Disease relevance of AD-143

• Similar experiments with Escherichia coli cells showed that AD 143 at the same concentrations did not have any effect [1].
• N-Trifluoroacetyladriamycin-14-O-hemiadipate (AD 143), a DNA nonbinding derivative of Adriamycin, was studied for its effect on the uptake of labeled nucleosides into human leukemia (ML-1) and lymphoma (P3HR-1) cells in culture [1].

High impact information on AD-143

• After preincubation with AD 143 at concentrations as low as 5.2 microM (ML-1) or 13 microM (P3HR-1), the ability of the cells to take up extracellular labeled nucleosides was decreased by more than 50% [1].
• These observations suggest that the decreased incorporation of [3H]thymidine and [3H]uridine into acid-precipitable material that we observed earlier in the AD 143-treated cells may in part be the result of the AD 143-induced alteration of cell membrane activities, which in turn causes an inhibition of nucleoside uptake [1].
• An increase in the membrane fluidity was observed after treatment of the cells with AD 143, as revealed by electron paramagnetic resonance spectroscopy studies [1].
• N-Trifluoroacetyladriamycin-14-O- Hemiadipate (AD 143), a new derivative of adriamycin with greater antitumor activity and lower cardiotoxicity, was shown not to interact with DNA and yet inhibit the activities of both RNA polymerases I and II of chicken myeloblastosis cells in vitro with ID50 values equal to 6.5 microM and 7 microM, respectively [2].

References