Abstract
An extract from Phyllanthus engleri was identified in a bioinformatic analysis of NCI 60-cell natural product extract screening data that selectively inhibited the growth of renal cancer cell lines. Bioassay-guided fractionation yielded two new guaiane sesquiterpenes, englerins A (1) and B (2). Englerin A showed 1000-fold selectivity against six of eight renal cancer cell lines with GI(50) values ranging from 1-87 nM. The structures of 1 and 2 and their relative stereochemistry were established by spectroscopic methods.
Publication types
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Research Support, N.I.H., Intramural
MeSH terms
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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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Biological Assay
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Dose-Response Relationship, Drug
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Drug Screening Assays, Antitumor
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Humans
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Inhibitory Concentration 50
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Kidney Neoplasms / pathology*
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Magnetic Resonance Spectroscopy / standards
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Molecular Conformation
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Phyllanthus / chemistry*
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Plant Bark / chemistry
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology*
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Plant Stems / chemistry
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Reference Standards
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Sesquiterpenes, Guaiane / chemistry
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Sesquiterpenes, Guaiane / isolation & purification
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Sesquiterpenes, Guaiane / pharmacology*
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Stereoisomerism
Substances
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Antineoplastic Agents, Phytogenic
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Plant Extracts
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Sesquiterpenes, Guaiane
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englerin A