry were used to detect cell viability, the cell cycle and apoptosis, and a Transwell assay was used to evaluate cell invasion. In addition, reverse transcription-semi-quantitative PCR and western blot were performed to detect the mRNA and protein expression levels of matrix metalloproteinase (MMP)-2 and MMP-9. In addition, the number of surface tumor nodules was measured in vivo, in mice bearing B16-F10 tumors, following treatment with luteolin. Luteolin inhibited the viability and induced the apoptosis of MDA-MB-231 cells, which was accompanied by cell cycle arrest. This was associated with a decrease in the expression of the pro-metastatic markers C-X-C chemokine receptor type 4 (CXCR4), MMP-2 and MMP-9, which was reversed by AhR inhibition. Furthermore, it was identified that luteolin could inhibit the metastasis in a B16F10 mouse xenograft model, and the levels of MMP-9, MMP-2 and CXCR4 were significantly decreased in the lung tissues isolated from tumor-bearing nude mice following luteolin treatment. In conclusion, luteolin is a potential molecule for inhibiting breast cancer invasion and metastasis, which could have promising clinical applications.
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