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DOI: 10.1055/s-2006-951767
© Georg Thieme Verlag KG Stuttgart · New York
Identification of a New Natural Camptothecin Analogue in Targeted Screening for HIF-1α Inhibitors
Publication History
Received: August 30, 2006
Accepted: October 20, 2006
Publication Date:
21 December 2006 (online)
![](https://www.thieme-connect.de/media/plantamedica/200701/lookinside/thumbnails/10.1055-s-2006-951767-1.jpg)
Abstract
Screening to detect compounds that inhibit the HIF-1α 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.
Key words
HIF-1α - camptothecin - Ophiorrhiza trichocarpon - Rubiaceae - dereplication
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Thomas G. McCloud
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