Paper
The endogenous oxindoles 5-hydroxyoxindole and isatin are antiproliferative and proapoptotic.
Published Sep 16, 2000 · Agnès Cane, M. Tournaire, Denis Barritault
Biochemical and biophysical research communications
107
Citations
3
Influential Citations
Abstract
Oxindole-core synthetic molecules are currently being developed as anticancer drugs that target protein tyrosine kinases associated with growth factor receptors. Oxindole, 5-Hydroxyoxindole, and 2, 3-dioxindole [isatin] are natural molecules found in mammalian body fluids and tissues and we addressed the question of similar properties of endogenous oxindoles. 5-Hydroxyoxindole and isatin, but not oxindole, inhibited N1E-115, BALB/c3T3, BBC, PC12, and HL60 proliferation at submicromolar concentrations. Acute treatment with 5-hydroxyoxindole and isatin reduced the activity of extracellular signal regulated protein kinases (ERKs) by 35% at 100 microM and ERK1 activity was strongly inhibited by 5-Hydroxyoxindole at 10 microM. Survival of PMA-differentiated HL60 and FGF(2)-differentiated PC12 cells was not affected by 5-Hydroxyoxindole and isatin treatment, suggesting that endogenous oxindoles interact with growth factors signaling. The physiological implications of these data and the potential utility of 5-Hydroxyoxindole and isatin as antitumor agents are discussed.
In Vitro Study
Highly CitedEndogenous oxindoles 5-hydroxyoxindole and isatin inhibit cell proliferation and may serve as potential antitumor agents by targeting growth factors signaling.
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