文摘
Bioactivity-directed fractionation of an extract of the leaves of Alvaradoa haitiensis, using the KB (human oral epidermoidcarcinoma) cell line, led to the isolation and identification of 10 new anthracenone C-glycosides, alvaradoins E-N(1-10), along with the known compound chrysophanol (11). The cytotoxicity of all compounds was evaluated, andpreliminary structure-activity relationships are suggested. The most potent compounds in the in vitro assays (1 and 2)were evaluated in vivo versus the P388 (murine lymphocytic leukemia) model, and alvaradoin E (1) showed antileukemicactivity (125% T/C) at a dose of 0.2 mg kg-1 per injection when administered intraperitoneally.