The cytotoxicity of T-2 toxin and related trichothecenes was studied in Adriamycin-sensitive and-resistant P388 leukemia cells in vitro. The structure-activity relationship indicated that a free hydroxyl in the C-3 position contributed to the activity. Free hydroxyls at the 4, 8, and 15 positions interfered with the activity, and their estrification resulted in improved cytotoxicity. The cytotoxic activity of these trichothecenes did not seem to be related to their degree of lipophilicity. Adriamycin-resistant P388 cells were cross-resistant to the trichothecenes, and this resistance could be circumvented by verapamil.
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Adriamycin-resistant P388 cells
- ED50 :
the concentration inhibiting the growth rate by 50%
octanol-water partitioning coefficient
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Ramu, A., Yagen, B. & Ramu, N. The cytotoxicity of T-2 toxin and related 12,13-epoxytrichothecenes to Adriamycin-sensitive and-resistant P388 leukemia cells. Cancer Chemother. Pharmacol. 24, 264–267 (1989). https://doi.org/10.1007/BF00257631
- Cancer Research
- Leukemia Cell