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- W2023282273 abstract "Highly toxic bacterial ionophores are commonly used in veterinary medicine, but their therapeutic index is too narrow for human usage. With the goal of developing ionophores with a broader therapeutic index, we constructed highly derivatized synthetic ionophores. The toxicities of crown ether host-rotaxanes (CEHRs) against the SKOV-3 cell line were measured. The effect of Mg2+ or Ca2+ on toxicity was explored because changes in the intracellular concentration of these cations can cause cell death through apoptosis. We found that Boc-CEHR is highly toxic and Arg-CEHR is slightly less toxic with IC50 values of 0.5 and 6 μM, respectively, in standard growth medium. Increasing the concentration of Ca2+ resulted in greater toxicity of the CEHRs, whereas increasing the concentration of Mg2+ was less effective on reducing IC50. Cell death occurs mainly through apoptosis. Although preliminary, these results suggest that the CEHRs deliver Ca2+ and perhaps Mg2+ into cells inducing apoptosis." @default.
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- W2023282273 date "2012-11-16" @default.
- W2023282273 modified "2023-10-10" @default.
- W2023282273 title "Crown Ether Host-Rotaxanes as Cytotoxic Agents" @default.
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- W2023282273 doi "https://doi.org/10.1021/ml3003204" @default.
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