Flavonoids Apigenin and Quercetin Inhibit Melanoma Growth and Metastatic Potential

Int J Cancer. 2000 Aug 15;87(4):595-600. doi: 10.1002/1097-0215(20000815)87:4<595::aid-ijc21>3.0.co;2-5.

Abstract

Flavonoids are a class of polyphenolic compounds widely distributed in the plant kingdom, which display a variety of biological activities, including chemoprevention and tumor growth inhibition. Our aim was to investigate the effects of several polyphenols on the growth and metastatic potential of B16-BL6 melanoma cells in vivo. Intraperitoneal administration of quercetin, apigenin, (-)-epigallocathechin-3-gallate (EGCG), resveratrol, and the anti-estrogen tamoxifen, at the time of i.m. injection of B16-BL6 cells into syngeneic mice, resulted in a significant, dose-dependent delay of tumor growth, without toxicity. The relative descending order of potency was EGCG > apigenin = quercetin = tamoxifen > resveratrol > control. Furthermore, polyphenols significantly potentiated the inhibitory effect of a non-toxic dose of cisplatin. When tested for the ability to inhibit lung colonization, quercetin, apigenin, and tamoxifen (but not EGCG or resveratrol) significantly decreased the number of B16-BL6 colonies in the lungs in a dose-dependent manner, with quercetin and apigenin being more effective than tamoxifen. Interestingly, quercetin, apigenin, and tamoxifen (but not EGCG or resveratrol) significantly decreased the invasion of B16-BL6 cells in vitro, with quercetin and apigenin being more effective than tamoxifen. This suggests that anti-invasive activity is one of the mechanisms underlying inhibition of lung colonization by quercetin and apigenin. In conclusion, quercetin and apigenin inhibit melanoma growth and invasive and metastatic potential; therefore, they may constitute a valuable tool in the combination therapy of metastatic melanoma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticarcinogenic Agents / pharmacology*
  • Anticarcinogenic Agents / therapeutic use
  • Apigenin
  • Catechin / analogs & derivatives
  • Catechin / pharmacology
  • Catechin / therapeutic use
  • Cell Division / drug effects
  • Curcumin / pharmacology
  • Curcumin / therapeutic use
  • Female
  • Flavonoids / pharmacology*
  • Flavonoids / therapeutic use
  • Growth Inhibitors / pharmacology
  • Growth Inhibitors / therapeutic use
  • Lung Neoplasms / prevention & control
  • Lung Neoplasms / secondary
  • Melanoma, Experimental / pathology*
  • Melanoma, Experimental / prevention & control
  • Melanoma, Experimental / secondary
  • Mice
  • Mice, Inbred C57BL
  • Neoplasm Invasiveness
  • Neoplasm Transplantation
  • Quercetin / pharmacology*
  • Quercetin / therapeutic use
  • Resveratrol
  • Stilbenes / pharmacology
  • Stilbenes / therapeutic use
  • Tamoxifen / pharmacology
  • Tamoxifen / therapeutic use
  • Tumor Cells, Cultured

Substances

  • Anticarcinogenic Agents
  • Flavonoids
  • Growth Inhibitors
  • Stilbenes
  • Tamoxifen
  • Apigenin
  • Catechin
  • Quercetin
  • epigallocatechin gallate
  • Curcumin
  • Resveratrol