Abstract
Screening to detect compounds that inhibit the HIF-1alpha transcriptional activation pathway identified an extract of Ophiorrhiza trichocarpon for investigation. A high throughput dereplication strategy was employed, involving chromatography with spectral data acquisition supported by bioactivity testing and literature referencing, which led to rapid identification of camptothecin (1) and three analogues (2 - 4) as the active compounds. 9,10-Methylenedioxy-(20S)-camptothecin (4) was found for the first time from a plant.
Publication types
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Evaluation Study
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Research Support, N.I.H., Extramural
MeSH terms
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Antineoplastic Agents, Phytogenic / administration & dosage
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Antineoplastic Agents, Phytogenic / pharmacology*
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Antineoplastic Agents, Phytogenic / therapeutic use
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Camptothecin / analogs & derivatives*
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Drug Screening Assays, Antitumor
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Humans
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Hypoxia-Inducible Factor 1, alpha Subunit / antagonists & inhibitors
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Hypoxia-Inducible Factor 1, alpha Subunit / drug effects*
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Phytotherapy*
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Plant Extracts / administration & dosage
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Plant Extracts / pharmacology*
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Plant Extracts / therapeutic use
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Plant Structures
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Rubiaceae*
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Sensitivity and Specificity
Substances
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Antineoplastic Agents, Phytogenic
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Hypoxia-Inducible Factor 1, alpha Subunit
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Plant Extracts
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Camptothecin