| 10915062 |
Fathi AR, Krautheim A, Kaap S, Eger K, Steinfelder HJ: Michael adducts of ascorbic acid as inhibitors of protein phosphatase 2A and inducers of apoptosis. Bioorg Med Chem Lett. 2000 Jul 17;10(14):1605-8.
Michael adducts of ascorbic acid with alpha,beta-unsaturated carbonyl compounds have been shown to be potent inhibitors of protein phosphatase 1 (PP1) without affecting cell viability at the respective concentrations. Here we were able to show that higher concentrations can partially inhibit PP2A activity and concomitantly induce apoptotic cell death. A nitrostyrene adduct of ascorbic acid proved to be a more potent and effective inhibitor of PP2A as well as a stronger inducer of apoptosis. These adducts only slightly lost their cytotoxic potential in multidrug resistant cells that were 10-fold less sensitive to apoptosis induction by okadaic acid and vinblastine. |
82(1,1,1,2) |