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Issue 9, 2010
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Toxicity of cucurbit[7]uril and cucurbit[8]uril: an exploratory in vitro and in vivo study

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Abstract

Cucurbit[n]urils (CB[n]) are potential stabilizing, solubilizing, activating, and delivering agents for drugs. The toxicity of the macrocyclic host molecules cucurbit[7]uril (CB[7]), the most water-soluble homologue, as well as cucurbit[8]uril (CB[8]) has been evaluated. In vitro studies on cell cultures revealed an IC50 value of 0.53 ± 0.02 mM for CB[7], corresponding to around 620 mg of CB[7] per kg of cell material. Live-cell imaging studies performed on cells treated with subtoxic amounts of CB[7] showed no detrimental effects on the cellular integrity as assessed by mitochondrial activity. For CB[8], no significant cytotoxicity was observed within its solubility range. The bioadaptability of the compounds was further examined through in vivo studies on mice, where intravenous administration of CB[7] showed a maximum tolerated dosage of 250 mg kg−1, while oral administration of a CB[7]/CB[8] mixture showed a tolerance of up to 600 mg kg−1. The combined results indicate a sufficiently low toxicity to encourage further exploration of CB[n] as additives for medicinal and pharmaceutical use.

Graphical abstract: Toxicity of cucurbit[7]uril and cucurbit[8]uril: an exploratory in vitro and in vivo study

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Publication details

The article was received on 04 Dec 2009, accepted on 26 Jan 2010 and first published on 17 Feb 2010


Article type: Paper
DOI: 10.1039/B925555A
Citation: Org. Biomol. Chem., 2010,8, 2037-2042
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    Toxicity of cucurbit[7]uril and cucurbit[8]uril: an exploratory in vitro and in vivo study

    V. D. Uzunova, C. Cullinane, K. Brix, W. M. Nau and A. I. Day, Org. Biomol. Chem., 2010, 8, 2037
    DOI: 10.1039/B925555A

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