| Background |
Camptothecin (CPT), CAS number: 7689-03-4, a cytotoxic quinoline alkaloid isolated from the bark and trunk of Camptotheca acuminata, is an effective inhibitor of Topoisomerase I (IC50=0.68 μM). Irreversibly bind to the DNA-Topo I cleavage complex, inducing DNA strand breaks. Camptothecin exhibits strong anti-tumor activity in various experimental tumor models and simultaneously inhibits DNA and RNA synthesis in mammalian cells. Cytotoxicity was observed in HT-29 cells (IC50=10 nM), and
DNA damage was induced at a working concentration as low as 51 nM in intact cells, while DNA damage was induced at a concentration as low as 12 nM in purified and isolated nuclei. Low concentrations of camptothecin can arrest the cell cycle in the S phase and induce apoptosis in a large number of normal or cancerous cells in a cell cycle-dependent or cycle-independent manner. |
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