A convenient approach for evaluating the toxicity profiles of in vitro neuroprotective alkylaminophenol derivatives

Free Radical Biology & Medicine
Amparo UriosManuel Blanco

Abstract

The cytotoxicity profiles of a series of quinol-type derivatives were examined through simple Escherichia coli plate assays discriminating the two main cytotoxicity mechanisms associated with polyphenol oxidation to quinone. Toxicity mediated by reactive oxygen species (ROS-TOX) was detected in the OxyR(-) assay using cells sensitive to oxidative stress due to a deficiency in the OxyR function. Toxicity arising from the high susceptibility of quinone toward endogenous nucleophiles (Q-TOX) was detected using OxyR(+) cells, in the presence of a nitric oxide donor to promote the quinol oxidation to the corresponding quinone. The toxicity profile markedly depended on structural features. Strong ROS-TOX required a pyrogallol arrangement (exifone; 2,3,4-trihydroxybenzophenone, 1; baicalein) or a 2-aminoresorcinol sequence (3-amino-2,4-dihydroxybenzophenone, 4). The pyrogallol moiety determined a low Q-TOX, suggesting the conversion of quinones into oxidation products of low toxicity. Compounds lacking a 2-hydroxyl substituent (derivatives 2 and 5, related to 1 and 4, respectively) induced a weak ROS-TOX, but a significant Q-TOX. The electrochemical oxidation of the studied compounds corroborated the crucial role of the 2-hydroxyl gro...Continue Reading

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Citations

Mar 24, 2009·IEEE Transactions on Nanobioscience·Eve-Marei DumasJay L Nadeau
Mar 21, 2009·Annales pharmaceutiques françaises·M-B FleuryM Largeron

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