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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anthracenes / chemistry
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Anthracenes / isolation & purification*
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Anthracenes / pharmacology*
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Antineoplastic Agents, Phytogenic / chemistry
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Antineoplastic Agents, Phytogenic / isolation & purification*
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Antineoplastic Agents, Phytogenic / pharmacology*
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Dominican Republic
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Drug Screening Assays, Antitumor
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Humans
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KB Cells
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Leukemia P388
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Models, Biological
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Molecular Structure
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Monosaccharides / chemistry
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Monosaccharides / isolation & purification*
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Monosaccharides / pharmacology*
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Plant Leaves / chemistry
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Plants, Medicinal / chemistry*
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Simaroubaceae / chemistry*
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Structure-Activity Relationship
Substances
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Anthracenes
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Antineoplastic Agents, Phytogenic
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Monosaccharides
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alvaradoin E