Isolation and structure of the strong cell growth and tubulin inhibitor combretastatin A-4

Experientia. 1989 Feb 15;45(2):209-11. doi: 10.1007/BF01954881.

Abstract

The African tree Combretum caffrum (Combretacae) has been found to contain a powerful inhibitor of tubulin polymerization (IC50 2-3 microM), the growth of murine lymphocytic leukemia (L 1210 and P 388 with ED50 approximately 0.003 microM and human colon cancer cell lines [(e.g. LoVo (ED50 = 0.005 microgram/ml), HT 29 (ED50 0.02 microgram/ml, Colo 205 (ED50 = 0.07 microgram/ml), DLD-1 (ED50 = 0.005 microgram/ml) and HCT-15 (ED50 = 0.0009 microgram/ml] designated combretastatin A-4 (1c). The structure assigned by spectral techniques was confirmed by synthesis.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic
  • Bibenzyls / chemical synthesis
  • Bibenzyls / isolation & purification*
  • Bibenzyls / therapeutic use
  • Colonic Neoplasms / drug therapy
  • Humans
  • Leukemia L1210 / drug therapy
  • Leukemia P388 / drug therapy
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Mice
  • Molecular Structure
  • Plant Extracts
  • Stilbenes*
  • Tubulin Modulators*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents, Phytogenic
  • Bibenzyls
  • Plant Extracts
  • Stilbenes
  • Tubulin Modulators
  • fosbretabulin