Rotenoids and flavonoids with anti-invasion of HT1080, anti-proliferation of U937, and differentiation-inducing activity in HL-60 from Erycibe expansa

Bioorg Med Chem. 2007 Feb 1;15(3):1539-46. doi: 10.1016/j.bmc.2006.09.024. Epub 2006 Dec 8.

Abstract

Principal rotenoids (deguelin, tephrosin, rotenone, and 12a-hydroxyrotenone) (3-30microM) isolated from the stems of Erycibe expansa significantly inhibited invasion of human fibrosarcoma HT1080 cells through Matrigel-coated filters and release of proMMPs-2 and 9. In addition, deguelin and tephrosin showed differentiation-inducing activity in human promyelocytic leukemia HL-60 cells. Furthermore, effects of various constituents isolated from the ethyl acetate-soluble fraction on proliferation of human leukemia U937 cells were examined. As a result, most of isoflavones and several flavans as well as rotenoids showed moderate or substantial anti-proliferative activities.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Differentiation / drug effects*
  • Cell Proliferation / drug effects*
  • Convolvulaceae / chemistry*
  • Enzyme Precursors / metabolism
  • Fibrosarcoma / drug therapy*
  • Fibrosarcoma / pathology
  • Flavonoids / pharmacology*
  • Gelatinases / metabolism
  • HL-60 Cells / drug effects
  • Humans
  • Matrix Metalloproteinase 9 / metabolism
  • Metalloendopeptidases / metabolism
  • Neoplasm Invasiveness / prevention & control*
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Rotenone / chemistry
  • Rotenone / pharmacology*
  • Tumor Cells, Cultured / drug effects
  • U937 Cells / drug effects

Substances

  • Enzyme Precursors
  • Flavonoids
  • Plant Extracts
  • Rotenone
  • Gelatinases
  • Metalloendopeptidases
  • pro-matrix metalloproteinase 9
  • progelatinase
  • Matrix Metalloproteinase 9