Oncocalyxones A and C, 1,4-anthracenediones from Auxemma oncocalyx: comparison with anticancer 1,9-anthracenediones.

Oncocalyxones A and C are 1,4-anthracenediones isolated from Auxemma oncocalyx (Boraginaceae) that have been shown to be cytotoxic to tumor cells in vitro. The present study compared the cytotoxicity of these compounds with that of two conventional anticancer agents doxorubicin and mitoxantrone, both 1,9-anthracenediones, in a panel of human tumor cell lines. The effect on cell growth was examined using an MTT microtiter assay in two leukemia lines, five solid tumor lines of different histological origin, and two multidrug-resistant sublines of a lung tumor line. The oncocalyxones showed much lower potency than the 1,9-anthracenediones, but were similarly more cytotoxic to leukemia cells compared to solid tumor lines. However, in the multidrug-resistant cells with 10 to 500 times decreased sensitivity to doxorubicin, the cytotoxicity of oncocalyxones A and C was only modestly reduced by about twofold, 1,4-Anthracenediones may be a promising novel class of chemotherapeutic agents effective against multidrug resistant tumors.