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

  • J Nat Prod. 2007 Jun;70(6):954-61. doi: 10.1021/np070005a.
Sharnelle S Phifer  1 ,  Dongho Lee ,  Eun-Kyoung Seo ,  Nam-Cheol Kim ,  Tyler N Graf ,  David J Kroll ,  Hernan A Navarro ,  Robert A Izydore ,  Francisco Jiménez ,  Ricardo Garcia ,  William C Rose ,  Craig R Fairchild ,  Robert Wild ,  Djaja D Soejarto ,  Norman R Farnsworth ,  A Douglas Kinghorn ,  Nicholas H Oberlies ,  Monroe E Wall ,  Mansukh C Wani
Affiliations
  • 1. Natural Products Laboratory, Research Triangle Institute, P.O. Box 12194, Research Triangle Park, North Carolina 27709, USA.
PMID: 17552563 DOI: 10.1021/np070005a
Abstract

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.