Identification of a New Natural Camptothecin Analogue in Targeted Screening for HIF-1α Inhibitors

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

References

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