Camptothecin

Camptothecin is a cytotoxic, quinoline alkaloid, discovered as the active principle of extracts from the Chinese tree C. acuminate, that inhibits the DNA enzyme topoisomerase I (Top1). It binds the Top1-DNA cleavage complex, inducing DNA-strand breaks.^1,2 Camptothecin has strong anti-tumor activity against a wide range of experimental tumors and inhibits both DNA and RNA synthesis in mammalian cells.³ It displays cytotoxity in HT-29 cells with an IC₅₀ value of 10 nM and induces DNA damage at concentrations as low as 51 nM in whole cells and 12 nM in isolated nuclei in in vitro assays.⁴

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1. Hsiang, Y.H., Hertzberg, R., Hecht, S., et al. Camptothecin induces protein-linked DNA breaks via mammalian DNA topoisomerase I. The Journal of Biological Chemisty 260(27), 14873-14878 (1985).

2. Marchand, C., Antony, S., Kohn, K.W., et al. A novel norindeniosoquinoline structure reveals a common interfacial inhibitor paradigm for ternary trapping of the topoisomerase I-DNA covalent complex. Mol. Cancer Ther. 5(2), 287-295 (2006).

3. Dancey, J., and Eisenhauer, E.A. Current perspectives on camptothecins in cancer treatment. Br. J. Cancer 74(3), 327-338 (1996).

4. Rothenberg, M.L. Topoisomerase I inhibitors: Review and update. Ann. Oncol. 8(9), 837-855 (1997).