1. Academic Validation
  2. Alvaradoins E-N, antitumor and cytotoxic anthracenone C-glycosides from the leaves of Alvaradoa haitiensis

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

Affiliation

  • 1 Natural Products Laboratory, Research Triangle Institute, P.O. Box 12194, Research Triangle Park, North Carolina 27709, USA.
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.

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