The citrus flavonoid, nobiletin, inhibits peritoneal dissemination of human gastric carcinoma in SCID mice

Jpn J Cancer Res. 2001 Dec;92(12):1322-8. doi: 10.1111/j.1349-7006.2001.tb02156.x.

Abstract

The flavonoid nobiletin (5,6,7,8,3',4'-hexamethoxyflavone), found in Citrus depressa Rutaceae, a popular citrus fruit in Okinawa, Japan, reportedly inhibits the production of pro-matrix metalloproteinase (proMMP)-1, 3, and 9 in rabbit synovial fibroblasts in vitro. In the present study, we demonstrated the inhibitory effects of nobiletin on the proliferation of the cancer cell line, TMK- 1, and its production of MMPs. In the SCID mouse model, we found that nobiletin inhibited the formation of peritoneal dissemination nodules from TMK-1. The enzymatic activity of MMP-9 expressed in culture medium obtained from a co-culture of TMK-1 and mouse fibroblastic cells was inhibited by nobiletin in a concentration-dependent manner. In the SCID mouse model, total weight of dissemination nodules was significantly lower in the treated group compared with the vehicle control group (0.07 g vs. 0.78 g, P = 0.0059). The total number of dissemination nodules was also significantly lower than in the vehicle control group (7.5 vs. 69.3 / body, P = 0.0001). These results suggest that nobiletin may be a candidate anti-metastatic drug for prevention of peritoneal dissemination of gastric cancer.

MeSH terms

  • Animals
  • Body Weight / drug effects
  • Cell Division / drug effects
  • Citrus / chemistry*
  • Dose-Response Relationship, Drug
  • Flavones*
  • Flavonoids / chemistry
  • Flavonoids / pharmacology
  • Flavonoids / therapeutic use*
  • Humans
  • Matrix Metalloproteinases / metabolism
  • Mice
  • Mice, SCID
  • Neoplasm Transplantation
  • Organ Size / drug effects
  • Organ Specificity
  • Peritoneal Neoplasms / drug therapy*
  • Peritoneal Neoplasms / pathology
  • Peritoneal Neoplasms / secondary*
  • Stomach Neoplasms / drug therapy*
  • Stomach Neoplasms / enzymology
  • Stomach Neoplasms / pathology*
  • Tumor Cells, Cultured

Substances

  • Flavones
  • Flavonoids
  • nobiletin
  • Matrix Metalloproteinases