Activity of D-glucarate analogues: synergistic antiproliferative effects with retinoid in cultured human mammary tumor cells appear to specifically require the D-glucarate structure

Life Sci. 1994;54(18):1299-303. doi: 10.1016/0024-3205(94)00507-9.

Abstract

D-Glucarate has shown modest chemopreventive and synergistic chemopreventive effects with retinoids in a number of tumor models as well as a similar antiproliferative effect in MCF-7 human tumor cells in culture. It has been postulated that D-glucarate exerts some of its effects by equilibrium conversion to D-glucarolactone, a potent beta-glucuronidase inhibitor. In the present study, D-glucarate and a number of its analogues, including D-glucarolactone, were evaluated as antiproliferatives in the MCF-7 model with and without added retinoid. Results suggest that the effects of glucarate are reasonably specific for its structure and may not require conversion to glucarolactone.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Breast Neoplasms
  • Cell Division / drug effects*
  • Cell Line
  • Drug Synergism
  • Female
  • Glucaric Acid / analogs & derivatives*
  • Glucaric Acid / chemical synthesis
  • Glucaric Acid / pharmacology*
  • Humans
  • Molecular Structure
  • Retinoids / pharmacology*
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • 2,3,4,5-tetra-O-methylglucaric acid
  • Retinoids
  • Glucaric Acid