Alvaradoins E-N, antitumor and cytotoxic anthracenone C-glycosides from the leaves of Alvaradoa haitiensis

Bioactivity-directed fractionation of an extract of the leaves of Alvaradoa haitiensis, using the KB (human oral epidermoid carcinoma) 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, and preliminary 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 antileukemic activity (125% T/C) at a dose of 0.2 mg kg-1 per injection when administered intraperitoneally.

Phifer, S., Lee, D., Seo, E-K., Kim, N. C., Graf, T., Kroll, D., ... Wani, M. (2007). Alvaradoins E-N, antitumor and cytotoxic anthracenone C-glycosides from the leaves of Alvaradoa haitiensis. Journal of Natural Products, 70(6), 954-961. DOI: 10.1021/np070005a